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Unit 2 Multi System Pharm
Unit 2 Multi System Pharm
1221
Pharmacology
Professional
08/30/2013
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Term
Initial therapy for most patients with RA?
 Definition
Methotrexate (Rheumatrex) or leflunomide (Arava)
Term
_______ plus ______ for moderate-to-high RA.
 Definition
Methotrexate

hydroxychloroquine (Plaquenil)
Term
_______ plus ________ plus ________ for patients with poor prognostic features and moderate-to-high levels of disease activity.
 Definition
Methotrexate

hydroxychloroquine

sulfasalazine (Azulfidine)
Term
The ______ DMARDs ______ and ______ should be reserved for patients with at least moderate disease activity and poor disease prognosis who were not helped by ______ and other ______ DMARDs.
 Definition
biologic DMARDs abatacept (Orencia)and rituximab (Rituxan)

methotrexate and other nonbiologic DMARDs
Term
______ are the new treatment of choice for spondylitis.
 Definition
Anti-TNF-a agents
Term
______ used to treat sacroiliitis
 Definition
NSAIDs
Term
Sjorgren's Syndrome treatment: _____
 Definition
Artificial Tears
Artificial Saliva
Vaginal Lubricant
Avoid anticholinergic medications
Treat systemic manifestations with anti inflammatory or immunosuppressive agents
Term
RA is characterized by ________.
 Definition
Symmetrical inflammatory polyarthritis
Term
In RA _______ forms at the interface between synovium and the bone and cartilage
 Definition
Synovial pannus "gunk"
Term
Initially in RA _____ cells release _____ and ______, which cause synovial cells to release inflammatory mediators.
 Definition
interleukin-1 (IL-1) and tumor necrosis factor-alpha (TNF-a)
Term
Radiographic characteristic of RA is inflamed _______ and _____ cartilage.
 Definition
synovial membrane

pitted cartilage
Term
The histologic features of the rheumatoid nodule (RA) are irregular zones of ______ surrounded by epithelioid cells (histiocytes) and chronic inflammatory cells.
 Definition
fibrinoid necrosis
Term
The histologic features of the rheumatoid nodule are irregular zones of fibrinoid necrosis surrounded by epithelioid cells (histiocytes) and chronic inflammatory cells. The epithelioid cells are frequently _______ around the necrotic zone.
 Definition
palisaded (Olden time log fence)
Term
RA: un/symmetrical ____arthritis.
 Definition
symmetrical polyarthritis
Term
Morning stiffness in RA lasts _____ as opposed to morning stiffness with osteoarthritis that lasts _____.
 Definition
More than one hours

few minutes
Term
Late stage RA Joint destruction: _______.
 Definition
Boutonniere deformity of thumb

ulnar deviation of MP

Swan Neck Fingers
Term
RA Systemic features: RA ______ can occur anywhere.
 Definition
Nodules
Term
RA Systemic features: _____ and _____ syndrome.
 Definition
Caplan’s Syndrome

Felty’s Syndrome
Term
Caplan’s Syndrome in RA, there are ______ nodules.
 Definition
Pulmonary nodules
Term
Felty’s Syndrom: in RA is characterized by ______ and _____ with recurrent _____ infections.
 Definition
splenomegaly & leukopenia with recurrent pulmonary infections
Term
RA Clinical Diagnosis: ___________.
 Definition
Symmetrical synovitis of small joints: warm, swollen joints with synovial hypertrophy, morning stiffness and fatigue are the classic feature.
Term
For patients with early RA (less than 3 months), ________ (along with ______) should be reserved only for patients with high disease activity who have never received DMARDs.
 Definition
anti-tumor necrosis factor (anti-TNF) biologic drugs (along with methotrexate)
Term
For longer duration RA, _______ are recommended for patients who have not been helped by methotrexate.
 Definition
anti-TNF drugs
Term
The three approved anti-TNF DMARDs are: ____________
 Definition
etanercept (Enbrel)
infliximab (Remicade)
adalimumab (Humira).
Term
Types of Spondyloarthropathies:
 Definition
Ankylosing Spondylitis
Reactive Arthritis
Inflammatory Bowel Disease
Psoriatic Arthritis
Term
Spondyloarthropathy is any joint disease of the vertebral column. WIKI
 Definition
Term
Sacroilitis is inflammation of the ________, which Spondylitis is inflammation of the ______.
 Definition
SI Joint

Vertebrae
Term
Enthesitis is inflammation of the ______.
 Definition
Tendon insertion site
Term
Uveitis is inflammation of the ______ and is considered an _______.
 Definition
anterior chamber of the eye

medical emergency
Term
The Spondyloarthropathies: Sacroiliitis, spondylitis, Enthesitis, and Uveitis all vary in their ______.
 Definition
Association with HLA-B27
Term
_____ is most associated with HLA-B27.
 Definition
Ankylosing Spondylitis
Term
Ankylosing Spondylitis is characterized by: ________.
 Definition
Sacroiliitis 5+
Spondylitis 4+
Peripheral Arthritis 1+
Term
_________ is the new treatment of choice for Ankylosing Spondylitis.
 Definition
Anti-TNF-a agents
Term
Following Ankylosing Spondylitis, _______ is has the second most association with HLA-B27.
 Definition
Posturethral Reactive Arthritis
Term
Posturethral Reactive Arthritis is characterized by: ________ and involvement of _______.
 Definition
Sacroiliitis 3+
Spondylitis 3+
Peripheral arthritis 4+

Eye, GU, GI and heart
Term
Posturethral Reactive Arthritis is commonly triggered by ______.
 Definition
chlamydial arthritis
Term
Postdysenteric Reactive Arthritis is characterized by _______ and involvement of _______.
 Definition
Sacroiliitis 2+
Spondylitis 2+
Peripheral arthritis 4+

GU and eye
Term
Inflammatory Bowel Syndrome is characterized by ______ and involvement of _______.
 Definition
Sacroiliitis 1+
Spondylitis 2+
Peripheral arthritis 3+

GI and eye
Term
Inflammatory Bowel Syndrome is caused by _______ and ________.
 Definition
Crohn’s disease & Ulcerative colitis (GI)
Term
Psoriatic Arthritis involves ______
 Definition
Skin rashes and eyes
Term
Spondylitis is treated with _____.
 Definition
Anti-TNF-a agent
Term
Sacroiliitis is treated with ______.
 Definition
NSAIDs
Term
Sjogren's Syndrome is a chronic ______, inflammatory disorder of ________ dysfunction.
 Definition
Chronic immune-mediated, inflammatory disorder of exocrine gland dysfunction
Term
Sjogren's Syndrome is characterized by, dry ____ and _____.
 Definition
Eyes and Mouth
Term
Sjogren's Syndrome has the presence of autoantibodies: ___________.
 Definition
(ANA, rheumatoid factor, anti-Ro (SS-A) or anti-La (SS-B)
Term
Sjogren's Syndrome is diagnosed by the presence of _____ and biopsy of the ______, which demonstrates characteristics of _______.
 Definition
Autoantibodies

Upper lip salivary gland

lymphocytic inflitrate
Term
Sjogren's Syndrome is treated with: _______.
 Definition
Artificial Tears
Artificial Saliva
Vaginal Lubricant
Term
Systemic lupus erythematosus involves _____ on certain target organs.
 Definition
Immune complex deposition
Term
Systemic lupus erythematosus partially results from impaired clearance of _______ and ______.
 Definition
apoptotic cells and immune complexes
Term
90% of the patients with SLE are ____.
 Definition
Females
Term
SLE has 25% concordance in ________ twins.
 Definition
monozygotic
Term
Null alleles with deficiency of ____, ____, or ______ — are a strong risk factor for lupus
 Definition
C1q, C2, or C4
Term
In 70% of patients with SLE there are ______ autoantibodies present.
 Definition
anti double stranded DNA
Term
Other autoantibodies associated with SLE are: __________.
 Definition
Anti Ro (ribonucleoprotein complex)
•Anti La (RNA binding protein)
•Anti C1q (subunit of C1 complement)
•Anti Sm (nuclear particles
Term
The detection of different autoantibody types in SLE is associated with ______.
 Definition
Different clinical manifestations
Term
The two most common autoantibodies associated with SLE are _____ and ____ and their main clinical effects are ________ & _______ disease.
 Definition
Anti-double stranded DNA
Nucleosomes

Kidney and Skin disease
Term
SLE Pathogenic autoantibodies in Lupus have properties that enable them to ______.
 Definition
damage tissue
Term
Autoantibody development in SLE is _______ driven
 Definition
antigen
Term
In order for the antigen to drive lupus it has to be recognized as _____ and presented by an APC to _____ or from a T cell to a ____.
 Definition
Foreign

T Cell

B Cell
Term
_______ can be provided by apoptotic cells.
 Definition
Autoantigens
Term
SLE Clinical manifestations: ____________.
 Definition
Rashes, arthritis, glomerulonephritis or nephrotic syndrome, neuropsychiatric lupus, hemolytic anemia
Term
SLE can present with a ____ rash.
 Definition
Butterfly Rash
Term
In addition to the butterfly rash, Lupus can present on the skin as ______.
 Definition
Discoid Lupus, localized raised areas of skin
Term
Drug Induced Lupus is associated with an _____ antigen in 95% of cases and 70% for SLE.
 Definition
Histone
Term
______ antigen is associated with 40% of SLE cases and none in Drug Induced Lupus.
 Definition
dsDNA
Term
Mixed connective tissue disease have overlap between _______, _______, and ______.
 Definition
SLE, scleroderma, and myositis
Term
40% of Mixed connective tissue disease has _______ involvement.
 Definition
Renal
Term
Mixed connective tissue disease is associated with the specific Ab, _______.
 Definition
U1-RNP Ab
Term
Antiphospholipid syndrome, Clinical manifestations: ___________.
 Definition
–Arterial thrombosis (including stroke, MI)
–Venous thrombosis
–Recurrent fetal loss
–Thrombocytopenia
–Catastrophic antiphospholipid syndrome
Term
Classic Antiphospholipid syndrome presentation is with _______.
 Definition
Livedo reticularis, a pale net like rash on the extremeties
Term
Antiphospholipid syndrome is diagnosed by detection of the _________ and _______ in the labs.
 Definition
Lupus anticoagulant (clots in body though)
Antiphopholipid antibodies
Term
Key history for individuals with Antiphospholipid syndrome, include ______ & _______.
 Definition
miscarriages and clots
Term
Antiphospholipid syndrome is treated with ______ and _______.
 Definition
Heparin

Warfarin
Term
Vasculitis is inflammation of the ______.
 Definition
Arteries
Term
Vasculitis Autoimmune markers include: _________ and ______.
 Definition
Anti-proteinase 3 antibodies

Anti-myeloperoxidase antibodies
Term
Vasculitis of the large sized arteries includes: __________.
 Definition
Takayasu arteritis

Giant cell arteritis

Behcet’s disease
Term
Takayasu arteritis occurs in _____ and is characterized by: _________.
 Definition
Young women

fever, weight loss, arthritis
Term
Giant cell arteritis occurs in _______ and presents with _____.
 Definition
>50

Large bulging temporal artery
Term
Behcet’s disease is characterized by _________ and _______.
 Definition
Mucocutaneous ulcers (oral, genital, ileum, cecal)

Ocular inflammation
Term
Behcet’s disease is diagnosed by _______.
 Definition
Pathergy, needle stick and look for circle reaction around injection site
Term
Vasculitis of Medium sized arteries includes: ___________.
 Definition
Polyarteritis nodosa

Buerger’s disease

Kawasaki
Term
Polyarteritis nodosa is developed in people who have active ______ and ______.
 Definition
Hepatitis B and C
Term
Polyarteritis nodosa are specific to the affected organ but often include: _________.
 Definition
skin, heart (MI, heart failure, pericarditis), kidneys (renal failure), and nervous system
Term
With Buerger’s Disease aka Thromboangiitis obliterans, blood vessels __________.
 Definition
blood vessels of the hands and feet become blocked
Term
With Buerger’s Disease aka Thromboangiitis obliterans occurs most in ________.
 Definition
Tobacco users (heavy smokers)
Term
Kawasaki is the leading cause of _____ in children.
 Definition
Heart disease
Term
Kawasaki affects the _____ arteries and can lead to aneurysms.
 Definition
coronary (medium sized)
Term
Kawasaki presents with ______, ______, and _______.
 Definition
Strawberry tongue

skin rashes on the middle of the body

edema of hands and feet
Term
Vasculitis of the small sized arteries can be _______ mediated or _____ associated.
 Definition
Immune complex mediated

ANCA associated
Term
Vasculitis of the small sized arteries Immune complex mediated: _______.
 Definition
•Leukocytoclastic (cutaneous) vasculitis
(Arthus reaction)
•Henoch-Schoenlein: children>adults
• Cryoglobulinemia;
Term
Vasculitis of the small sized arteries ANCA associated: __________.
 Definition
•Wegener’s granulomatosus (cANCA)
•Churg Strauss syndrome: middle age onset asthma vasculitis
•Microscopic polyangiitis (cANCA, MPOab
and proteinase 3)
Term
ANCA associated Vasculitis of the small sized arteries in Wegener's is due to the autoantibody ________.
 Definition
Anti-proteinase 3 Ab
Term
SYSTEMIC SCLEROSIS (________)
 Definition
SCLERODERMA
Term
Systemic Sclerosis is characterized by: ________, _____, _______.
 Definition
Cutaneous and visceral fibrosis

Vascular Dysfunction

Immune activation
Term
The Vascular Dysfunction associated with Systemic Sclerosis is responsible for the _________ phenomenon.
 Definition
Raynaud’s phenomenon
Term
Classic Antiphospholipid syndrome presentation is with _______.
 Definition
Livedo reticularis, a pale net like rash on the extremeties
Term
Antiphospholipid syndrome is diagnosed by detection of the _________ and _______ in the labs.
 Definition
Lupus anticoagulant (clots in body though)
Antiphopholipid antibodies
Term
Key history for individuals with Antiphospholipid syndrome, include ______ & _______.
 Definition
miscarriages and clots
Term
Antiphospholipid syndrome is treated with ______ and _______.
 Definition
Heparin

Warfarin
Term
Vasculitis is inflammation of the ______.
 Definition
Arteries
Term
Vasculitis Autoimmune markers include: _________ and ______.
 Definition
Anti-proteinase 3 antibodies

Anti-myeloperoxidase antibodies
Term
Vasculitis of the large sized arteries includes: __________.
 Definition
Takayasu arteritis

Giant cell arteritis

Behcet’s disease
Term
Takayasu arteritis occurs in _____ and is characterized by: _________.
 Definition
Young women

fever, weight loss, arthritis
Term
Giant cell arteritis occurs in _______ and presents with _____.
 Definition
>50

Large bulging temporal artery
Term
Behcet’s disease is characterized by _________ and _______.
 Definition
Mucocutaneous ulcers (oral, genital, ileum, cecal)

Ocular inflammation
Term
Behcet’s disease is diagnosed by _______.
 Definition
Pathergy, needle stick and look for circle reaction around injection site
Term
In SYSTEMIC SCLEROSIS, Scleroderma results in ______ skin.
 Definition
Thickened
Term
SYSTEMIC SCLEROSIS's visceral organ involvement can result in intestinal _______, leading to ______, ______, and ______.
 Definition
Intestinal hypomotility
Bacterial overgrowth
Diarrhea/malabsorption
Constipation/bloating
Term
SYSTEMIC SCLEROSIS's visceral organ involvement can result in Esophageal _____motility causing ______.
 Definition
hypo

Dysphagia
Term
SYSTEMIC SCLEROSIS results from a _______ defect in ________, that leads to the ________.
 Definition
Metabolic defect in fibroblast metabolism leading to the overproduction of collagen and other matrix proteins
Term
SYSTEMIC SCLEROSIS damage is caused by ________ activation and _______.
 Definition
Immune cell activation and autoimmunity
Term
In SYSTEMIC SCLEROSIS, Connective tissue matrix replaces: _________.
 Definition
subcutaneous fat, hair follicles, sweat and sebaceous glands
Term
In SYSTEMIC SCLEROSIS, the dermis contains infiltrates of: _______.
 Definition
mononuclear cells, T lymphocytes and monocytes
Term
Although there is endothelial damage, there is no ________ with systemic sclerosis as there is in Lupus and Wegners.
 Definition
No vasculitits (inflammation)
Term
Two types of Systemic Sclerosis: _______.
 Definition
Limited cutaneous (lcSSc)

Diffuse cutaneous (dcSSc)
Term
Limited cutaneous (lcSSc) is characterized by skin thickening that is ________.
 Definition
limited to the distal extremities (Fingers, toes and face)
Term
Limited cutaneous (lcSSc) results in loss of joint mobility with _______. Their is also a loss of ______ and _____, which leaves the skin dry and prone to ________.
 Definition
Contractures

Loss of hair and sweat glands which leads to dry skin that is prone to fissures and infections
Term
In Limited cutaneous (lcSSc), ______ involvment is more uncommon.
 Definition
organ
Term
Diffuse Cutaneous (dcSSc) is characterized by Rapid and progressive symmetrical induration of the skin of the __________.
 Definition
extremities, face and trunk
Term
In Diffuse Cutaneous (dcSSc), visceral organ involvement is common with ______ disease, _______ lung disease, and _______ involvement.
 Definition
Visceral organ involvement common with renovascular disease, interstitial inflammatory lung disease and cardiac involvement the most serious.
Term
With SYSTEMIC SCLEROSIS, Raynaud’s phenomenon is a _______ response consisting of: _________.
 Definition
Triphasic vascular response
Pallor
Cyanosis
Reactive hyperemia
Term
Raynaud’s phenomenon May be seen in _____% of pts with SSc and may precede other manifestations by years
 Definition
>90%
Term
In addition to SSc, Raynaud’s phenomenon is seen in other connective diseases: __________.
 Definition
SLE
Dermatomyositis
Rheumatoid arthritis
Term
The vascular features of SSc, include _____ of the face, hands, chest, and intestines (which may cause _____)
 Definition
Telangiectasia

Bleeding
Term
The vascular features of SSc, include dilated _______ capillaries and ______ ischemia.
 Definition
Dilated nail fold capillaries
Digital ischemia, infection and infarction
Term
SSc is a clinical diagnosis and is suggested by: _____________________.
 Definition
Raynaud’s phenomenon
Esophageal reflux – heartburn
Telangiectasias
Sclerodactyly
Antinuclear antibodies
Term
For SSc, which type is suggested by the detection of Antinuclear Ab that are Nucleolar Pattern?
 Definition
Both types
Term
For SSc, which type is suggested by the detection of Antinuclear Ab that are Anticentromeres?
 Definition
lcSSc
Term
For SSc, 30-50% of dcSSc patients have ______ antibody, which is an auto antibody against _________ and leaves patients with a higher risk for ______ and ____ disease.
 Definition
Scl-70

topoisomerase

renal and lung disease
Term
For lcSSc patients, 50% have the ______ antibody, which leaves them at higher risk for _______.
 Definition
Anticentromere antibodies

Pulmonary Hypertension
Term
SSc presentation, CREST Syndrome:
 Definition
Calcinosis
Raynaud phenomenon
Esopageal dysmotility
Sclerodactyly
Telangiectasias
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS): ____________
 Definition
Polymyositis
Dermatomyositis
Myositis associated with malignancy
Myositis associated with connective tissue disease
Inclusion body myositis
Term
The older you get, the higher chance you have of getting _____ and ______ type of THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS)
 Definition
Malilgnancy and inclusion body
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) are mostly ________.
 Definition
lymphocytic
Term
With THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS), ______ is inflammation of the endomysial.
 Definition
Polymyositis
Term
With THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS), ______ is inflammation of the perimysial and
blood vessels
 Definition
Dermatomyositis
Term
Anti-Jo 1 (also known as antisynthetase) is associated with which IIMS?
 Definition
Polymyositis or dermatomyositis
Term
Anti-Jo 1 (also known as antisynthetase) is associated with the IIMS's Polymoysitis and dermatomyositis. It's clinical features are _______ and ______.
 Definition
Acute interstitial lung disease
Arthritis
Raynaud’s phenomenon
Term
Anti-SRP is associated with which IIMS?
 Definition
Polymyositis
Term
Anti-SRP is associated with the IIMS Polymoysitis. Its clinical features include an _____ onset with severe _______ and ______.
 Definition
Abrupt

Severe weakness
Palpitations
Term
Anti-Mi2 is associated with which IIMS's?
 Definition
Dermatomyositis
Term
Anti-Mi2 is associated with the IIMS, Dermatomyositis, and its clincial features are the ______ sign and _________
 Definition
V sign (shawl sign)
Cuticular overgrowth
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) are a ______ type of disorder with ______ present.
 Definition
autoimmune

autoantibodies
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) are associated with: ________ especially, ________.
 Definition
Hashimoto’s thyroiditis, myasthenia gravis, primary biliary cirrhosis

connective tissue diseases
Term
With THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) there are _______ in a biopsy.
 Definition
T cells cytoxic to muscle
Term
In addition to the cytoxic T cells against muscle tissue, there is immunoglobulin ______ in dermatomyositis
 Definition
deposition and complement components in the capillaries and small arterioles (dermatomyositis)
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) can occur insidious, over months and present with ________.
 Definition
PROXIMAL muscle weakness
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) can occur Indolent, over years with __________ weakness
 Definition
proximal and distal muscle weakness
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS), 50% present with ______, others with _______ indicating cardiac/lung involvement, and others with __________ (_________).
 Definition
Myalgia,

Dyspnea

Dermatomyositis (skin eruption prior to myositis)
Term
Dermatomyositis (skin eruption prior to myositis) is characterized by a _____ rash that has several different varietis: _______lesions
Erythematous rash
Poikilodermatous rash
Heliotrope rash
 Definition
Rthe rash

Gottron lesions/papules
Term
Gottron papules consist of _______, sometimes ____ papules, plaques, or macules.
 Definition
erythematous,

scaly
Term
Gottron sign for THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) is _________.
 Definition
Lesions over metacarpophalangeal and proximal interphalangeal joints
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) for dermatomyotis presents with a _______ on the anterior ________ or the _______ sign on the _______.
 Definition
V shape on anterior chest

Shawl sign on the back
Term
EXTRAMUSCULAR MANIFESTATIONS of IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) are primarily of _______ involvement.
 Definition
Pulmonary
Cardiac
GI
Term
The Extramuscular manifestations of IIMS with Interstitial Lung Disease, 10-30% have the auto antibody _____.
 Definition
anti-Jo-1
Term
Cardiac extramuscular manifestations in Polymyositis and Dermatomyositis include: __________.
 Definition
• Heart block
• Arrhythmias
• Cardiomyopathy
Term
Gastrointestinal extramuscular manifestations in Polymyositis and Dermatomyositis include __________.
 Definition
Esophageal dysmotility
Term
Pulmonary extramuscular manifestations in Polymyositis and Dermatomyositis include __________.
 Definition
Interstitial lung disease
Term
Polymyositis WIKI
 Definition
Polymyositis is a rare inflammatory disease that leads to muscle weakness, swelling tenderness, and tissue damage. It is part of a larger group of diseases called myositis.
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS) are diagnosed by a ______.
 Definition
muscle biopsy
Term
THE IDIOPATHIC INFLAMMATORY MYOPATHIES (IIMS), Therapy: _______.
 Definition
(Unlike SSc, there is therapy)
Steroids
Azathiopine
Methotrexate
Cyclosporine
Cyclophospamide
Mycophenolate
IVIG for dermatomyositis
Term
With the IDIOPATHIC INFLAMMATORY MYOPATHIES there is a 2-fold increase in _____ risk.
 Definition
Cancer
Term
Cardinal feature of OA is the _____ of articular cartilage and the ________.
 Definition
progressive loss

remodeling of subchondral bone
Term
Joint failure results from a variety of pathways subsequent to _____ or repetitive injury
 Definition
bone trauma
Term
Steps in OA pathogenic development: ________.
 Definition
1, stress
2, inflammatory response
3, cartilage breakdown products enhance inflammatory response
4, perpetuation of cartilage damage
5, complete loss of cartilage, erosion of subchondral bone, formation of osteophytes
Term
Clinical Features of OA: _______, ______ and ______ examination.
 Definition
Pain
Stiffness of Short Duration (less than 30 mins, RA is >1 hr)
Joint examination
Term
Joint examination of OA will reveal _______ with movement, a limitation of _______, and joint _______.
 Definition
–Crepitus with movement
–Limitation of motion
–Joint deformity and/or laxity
Term
OA has maximal or minimal swelling?
 Definition
Minimal
Term
In order to differentiate OA from RA, joints that are not typically involved in OA include: ____________ (unless trauma/conginetal)
 Definition
shoulder, elbow, wrist and ankle
Term
Joints commonly affected by OA: _______.
 Definition
Cervical Spine
Lumbar Spine
Hips
Distal Interphalangeal
Knees
Metatarsals
Term
Palpation of the joints:
RA ______
OA _______
 Definition
RA Squishy

OA Bony
Term
Presence of ________ suggests other etiology other than RA.
 Definition
extra-articular manifestations
Term
Extra-articular manifestation, Fever, is more likely: ________ than OA.
 Definition
gout, infectious arthritis
Term
Extra-articular manifestation, Rash, is more likely: ________ than OA.
 Definition
SLE, psoriatic arthritis
Term
Extra-articular manifestation, Nodules, is more likely: ________ than OA.
 Definition
RA, gout
Term
Extra-articular manifestation, Neuropathy, is more likely: ________ than OA.
 Definition
polyarteritis nodusa, Wegener granulamatosis
Term
Typical hand deformities in osteoarthritis:
–__________ on DIPs
–__________ on PIPs
 Definition
Heberden's nodes

Bouchard's nodes
Term
Radiographic Diagnosis of OA: ______.
 Definition
Osteophytes (arrows) and medial joint space narrowing more on one side
Term
Radiographic Diagnosis of RA: _______.
 Definition
Almost complete symmetrical loss of joint space in both the medial and the lateral compartment, but with little subchondral sclerosis or osteophyte formation
Term
Three types of OA: _______.
 Definition
Erosive inflammatory OA
Nodal OA
Routine OA
Term
Erosive inflammatory OA, flares of _____ occur and is destructive of the ______.
 Definition
inflammation

finger joints
Term
Erosive inflammatory OA can be differentiated from RA by _______.
 Definition
lack of rheumatoid factor and asymmetrical
Term
Nodal OA occurs mainly in _____ and has a correlation with _______.
 Definition
females

family history
Term
In Nodal OA, the ______ joints are mainly involved.
 Definition
DIPs
Term
Routine OA is due to ______.
 Definition
Wear and tear
Term
In the treatment of Mild – moderate OA, ________.
 Definition
Acetaminophen
Term
In the treatment of Moderate to severe OA, ________ (In order of increasing severity).
 Definition
–NSAIDS at lowest effective dose
–High-dose NSAIDS plus proton pump inhibitor of misoprostol for gastric protection
–Intra-articular corticosteriods
–Opiates or synthetic opioids (e.g, tramadol)
Term
Proton pump inhibitor drug, _______.
 Definition
misoprostol
Term
Pharmacologic Treatment of OA can be supplemented with ________ or _______.
 Definition
Topical NSAIDS or capsaicin
Term
Crystals Observed in Joints: _______.
 Definition
Monosodium urates
Calcium pyrophosphate dihydrate
Term
Monosodium urates crystals are associated with ________.
 Definition
Gout
Term
Calcium pyrophosphate dihydrate are associated with ________.
 Definition
CPPD deposition disease
Term
Monosodium urates crystals are ______ in Tissue and _______ in fluid.
 Definition
Brown

Needles
Term
Calcium pyrophosphate dihydrate crystals are ______ in Tissue and _______ in fluid.
 Definition
Purple

Rhomboids
Term
Main classes of people at risk for Gout: ________.
 Definition
Men >35 years of age, post-menopausal women, organ transplant recipients
Term
Why are post menopausal women more susceptible to gout?
 Definition
Estrogen enhances rate of uric acid excretion
Term
Serum uric acid levels must be at least ______ to develop gout.
 Definition
>6.8
Term
10% of the cases of Gout are the result of _____ or _____ of uric acid.
 Definition
Overproduction or overconsumption
Term
Primary causes of gout account for _____ cases and are _______.
 Definition
<2%

Genetic deficiencies in enzymes
Term
Secondary causes of Gout include: ________.
 Definition
•Myeloproliferative and lymphoproliferative diseases (producing lots of cells and therefore need lots of purines)
•Chemotherapy of malignancies (purines from dead cells)
•Ethanol consumption
Term
_____ of uric acid accounts for 90% of the cases of Gout.
 Definition
Underexcretion
Term
Acute gout is characterized by ______ onset of _________, accompanied by _____ and _____.
 Definition
Rapid onset of intense pain

Erythema, swelling
Term
Most frequent site for first attack of acute gout is ______.
 Definition
1st MTP (podagra sign)
Term
Polyarticular gout aka (________) involves _______.
 Definition
(gouty arthritis)

multiple joints
Term
Chronic tophaceous gout is characterized by ______.
 Definition
Nodules
Term
Gout is associated with increased levels of urate in the urine, leading to _______.
 Definition
kidney stones (calcium oxalate stones – nephrolithiasis)
Term
Gout is associated with high levels of Monosodium urate (MSU) which can cause ______ around the joints.
 Definition
erode joint to bone
Term
Monosodium urate (MSU) deposition is associated with Gout and can cause _______.
 Definition
nephropathy
Term
Podagra / gouty arthritis is characterized by swelling of the ______, and a dusky blue hue over an _________.
 Definition
1st MTP

intense erythema
Term
Tophaceous gout, nodules are _______ and full of _______ and there is no surrounding ________.
 Definition
painless

uric acid crystals

swelling or erythema
Term
Chronic gout is characterized by chronic ________ with tenderness and swelling.
 Definition
arthritis
Term
In chronic gout _______ are present.
 Definition
tophi
Term
Gout can be differentiated from Septic arthritis by checking for ______.
 Definition
presence of infection
Term
Gout can be differentiated from Cellulitis by checking for ______.
 Definition
skin disease
Term
Acute gout, in 95% of the patients there was ______
 Definition
Serum uric acid >7.5 mg/dL
Term
Monosodium urate crystals are _____ in fluid and _____ refractile
 Definition
needle

highly
Term
Monosodium urate crystals are ______ under polarized light microscopy.
 Definition
Negatively birefringent
Blue/Red
Term
For Acute Gouty attacks, treat initially with the ________, _________.
 Definition
NSAIDS – Indomethacin
Term
For Acute Gouty attacks, treat with any NSAIDS, especially Indomethacin, but not ______ or _____.
 Definition
aspirin or salicylates
Term
In addition to the primary treatment of NSAIDS (Indomethacin) for Acute Gout, _______ can be administered.
 Definition
Corticosteroids
Term
In order to decrease urate formation, a ________ inhibitor, _________ can be administered for moderate to severe gout to prevent the conversion of ______ to ______.
 Definition
ALLOPURINOL

Xanthine oxidase inhibitor

inhibit conversion of hypoxanthine to xanthine to uric acid
Term
In order to increase urate excretion, a ______ type of drug called _______ can be administered, which inhibits ________.
 Definition
Uricosuric

Probenecid

Inhibits tubular reabsorption of urate
Term
NSAIDs first-line treatment for acute gout – _____ or ______.
 Definition
indomethacin or COX-2 inhibitor
Term
First line for lowering Urate for Chronic Tophi Gout is: a xanthine oxidase inhibitor such as ______ or a uricosuric agent such as ________.
 Definition
allopurinol

probenicid
Term
Do NOT give allopurinol during _______ – any change in uric acid level worsens attacks
 Definition
acute gout
Term
______ can be used for prophylaxis treatment of Chronic Tophi Gout.
 Definition
colchicine
Term
If there is failure to lower uric acid levels with single therapy, use one _______ and one _______. If still unsuccessful add ________.
 Definition
1 xanthine inhibitor (allopurinol) and 1 uricosuric agent (probenicid)

pegloticase
Term
Patients with hyperuricemia caused by tumor lysis syndrome are treated with ______ or ______.
 Definition
Rasburicase (allergenic) or pegloticase (uricosuric agents)
Term
Corticosteroids are used to treat which type of gout?
 Definition
Acute
Term
Calcium Pyrophosphate Dihydrate Deposition Disease (CPDD) affects _____ and ______.
 Definition
cartilage and fibrocartilage
Term
Calcium Pyrophosphate Dihydrate Deposition Disease (CPDD) presents as ______.
 Definition
Acute arthritis (Often seen in post-op patient)
Term
Calcium Pyrophosphate Dihydrate Deposition Disease (CPDD) is diagnosed by the presenced of ______ crystals in the fluid, which are _____ refractive.
 Definition
Rhomboid

Poorly
Term
Calcium Pyrophosphate Dihydrate Deposition Disease (CPDD), Calcium pyrophosphate crystals are ________ bifringment.
 Definition
Positively birefringent
Term
CPDD, Acute pseudogout is treated with _______ and ______.
 Definition
Systemic corticosteroids or NSAIDs
Term
CPDD, Pseudo RA is treated with _______ and ______.
 Definition
corticosteroids and methotrexate
Term
Uric acid is produced from the breakdown of _______.
 Definition
purines (adenine, guanine)
Term
2/3 of the uric acid in the body comes from ______ and 1/3 from ______.
 Definition
2/3 comes from de novo synthesis and/or salvage pathways

1/3 diet
Term
Uric acid, 2/3 excreted via _____; 1/3 through _______.
 Definition
kidney

GI tract
Term
Sarcoidosis is a chronic disease of _________.
 Definition
disordered immunity
Term
Sarcoidosis is a multisystem _______ disease of _______ etiology.
 Definition
inflammatory

unknown
Term
Sarcoidosis is a disease of disordered immune ______ in _______ persons exposed to ________.
 Definition
Disease of disordered immune regulation in genetically predisposed persons exposed to certain environmental agents
Term
For Sarcoidosis, the diagnostic histopathic feature is _____________.
 Definition
noncaseating granulomas in various tissues
Term
Sarcoidosis, high levels of ______ cells in the lungs or sites of ________.
 Definition
CD4+ T cells

granulomas
Term
In Sarcoidosis there is massive local secretion of ____-dependent cytokines-_____.
 Definition
Local secretion of Th1-dependent cytokines – IFN-g (by CD4+ T cells )
Term
Primary organ affected in Sarcoidosis?
 Definition
Lungs
Term
Sarcoidosis 75-95% exhibit _______ whiles 75% exhibit ________.
 Definition
lymphadenopathy

spleen granulomas
Term
Sarcoidosis primarily affects _____ lymph nodes.
 Definition
intrathoracic
Term
Sarcoidosis can affect glands, particularly the ______ resulting in _____ from the production of active _____ by activated macrophages.
 Definition
parathyroid gland

hypercalcaemia

Vitamin D
Term
Sarcoidosis manifests in the skins as ________.
 Definition
erythema nodosum (skin nodules, so does gout)
Term
Sarcoidosis, multisystem disease, affects: ________
 Definition
Lungs
Heart
Skeletal Muscle
Liver
Lymph Nodes
Spleen
Glands
Skin
Eyes
Bone Marrow
Term
Sarcoidosis surprisingly does not have a higher incidence among ______.
 Definition
smokers
Term
Sarcoidosis Appears to be due to development of ______ response against an unidentified antigen
 Definition
cell-mediated
Term
Sarcoidosis, there is initially an Intra-alveolar and interstitial accumulation of ______ cells.
 Definition
CD4+ TH1
Term
In Sarcoidosis, the T cell subsets are of ______ origin.
 Definition
from one common, Oligoclonal expansion
Term
In Sarcoidosis, the CD4+ TH1 cells release TH1 cytokines _______ causing _______, and ______ causing _______.
 Definition
IL-2 (T cell expansion) and IFN-γ (macrophage activation)
Term
In Sarcoidosis, following macrophage activation, additional cytokines are released resulting in ______.
 Definition
granuloma formation
Term
One of the common side effects of Sarcoidosis is the anergy to ______, due to the ________.
 Definition
common skin test antigens

peripheral T cell depletion
Term
After the T cells have gone haywire in Sarcoidosis, ______ results for the B cells.
 Definition
Polyclonal hypergammaglobulinemia
Term
Sarcoidosis has genetic involvement and association with certain _____ genotypes.
 Definition
HLA genotypes
Term
2/3 of Sardoisis cases present with ______ that appeared gradually
 Definition
respiratory symptoms (Shortness of breath, cough, vague chest pain)
Term
In addition to resp sympts Sardoisis patients also present with ____, ____, _____, or ______.
 Definition
peripheral LAD, cutaneous lesions, splenomegaly, or hepatomegaly
Term
Sarcoidosis remission may be spontaneous or initiated by ______ therapy.
 Definition
glucocorticoid therapy
Term
10-15% of Sarcoidosis pts die from _____.
 Definition
progressive pulmonary fibrosis
Term
Sarcoidosis should be considered for any patients of the age of _________ with _______ complaints, _______ vision, _______ skin condition, or ________.
 Definition
20-40 with respiratory complants, blurry vision, erythema nodosum and hilar lymphadenopathy
Term
Sarcoidosis WBC will indicate _______ and _______.
 Definition
lymphocytopenia and eosinophila
Term
Sarcoidosis will show a decreased/increased erythocyte sedimentation rate
 Definition
increased
Term
Sarcoidosis will show hypo/hyperglobulinemia
 Definition
hyperglobulinemia
Term
Sarcoidosis labs will show elevated _____ levels.
 Definition
ACE (angiotensin-converting enzyme)
Term
Definitive diagnosis of Sarcoidosis requires ______.
 Definition
biopsy
Term
Sarcoidosis ex. presentation: _____________.
 Definition
A 26-year-old African American woman presented with fever, malaise, weight loss, and erythema nodosum
She reported shortness of breath and dry cough.
Radiograph showed hilar LAD and mediastinal LAD; nodules were also present in the lungs
Term
Sarcoidosis tissue samples have _______ and an absolute indicator is the presence of ______.
 Definition
Noncaseous granulomas

Asteroid bodies
Term
Sarcoidosis is treated with a high dose _______.
 Definition
glucocorticoid taper (prednisolone)
Term
For the treatment of steroid resistant Sarcoidosis: ___________.
 Definition
(Autoimmune Drugs)
Methotrexate
Hydroxychloroquine (antimalarial)
TNF-a inhibitors
Term
Primary immunodeficiency ______ determined.
 Definition
genetically determined
Term
Secondary immunodeficiency states are the results of ______ and ______.
 Definition
Complications of cancers, infections

Side effects of immunosuppression/chemotherapy
Term
X-linked agammaglobulinemia (Bruton’s) results from a mutation in _______, causing a ____ cell immunodeficiency.
 Definition
BTK

Primary B Cell
Term
X-linked agammaglobulinemia (Bruton’s) mutation in BTK results in the failure of ________.
 Definition
Failure of B cell maturation
Term
X-linked agammaglobulinemia (Bruton’s)
overall affect is an _________.
 Definition
Absence of antibodies, circulating B cells, and plasma cells
Term
X-linked agammaglobulinemia (Bruton’s), 20% develop ______.
 Definition
develop autoimmune diseases – RA, dermatomyositis
Term
X-linked agammaglobulinemia (Bruton’s), infection onset by ______.
 Definition
6 months
Term
Selective (isolated) IgA deficiency is the most common ____ deficiency. It is a deficiency of ____ cells.
 Definition
primary

B cell
Term
Selective (isolated) IgA deficiency results in a block in ______.
 Definition
differentiation of IgA-secreting cells
Term
With Selective (isolated) IgA deficiency other than IgA, other Ig are _______.
 Definition
Other immunoglobulins normal or increased
Term
Selective (isolated) IgA deficiency present clinically with ______.
 Definition
early childhood with recurrent sinopulmonary infections and diarrhea
Term
Selective (isolated) IgA deficiency has a significant association with ________.
 Definition
autoimmune disorders
Term
Common variable immunodeficiency is characterized by _______.
 Definition
hypogammaglobulinemia
Term
With Common variable immunodeficiency, _______ cells are present, but _______ cells are absent.
 Definition
B cells present, plasma cells absent
Term
Common variable immunodeficiency is clinically similar to _______, with onset instead around ______.
 Definition
Bruton’s agammaglobulinemia

second decade of life
Term
Common variable immunodeficiency is a _____ type of immunodeficiency.
 Definition
B cell
Term
Common variable immunodeficiency leaves pts prone to developing autoimmune diseases and ________.
 Definition
Lymphoid tumors
Term
Another type of B-Cell Deficiency is Transient hypogammaglobulinemia of infancy which occurs ________, when _______ is disappearing and baby B cells are not producing enough.
 Definition
3-6 months of age when materal IgG is disappearing
Term
DiGeorge syndrome aka (________).
 Definition
Thymic aplasia
Term
DiGeorge syndrome (Thymic aplasia) results from the failure of the development of the _________.
 Definition
3rd and 4th pharyngeal pouches
Term
DiGeorge syndrome (Thymic aplasia) results in _____, ______, and _____ defects (______ syndrome).
 Definition
Cardiac, vascular craniofacial defects

(velocardiofacial syndrome)
Term
Complete absence of the thymus and T cells with DiGeorge syndrome (rare) is called _____.
 Definition
SCID
Term
Two types of Severe Combined Immunodeficiency Disease: _____.
 Definition
X linked and Autosomal
Term
Autosomal SCID are half due to mutations in _______, leading to toxic accumulation during ______ maturation and proliferation.
 Definition
adenosine deaminase (ADA)

lymphocyte
Term
X-linked SCID is due to mutations in gene encoding _______ leading to loss of ______ receptors.
 Definition
common g chain

cytokine (for IL's)
Term
With Severe Combined Immunodeficiency Disease May present with graft-versus-host disease from maternal T cells – ________ after birth
 Definition
morbilliform rash
Term
Severe Combined Immunodeficiency Disease have _____ thymuses, lymph nodes, and mucosal lymphoid tissue.
 Definition
hypoplastic
Term
Severe Combined Immunodeficiency Disease presents when?
 Definition
first months
Term
Severe Combined Immunodeficiency Disease presents with?
 Definition
Diarrhea, otitis media, thrush, and respiratory infections
Term
Hyper-IgM syndrome is an example of ______ Deficiency.
 Definition
Combined
Term
Hyper-IgM syndrome is a failure to produce _________.
 Definition
isotype-switched high-affinity antibodies (IgG, IgA, IgE)
Term
Hyper-IgM syndrome exhibits normal to high levels of ______.
 Definition
IgM
Term
Hyper-IgM syndrome, 70% X-linked mutation in gene encoding _____ (T cell) and 30% autosomal, related to mutation in _____ (B cell)
 Definition
CD40L

CD40
Term
With Hyper-IgM syndrome and the failure of CD40-CD40L T-cell mediated activation of ______, pts are susceptible to _______.
 Definition
macrophages

intracellular pathogens and Pneumocystis jiroveci
Term
Secondary (Acquired) Immune Deficiencies are Much more common than the primary (inherited) disorders, encountered in patients with: ___________.
 Definition
Malnutrition
Infection
Cancer
Renal disease
SarcoidosisMalnutrition
Infection
Cancer
Renal disease
Sarcoidosis**************
Term
Most common cause of immune deficiency is _________.
 Definition
therapy-induced suppression of the bone marrow or of lymphocyte function
Term
Asprin is a _____.
 Definition
NSAIDS
Term
Asprin is a ______ derivative.
 Definition
Salicyclic acid
Term
2 major class of NSAIDS and ex of each: _______.
 Definition
Salicyclic acid, Asprin
Para-aminophenol, Acetaminophen
Term
NSAIDS act by inhibiting the _______.
 Definition
cyclooxygenase (COX) enzyme
Term
Inhibition of the COX enzyme by NSAIDS, blocks the production of _______ which mediate the pathogenesis of ______ and _____.
 Definition
prostaglandins

inflammation and fever
Term
Inhibition of COX-_ is responsible for the therapeutic benefits.
 Definition
2
Term
AA is cleaved from phospholipids by ______.
 Definition
Phospholipase
Term
AA is cleaved by _____ and _____.
 Definition
COX-1/2 & Lipoxygenase
Term
AA cleaved by Lipoxygenase generates ________.
 Definition
Leukotrines (bronchoconstirctors)
Term
COX-1/2 cleavage of AA leads to the production of _____, _____, and _____.
 Definition
Thromboxanes Prostaglandins Prostacyclins
Term
Loss of the therapuetic function of COX-1 leads to _____, _____, and _____ problems.
 Definition
Stomach (Bleeding/ulcers)

Hemostatis (loss of Thx, platelet aggregation)

Kidney (PG/PC)
Term
COX-1 is a _____ structure found where?
 Definition
Dimer

anchored to the membrane
Term
What are the two key active site amino acids that bind AA in COX-1?
 Definition
ARG120 and SER350
Term
In addition to the key amino acids, what motility also helps binding at the active site of AA by COX-1?
 Definition
Heme
Term
Asprin is a unique NSAIDS because it _______.
 Definition
Acetylates the serine residue on COX and therefore knocks it out permanetly
Term
Asprin is used to knock out COX permanently and deprive ______ cells of ______.
 Definition
platelets

Thromboxane A-2
Term
NSAIDS are what kinds of inhibitors?
 Definition
Competitive, bind at active site
Term
COX-_ is expressed constitutively and in all tissues.
 Definition
1
Term
COX2 is only expressed constitutively in: _______.
 Definition
Brain and parts of kidney
Term
COX-2 is involved in the _____, while COX-1 is involved in ______.
 Definition
Inflammatory processes

Housekeeping
Term
Side effects of NSAIDs because of the block of COX-1: _______ & _______.
 Definition
GI ulceration
Blockade of platelet aggregation (Inhibition of Thbx synthesis)
Term
Asprin is primarily a COX-_ inhibitor.
 Definition
1
Term
Naproxen (NSAID) is an inhibitor of _____.
 Definition
Almost COX-1 and 2 equally (little more COX-2)
Term
Selective for COX-2, ______.
 Definition
Celecoxib (Celebrex)
Term
How do COX-2 selective inhibitors work?
 Definition
Bind to side pocket in COX-2 that is not present in COX-1
Term
Celecoxib (Celebrex) was not withdrawn from the market, but other COX-2 selective inhibitors, ______ and ______, was.
 Definition
Vioxx*** and Bextra
Term
AA through the COX-2 pathway eventually produces a ____thrombotic Prostaglandin-I2.
 Definition
Anti
Term
The addition of Vioxx a COX-2 selective inhibitor, removes ______thrombotic.
 Definition
Antithrombotic
Term
In platelets, AA through COX-1 (which Asprin targets) produces ______, which is a _____thrombotic factor.
 Definition
TXA2

Prothrombotic
Term
The addition of Asprin through the blockage of COX-1 removes a ______thrombotic factor.
 Definition
Prothrombotic
Term
Vioxx puts you at risk for _____ because it removes an _______.
 Definition
MI

Antithrombotic
Term
Acetylsalicylic acid (_____)
 Definition
aspirin
Term
Traditional NSAID as a whole have functions: ______________.
 Definition
Anti-inflammatory
Analgesia
Antipyretic
Term
Asprin is the only NSAID that is used for ______ function.
 Definition
Antiplatelet
Term
All NSAIDs have an Anti-inflammatory function except for _______.
 Definition
Acetominophen
Term
NSAIDs achieve their Antipyretic by producing ____ which act on the Hypothalamus.
 Definition
PGs
Term
NSAIDs achieve their Analgesia function by ______.
 Definition
Lowering pain transmission
Term
All currently available NSAIDs inhibition _____ and _____ synthesis via inhibition of COX-1.
 Definition
TXs and PGs
Term
NSAIDs are ______ protein bound.
 Definition
Heavily, nearly all
Term
NSAIDs undergo ____ metabolism and many are excreted as _____ conjugates.
 Definition
hepatic

glucuronide conjugates
Term
NSAIDs have ____ half lives.
 Definition
Varying, some short, some long
Term
In order to prevent the GI toxicity associated with NSAIDs, a ______ analog, ________ is used to prevent ulceration and bleeding by acting as a _______.
 Definition
Prostagalandin E analog

misoprostol (Cytotec)

H2 antagonist (proton pump inhibitor)
Term
PGs are responsible for ______.
 Definition
Maintaining the integrity of the stomach
Term
In addition to GI toxicity, NSAIDs are also associated with _____ toxicity.
 Definition
Nephro
Term
Do hypersensitivities of NSAIDs exist?
 Definition
Yes
Term
Because of their high plasma protein binding and antiplatelet function, NSAIDs can _______ toxic effects.
 Definition
Blood dyscrasias
Term
NSAIDs can cause CNS effects of, _________ at _______.
 Definition
Dizziness, anxiety, tinnitus, and confusion

Large Doses (>>2 grams)
Term
______ NSAID is associated with heaptic toxicity.
 Definition
Acetaminophen
Term
Acetaminophen is what class of NSAIDs?
 Definition
Para-aminophenol derivatives
Term
Acetylsalicylic acid, (aspirin) serves as the prototype drug for the _______.
 Definition
nonnarcotic analgesics
Term
Acetylsalicylic acid, (aspirin) possesses functions of: _______ properties.
 Definition
analgesic, antipyretic, anti-inflammatory and antiplatelet
Term
Aspirin (acetylsalicylic acid) is a weak organic ____ with a pKa of ___.
 Definition
Acid

3.5
Term
The breakdown of acetylsalicylic acid (Asprin) into _____ and _____ often leads to the ____-like odor of old aspirin tablets.
 Definition
acetic acid and salicylate

vinegar
Term
Aspirin relieves _______ intensity pain such as headache, myalgia, arthralgia and other pains arising from integumental structures.
 Definition
low-to-moderate
Term
Aspirin ______ ______ body temperature.
 Definition
lowers elevated
Term
Salicylates Antipyretic effect?
 Definition
An effective reset the "thermostat"
Term
Salicylates Antipyretic mechanism?
 Definition
heat loss is enhanced as a result of cutaneous vasodilation and sweating
Term
Salicylates do/don't reduce exercise-induced hyperthermia.
 Definition
don't
Term
The salicylates are used in the treatment of _____ diseases, bc of their Anti-inflammatory Effects.
 Definition
rheumatic
Term
For salicylates, inhibition of ______ and _______ synthesis is the mechanism of anti-inflammatory action.
 Definition
prostaglandin

thromboxane
Term
For salicylates, higher doses are required for effective _____ action, as compared to ________ doses.
 Definition
anti-inflammatory (Need higher to get COX-2)

analgesic and antipyretic
Term
Aspirin does/doesn't inhibit the formation of leukotrienes via the lipoxygenase pathway.
 Definition
doesn't
Term
The antiplatelet effect of aspirin comes _______.
 Definition
Knock out of COX-1
Term
Aspirin's Antiplatelet Effect significantly reduces the incidence of ______ and ______ in patients at risk
 Definition
stroke and myocardial infarction
Term
At the lowest therapuetic doses, aspirin produces prolongation of _______, due to decreased ________.
 Definition
bleeding time

platelet aggregation
Term
Aspirin covalently ______ a serine at the active site of platelet cyclooxygenase, thereby reducing the formation of _______ which promotes platelet aggregation.
 Definition
acetylates

thromboxane A2
Term
Salicylates _______ respiration directly and indirectly.
 Definition
stimulate
Term
The direct stimulation by Salicylates on respiration is due primarily to an action on ______ which control rate.
 Definition
medullary respiratory neurons
Term
Respiratory ______ nearly always occurs at some stage of salicylate poisoning due to the direct stimulation of respiration.
 Definition
alkalosis
Term
The indirect effect on respiration by Salicylates is due to salicylate-induced _____________.
 Definition
uncoupling of oxidative phosphorylation
Term
High toxic doses of Salicylates _______ respiration.
 Definition
depressed
Term
If the toxic dose is high enough, the salicylates depress the medulla and cause ______ and ________.
 Definition
central respiratory paralysis and circulatory collapse (vasomotor depression)
Term
With salicylates SEVERE toxicity can cause respiratory _______ and metabolic ________.
 Definition
acidosis

acidosis
Term
In infants and children, toxicity has usually developed beyond the initial phase of respiratory _____ before they are seen by the physician (respiratory _____ is then more commonly observed in children).
 Definition
alkalosis

acidosis
Term
Dehydration may occur due to _______ through the lungs during hyperventilation and salicylate-induced ______.
 Definition
water loss

sweating
Term
________ is the main adverse effect associated with normal aspirin usage.
 Definition
Gastric intolerance
Term
Salicylates may induce _____ and _____ due to stimulation of gastric mucosal receptors and stimulation of the medullary chemoreceptor trigger zone.
 Definition
nausea and vomiting
Term
The mechanism of salicylate-induced gastric bleeding and damage also involves inhibition of _______ synthesis.
 Definition
prostaglandin
Term
_____ & ________, which are inhibited by salicylates serve as cytoprotective agents in the gastric mucosa.
 Definition
PGI2 and PGE2
Term
PGI2 and PGE2 serve as cytoprotective agents in the gastric mucosa by inhibiting _______, increasing ________, and enhancing __________.
 Definition
inhibit acid secretion, increase mucosal blood flow, and enhance secretion of protective gastric mucous.
Term
______ excretion is altered by salicylates.
 Definition
Uric acid
Term
Low doses of salicylates (2 g or less) decrease urate excretion by _________.
 Definition
competing with urate for the organic acid secretory mechanism.
Term
Inhibition of prostaglandin synthesis by salicylates can lead to decreased/increased renal blood flow.
 Definition
decreased
Term
In toxic doses (>>2 g per day), salicylates produce CNS _______, followed by ________.
 Definition
stimulation (including convulsions)

depression
Term
Primary CNS symptoms of toxic doses of salicylates: ___________.
 Definition
dizziness, tinnitus, high tone deafness
Term
Orally ingested salicylates are ______ absorbed, partly from the _____ and mostly from the _______.
 Definition
rapidly

stomach

small intestine
Term
Salicylates rapidly distribute throughout the body, primarily by _______.
 Definition
pH-dependent passive diffusion.
Term
Salicylate is _____ bound to plasma proteins.
 Definition
highly
Term
Metabolism of salicylates takes place primarily in the liver ______ system and mitochondria.
 Definition
liver microsomal system
Term
The primary metabolites of salicylates are conjugates with _______ and ______ acid.
 Definition
glycine (salicyluric acid)

glucuronic (glucuronide)
Term
Salicylate metabolism demonstrates _______ kinetics.
 Definition
biphasic
Term
For Salicylates, at high and toxic doses metabolism occurs according to _____ order kinetics, while at lower doses metabolism proceeds according to ____ order kinetics
 Definition
zero

first
Term
*The half-life for salicylate is _______ hours in low doses and ______ hours at high doses.
 Definition
3 to 6

15 to 30 (due to 0 order kinetics)
Term
Salicylate is excreted in the _____ as the free compound and as ______.
 Definition
urine

conjugated metabolites
Term
The amount of unchanged salicylate excreted may vary between 10% (_____ urine) and 85% (______ urine).
 Definition
acid

alkaline
Term
Excretion of the metabolites is pH _______.
 Definition
independent
Term
_______ of the urine markedly enhance salicylate clearance.
 Definition
Alkalinization
Term
Mild chronic salicylate intoxication occurring after repeated administration of high doses (>> 2g) is termed _______.
 Definition
salicylism
Term
In severe toxic overdoes of salicylates _____thermia is usually present and dehydration often occurs.
 Definition
Hyper
Term
Treatment of severe salicylate poisoning must be _______.
 Definition
immediate
Term
For severe salicylate poisoning, gastric lavage or induction of emesis will prevent further absorption if performed within a reasonable time after ingestion. ______ may be given to adsorb drug left in the stomach.
 Definition
Activated charcoal
Term
An association exists between the administration of aspirin to children with __________ and concomitant development of _______ with severe ______ and ______.
 Definition
acute febrile illness (influenza and chicken pox)

Reye's syndrome

severe hepatic injury and encephalopathy
Term
Acetaminophen (_____)
 Definition
Tylenol
Term
Acetaminophen (Tylenol) is an alternative to aspirin for ______ and ______ properties
 Definition
analgesic and antipyretic
Term
Acetaminophen (Tylenol) is ineffective as a ________agent and is not considered useful as sole long-term therapy in _______.
 Definition
anti-inflammatory

rheumatic disease
Term
Acetaminophen, in acute overdosage, acetaminophen can cause fatal _____.
 Definition
hepatic necrosis
Term
Unlike asprin Acetaminophen produces little or no effect on: ________.
 Definition
respiration, cardiovascular function, acid-base balance, platelet aggregation, or uric acid excretion, gastric irritation, erosion and bleeding characteristic of aspirin.
Term
Acetaminophen's half life is ______.
 Definition
1 to 4 hours (short)
Term
Acetaminophen's metabolism occurs by way of liver microsomal enzymes primarily by __________.
 Definition
the conjugating of glucuronic acid and sulfuric acid (as opposed to glycine with asprin).
Term
In acute overdose, acetaminophen produces a dose-_______, potentially fatal_______.
 Definition
dependent

hepatic necrosis
Term
Normally, acetaminophen is conjugated either as a ______ or a _______.
 Definition
sulfate

glucuronide
Term
Normally, acetaminophen is conjugated either as a sulfate or a glucuronide, but with toxic doses, this system is ______ and microsomal enzymes produce other metabolites which can bind _______ groups on cell constituents.
 Definition
saturated

sulfhydryl
Term
The toxic metabolites the build up following acute overdose or acetaminophen are normally inactivated by ______.
 Definition
glutathione
Term
If glutathione stores are depleted by large amounts of metabolites resulting from toxic doses of acetaminophen, then ______ damage ensues.
 Definition
hepatic
Term
The hepatotoxicity caused by acetaminophen is immediate/delayed.
 Definition
delayed
Term
In toxic overdose of acetaminophen, GI symptoms reside _____ hours after ingestion. However, after _____ hours, hepatic enzymes, bilirubin, and prothrombin time become abnormal as hepatic injury occurs.
 Definition
24-48

36-72
Term
Protection against hepatic damage from acetaminophen overdose may be obtained by early administration of _____ compounds, ________ (________drug name) to inactivate the toxic metabolites.
 Definition
sulfhydryl

N-Acetylcysteine (Mucomyst, Mucosol)
Term
N-Acetylcysteine (Mucomyst, Mucosol) is effective if given less than ____ hours after ingestion of toxic doses of acetaminophen.
 Definition
24
Term
Naproxen, an NSAID is unique in that it has a _______.
 Definition
long half life
Term
__________ (_________), is a new class of NSAIDs that are COX-2 SELECTIVE AGENTS.
 Definition
Celecoxib (Celebrex)
Term
Celecoxib exhibits ______ activity.
 Definition
anti-inflammatory, antipyretic, and analgesic activity
Term
The mechanism of action of Celecoxib is inhibition of ______ synthesis, primarily via inhibition of __________.
 Definition
prostaglandin (Not TX also)

cyclooxygenase-2
Term
Celecoxib does not inhibit the cyclooxygenase-_ isoenzyme.
 Definition
1
Term
Clinical trials indicate that Celecoxib appears to be as effective as other NSAIDS in treating _______ and ______.
 Definition
osteoarthritis and rheumatoid arthritis
Term
In short-term studies, celecoxib caused significantly fewer _______ than other NSAIDS and did not increase _______, consistent with a lack of COX-1 inhibition.
 Definition
gastrointestinal ulcers

bleeding time
Term
Celecoxib is ___% bound to protein
 Definition
97
Term
Celecoxib is metabolized hepatically by _________.
 Definition
cytochrome P450
Term
Celecoxib metabolites are excreted in _______.
 Definition
feces and urine
Term
Celecoxib half life: ______.
 Definition
11 hours (fairly long)
Term
Main adverse effect of Celecoxib?
 Definition
Prothrombotic effect: may increase the chance for MI in certain patients.
Term
THERAPEUTIC INDEX = _____.
 Definition
TD50 / ED50
Term
BS DRUGS NEED ______.
 Definition
HOST DEFENSE
Term
ANTAGONISM example: _______
 Definition
BACTERIOSTATIC + BACTERICIDAL
Term
Exception to the antagonism of BS + BC: ________.
 Definition
***PENICILLILN + CLINDAMYCIN
Term
ANTIBIOTIC COMBINATIONS advantages:_______.
 Definition
ENHANCE THERAPEUTIC (MUTATION): TB

DELAY RESISTANCE RELATED TOXICIT

DECREASE DOSE RELATED TOXICITY
Term
AMINOGLYCOSIDE + _________ can enhance be used to enhance cell penetration and extension to gram +.
 Definition
LOW DOSE PENICILLIN
Term
ERYTHROMYCIN spectrum: _______.
 Definition
+
Term
AMINOGLYCOSIDES spectrum: _______.
 Definition
- (+ also if combined with low dose penicillin)
Term
CLINDAMYCIN spectrum: _______.
 Definition
+/- (Broad)
Term
TETRACYCLINES spectrum: _______.
 Definition
+/- (Broad)
Term
CHLORAMPHENICOL spectrum: _______.
 Definition
+/- (Broad)
Term
NATURAL (INTRINSIC) RESISTANCE types: ________.
 Definition
NON - SUSCEPTIBLE METABOLISM

DESTROYS DRUG (ex. PENICILLINASE)

INABILITY OF DRUG TO PENETRATE
Term
Example of NON - SUSCEPTIBLE METABOLISM, NATURAL (INTRINSIC) RESISTANCe?
 Definition
FOLIC ACID AS PRE - FORMED VITAMIN
Term
ACQUIRED RESISTANCE types: _______.
 Definition
MUTATION
ADAPTATION: BIOCHEMICAL INDUCTION (LOW DOSE)
INFECTIOUS DRUG RESISTANCE
Term
INFECTIOUS DRUG Aquired RESISTANCE sources: _______.
 Definition
*R – FACTORS: CONJUGATION

BACTERIOPHAGES – TRANSDUCTION

TRANSPOSITION
Term
Conjugation Resistance is a big factor for __________.
 Definition
AMINOGLYCOSIDES
Term
Use ___ times the MIC.
 Definition
Four times
Term
SUPERINFECTION DEF: ___________
 Definition
REPLACEMENT (NEW) INFECTION
Term
CELEBREX (NSAID) is a ______ drug. So if you are allergic to it you will be sensitive to ______.
 Definition
Sulfa (-SO2-NH)

Sulfonamides
Term
Two main antibiotic missuses: ________.
 Definition
*UNTREATABLE INFECTIONS (VIRUS)

*FEVER OF UNDETERMINED ORIGIN
Term
SULFONAMIDES chemical group _______.
 Definition
SO2NH2
Term
SULFONAMIDE derivatives are made by attaching an R group to ______.
 Definition
the N of SO2-NH2
Term
No change in the ______ of SULFONAMIDES is tolerated.
 Definition
Benzene ring
Term
If the NH2 group of the other end of SULFONAMIDES (opposite of the SO2-NH2) is replaced by COOH, H, OH, alkyll ______.
 Definition
Activity is destroyed.
Term
Original SULFANILAMIDE drug (2 SULFANILAMIDEs linked): _______.
 Definition
PRONTOSIL (not used anymore)
Term
PRONTOSIL is a _____ drug and must be ______.
 Definition
pro

metabolized to active form
Term
PRONTOSIL is a prodrug that is metabolized into its active metabolite by _______, which cleaves _______ to release ________.
 Definition
Liver

The double bond between the two Nitrogen groups to release two molecules of sulfanilmide
Term
SULFANILAMIDEs are _______ inhibitors of ________.
 Definition
competitive

PABA (para-Aminobenzoic Acid)
Term
Sulfanilamides adhere to ________, the ________ concept.
 Definition
WOODS - FILES THEORY

ANTIMETABOLITE CONCEPT
Term
Sulfanilamides disrupt metabolic pathways by mimicking ______.
 Definition
PABA
Term
In order for Sulfanilamides to inhibit growth the organism must: ______.
 Definition
Not absorb FA (Folic Acid)
Not require an external source (FA)
Synthessize FA
Term
Sulfanilamides blocks the incorporation of _______ by the _______ enzyme.
 Definition
PABA

COUPLING enzyme
Term
COUPLING enzyme aka ____________.
 Definition
Dihydropteroate synthase
Term
RESISTANCE TO THE Sulfanilamides mechanisms: __________.
 Definition
1) DECREASED PERMEABILITY AND TRANSPORT 2) GENETIC CHANGES: COUPLING ENZYME (decreased affinity for Sulfanilamides and increased affinity for PABA) 3) Increased PRODUCTION OF PABA
Term
There exists different _______ of Folic Acid.
 Definition
Different oxidation
Term
In addition to different oxidation states ,different ______ can be linked to _______.
 Definition
methyl

N5, N10
Term
REACTIONS INVOLVING FH4: __________.
 Definition
Purine synthesis
Thymine synthesis*
Methionine synthesis*
Serine synthesis
Term
Sulfanilamides distribution: ________.
 Definition
ALL TISSUES: PLEURAL, PERITONEAL, SYNOVIAL, OCULAR FLUIDS, CSF
Term
Sulfanilamides: ______ plasma proteins.
 Definition
Highly bound
Term
What is active, bound or free drug?
 Definition
Free drug
Term
Sulfanilamides excretion: ________.
 Definition
Urine
Term
Sulfanilamides T1/2 is dependent on ______.
 Definition
Renal function
Term
For Sulfanilamides, does kidney function affect dosage?
 Definition
Yes, decrease with disease
Term
Sulfanilamides is metabolized by the _________ by ________.
 Definition
Liver

ACETYLATION
Term
Sulfanilamides once acetylated in the liver _______ function and ______ toxic potential.
 Definition
loses biological function but maintains toxic potenital
Term
Sulfanilamides solubility ______ in acidic urine and ______ in alkaline urine.
 Definition
Decreases

Increases
Term
A rare problem associated with Sulfanilamides and the kidneys is _________.
 Definition
CRYSTALLURIA HEMATURIA OBSTRUCTION
Term
CRYSTALLURIA HEMATURIA OBSTRUCTION following Sulfanilamides admin is treated with ________.
 Definition
Na bicarbonate
Term
TRISULFAPYRIMIDINES is a TRIPLE SULFONAMIDE and gets around the solubility issue with CRYSTALLURIA HEMATURIA OBSTRUCTION by _______.
 Definition
Combining 3 sulfa drugs so to lower their individual doses
Term
SULFONAMIDE main complication: ________.
 Definition
Hypersensitivity 10%
Term
HEMATOLOGICAL complications can arise from Sulfanilamides because _______.
 Definition
if a patient is deficient in G6PDH, there will be an increase in hemolytic reactions and anemia, bc they cannot reduce the GLUTATHIONE necessary for RBC structure.
Term
A rare, .1% side effect of Sulfanilamides is ________, resulting in ________.
 Definition
AGRANULOCYTOSIS

LEUKOPENIA
Term
Sulfanilamides can cause hemolysis because they are ______ drugs and ______ GLUTATHIONE.
 Definition
Oxidant

oxidize
Term
Acetylation of Sulfanilamides makes them more or less soluble, and therefore ________ CRYSTALLURIA.
 Definition
less

worsen
Term
Best way to prevent CRYSTALLURIA with Sulfanilamides is to __________.
 Definition
Drink lots of fluids
Term
Sulfanilamides have ______ half lives.
 Definition
LONG (T½ = 7 – 9 DAYS)
Term
Because of their long half lives, Sulfanilamides, can have ________, which is characterized as ________.
 Definition
STEVENS - JOHNSON SYNDROME

a HYPERSENSITIVITY RX, with ERYTHEMA, MULTIFORME, and BLISTERING OF MUCOUS MEMBRANES
Term
Sulfanilamides have GI complications of __________, resulting from __________.
 Definition
bowel bleeding

Reduced Vitamin K synthesis, required for the prothrombin factors, VII IX and X, the Sulfanilamides kill off the Vit K synthesizing bacteria of the bowel.
Term
Sulfonamides have a drug interaction with ______ in neonates where it ______.
 Definition
Bilirubin

displaces the bilirubin bound, called KERNICTERUS
Term
Bc of its high plasma binding Sulfonamides can elicit a __________ effect by displacing ____________, decreasing ______ synthesis, and inhibiting ________ metabolism.
 Definition
HYPOPROTHROMBINEMIC

BOUND WARFARIN

Vit K

Warfin
Term
Sulfonamides displace ______ drug and therefore its doses need to be lowered.
 Definition
THIOPENTAL ANESTHESIA
Term
Sulfonamides increase the half life of _______, by competing for _______.
 Definition
PHENYTOIN

Microsomal enzymes of the liver for metabolism
Term
Phenytoin- anti seizure medicine WIKI

half life increased by Sulfonamides
 Definition
Term
______ is an NSAID that has a sulfa group and therefore has cross reactivity with individuals who are allergic to Sulfonamides
 Definition
Celebrex
Term
Sulfonamides spectrum?
 Definition
Broad
Term
***Primary use of Sulfonamides?
 Definition
combined with TRIMETHOPRIM to treat UTI
Term
Sulfonamides used to treat: __________.
 Definition

*NOCARDIOSIS

*Shigella

*Chlamydia

*PNEUMOCYTIS JIROVECI (pneumonia)

*TOXOPLASMA
Term
Sulfanilamides solubility ______ in acidic urine and ______ in alkaline urine.
 Definition
Decreases

Increases
Term
A rare problem associated with Sulfanilamides and the kidneys is _________.
 Definition
CRYSTALLURIA HEMATURIA OBSTRUCTION
Term
CRYSTALLURIA HEMATURIA OBSTRUCTION following Sulfanilamides admin is treated with ________.
 Definition
Na bicarbonate
Term
TRISULFAPYRIMIDINES is a TRIPLE SULFONAMIDE and gets around the solubility issue with CRYSTALLURIA HEMATURIA OBSTRUCTION by _______.
 Definition
Combining 3 sulfa drugs so to lower their individual doses
Term
SULFONAMIDE main complication: ________.
 Definition
Hypersensitivity 10%
Term
HEMATOLOGICAL complications can arise from Sulfanilamides because _______.
 Definition
if a patient is deficient in G6PDH, there will be an increase in hemolytic reactions and anemia, bc they cannot reduce the GLUTATHIONE necessary for RBC structure.
Term
A rare, .1% side effect of Sulfanilamides is ________, resulting in ________.
 Definition
AGRANULOCYTOSIS

LEUKOPENIA
Term
Sulfanilamides can cause hemolysis because they are ______ drugs and ______ GLUTATHIONE.
 Definition
Oxidant

oxidize
Term
Acetylation of Sulfanilamides makes them more or less soluble, and therefore ________ CRYSTALLURIA.
 Definition
less

worsen
Term
Best way to prevent CRYSTALLURIA with Sulfanilamides is to __________.
 Definition
Drink lots of fluids
Term
Sulfanilamides have ______ half lives.
 Definition
LONG (T½ = 7 – 9 DAYS)
Term
Because of their long half lives, Sulfanilamides, can have ________, which is characterized as ________.
 Definition
STEVENS - JOHNSON SYNDROME

a HYPERSENSITIVITY RX, with ERYTHEMA, MULTIFORME, and BLISTERING OF MUCOUS MEMBRANES
Term
Sulfanilamides have GI complications of __________, resulting from __________.
 Definition
bowel bleeding

Reduced Vitamin K synthesis, required for the prothrombin factors, VII IX and X, the Sulfanilamides kill off the Vit K synthesizing bacteria of the bowel.
Term
The Sulfonamide, Sulfasalazine is used to treat ________ & _________.
 Definition
ULCERATIVE COLITIS

RHEUMATOID ARTHRITIS
Term
The Sulfonamide, Sulfasalazine is used to treat ULCERATIVE COLITIS using the _______ component and to treat RA using the ________ component.
 Definition
5 - ASA

SULFAPYRIDINE
Term
Sulfasalazine has an antiinflammatory component, ___________.
 Definition
5 -AMINOSALICYLIC ACID (5-ASA)
Term
Sulfasalazine is split at its _____ bond into two active components, _______ & ______.
 Definition
DIAZO BOND (double bond between two N's)

SULFAPYRIDINE & 5-AMINOSALICYLIC ACID
Term
Sulfonamides are administered _______.
 Definition
orally
Term
**Sulfonamides have a synergestic effect with __________.
 Definition
Antifolic agents
Term
All Sufa agents risk the development of ______ syndrome, especially those with _____, such as _______.
 Definition
STEVENS – JOHNSON SYN

long half lives

SULFADOXINE
Term
FH4 is used in the conversion of ______ to _____ for DNA synthesis.
 Definition
Uracil to Thymidine

(dUMP to dTMP)
Term
A methyl group from FH4 is required for the activation of ________, which is responsible for the __________.
 Definition
METHIONINE-tRNAF (inactive) -> FORMYL METHIONINE-tRNAF (active)

Initiation of protein synthesis
Term
________ is an example of a large molecule antifolate.
 Definition
Methotrexate
Term
Methotrexate's effect is due to the ________ theory.
 Definition
ANTIMETABOLITE theory
Term
Methotrexate is too ______ to be used as a __________.
 Definition
toxic

Antibacterial
Term
Methotrexate can be used in acute high doses to be used as a ________ agent and treat: _______.
 Definition
Antineoplastic agent

- ACUTE LYMPHOCYTIC LEUKEMIA
– CHORIOCARCINOMA
- BURKITT’S LYMPHOMA
Term
Methotrexate can be used in low dose chronic for treating: __________.
 Definition
PSORIASIS / R. ARTHRITIS

IMMUNOSUPPRESSION
Term
METHOTREXATE toxicity ______.
 Definition
TERATOGENIC
Term
High doses of METHOTREXATE used for cancer treatment toxicities: ________.
 Definition
**GI ulcers
**BONE MARROW DEPRESSION
**NEPHROTOXICITY
Term
High doses of METHOTREXATE used for cancer treatment can be fatal, unless treated with the antidote, ______.
 Definition
FOLINIC ACID
Term
Low doses of METHOTREXATE used for RA/PSORIASIS & Immunosuppresion treatment toxicities: ________.
 Definition
**LIVER (HEPATIC FIBROSIS / CIRRHOSIS) *LUNG (PNEUMONITIS - RARE)
**BONE MARROW / GI (ulcers) = RAPIDLY DIVIDING CELLS
Term
Chronic METHOTREXATE treatment is supplemented with _______.
 Definition
FOLIC ACID
Term
Acute METHOTREXATE treatment is supplemented with _______.
 Definition
FOLINIC ACID
Term
Two classes of Small Molecule Antifolates: __________.
 Definition
ANTI-MALARIAL- Pyrimethamine & Chloroguanide

ANTI-BACTERIAL- Trimethoprim
Term
SMALL MOLECULE ANTIFOLATES serve as ______.
 Definition
ANTIBACTERIAL AGENTS
Term
SMALL MOLECULE ANTIFOLATES' spectrum is decided by __________.
 Definition
the R1 and R2 groups
Term
SMALL MOLECULE ANTIFOLATES act as ANTIBACTERIAL agents through their ________.
 Definition
Inhibition of FOLATE REDUCTASE
Term
Chloroguanide is a _______ drug that must be __________.
 Definition
Small Molecule Antifolate antimalrial pro drug

be metablized into its cyclic form to become active
Term
F-> FH2 (enzyme?)
 Definition
DIHYDROFOLATE REDUCTASE
Term
FH2 -> FH4 (enzyme?)
 Definition
DIHYDROFOLATE REDUCTASE
Term
DIHYDROFOLATE REDUCTASE uses ______ to reduce F or FH2.
 Definition
NADPH
Term
Large molecule antifolates act at ____________.
 Definition
DIHYDROFOLATE REDUCTASE
Term
Small molecule antifolates act at ____________.
 Definition
DIHYDROFOLATE REDUCTASE
Term
Trimethroprim is a _______ type of drug and is good against _______.
 Definition
Small molecule antifolate

Bacteria
Term
Methotrexate is a _______ type of drug and is good against _______.
 Definition
Large molecule antifolate

Humans
Term
Pyrimethamine is a _______ type of drug and is good against _______.
 Definition
Small molecule antifolate

Malria
Term
The addition of _______ on Antifolates cause their inhibition of DIHYDROFOLATE REDUCTASE to _______.
 Definition
HYDROPHOBIC SIDECHAINS

Increase
Term
Main toxicity of small molecule antifolates: __________.
 Definition
MEGALOBLASTIC ANEMIA
Term
Which of the small molecule antifolates, cause MEGALOBLASTIC ANEMIA?
 Definition
PYRIMETHAMINE

TRIMETHOPRIM
Term
What are less toxic, large or small molecule antifolates?
 Definition
Small
Term
BACTERIAL RESISTANCE against small molecule antifolate arises from?
 Definition
INCREASE IN FOLATE REDUCTASE
Term
Sulfas prevent FH4 synthesis by ______.
 Definition
competing with PABA
Term
Antifolates prevent FH4 synthesis by ________.
 Definition
binding dihydrofolate reductase
Term
Synergestic effect occurs between Sulfas and________.
 Definition
Tyimethoprim (small molecule antifolate)
Term
For Sulfa + Tyimethoprim (small molecule antifolate) _______ organ is important because _____.
 Definition
Kindey

excretion
Term
Sulfa + Tyimethoprim (small molecule antifolate) toxicity: ________.
 Definition
**URINARY TRACT INFECTIONS
*PROSTATITIS
Term
In addition to Sulfa + Tyimethoprim, another synergistic effect exists for antimalarial- ________ + _______.
 Definition
PYRIMETHAMINE (Small Mol Antifolate)+ SULFADIAZINE
Term
Inhibitors of DNA Synthesis: ______.
 Definition
QUINOLONES, FLUOROQUINOLONES
Term
FLUOROQUINOLONES INHIBIT ________ OR ________.
 Definition
DNA GYRASE (TOPOISOMERASE II)

TOPOISOMERASE IV
Term
FLUOROQUINOLONES types: ____________.
 Definition
–**CIPROFLOXACIN (CIPRO®)
–**LEVOFLOXACIN (LEVAQUIN®)
Term
Inhibition of _________ by FLUOROQUINOLONES targets gram -.
 Definition
TOPOISOMERASE II (DNA GYRASE)
Term
Inhibition of _________ by FLUOROQUINOLONES targets gram +.
 Definition
TOPOISOMERASE IV
Term
EUKARYOTIC CELLS -> NO _______ (with respect to FLUOROQUINOLONES).
 Definition
DNA Gyrase
Term
FLUOROQUINOLONES are used in the treatment of: __________.
 Definition
*same as sulfa drugs
*URINARY TRACT PATHOGENS
*PROSTATITIS *SEXUALLY TRANSMITTED DISEASES
*GI AND ABDOMINAL INFECTIONS
*RESPIRATORY TRACT INFECTIONS (SERIOUS)

**BONE, JOINT AND SOFT TISSUE INFECTIONS
** Anthrax
Term
Problem with FLUOROQUINOLONES use?
 Definition
Been used extensively in CHICKEN / CATTLE FEED
Term
FLUOROQUINOLONES activity is decreased by _______.
 Definition
ACID PH
Term
*FLUOROQUINOLONES are metabolized by ________.
 Definition
LIVER
Term
FLUOROQUINOLONES, ________ decrease absorption, because they _________.
 Definition
Antacids

Chelate
Term
FLUOROQUINOLONES toxicity: ______.
 Definition
**GI
**CRYSTALLURIA (Rare)
** decrease CYT P450 ( therefore increase CAFFEINE, THEOPHYLLINE)
***TENDINITIS
***CARTILEGE DAMAGE
Term
Because of the ***CARTILEGE DAMAGE associated with FLUOROQUINOLONES, FLUOROQUINOLONES are _________.
 Definition
Not recommended for CHILDREN / FETUS / PREGNANCY
Term
URINARY ANTISEPTIC drug: ________.
 Definition
NITROFURANTOIN
Term
NITROFURANTOIN excretion?
 Definition
Rapidly, kidneys
Term
NITROFURANTOIN have no ________.
 Definition
systemic action
Term
NITROFURANTOIN is only used to treat ________.
 Definition
CHRONIC LOWER URINARY TRACT INFECTIONS
Term
NITROFURANTOIN is administered in ______.
 Definition
for MONTHS (14 DAY INTERVALS)
Term
NITROFURANTOIN are not to be used for individuals that _________.
 Definition
Have severe renal insufficiency
Term
NITROFURANTOIN spectrum: _______.
 Definition
Broad, many +/- but not P. AERUGINOSA, PROTEUS
Term
NITROFURANS side effects: ________.
 Definition
**GASTROINTESTINAL EFFECT
HEMATOLOGICAL REACTIONS
(HEMOLYTIC ANEMIA – if low in G6PDH)
Term
Three main FLUOROQUINOLONES side effects: _______.
 Definition
**GASTROINTESTINAL EFFECTS
**DAMAGE TO GROWING CARTILAGE
***TENDINITIS -> TENDON RUPTURE
Term
PENICILLIN structure is two rings: ________.
 Definition
Beta-Lactam Ring

Thiazolidine Ring
Term
PENICILLIN acidic or basic?
 Definition
Weak acid (COOH)
Term
Penicillins are formed by _______>
 Definition
Adding R groups to the NH2 of 6-aminopenicillanic acid
Term
PENICILLIN R group determines: ________.
 Definition
– ANTIBACTERIAL SPECTRUM
– ACID STABILITY
– STABLE TO LACTAMASE
Term
PENICILLIN G's problem of a short T1/2 was because it _______.
 Definition
Was rapidly cleared by the kidneys
Term
PENICILLIN G's short half life was solved by _________.
 Definition
Combining it with another acid to decrease its excretion
Term
PENICILLIN G's short half life was solved by Combining it with ______ or ________ to decrease its excretion.
 Definition
PROBENECID (increases urate excretion for gout treatment)
Term
PENICILLIN G ACID INSTABILITY made it unable to be ________.
 Definition
orally administered
Term
PENICILLIN G's ACID INSTABILITY problem was solved by the addition of ______.
 Definition
The addition of oxygen to its R group, PHENOXYACETIC ACID
Term
PENICILLIN G's problem of penicillin resistant staph was solved by _______.
 Definition
Adding a different R group and forming METHICILLIN
Term
PENICILLIN G's problem of a narrow spectrum (gram +) was solved by the addition of new R groups and formation of _______ and _______.
 Definition
AMPICILLIN

CARBENICILLIN
Term
_______ formed from Penicillin in the presence of ________, is used to treat Copper-Wilson;s disease.
 Definition
β – β - DIMETHYL CYSTEINE

Strong H+
Term
When PENICILLIN's beta lactam ring is broken it forms ______ and gains a free _______, which can react with _______ to form ________.
 Definition
PENICILLOIC ACID

FREE -COOH

Lysine on proteins

HAPTEN
Term
HAPTEN formation is an _________.
 Definition
Allergy complex
Term
PENICILLINS ARE toxicity?
 Definition
PENICILLINS ARE REMARKABLY NONTOXIC
Term
Although Penicillins may be relatively non-toxic they are relatively prone to __________.
 Definition
HYPERSENSITIVITY (10-15%)
Term
Lethal component of Penicillin HYPERSENSITIVITY?
 Definition
ANAPHLAXIS
Term
IMMEDIATE REACTION of HYPERSENSITIVITY to Penicillin occurs when? and is characterized as?
 Definition
Within MINUTES

REAL SERIOUS
Term
ACCELERATED REACTION of HYPERSENSITIVITY to Penicillin occurs when? and is characterized as?
 Definition
30 MINUTES – 48 HOURS (FLUSH, ITCH)
Term
DELAYED REACTION of HYPERSENSITIVITY to Penicillin occurs when? and is characterized as?
 Definition
SEVERAL DAYS TO SEVERAL WEEKS (ITCH, JOINT PAIN, FEVER)
Term
TREATMENT OF SEVERE penicillin HYPERSENSITIVITY REACTIONS: _______.
 Definition
**EPINEPHRINE
*DIPHENHYDRAMINE
Term
ANAPHYLAXIS of HYPERSENSITIVITY REACTIONS symptoms: _________.
 Definition
–***SUDDEN, SEVERE HYPOTENSION
–***RAPID DEATH
–***BRONCHOCONSTRICTION
–***SEVERE ASTHMA
Term
Narrow Spectrum Penicillins that are Gram +: ________.
 Definition
Penicillin G and Penicillin V
Term
Beta Lactamase RESISTANT PENICILLINS: _________.
 Definition
OXACILLIN
NAFCILLIN
DICLOXACILLIN
Term
Problem with the Beta Lactamase RESISTANT PENICILLINS (OXACILLIN, NAFCILLIN, DICLOXACILLIN)
 Definition
**NARROW SPECTRUM
Term
BROAD SPECTRUM PENICILLIN, _________ aka the amino penicilins.
 Definition
AMPICILLIN

AMINO penicillins
Term
AMPICILLIN is a broad spectrum penicillin, bc unlike other penicillins it covers gram __ also.
 Definition
gram -
Term
The broad spectrum penicillin, AMPICILLIN, is not active against _______ & ______.
 Definition
–**PSEUDOMONAS
–**KLEBSIELLA
Term
Broad spectrum Penicillins: __________.
 Definition
AMPICILLIN
AMOXICILLIN
BACAMPICILLIN
TICARCILLIN
PIPERACILLIN
Term
The broad spectrum penicillins disadvantage, __________.
 Definition
inactivated by β - LACTAMASES
Term
BACAMPICILLIN, the broad spectrum penicillin, works by ______.
 Definition
freeing AMPICILLIN, broad spectrum, after ingestion
Term
PIPERACILLIN & TICARCILLIN are used to treat ______ and _____, or just serious gram ___ infections.
 Definition
*EXCELLENT FOR PSEUDOMONAS
**PICK UP KLEBSIELLA

-
Term
Pseudomonas aeruginosa is treated using combination drug therapy of _______ or _______ + an _______ or _______.
 Definition
TICARCILLIN OR PIPERACILLIN (broad spectrum pencillins)


AMINOGLYCOSIDE OR FLUOROQUINOLONE
Term
PENICILLINS target the last enzyme in _______.
 Definition
CELL WALL SYNTHESIS
Term
___isomer is normal.
 Definition
L isomer
Term
D - CYCLOSERINE interferes with _______ by ________.
 Definition
cell wall synthesis

inhibiting Racemase and ligase preventing the formation of D-alanine-D-alanine
Term
In order to form the D- ALANYL – D – ALANINE from L - ALANINE for bacterial cell walls, two enzymes are used: ________.
 Definition
Racemase and ligase
Term
D - CYCLOSERINE is used for _______.
 Definition
Treating TB
Term
Pencillin inhibits the __________ reaction between _______ and _____ of cell wall synthesis.
 Definition
TRANSPEPTIDATION REACTION

D - ALANINE and GLYCINE
Term
Pencillin can inhibit the TRANSPEPTIDATION REACTION of gram_ bacteria.
 Definition
+
Term
Pencillin inhibits the transpeptidase reaction by _______.
 Definition
forming covalently bond to the enzyme
Term
PENICILLIN inhibits the transpeptidase reaction by mimicking _________.
 Definition
D - ALANYL – D - ALANINE
Term
In addition to binding and inhibting the transpeptidase reaction, penicillin also binds ________ and activates _______.
 Definition
PENICILLIN – BINDING PROTEINS

AUTOLYTIC ENZYMES
Term
β-LACTAMASE is located where for Gram +?
 Definition
Surface
Term
β-LACTAMASE is located where for Gram -?
 Definition
Between wall and membrane
Term
If penicillin binds PENCILLIN BINDING PROTEINS ________, it leads to _______.
 Definition
ACTIVATION OF AUTOLYTIC ENZYMES
&
INHIBITION of PEPTIDOGLYCAN SYNTHESIS
Term
CEPHALOSPORINS are similar in structure to _______.
 Definition
Penicillin
Term
Advantage of CEPHALOSPORINS over Penicillins?
 Definition
**LESS SUSCEPTIBLE TO PENICILLINASE
Term
CEPHALOSPORINS have a _______ spectrum.
 Definition
Broad
Term
CEPHALOSPORINS have a broad spectrum and are used especially to treat ______, _____, and ______
 Definition
– *PROTEUS (Broad Spectrum Penicillins innefective)
– *E. COLI (Broad Spectrum Penicillins innefective)
– *KLEBSIELLA
Term
CEPHALOSPORINS mechanism of action?
 Definition
Same as penicillin
Term
Problem with the second generation of CEPHALOSPORINS?
 Definition
BLEEDING PROBLEMS
&
DISULFIRAM (nausea following drinking) both because the presence of (MTT = METHYL - TETRAZOLE - THIOMETHYL)
Term
Each generation of CEPHALOSPORINS got better in which respect?
 Definition
Better against gram -
Term
Cephalosporin, ________, demonstrates excellent _______ and is not _______.
 Definition
CEFEPIME

*EXCELLENT CSF LEVELS

HYDROLYSED BY β - LACTAMASES
Term
CEFEPIME, a Cephalosporin, is used to treat: ___________.
 Definition
PSEUDOMONAS
ENTEROBACTERIACEAE
Term
In the third generation of Cephalosporins, they gained the ability to _______.
 Definition
Cross BBB
Term
CEPHALOSPORINS are all potentially _____ toxic.
 Definition
Nephrotoxic
Term
CEPHALOSPORINS are relatively non toxic, but should be cautious with _______ if ________.
 Definition
HYPERSENSITIVITY REACTIONS IF SEVERE RX TO PENICILLIN
Term
CEPHALOSPORINS are _____ antibiotics.
 Definition
B-lactam
Term
In addition to CEPHALOSPORINS, ______ & ______ are also beta-lactam antibiotics.
 Definition
CARBAPENEMS

MONOBACTAM
Term
The CARBAPENEM, Impienem, is a ______ inhibitor.
 Definition
Cell wall inhibitor (eta-lactam antibiotics)
Term
The Carbapenem,Impienem, has ______ spectrum.
 Definition
BROAD SPECTRUM
Term
The Carbapenem, Impienem, is used to treat: ______ infections.
 Definition
URINARY TRACT / LOWER RESPIRATORY
ABDOMINAL / GYN
Term
The Carbapenem, Impienem, must be administered with _______, because it _________.
 Definition
Cilastatin decreases renal tubular dihydropeptidase, which normally destroys Carbapenem
Term
The Carbapenem, Impienem, has a _____ with penicillin.
 Definition
cross allergy
Term
The Carbapenem, Meropenem, is similar to _______, but does not _______.
 Definition
Impienem

require Cilastatin
Term
The Carbapenem, Meropenem side effect?
 Definition
Cross allergy with Penicillin

(Carbapenem, which are Beta Lactam Antibio)
Term
Carbapenems (Impienem/Meropenem ) are used for ___________.
 Definition
Last resort therapy:
E. COLI
KLEBSIELLA PNEUMONIAE
Term
Monobactams is a type of _______.
 Definition
Beta-lactam antibiotic
Term
Monobactams are only used to treat _______.
 Definition
Only gram - rods (PSEUDOMONAS)
Term
Monobactams like other Beta-lactam antibiotics are ________.
 Definition
Resistant to many β - LACTAMASES
Term
Monobactams unique advantage over other Beta-lactam antibiotics?
 Definition
*CAN USE WITH PENICILLIN SENSITIVE PATIENT
Term
Beta-Lactamase Inhibitors: ________.
 Definition
Clavulanate (Clavulanic Acid)
Sulbactam
Tazobactam
Term
Beta-Lactamase Inhibitors are combined with ________.
 Definition
Penicillins
Term
Beta-Lactamase Inhibitors extend the coverage of Penicillins to ______.
 Definition
Gram - Rods
Term
Cycloserine is used to treat TB and it's MOA is inhibition of ________ and _______, leading to disruption of ______.
 Definition
Alanine Racemase

Alanine Ligase

Cell Wall Synthesis
Term
Vancomycin, mechanism of action: ________, which disrupts _______.
 Definition
*BINDS D – ALA – D – ALA

Cell wall synthesis
Term
Vancomycin used to treat ________, especially for _______ & ________.
 Definition
Gram +

MRSA, CLOSTRIDIUM DIFFICILE (Both Gram +)
Term
Vancomycin can be _____toxic.
 Definition
Ototoxic
Term
Vancomycin can cause __________ syndrome, which is _____________ and is caused by __________.
 Definition
RED MAN SYNDROME

*ERYTHEMATOUS, URTICARIA, *FLUSHING, *TACHCARDIA, HYPOTENSION

Histamine release from administered IV too quickly.
Term
A major problem for Vancomycin resistance of is ________, which lead to ________ resistant bacteria.
 Definition
ALTERED D – ALA – D - ALA TARGET

VRSA (STAPH. AUREUS)
Term
Vancomycin + _______ can have a synergestic effect on its Ototoxic property.
 Definition
Aminoglycosides
Term
_______ is similar to Vancomycin and acts as a __________ inhibitor.
 Definition
Teicoplanin

Cell wall syntehsis inhibitor
Term
Teicoplanin's main treatment use is for: __________.
 Definition
STEOMYELITIS, ENDOCARDITIS caused by Methicillin and Endocarditis caused by methicillin-resistant and methicillin-susceptible Staph, Strep, and Enterococci
Term
Teicoplanin can be combined with ______ when treating S. Aureus.
 Definition
AG
Term
Bacitracin disrupts _______, by inhibiting _______.
 Definition
Interferes with transport across the membrane for molecules to be used in cell wall synthesis. Therefore it is a membrane inhibitor not a cell wall inhibitor.
Term
Bacitracin is used to treat ________ and ________.
 Definition
Staph

Gram + infections that have not responded to other treatments
Term
Bacitracin can be administered Intrathecal/Intrapleurally to treat ________.
 Definition
Resistant Staph Meningitis/ Empyema (pus in the body cavity)
Term
Bacitracin possess serious _______toxicity, especially when given with ___________ and when administered _______, but not when administered _____.
 Definition
Nephrotoxicity

AG

Parenteral

Orally
Term
A clinical problem with Bacitracin is it becomes nephrotoxic if it ___________, therefore it is primarily administered ________.
 Definition
enter systemic circulation

Topically
Term
Polymyxin B Sulfate is a _________ (overall structure).
 Definition
Cyclic Poplypeptide Antibitoic
Term
Polymyxin B Sulfate is a ________ that disrupts ________.
 Definition
Cationic detergent

Cell membranes
Term
Polymyxin B Sulfate is administered ______.
 Definition
Topically
Term
Polymyxin B Sulfate exhibits extreme ______toxicity when administered ________.
 Definition
nephro

parentaly
Term
Polymyxin B Sulfate is used to treat _______ and ______.
 Definition
Resistant Gram -

Pseudomonas in CF
Term
Colistin sulfate is a ________ that disrupts ________.
 Definition
Cationic detergent

Cell membranes
Term
Colistin sulfate is used to treat ______.
 Definition
Gram -
Term
Colistin sulfate toxicity?
 Definition
Non unless administered parenterally (not recommended)
Term
Polymyxin B and Colistin Sulfate are old antibiotics that are being used to treat ________.
 Definition
Emerging multiresistant gram -
Term
Vancomycin, mechanism of action: ________, which disrupts _______.
 Definition
*BINDS D – ALA – D – ALA

Cell wall synthesis
Term
Vancomycin used to treat ________, especially for _______ & ________.
 Definition
Gram +

MRSA, CLOSTRIDIUM DIFFICILE (Both Gram +)
Term
Vancomycin can be _____toxic.
 Definition
Ototoxic
Term
Vancomycin can cause __________ syndrome, which is _____________ and is caused by __________.
 Definition
RED MAN SYNDROME

*ERYTHEMATOUS, URTICARIA, *FLUSHING, *TACHCARDIA, HYPOTENSION

Histamine release from administered IV too quickly.
Term
A major problem for Vancomycin resistance of is ________, which lead to ________ resistant bacteria.
 Definition
ALTERED D – ALA – D - ALA TARGET

VRSA (STAPH. AUREUS)
Term
Vancomycin + _______ can have a synergestic effect on its Ototoxic property.
 Definition
Aminoglycosides
Term
_______ is similar to Vancomycin and acts as a __________ inhibitor.
 Definition
Teicoplanin

Cell wall syntehsis inhibitor
Term
Teicoplanin's main treatment use is for: __________.
 Definition
STEOMYELITIS, ENDOCARDITIS caused by Methicillin and Endocarditis caused by methicillin-resistant and methicillin-susceptible Staph, Strep, and Enterococci
Term
Teicoplanin can be combined with ______ when treating S. Aureus.
 Definition
AG
Term
Bacitracin disrupts _______, by inhibiting _______.
 Definition
Interferes with transport across the membrane for molecules to be used in cell wall synthesis. Therefore it is a membrane inhibitor not a cell wall inhibitor.
Term
Bacitracin is used to treat ________ and ________.
 Definition
Staph

Gram + infections that have not responded to other treatments
Term
Bacitracin can be administered Intrathecal/Intrapleurally to treat ________.
 Definition
Resistant Staph Meningitis/ Empyema (pus in the body cavity)
Term
Daptomycin is similar to ______ and is used to treat ______ and _______.
 Definition
VANCOMYCIN

VANCOMYCIN- resistant Enterococci & Staph. Aureus
Term
Daptomycin's MofA: _______.
 Definition
Depolarizes membrane and causes K efflux
Term
Daptomycin is an alternative for _____.
 Definition
Vancomycin
Term
______ can diminish the effects of oral contraceptives.
 Definition
Ampicillin
Term
A site, aka __________.
 Definition
Aminoacyl Site
Term
The incoming _______ binds at the Aminoacyl Site.
 Definition
aminoacyl-tRNA
Term
The peptide linkage is formed between the ____ and ____ site.
 Definition
A and P
Term
The peptide linkage between the P and A is catalyzed by _____ enzyme.
 Definition
PEPTIDYL TRANSFERASE
Term
What is the name of the reaction when that follows the peptidyl transferase reaction and what happens?
 Definition
The translocation reaction

A site shifts to P side and next aminoacyl tRNA goes into A site
Term
Erythromycin is a _______ type of antibiotic.
 Definition
Macrolide
Term
A macrolide antibiotic is a ______ structure with ______ attached.
 Definition
14 carbon ring

2 sugars
Term
3 macrolide antibiotics: ________.
 Definition
Erythromycin
Clarithromycin
Azithromycin
Term
Erythromycin disrupts _______.
 Definition
Protein synthesis
Term
Erythromycin disrupts protein synthesis by ________.
 Definition
Inhibiting the incorporation of Amino Acids
Term
Erythromycin binds to ________ in order to inhibit protein synthesis.
 Definition
50s ribosome
Term
Erythromycin mainly inhibits the _____ step of protein synethesis. It also inhibits ______ (minor) and _______ by binding to ________.
 Definition
TRANSLOCATION STEP

Formation of initiation complex

Peptidyl Transferase by binding to 23S rRNA
Term
Erythromycin static/cydial?
 Definition
Static
Term
Erythromycin's activity is dependent upon?
 Definition
pH
Term
Erythromycin's activity increases at _____pHs.
 Definition
high
Term
Erythromycin's spectrum?
 Definition
Gram +
Term
In addition to Erythromycin's main targets of Gram +, what unique gram - can it also be used to treat?
 Definition
Legionella
Term
The spectrum of Erythromycin is dependent upon ______.
 Definition
Penetration into the cell
Term
Resistance to Erythromycin is through: __________.
 Definition
MUTATION – 50S (decrease binding)

EFFLUX BY ACTIVE PUMP

HYDROLYSIS OF MACROLIDES

INDUCED RESISTENCE – LOW DOSE
Term
Resistance to Erythromycin is cross resistance with ______.
 Definition
Other macrolides
Term
Why is the estolate form of Erythromycin no longer used?
 Definition
CHOLESTATIC HEPATITIS (10 - 12%)
Term
The free/sterate form of Erythromycin's main side effect is _______.
 Definition
**Epigastric Distress (Nausea, Vomiting, diarrhea)
Term
Erythromycin has good _______ and low ______ and becomes concentrated in _______.
 Definition
*GOOD BODY DISTRIBUTION *LOW IN CSF *CONCENTRATED IN LIVER
Term
Erythromycin *H. PYLORI (PEPTIC ULCERS)is excreted __________.
 Definition
In bile
Term
Erythromycin is excreted in the bile in its _____ form, because it is _________ in the liver.
 Definition
bile

concentrated in the liver
Term
_______ excretion is low in Ertyhtromycin.
 Definition
Kidney
Term
Ertyhtromycin dosage for kidney disease?
 Definition
same dose
Term
Ertyhtromycin dosage for liver disease?
 Definition
same dose (unless severely damaged)
Term
Ertyhtromycin is the drug of choice for: _______.
 Definition
Mycoplasma Pneumoniae
Legionella
Diphtheria
Term
Ertyhtromycin can be used as a substitute for _________.
 Definition
Penicillin
Term
Ertyhtromycin can be used as a substitute for penicillin for those who are allergic for _______ & ______ infections.
 Definition
Strep infections

Staph infections
Term
Clarithromycin is a _____ type of drug.
 Definition
Macrolide
Term
Clarithromycin is used to treat: __________.
 Definition
*H. INFLUENZE
*MYCOBACTERIUM AVIUM (AIDS PATIENT)
*H. PYLORI (PEPTIC ULCERS)
Term
Azithromycin is a ______ type of drug.
 Definition
Macrolide/KETOLIDE
Term
Azithromycin is used to treat: __________.
 Definition
MYCOBACTERIUM AVIUM (AIDS) (Just like Clarithromycin)

TOXOPLASMOSIS ENCEPHALITIS (AIDS)

URETHRITIS (CHYLAMYDIA TRACHOMATIS)
Term
Telithromycin is a macrolide that can be used to treat __________.
 Definition
COMMUNITY- ACQUIRED PNEUMONIA
Term
Macrolide main drug drug interactive?
 Definition
Decrease the activity of CYT P450
Increase the activity of other drugs
Term
Which macrolides decrease CYT P450 and which have no affect?
 Definition
Decrease:
Clarithromycin
Ertyhtromycin

AZITHROMYCIN
Term
Erythromycin has good _______ and low ______ and becomes concentrated in _______.
 Definition
*GOOD BODY DISTRIBUTION *LOW IN CSF *CONCENTRATED IN LIVER
Term
Erythromycin *H. PYLORI (PEPTIC ULCERS)is excreted __________.
 Definition
In bile
Term
Erythromycin is excreted in the bile in its _____ form, because it is _________ in the liver.
 Definition
bile

concentrated in the liver
Term
_______ excretion is low in Ertyhtromycin.
 Definition
Kidney
Term
Ertyhtromycin dosage for kidney disease?
 Definition
same dose
Term
Ertyhtromycin dosage for liver disease?
 Definition
same dose (unless severely damaged)
Term
Ertyhtromycin is the drug of choice for: _______.
 Definition
Mycoplasma Pneumoniae
Legionella
Diphtheria
Term
Ertyhtromycin can be used as a substitute for _________.
 Definition
Penicillin
Term
Ertyhtromycin can be used as a substitute for penicillin for those who are allergic for _______ & ______ infections.
 Definition
Strep infections

Staph infections
Term
Clarithromycin is a _____ type of drug.
 Definition
Macrolide
Term
Clarithromycin is used to treat: __________.
 Definition
*H. INFLUENZE
*MYCOBACTERIUM AVIUM (AIDS PATIENT)
*H. PYLORI (PEPTIC ULCERS)
Term
Azithromycin is a ______ type of drug.
 Definition
Macrolide
Term
Azithromycin is used to treat: __________.
 Definition
MYCOBACTERIUM AVIUM (AIDS) (Just like Clarithromycin)

TOXOPLASMOSIS ENCEPHALITIS (AIDS)

URETHRITIS (CHYLAMYDIA TRACHOMATIS)
Term
Types of Lincosamides: _______.
 Definition
Clindamycin

Clindamycin Phosphate
Term
Lincosamides (Clindamycin & Clindamycin Phosphate) disrupt?
 Definition
Protein synthesis
Term
Lincosamides (Clindamycin & Clindamycin Phosphate) bind?
 Definition
50S ribosome
Term
Lincosamides (Clindamycin & Clindamycin Phosphate) have an antagonist relationship with ________.
 Definition
Ertyhtromycin
Term
Lincosamides (Clindamycin & Clindamycin Phosphate) block the ______ step of protein synthesis.
 Definition
Translocation
Term
Lincosamides (Clindamycin & Clindamycin Phosphate) have a ______ spectrum?
 Definition
Broad
Term
Lincosamides (Clindamycin & Clindamycin Phosphate) have spectrum similar to ERYTHROMYCIN, _______, but in addition it also is useful for _______ infections.
 Definition
Broad Spectrum

**ANAEROBIC INFECTIONS
Term
Lincosamides (Clindamycin & Clindamycin Phosphate) can be used to treat severe anaerobic infections, such as ________.
 Definition
–** BACTEROIDES (RESP STRAINS)
–** BACTEROIDES (GI STRAINS)
Term
Clindamycin has cross resistance with _______.
 Definition
ERYTHROMYCIN (both bind 50s and block the translocation step)
Term
Clindamycin is metabolized by the __________.
 Definition
Liver
Term
Clindamycin is excreted by the _______.
 Definition
Kidney
Term
Clindamycin dose if liver disease?
 Definition
Decrease
Term
Clindamycin dose if kidney disease?
 Definition
Same dose
Term
If poor kidney function, Clindamycin's ________.
 Definition
T1/2 2.5->6
Term
Clindamycin's main toxicity?
 Definition
Selects for C. DIFFICILE and causes *PSEUDOMEMBRANEOUS ENTEROCOLITIS
Term
Clindamycin's main toxicity is it selects for DIFFICILE and causes PSEUDOMEMBRANEOUS ENTEROCOLITIS, this can be treated with either _______ or _______.
 Definition
METRONIDAZOLE

VANCOMYCIN
Term
Clindamycin is used for patients that are _________ and to treat ______.
 Definition
PENICILLIN (Just like ERYTHROMYCIN is)

Anaerobic infections
Term
Clindamycin has an antagonist affect with _________.
 Definition
ERYTHROMYCIN
Term
Tetracyclines are _______ spectrum.
 Definition
Broad
Term
Tetracycline drugs: __________.
 Definition
Doxycycline
Minocycline
Term
Tetracyclines bind ________ in order to distrupt.
 Definition
30s

Protein synthesis
Term
Tetracycline inhibit the __________.
 Definition
Attachment of the amino-acyl tRNA to "A" site
Term
Is there much difference between the spectrums of Tetracyclines?
 Definition
No
Term
Tetracylcine resistance is _______ mediated.
 Definition
Plasmid
Term
The main mechanisms of resistance against Tetracyclines is: __________.
 Definition
**+ENERGY – DEPENDENT increase in Efflux
**RIBOSOME PROTECTION PROTEINS (can't reach ribosome)
R+ Factor
Term
Tetracylcine pharmokinetic drawback is __________, except for ________.
 Definition
Incomplete absorption

Doxycycline
Term
Due to the incomplete absorption of Tetracylcines, complications: _______.
 Definition
1) *ERRATIC BLOOD LEVELS
2) *RESIDUAL IN GI TRACT -> NAUSEA / VOMITING / GI IRRITATION
3) *SUPERINFECTION
Term
Tetracylcines' poor absorption can be partially attributed to _______, including: __________.
 Definition
CHELATORS

MILK PRODUCTS
Iron
ANTACIDS FOR ULCERS
Term
Which Tetracyclines have long half life and which ones have short?
 Definition
Tetracycline short

Minocycline/Doxycycline Long
Term
The Tetracyclines, DOXYCYCLINE / MINOCYCLINE, have a longer half life and thus a lower ________, than Tetracycline.
 Definition
Renal Clearence
Term
Tetracyclines can develop ______ toxicity which means you have to discontinue use.
 Definition
GI irritation
Term
In addition to GI toxicity, Tetracyclines have: ________ toxicities.
 Definition
PHOTOSENSITIVITY
ONYCHOLYSIS (LOOSE NAILS) / PIGMENTATION OF THE NAILS
*RENAL TOXICITY
*TEETH: FLUORESCENCE DISCOLORATION
*Bone: deformity
DIZZINESS / VERTIGO – VESTIBULAR REACTIONS
*SUPERINFECTION
Term
The renal toxicity of Tetracyclines can cause __________, from the use of ________, which affects __________.
 Definition
Fanconi Syndrome

Outdated drugs

Proximal Tubules
Term
In patients with impaired kidney function, Tetracyclines __________, except for _________ and ________.
 Definition
Accumulate

Minocycline/Doxycycline
Term
Why do Tetracyclines accumulate in impaired kidneys, while Minocycline/Doxycycline do not?
 Definition
The have low renal clearence
Term
Tetracyclines can have toxic effects on the teeth by causing ______ and ______.
 Definition
FLUORESCENCE
DISCOLORATION
Term
Because of their ______ toxicity Tetracyclines, are not recommended for use in ________.
 Definition
Bone (deformities)

Children
Term
With _______ use, Tetracyclines can cause _______ superinfections.
 Definition
chronic

fungal
Term
Tetracyclines effect on teeth is ______ discoloration.
 Definition
Brown
Term
Tetracyclines static or cidal?
 Definition
Static
Term
Tetracyclines should not be combined with?
 Definition
Cidal agents
Term
Tetracyclines + ________ or ______ or _______ increases the metabolism of Tetracyclines and therefore __________.
 Definition
CARBAMAZEPINE
PHENOBARBITAL
PHENYTOIN
(Anti EPILEPSY agents)

Reduces their half lives
Term
Tetracylcines can diminish the effects of ________.
 Definition
Oral contraceptives (just like ampicillin)
Term
Tetracylcines is the drug of choice for: _____________.
 Definition
Diseases caused by Rickettsia (RMSF)
and Coxillea (Q Fever)

Lyme Disease (Borrelia)
Term
Lyme Disease Stages: __________.
 Definition
– 1) ERYTHEMA MIGRANS (RASH)
– 2) NEUROLOGIC DISEASE
– 3) CARDIAC DISEASE
– 4) ARTHRITIS
Term
______ or ______ can be used to treat Lyme Disease.
 Definition
Doxycycline (Tetracylcine) or Amoxicillin
Term
Tigecycline is a derivative of _______.
 Definition
Minocycline
Term
Tigecycline binds to _____.
 Definition
30S
Term
Tigecycline binds to 30S and blocks _______.
 Definition
Amino-Acyl tRNA binding
Term
Tigecycline spectrum?
 Definition
Broad
Term
Tigecycline toxicities: ________.
 Definition
NAUSEA, VOMITING, PHOTOSENSITIVITY, ELEVATED SERUM AMYLASE, HYPERBILIRUBINEMIA, ELEVATED BUN
Term
Tigecycline is not for use in __________.
 Definition
Children
Term
Tigecycline is used to treat complicated ________ and ______ infections.
 Definition
Skin/intra abdominal
Term
Tigecycline's main use is to treat _______.
 Definition
where other drugs have not been successful
Term
Cholramphenicol binds ______.
 Definition
50S
Term
Cholramphenicol inhibits ________.
 Definition
Peptidyl Transferase
Term
Cholramphenicol also prevents _______
 Definition
mRNA from binding 50S
Term
Cholramphenicol disrupts:________
 Definition
Protein Synthesis
Term
Cholramphenicol can react with the ________ of Eukaryotic cells.
 Definition
MT 80S
Term
Cholramphenicol spectrum?
 Definition
Broad
Term
Cholramphenicol resistance is primarily from?
 Definition
****INACTIVATION – ACETYLATION
Term
The resistance against Cholramphenicol by acetylation is gained via ______ from the ________?
 Definition
conjugation
R-Factor
Term
If Cholramphenicol is acetylated it becomes ________.
 Definition
Inactive
Term
The R-Factor Plasmid through acetylation grants resistance against: ______.
 Definition
CHLORAMPHENICOL, AMINOGLYCOSIDES (ALL), SULFONAMIDES
Term
The R-Factor Plasmid through adenylation grants resistance against: ______.
 Definition
Some AG
Term
The R-Factor Plasmid through phosphoryaltion grants resistance against: ______.
 Definition
Some AG
Term
The R-Factor Plasmid through transporters grants resistance against: ______.
 Definition
Tetracycline
Term
The R-Factor Plasmid through beta-lactamse grants resistance against: ______.
 Definition
Penicillins
Term
Cholramphenicol has good _______.
 Definition
CSF Levels
Term
Because of its good CSF levels Cholramphenicol can be used to treat ________.
 Definition
MENINGITIS
Term
Cholramphenicol is metabolized by the ________ into _______.
 Definition
Liver

Inactive Form
Term
With liver disease______ the dose of Cholramphenicol.
 Definition
Decrease
Term
With kidney disease ______ the dose of Cholramphenicol.
 Definition
Do nothing to
Term
Cholramphenicol is excreted by ______.
 Definition
kidneys
Term
Bc Cholramphenicol is a broad spectrum it can cause a _______.
 Definition
Superinfection
Term
Cholramphenicols are metabolized by the liver via ________.
 Definition
Gluccuornization
Term
Cholramphenicol in its Glucuronide form is ______.
 Definition
Inactive
Term
In neonates, Cholramphenicol toxicity can cause _______.
 Definition
***GRAY BABY SYNDROME
Term
In neonates, Cholramphenicol toxicity can cause ***GRAY BABY SYNDROME, which is a failure to form ________ with inadequate ________ leading to ________ and __________.
 Definition
GLUCURONIC ACID (used to metabolize)

RENAL EXCRETION

HYPOTHERMIA / ACUTE VASCULAR COLLAPSE (40 % FATAL)
Term
Cholramphenicol's main toxicity affects the _______ system by causing ________ or ________.
 Definition
Hematological

Transient bone marrow depression

Aplastic anemia
Term
Cholramphenicol transient bone marrow depression is dose unrelated/related and reversible/irreversible.
 Definition
related

reversible
Term
Cholramphenicol aplastic anemia is dose unrelated/related and reversible/irreversible.
 Definition
unrelated

irreversible
Term
Cholramphenicol aplastic anemia has an onset of _______.
 Definition
Very delayed, months after dose
Term
If the onset for Cholramphenicol aplastic anemia is ______ then the patient will survive.
 Definition
less than 2 months
Term
If the onset for Cholramphenicol aplastic anemia is ______ then the patient will die.
 Definition
Greater than 2 months
Term
Cholramphenicol toxicity can possibly be attributed to its effect on _______.
 Definition
Eukaryotic MT 50S
Term
Cholramphenicol has physical incompatibilities with: __________.
 Definition
TETRACYCLINES
POLYMYXIN B V
ANCOMYCIN
HYDROCORTISONE
Term
If cephalosporins fail to treat _________, Cholramphenicol can then be used to treat.
 Definition
*SALMONELLA (TYPHOID FEVER
Term
****If TETRACYCLINES fail to treat _________ or ________, Cholramphenicol can then be used to treat.
 Definition
*BRUCELLA (BRUCELLOSIS
****RICKETTSIAL DISEASES (RMSF)
Term
If β-LACTAMS fail to treat _________, Cholramphenicol can then be used to treat.
 Definition
*NEISSERIA MENINGITIDIS (Chorl has good CSF levels)
Term
Cholramphenicol has an antagonist interaction with?
 Definition
CHLORAMPHENICOL + ERYTHROMYCIN (COMPETE FOR 50S SUBUNIT)
Term
Cholramphenicol has an synergistic interaction with?
 Definition
CHLORAMPHENICOL + PENICILLINS
Term
Cholramphenicol has an overall drug interaction with other drugs because of its ________.
 Definition
Inhibition of CYT P450
Term
__________ and ________ decrease the half life of Cholramphenicol.
 Definition
PHENOBARBITAL / RIFAMPIN
Term
Aminoglycosides, Static or Cidal?
 Definition
Cidal
Term
Aminoglycosides structure?
 Definition
3 sugars linked
Term
Aminoglycoside drugs can be distinguished by their ______ ending.
 Definition
Mycin
Term
Aminoglycosides disrupt _______ by binding _______.
 Definition
Protein synthesis

30S (at 30S/50S interface)
Term
Aminoglycosides mechanisms of action for disrupting protein synthesis: ___________.
 Definition
Block initiation of protein synthesis

Block further translation and causing premature termination of the 70S complex

Incorporation of the wrong AA
Term
Aminoglycosides block the initiation of protein synthesis by inhibiting the binding of ______ to _______.
 Definition
*Met-amino-acyl tRNAs to ribosomes
Term
For Aminoglycosides penetration of the cell wall is dependent upon _______.
 Definition
Oxygen
Term
Aminoglycosides can get through the ________ using passive transport without Oxygen.
 Definition
Outermembrane
Term
Aminoglycosides can get through cell membrane into the cytoplasm using _________ with ________.
 Definition
Active transport

Oxygen
Term
Aminoglycosides are not effective against?
 Definition
Anaerobe bacteria
Term
Resistance against Aminoglycosides can be gained by a change in _____ structure.
 Definition
30S
Term
The main mechanism for resistance for Aminoglycosides is __________.
 Definition
***Acetylation provided by the R factor
Term
Acetylation of Aminoglycosides results in ______.
 Definition
Inactivation
Term
Aminoglycosides' absorption?
 Definition
Poor, cannot be administered orally
Term
Aminoglycosides are administered via?
 Definition
IV
Term
Aminoglycosides CSF concentration?
 Definition
Poor
Term
Aminoglycosides metabolism?
 Definition
None
Term
Aminoglycosides excretion?
 Definition
*100% kidneys
Term
Aminoglycosides, Static or Cidal?
 Definition
Cidal
Term
Aminoglycosides structure?
 Definition
3 sugars linked
Term
Aminoglycoside drugs can be distinguished by their ______ ending.
 Definition
Mycin
Term
Aminoglycosides disrupt _______ by binding _______.
 Definition
Protein synthesis

30S (at 30S/50S interface)
Term
Aminoglycosides mechanisms of action for disrupting protein synthesis: ___________.
 Definition
Block initiation of protein synthesis

Block further translation and causing premature termination of the 70S complex

Incorporation of the wrong AA
Term
Aminoglycosides block the initiation of protein synthesis by inhibiting the binding of ______ to _______.
 Definition
*Met-amino-acyl tRNAs to ribosomes
Term
For Aminoglycosides penetration of the cell wall is dependent upon _______.
 Definition
Oxygen
Term
Aminoglycosides can get through the ________ using passive transport without Oxygen.
 Definition
Outermembrane
Term
Aminoglycosides can get through cell membrane into the cytoplasm using _________ with ________.
 Definition
Active transport

Oxygen
Term
Aminoglycosides are not effective against?
 Definition
Anaerobe bacteria
Term
Resistance against Aminoglycosides can be gained by a change in _____ structure.
 Definition
30S
Term
The main mechanism for resistance for Aminoglycosides is __________.
 Definition
***Acetylation provided by the R factor
Term
Acetylation of Aminoglycosides results in ______.
 Definition
Inactivation
Term
Aminoglycosides' absorption?
 Definition
Poor, cannot be administered orally
Term
Aminoglycosides are administered via?
 Definition
IV
Term
Aminoglycosides CSF concentration?
 Definition
Poor
Term
Aminoglycosides metabolism?
 Definition
None
Term
Aminoglycosides excretion?
 Definition
*100% kidneys
Term
Aminoglycosides, Static or Cidal?
 Definition
Cidal
Term
Aminoglycosides structure?
 Definition
3 sugars linked
Term
Aminoglycoside drugs can be distinguished by their ______ ending.
 Definition
Mycin
Term
Aminoglycosides disrupt _______ by binding _______.
 Definition
Protein synthesis

30S (at 30S/50S interface)
Term
Aminoglycosides mechanisms of action for disrupting protein synthesis: ___________.
 Definition
Block initiation of protein synthesis

Block further translation and causing premature termination of the 70S complex

Incorporation of the wrong AA
Term
Aminoglycosides block the initiation of protein synthesis by inhibiting the binding of ______ to _______.
 Definition
*Met-amino-acyl tRNAs to ribosomes
Term
For Aminoglycosides penetration of the cell wall is dependent upon _______.
 Definition
Oxygen
Term
Aminoglycosides can get through the ________ using passive transport without Oxygen.
 Definition
Outermembrane
Term
Aminoglycosides can get through cell membrane into the cytoplasm using _________ with ________.
 Definition
Active transport

Oxygen
Term
Aminoglycosides are not effective against?
 Definition
Anaerobe bacteria
Term
Resistance against Aminoglycosides can be gained by a change in _____ structure.
 Definition
30S
Term
The main mechanism for resistance for Aminoglycosides is __________.
 Definition
***Acetylation provided by the R factor
Term
Acetylation of Aminoglycosides results in ______.
 Definition
Inactivation
Term
Aminoglycosides' absorption?
 Definition
Poor, cannot be administered orally
Term
Aminoglycosides are administered via?
 Definition
IV
Term
Aminoglycosides CSF concentration?
 Definition
Poor
Term
Aminoglycosides metabolism?
 Definition
None
Term
Aminoglycosides excretion?
 Definition
*100% kidneys
Term
Aminoglycosides' two main toxicities: ________.
 Definition
1) **8TH CRANIAL NERVE
2) **RENAL DAMAGE
Term
Aminoglycosides' ototoxicity manifests as _______ or ______ damage.
 Definition
Auditory

Vestibular
Term
Aminoglycosides' ototoxicity Auditory damage manifests as: ___________.
 Definition
TINNITUS
HIGH – FREQUENCY HEARING LOSS
Term
Aminoglycosides' ototoxicity Vestibular damage manifests as: ___________.
 Definition
VERTIGO
ATAXIA
LOSS OF BALANCE
Term
Aminoglycosides' ototoxicity is resultant of damage to ______ and ______.
 Definition
Hair cells

Auditory nerve
Term
What frequency of hearing goes first with Aminoglycosides' ototoxicity?
 Definition
High
Term
Aminoglycosides exhibit synergistic ototoxicity with _______.
 Definition
ETHACRYNIC ACID / FUROSEMIDE
(LOOP – INHIBITING DIURETICS)
Term
Aminoglycosides cause renal toxicity because _______, which ends up damaging _________.
 Definition
Aminoglycosides get trapped in lyososomes

Brush border
Term
Aminoglycosides exhibit synergistic renal toxicity with _______.
 Definition
Any drug that causes renal toxicity...

(don't know how impt:
VANCOMYCIN AMPHOTERTICIN B CEPHALOSPORINS: EXAMPLE KEFLIN POLYMYXIN B)
Term
Aminoglycosides are not to be administered to _______.
 Definition
Pregnant women
Term
Just as with Tetracyclines, Aminoglycosides have the potential to cause ______ syndrome, which results in _______.
 Definition
Falconi Syndrome (from outdated drugs)

Decrease in electrolyte reabsorption
Term
The Aminoglycoside, ___________, can be used to sterilize the bowel, because it ______.
 Definition
Neomycin

not absorbed orally
Term
Neomycin is administered _______, because _________.
 Definition
Topically

toxicity
Term
Gentamicin is a ________, it's structure is ________.
 Definition
AG

mixture of 3 sugars with 3 R groups
Term
Gentamicin is ineffective in treating _________, because ________.
 Definition
Anaerobes (AGs)

need O2 for entry
Term
Gentamicin spectrum?
 Definition
Gram -
Term
Gentamicin is the drug of choice for treating: ___________.
 Definition
*KLEBSIELLA PNEUMONIAE (HOSPITAL - ACQUIRED)

*PROTEUS MIRABILIS

**PSEUDOMONAS AERUGINOSA (resistance problem)
Term
Aminoglycosides are used to treat _______ bacteria.
 Definition
Enteric Bacteria- gram -
Term
Aminoglycosides are used to treat when suspension of _____ in combination with _________.
 Definition
SEPSIS

β – LACTAM
Term
β – LACTAM + Aminoglycosides has what three effects: ________.
 Definition
Extend coverage to gram +
Increase cidal activity
synerigism
Term
Aminoglycosides + β – LACTAM are used to treat sepsis and _______ and ________ infections.
 Definition
ENTEROCOCAL ENDOCARDITIS

STAPHYLOCOCCAL ENDOCARDITIS
Term
*GENTAMICIN + CEPHALOTHIN (KEFLIN® ) = ________
 Definition
– NEPHROTOXIC
Term
*GENTAMICIN + POLYMYXIN B: = ________
 Definition
– NEPHROTOXIC
Term
*GENTAMICIN + ETHACRYNIC ACID: = ________
 Definition
OTOTOXIC
Term
Spectinomycin can be used to treat _______ infections in substitute of __________.
 Definition
ACUTE GONOCOCCAL

**ALTERNATIVE: IF PENICILLIN ALLERGY / RESISTANCE
Term
Spectinomycin dosage?
 Definition
1 2gm dose
Term
Spectinomycin toxicity?
 Definition
– LOW RENAL TOXICITY (RARE)
– NO OTOTOXICITY

(Low compared to true AGs)
Term
Aminoglycoside, Cidal/Static?
 Definition
Cidal
Term
CHLORAMPHENICOL, Cidal/Static?
 Definition
Static
Term
TETRACYCLINES, Cidal/Static?
 Definition
Static
Term
TETRACYCLINES, bind _______.
 Definition
30S
Term
SPECTINOMYCIN, bind _______.
 Definition
30S
Term
ERTHYROMYCIN, bind _______.
 Definition
50S
Term
CLINDAMYCIN, bind _______.
 Definition
50S
Term
AMINOGLYCOSIDES, bind _______.
 Definition
30S
Term
Aminoglycosides have _______-dependent cidal activity.
 Definition
concentration
Term
Aminoglycoside's toxicity ______ is most critical.
 Definition
Time
Term
Aminoglycosides (specifically Gentamicin) are dosed?
 Definition
One large dose/day
Term
Dosage of Gentamicin (Aminoglycoside) varies with ___________.
 Definition
Renal Clearence (measured by Creatine clearance)

Decrease with lower clearance
Term
Streptogramins A & B (________ & ______)
 Definition
Quinupristin & Dalfoprisitin

"prisitin "
Term
Streptogramins A & B (Quinupristin & Dalfoprisitin) disrupt _______ by binding to _____.
 Definition
Protein synthesis

50S
Term
Streptogramins A & B (Quinupristin & Dalfoprisitin) mechanism of action is ______.
 Definition
Inhbiting peptidyl transferase
Term
Streptogramins A & B (Quinupristin & Dalfoprisitin) bind 50S at _______ and therefore _______.
 Definition
different sites on 50S

have synergestic effects
Term
Quinupristin & Dalfoprisitin is used to treat __________.
 Definition
**VANCOMYCIN RESISTANT ENTEROCOCCUS FAECIUM
Term
Quinupristin & Dalfoprisitin is reserved for _____.
 Definition
Serious infections
Term
Quinupristin & Dalfoprisitin (Streptogramins) drug-drug interaction?
 Definition
Inhibit CYT P450

Increase activity of other drugs
Term
Quinupristin & Dalfoprisitin (Streptogramins) toxicity?
 Definition
PHLEBITIS
HYPERBILIRUBINEMIA
Term
Oxazoladinones (Linezolid trade name) is used to treat ______ & ______.
 Definition
VANCOMYCIN - RESISTANT E. FAECIUM (VRE)

MRSA  VRSA  LRSA
Term
Oxazoladinones (Linezolid trade name) disrupts _______ and binds to _______.
 Definition
Protein synthesis

50S at A site
Term
Anti-Fungal Agents, Cell wall inhibitors: ______.
 Definition
Echinocandins
Term
Anti-Fungal Agents, Cell membrane inhibitors: ______.
 Definition
Polyenes (Nystatin)
Azoles
Term
Anti-Fungal Agents, nuclear division inhibitors: ______.
 Definition
Griseofluvin
Term
Anti-Fungal Agents, nucleic acid (DNA/RNA) inhibitors: ______.
 Definition
5-Flucytosine
Term
Nystatin is a _________, with a _______ structure, antifungal agent.
 Definition
Macrolide

*Polyene
Term
Does Nystatin posses antibacterial capabilities?
 Definition
No
Term
Nystatin main use is against ______.
 Definition
Canadidiasis
Term
Nystatin mechanism of action: _________.
 Definition
Increase the permeability of the membrane
Term
Nystatin Increases the permeability of the membrane, which causes the ________.
 Definition
loss of small molecules
Term
If __________, then the fungus is sensitive to Nystatin
 Definition
There are no sterols in media
Term
Nystatin has selective binding toxicity with ________, which affects ______ and ______.
 Definition
Lysosomal Membranes

RBC hemolysis

Kidney Damage
Term
Nystatin is administered _______.
 Definition
Topically
Term
Nystatin displays selective binding toxiciity when _______.
 Definition
Administered systemically
Term
Nystatin is used as an ointment to treat _______ and topically to treat _______ and orally to treat ______.
 Definition
Candida

Moniliasis skin

Moniliasis GI
Term
Overall Nystatin is used to treat ______ infections.
 Definition
Yeast
Term
Amphotericin B is a _________, with a _______ structure, antifungal agent.
 Definition
Macrolide with a *Polyene
Term
Amphotericin B binds to ________ causing ________ by ________.
 Definition
Fungal Membranes

Ions to leak out

Causing pores to form in the membrane
Term
Amphotericin B has selectivity of action against __________.
 Definition
Lysosomal Membranes
Term
Amphotericin B is administered ______.
 Definition
IV
Term
Amphotericin B toxicity with IV admin?
 Definition
Thrombophlebitis (WIKI inflammation of a vein caused by a blood clot.)
Term
Plasma Concentration target for Amphotericin B?
 Definition
2x needed to kill in vitro (vs 4x as with other antibiotics)
Term
Amphotericin B can be administered to treat _____________, but runs the side effect of developing __________.
 Definition
intrathecally

FUNGAL MENINGITIS

CHEMICAL MENINGITIS
Term
intrathecal (WIKI)
 Definition
introduced into or occurring in the space under the arachnoid membrane of the brain or spinal cord
Term
Amphotericin B's most common, but not most serious, toxicity is _________, resulting from a ________.
 Definition
Anemia

Decrease in the production of erythroid proteins
Term
Amphotericin B anemia toxicity is treated with _______.
 Definition
Epogen
Term
Amphotericin B's primary toxicity of concern is ________.
 Definition
Renal
Term
Amphotericin B's renal toxicity consists of: ____________.
 Definition
Increase BUN
Increase Serum Creatine
Decrease Urea Clearance
Decrease ability to concentrate
Deposition of Ca2+ in kindeys
Renal Tubular Alkalosis
Term
Amphotericin B is dosed _________.
 Definition
Low and
Term
Amphotericin B permanent kidney damage occurs when ______.
 Definition
5 gm cumulative
Term
Azoles are anti _______.
 Definition
Fungal drugs
Term
Azole drug name pattern?
 Definition
All end in azole
Term
Ketoconazole is administered?
 Definition
Orally
Term
Ketoconazole is used to treat _________ infections.
 Definition
Systemic
Term
***Ketoconazole's main issue is that it __________, which interferes with ________ and ________, leading to _________.
 Definition
Decreases CYT P450 activity

Interferes with steroid biosynthesis
Metabolism of other drugs
(gyneomastia)
Term
Ketoconazole mechanism of action?
 Definition
Inhibits ergosterol synthesis
Term
ergosterol is essential for _______.
 Definition
Fungal cell membranes
Term
Ketoconazole has partially replaced ________.
 Definition
Amphotericin B
Term
Itraconazole mechanism of action?
 Definition
Inhibits ergosterol synthesis
Term
Itraconazole is related to ______.
 Definition
Ketoconazole
Term
Itraconazole advantage over Ketoconazole?
 Definition
Less P450 problems
Term
Voriconazole main advantage, ______.
 Definition
Low P450 problems
Term
Voriconazole is used to treat ______.
 Definition
Aspergillosis
Term
Voriconazole mechanism of action?
 Definition
Inhibits ergosterol synthesis
Term
Miconazole mechanism of action?
 Definition
Inhibits ergosterol synthesis
Term
Miconazole is administered _______.
 Definition
Topically, too toxic to be systemically
Term
Miconazole is used topically to treat _______ and ___________.
 Definition
Candida Albicans (skin and vagina)

Tinea (ringworm)
Term
Miconazole is used to treat Tinea (ringworm) which includes: __________.
 Definition
PEDIS (FEET)
CRURIS (THIGHS, PERINEUM)
VESICOLOR (TRUNK)
Term
Which azole has good CSF penetration?
 Definition
Fluconazole
Term
Fluconazole mechanism of action?
 Definition
Inhibits ergosterol synthesis
Term
Fluconazole toxicity?
 Definition
Teratogenic (SKELETAL / CARDIAC DEFORMITIES)

**Rash (AIDS patient)
Stevens-Johnson Syndrome (AIDS)
Liver (AIDS)
Thrombocytopenia (AIDS)
Term
Fluconazole drug drug interaction: ________.
 Definition
*
Increase Phenytoin
Increase Sulfonylureas
Increase Warfarin
Increase Cyclosporin
Term
Main issue with Fluconazole usage?
 Definition
*Developing resistance
[ ESPECIALLY PROPHYLACTIC USE – TRANSPLANT / AIDS ]
Term
Fluconazole is used to treat: ________.
 Definition
*Oral/Esophageal Candidiasis (AIDS have issues, but still used)

*Cryptococcal Meningitis relapse after Amp B administration (Good CSF penetration, but AIDS patient trouble)

Coccidioidal Meningitis (Good CSF Pen)
Term
_________ is the broadest spectrum of all the Azoles?
 Definition
Posaconazole
Term
Griseofulvin mechanism of action?
 Definition
Inhibits fungal Mitosis
Term
Griseofulvin is used to treat: _______.
 Definition
Candida Albicans

Ringworm:
Microsporum
Trichophyton
Epidermophyton
Term
Griseofulvin route of administration?
 Definition
Oral*
Term
Griseofulvin absorption can be increased by?
 Definition
Taking with a fatty meal
Term
Griseofulvin treatment duration?
 Definition
4-6 weeks skin

Months for nails
Term
Griseofulvin treats ______ infections of the skin, hair, and nails.
 Definition
Dermatophyte
Term
Griseofulvin primary side effect is ________ and has a drug drug interaction with ______, which causes _________.
 Definition
Headache

Warfarin, increase its metabolism
Term
Griseofulvin's therapeutic effect is in treating ________ foot and fungal infections of the _____ & ______.
 Definition
Athlete's foot

skin/nails
Term
Griseofulvin is a Cidal/Static agent?
 Definition
Static (why takes so long))
Term
Flucytosine undergoes _____ in the fungal cell.
 Definition
Lethal synthesis
Term
Flucytosine undergoes Lethal synthesis in the fungal cell, converting it from the ______ form, Flucytosine, to the ________ form, ___________.
 Definition
prodrug

active/antimetabolite

5-Flurouracil
Term
What does 5-Flurouracil do?
 Definition
Inhibits Thymidylate synthesis disrupting nucleic acid synthesis
Term
5-Flurouracil (Flucytosine) is administered?
 Definition
Not as a single drug, but in combination with other drugs bc of resistance
Term
5-Flurouracil (Flucytosine) is combined with ______ or ______ because of emerging resistance problems.
 Definition
Amp B

Itraconazole
Term
5-Flurouracil (Flucytosine) is used mainly to treat __________.
 Definition
**Cryptococcosis
Term
5-Flurouracil (Flucytosine) admin route?
 Definition
Orally
Term
5-Flurouracil (Flucytosine) is more toxic in __________.
 Definition
**AIDS pts.
Term
5-Flurouracil (Flucytosine)'s main toxicity is _______.
 Definition
**Serious bone marrow depression
Term
Antifungals can be potentated by being combined with ________.
 Definition
Amp B
Term
Terbinafine ( a Allylamine) mechanism of aciton?
 Definition
Inhibits Squalene epoxidase (part of ergosterol synthesis
Term
Terbinafine ( a Allylamine) main side effect?
 Definition
*Change in tastes
Term
Terbinafine ( a Allylamine) is used to treat _______ & _______?
 Definition
ATHELETE’S FOOT, RINGWORM
Term
Terbinafine ( a Allylamine) and P450?
 Definition
No effect
Term
Echinocandins drugs?
 Definition
caspoFUNGIN
micaFUNGIN
anidulaFUNGIN
Term
Echinocandins mechanism of action?
 Definition
1,3- β-GLUCAN SYNTHASE INHIBITORS, which blocks cell wall synthesis
Term
Caspofungin is used to treat _________.
 Definition
Invasive Aspergillos

Mucocutaneous Candidas

Bld Stream Candidas
Term
Micafungin is used to treat __________.
 Definition
Esophageal Candididasis
(HIV + Patients)
Term
Anidulafungin is used to treat __________.
 Definition
Esophageal Candididasis
Term
Echinocandins toxicity?
 Definition
Very low
Term
Phenobarbital lowers the serum levels of ________, having an absorption effect.
 Definition
Griseofulvin
Term
**Griseofulvin induces ______ enzymes and leads to a decrease in ___________.
 Definition
Microsomal enzymes

Warfarin
Term
**Griseofulvin induces _______ which can cause Porphyria.
 Definition
δ - AMINOLEVULINIC ACID SYNTHETASE
Term
Major Agents of Anti-TB: ________.
 Definition
INH
Rifampin
Ethambutol
Pyrazinamide
Streptomycin
Term
For INH RESISTANCE <4%, TB Drug Regiment: __________.
 Definition
INH
Rifampin
Ethambutol
Pyrazinamide
Term
For INH RESISTANCE >4%, TB Drug Regiment: __________.
 Definition
Rifampin
Ethambutol
Pyrazinamide
Fluroquinolone
Term
Have to undergo DRUG REGIMEN (IRPE/S) if you meet any of these criteria: ___________.
 Definition
*PREVIOUS EXPOSURE TO DRUG - RESISTANT TB
*ASIANS & HISPANICS IF RECENT IMMIGRANTS
*MILIARY TB (NODULES & disseminated)
*TB MENINGITIS
*EXTENSIVE PULMONARY DISEASE
*HIV
Term
After treatment for TB, should see results within ______.
 Definition
2 weeks
Term
______ anti TB drug can be used prophylactically for those ________.
 Definition
Exposed to TB, but no infection
+ skin test, but no disease
HIV
Term
INH aka _______.
 Definition
Isoniazid
Term
Isoniazid must ______.
 Definition
be cleaved to active form
Term
Isoniazid, prodrug, is cleaved by _______ into _______, the active form of the drug.
 Definition
Catalase/Peroxidase

Isonicotinic Acid
Term
Isonicotinic Acid affects the TB cell by: ________.
 Definition
causing H2O2 to increase and target small molecules (Minor)

**Decreasing Mycolic Acid synthesis leading to cell wall synthesis
Term
INH disrupts ______.
 Definition
TB cell wall
Term
Mycobacterium have _____ in their cell walls.
 Definition
Mycolic acid
Term
Isoniazid spectrum?
 Definition
Only mycobacterium (TB)
Term
Isoniazid has a ______ problem.
 Definition
Resistance
Term
____ % of strains of TB are Isoniazid resistant in US.
 Definition
8-10%
Term
Isoniazid resistance is conferred by a mutation in _____ that results in _______.
 Definition
**Catalase, reduced activity
Term
Isoniazid resistance is conferred by an alteration in biosynthesis of _____ that results in _______.
 Definition
Mycolic acid

less inhibition
Term
**Isoniazid is metabolized by _________, which results in ________.
 Definition
Acetylation

Innactivation
Term
Isoniazid can be _______ into its active form ISONICOTINIC ACID or it can be ________ into its inactive form.
 Definition
catalase

acetylated
Term
Metabolism of Isoniazid varies between _______.
 Definition
Fast and slow acetylators
Term
Fast and slow acetylators is determined by _______.
 Definition
Race
Term
Fast acetylators: __________.
 Definition
Japanese
Inuit
Term
Acetylator activity is determined by levels of ________ enzyme.
 Definition
ACETYLTRANSFERASE
Term
Fast Acetylator genotype is inherited __________.
 Definition
Autosomal dominant
Term
Acetylation activity of Isoniazid affects ________ toxicity.
 Definition
Pyridoxine Deficiency
Term
Isoniazid can cause Pyridoxine Deficiency (especially ______ aceylators), because _______.
 Definition
slow

INH mimics vit B6
Term
**Isoniazid's two main toxicities: ___________.
 Definition
Peripheral Neuropathy

Hepatic
Term
**Isoniazid's Peripheral Neuropathy
toxicity is due to ________ and is treated by __________.
 Definition
Isoniazid and B6 structure similarity

Supplemental B6 (slow and fast acetyl)
Term
**The hepatotoxicity associated with Isoniazid use risk is increased with ______.
 Definition
Alcohol
Term
**The Isoniazid hepatotoxicity causes __________.
 Definition
Hepatitis (liver necrosis)
Term
*When administering Isoniazid, especially to _______, ________ needs to be monitored, especially if being taken with ______..
 Definition
children

Liver function tests

Rifampin
Term
INH is the only drug used for _______.
 Definition
PROPHYLAXIS for TB
Term
Ethambutol is a ________.
 Definition
Anti TB primary agent
Term
Ethambutol mechanism of action: _______.
 Definition
Inhibits Arabinosyl transferase (Cell wall inhibitor)
Term
Ethambutol spectrum?
 Definition
Only TB (mycobacterium)
Term
Ethambutol's main toxicity?
 Definition
**Retrobulbar Neuritis
Term
Ethambutol's main toxicity, Retrobulbar Neuritis, manifests as ________.
 Definition
Loss of visual acuity
Red Green color blindness
Term
Before giving Ethambutol you must?
 Definition
Test visual acuity and color blindness
Term
Rifampin is a ______ anti TB agent.
 Definition
Primary
Term
*Rifampin is used to treat: ______.
 Definition
Systemic TB
TB Meninigitis
MENINGOCOCCAL carrier state (cause of meningitis)
Term
Rifampin binds to _______ and blocks ________.
 Definition
DNA dependent RNA Pol

Transcription of RNA
Term
**Rifampin has no effect on __________.
 Definition
Mammalian DNA dependent RNA Pol
Term
Rifampin resistance comes from a mutation in _______.
 Definition
DNA dependent RNA Pol
Term
Rifampin has very good distribution especially _______.
 Definition
in CSF
Term
Rifampin toxicity overall is?
 Definition
Very low
Term
Rifampin Main toxicities: __________.
 Definition
***Hepatitis (rare, 1/30,000 have to worry when combined with INH)

**Orange stain teats/sweat (contacts)

**Flu like symptoms
Term
Rifampin is used to treat: __________.
 Definition
**Active TB

**Meningococcal

**TB meningitis

M. leprae
Term
Rifampin spectrum?
 Definition
Mycobacterium (leprae/TB)

Some gram +
Term
Rifampin's main drug drug interaction is __________, because it is a _____________.
 Definition
Decrease the half life of other drugs
*Oral contraceptives (double whammy bc also kills the bacteria used to regen)

Potent inducer of liver microsomal enzymes
Term
Pyrazinamide, primary or secondary?
 Definition
Primary
Term
Pyrazinamide mechanism of action?
 Definition
Lowers pH leading to no growth for mycobacteria

Disrupt mycolic acid
Term
Pyrazinamide is a _____.
 Definition
Pro drug
Term
Pyrazinamide main toxicity?
 Definition
**Hepatic
Term
Because of Pyrazinamide's liver toxicity you must _______.
 Definition
**Check liver function
Term
Pyrazinamide toxicity is ______.
 Definition
Tolerable for short durations
Term
Streptomycin, primary or secondary?
 Definition
Primary anti Tb
Term
Streptomycin main toxicities?
 Definition
**oto

**nephro
Term
Streptomycin class of drugs?
 Definition
AG
Term
Cycloserine primary or secondary?
 Definition
secondary antitb
Term
Cycloserine MOA: _______.
 Definition
Inhibits Racemase Ligase
Term
Cycloserine main toxicities: ____________.
 Definition
*Periph Neuropathy

*CNS dysfunction (depression etc.)

*Grand MAL/ Petit MAL convulsions (seizures), especially when combined with ALCOHOL*
Term
Cycloserine is not recommend for: _______.
 Definition
epileptics

depressed
Term
Cycloserine is administered with _______ in order to __________.
 Definition
B6

combat neurotoxicity
Term
Ethionamide is a ______ drug.
 Definition
Secondary AntiTB
Term
Ethionamide main toxicities: ________.
 Definition
*GI
*Depression
*Neurological (vision)
Term
Capreomycin is a ______ drug and _____ chemical class.
 Definition
Secondary AntiTB

Cyclic Peptide
Term
Capreomycin toxicity?
 Definition
Auditory

Renal
Term
Kanamycin is a ______ drug and _____ chemical class.
 Definition
Secondary AntiTB

AG
Term
Kanamycin toxicity?
 Definition
Nephro

Oto
Term
Which secondary AntiTB agent is rarely used?
 Definition
Aminosalicylic Acid (PAS)
Term
Aminosalicylic Acid (PAS) is rarely used as secondary AntiTB agent because of its ________.
 Definition
***GI problems

***Compliance (won't take bc of GI problems)

*Hypersensitivity
Term
Aminosalicylic Acid (PAS) MOA: ________.
 Definition
Inhibits coupling enzyme, disrupting Folic acid synthesis
Term
______ + _______ increases hepatoxicity for AntiTB drugs.
 Definition
*INH + Rifampin
Term
______ + _______ causes absorption problems for AntiTB drugs
 Definition
Rifampin + Aminosalicylic Acid (PAS)
Term
______ antiTB agent interferes with oral contraceptives use.
 Definition
*Rifampin
Term
_______ antiTB agent induces _________ leading to a ________ for other drugs, especially _________.
 Definition
*Rifampin

Liver microsomal enzymes

decrease in T1/2

Oral contraceptives
Term
**Dapsone is a _______ drug.
 Definition
Anti-Leprosay (Hansen's Disease)
Term
Dapsone is related to _____ drugs.
 Definition
Sulfa
Term
**Dapsone MOA:_________.
 Definition
*Inhibits Folic Acid Synthesis

*Competes with PABA
Term
Dapsone Toxicities: __________.
 Definition
GI

Blood Dyscrasis (Hemolytic anemia & Methemoglobinenmia)
Term
Dapsone causes Hemolytic anemia in ________.
 Definition
Pts deficient in G6PDH
Term
Dapsone causes Methemoglobinenmia by __________.
 Definition
Locking iron in Fe3+
Term
Anti-Leprosay is accomplished through ______ drug therapy.
 Definition
*combination
Term
_______ Anti-Leprosay drug is not used anymore because of it causing the birth defect _______.
 Definition
Thalidomide

Phocomelia
Term
Anti-Leprosay treatment minimum time frame ______.
 Definition
2 years
Term
MYCOBACTERIUM AVIUM COMPLEX is treated using ______ drug therapy.
 Definition
polypharmacy
Term
Most common species of Plasmodium?
 Definition
P. Vivax
Term
Most lethal species of Plasmodium?
 Definition
P. Falciparum****
Term
P. Falciparum fever pattern?
 Definition
Quotidian (Every day) or *Irregular
Term
P. Vivax ever pattern?
 Definition
Tertain

(EVERY OTHER, 3RD DAY)
Term
P. Malariae ever pattern?
 Definition
Quartan
(EVERY 3 DAYS) 4TH DAY
Term
P. Ovale ever pattern?
 Definition
Tertain

(EVERY OTHER, 3RD DAY)
Term
P. Falciparum causes ______ Tertain malaria.
 Definition
Malignant
Term
Liver dormant capable Plasmodium: ________.
 Definition
P. Vivax

P. Ovale
Term
**Strictly erythrocyte form plasmoidum: ________.
 Definition
P. Falciparum

P. Malariae
Term
P. Falciparum & P. Malariae, how many cycles of liver invasion?
 Definition
Just one
Term
P. Vivax & P. Ovale can relapse between blood and liver, what is the term for this?
 Definition
EXOERYTHROCYTIC
Term
Chloroquine is a ________ class of drug that targets ________ form.
 Definition
4-Aminoquinolones

BLOOD SCHIZONTICIDE

Blood
Term
4-Aminoquinolone class MOA: ____________.
 Definition
Inhibits DNA synthesis by intercalating

Build up free heme
Term
Chloroquine toxicity: _______.
 Definition
*Ocular toxic
Excreted in tears and reabsorbed by cornea

**Cardiac
Hypotension/Arrest

**RBC Hemolytic Anemia
Term
Chloroquine has a low _______.
 Definition
TI
Term
Chloroquine is contradicted for: ___________.
 Definition
**Retinal/Visual abnormalities

**Alcoholism

**Neurological Disorders (epilipsy)

***Hematologic Disorders (G6PDH Defic)
Term
Chloroquine targets _____ forms.
 Definition
Erythrocytic
Term
Chloroquine is uses: __________.
 Definition
*Suppressive Prophylatic

**8Terminates the acute attacks and cures Falciparum/Malariae

****Terminates acute attack, no cure Vivax/Ovale
Term
Chloroquine is not effective against _______.
 Definition
Liver stage
Term
Chloroquine *Suppressive Prophylatic treatment schedule?
 Definition
500mg/weekly 3 weeks before during and 3 weeks after
Term
Amodiaquine is a _______ class of drugs.
 Definition
4-Aminoquinolone
Term
Amodiaquine is similar to _______.
 Definition
Chloroquine
Term
Unlike Amodiaquine is not used _______.
 Definition
for Suppressive Prophylatic
Term
Why is Amodiaquine not used for Suppressive Prophylaxis?
 Definition
Toxicity increases with long term use
Term
Chloroquine MOA: __________
 Definition
(4-Aminoquinolone)
Inhibits DNA synthesis by intercalating

Build up free heme
Term
Amodiaquine MOA: __________
 Definition
(4-Aminoquinolone)
Inhibits DNA synthesis by intercalating

Build up free heme
Term
Artemisinin is used to treat _______.
 Definition
P. Falciparum
Term
Artemisinin toxicity?
 Definition
Teratogen
Term
Artemisinin MOA?
 Definition
Heme iron damage/ Alkylation
Term
Artemisinin is used ________.
 Definition
in combination, because of resistance concern
Term
Artemisinin is used in combination with
 Definition
CHLOROQUINE / AMODIAQUINE
SOME/ MEFLOQUINE
Term
Mefloquine is a _______ class of drug.
 Definition
4-Quinoline
Term
Mefloquine targets the _______ forms.
 Definition
Erythrocytic
Term
Mefloquine use?
 Definition
**Prophylaxis + Treatment of Chloroquine-resistant and multi-resistant Falciiparum

(Chloroquine is usually used for propholyatic)
Term
Mefloquine is propholyatic against?
 Definition
Probably all forms
Term
Mefloquine is contradicted in: _______.
 Definition
People with epilipsy
Mood disorders (causes risk of suicide/weird dreams)
Cardiac Conditions (exacerbates them)
Term
Quinine targets _____ forms.
 Definition
Erythrocytic
Term
Quinine MOA: ________.
 Definition
Inhibits DNA synthesis
Term
Quinine is a _______ Schizonticide for _______ parasites.
 Definition
blood

**all 4 plasmodium
Term
Quinine kills the gametophytes of __________.
 Definition
Vivax/ovale
Term
Quinine is/isn't effective against liver forms?
 Definition
isn't
Term
Problem with Quinine?
 Definition
*Resistance
Term
Quinine toxicity?
 Definition
**Cinchonism (overdose of Quinine)

**Blackwater Fever
Term
**Cinchonism (overdose of Quinine) manifests with: ___________.
 Definition
Ototoxic
GI Toxicity
Visual Toxicity (retinal toxicity, blindness)
Term
In addition to Cinchonism, Quinine can be toxic by causing _______, especially dangerous for __________.
 Definition
*Hypoglycemia

Pregnant women
Term
Quinine **Blackwater Fever has a ______% fatality rate.
 Definition
25-50%
Term
Quinine **Blackwater Fever manifests itself: ____________.
 Definition
Hemolysis
Renal Failure
G6PDH Deficiency
Term
Quinine is contradicted for: ________.
 Definition
G6PDH Deficiency
History of: Tinnitus, optic neuritis, myasthenia gravis
Term
Quinine main use it to treat ______.
 Definition
**Severe Falciparum
Term
Quinine can also be used to treat Falciparum that is _______ resistant.
 Definition
Chloroquine
Term
Quinidine vs. Quinine?
 Definition
Quinidine is more potent/toxic
Term
Primaquine is ______ class of drug.
 Definition
8-Aminoquinolines
Term
Primaquine is used to treat ______ form.
 Definition
Exo-Erythrocytic
Term
Primaquine is a _______ Schizonticide.
 Definition
Tissue
Term
****Primaquine can be combined with _______ to be used as a radical cure for _______.
 Definition
Chloroquine (get RBC form)

Vivax/ Ovale
Term
Primaquine is the primary _______ treatment.
 Definition
EXO – ERYTHROCYTIC
Term
Primaquine Toxicity: ________.
 Definition
**
Hemolytic Anemia (G6PDH)
Methemoglobinemia (G6PDH)
Term
______, _______, & __________ anti malarial agents that affect individuals with G6PDH deficiency.
 Definition
Primaquine
Quinine
Chloraquine
Term
Anti-folate anti-malaria drugs: ________.
 Definition
Biguanide
Primethamine
Term
Biguanide must __________.
 Definition
be metabolized in the liver from its pro form to active drug, dihydrotriazine
Term
Anti bacterial small molecule antifolate, __________.
 Definition
Trimethoprim
Term
Primethamine MOA: ________.
 Definition
Inhibits Dihydrofolate reductase
Term
Malaria can also be treated by ______ drugs which are also anti-bacterial.
 Definition
Sulfanomides
Term
Sulfanomides MOA: _________.
 Definition
Compete with PABA and inhibit the Coupling Enzyme (Dihydropteroate Synthase)
Term
Sulfanomides are _____ acting Anti-Malaria drugs.
 Definition
**Slow
Term
Atovaquone-Proguanil is used for _________.
 Definition
PROPHYLAXIS / TREATMENT of Chloroquine resistant Falciparum
Term
Atovaquone-Proguanil MOA: _________.
 Definition
Inhibits MT Electron Transport

Inhibits Folate Reductase
Term
Babesiosis is a rare severe ___________.
 Definition
Fatal dick borne disease
Term
Babesiosis affects __________.
 Definition
Elderly/Immunocompromised
Term
Babesiosis manifests: __________.
 Definition
Fever and *Hemolytic Anemia
Term
Babesiosis is treated with: __________.
 Definition
Quinine and Clindamycin
Term
Babesiosis is treated with Quinine and Clindamycin, MOA?
 Definition
Quinine: Inhibit DNA synthesis and Heme buildup

Clindamycin: inhibits translocation
Term
Amebicide that is a tissue and luminal (not reliable)?
 Definition
Metronidazole
Term
Metronidazole is a _____ drug and is _________.
 Definition
Prodrug

activated in anaerobic conditions
Term
Metronidazole is used to treat: _______.
 Definition
Ameba, Giardia, Trichomonas

Anaerobic Bacteria
Term
Indirect acting Luminal Amebicides: ___________.
 Definition
(affect the bacteria supporting it)
TETRACYCLINES
ERYTHROMYCIN
PAROMOMYCIN (also direct)
Term
Direct acting Luminal Amebicides: ___________.
 Definition
DIIODOHYDROXYQUIN
PAROMOMYCIN (also indirect)
DILOXANIDE FUROATE
Term
Tissue Amebicides: ___________.
 Definition
EMETINE / DEHYDROEMETIN
Chloroquine
Term
EMETINE / DEHYDROEMETIN toxicity?
 Definition
*Cardiac Toxicity
Term
Melarsoprol is used to treat: _______.
 Definition
African Sleeping Sickeness
Term
Melarsoprol toxicity?
 Definition
***Neurotoxin
Term
Why is Melarsoprol so neurotoxic?
 Definition
Arsenic
Term
Pentamidine is used to treat: ____________.
 Definition
Pneumocycstis Jiroveci (AIDS)
Trypansomes (sleeping sickness)
Term
Pentamidine toxicity?
 Definition
Severe hyptoension if IV too quickly
Term
SODIUM Stibogluconate used to treat?
 Definition
LEISHMANIASIS (TRANSMITTED BY SANDFLY)
Term
SODIUM Stibogluconate toxicity?
 Definition
EKG changes
Term
Nifurtimox/Benznidazole used to treat?
 Definition
CHAGA’S DISEASE (TRYPANOSOMIASIS)
Term
Giardia Treatment?
 Definition
**Metronidazole, NITAZOXANIDE

TINIDAZOLE less toxicity
Term
Vaginal TRICHOMONIASIS Treatment?
 Definition
Metronidazole
Term
Thiabendazole is used to treat?
 Definition
*Trichinella (Raw pork/beef)
NEMATODES
Term
Thiabendazole works by?
 Definition
Inhibiting Fumarate Reductase
Term
Albendazole is used to treat?
 Definition
NEMATODES
Term
Albendazole works by?
 Definition
Inhibiting Fumarate Reductase
Term
Mebendazole treats?
 Definition
Broad spectrum of NEMATODES
Term
Mebendazole MOA?
 Definition
Impairs GLC uptake by nematode leading to its paralysis
Term
Ascaris + Hookworms treated with?
 Definition
Mebendazole or Albendazole
Term
Thiabendazole is being replaced by?
 Definition
Mebendazole & Albendazole
Term
Praziquantal is used to treat?
 Definition
****Schistosomiasis and Liver Flukes

Broad spectrum
Term
Praziquantal MOA: __________.
 Definition
Increases permability, causing influx of Ca2+, Paralysis of Fluke
Term
Praziquantal is not to be used by __________.
 Definition
People breast feeding
Term
Praziquantal cross problem: __________.
 Definition
Ocular Cysticercosis (pork tapeworm)

kill tapeworm in eye -> ocular lesions
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