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Pharmacology chapters 33/34/36
for test 3
213
Medical
Undergraduate 4
04/06/2009

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Term
Bleeding disorders are caused by:
Definition
plasma protein defect; platelet abnormality; defect in platelet-endothelial cell interactions
Term
4 examples of coagulation protein defects leading to bleeding
Definition
True protein deficiency; inhibition of active region of protein; production of abnormal protein molecule; enhanced protein clearance
Term
Causes of decrease in platelet count:
Definition
thrombocytopenia; metastatic cancer; B12 deficiency; folate deficiency
Term
True platelet defects:
Definition
disorders of adhesion; acquired platelet disorders
Term
example of disorder of adhesion
Definition
von willebrand's
Term
examples of acquired platelet disorder:
Definition
liver disease; cardiopulmonary bypass; carious drugs
Term
to diagnose prolonged bleeding with normal platelet count look at:
Definition
vWF, platelet function, and for rare connective tissue disorders
Term
Examples of rare connective tissue disorders:
Definition
scurvy; ehlers-danlos syndrome
Term
scurvy
Definition
severe ascorbic acid deficiency
Term
ehlers-danlos syndrome
Definition
hyperplasticity of skin
Term
examples of screening tests for bleeding disorders:
Definition
aPTT (6-9 mins); PT (15-30 secs), platelet count; bleeding time; TCT
Term
screening test to determine bleeding disorders associated with intrinsic pathway
Definition
aPTT
Term
Prolonged PT and aPTT cause:
Definition
disseminated IV coagulation; liver disease; VitK deficiency; abnormal fibrinogen molecules
Term
Prolonged PT and aPTT must be treated by:
Definition
Heparin; LMWH; warfarin
Term
2 types of anticoagulation systems
Definition
Protein C and Protein S
Term
inherited disorders can form thrombi through:
Definition
antithrombin; protein c; protein s; FV leiden mutation; hyperhomocysteinemia; prothrombin 20210
Term
acquired disorders that increase risk of clotting in the heart are:
Definition
arrhythmias; AF (primary cause); placement of mechanical heart valve; prolonged bed rest; cancer
Term
types of drugs used in coagulation disorders:
Definition
anticoagulant inhibitors; antiplatelet inhibitors; thrombin inhibitors; fibrinolytic inhibitors
Term
medications reducing clotting and dissolving clots:
Definition
Heparin; LMWH; Hirudin; warfarin, aspirin, GP IIb/IIIa inhibitors; recombinant coag factor
Term
risk factors for development of venous thrombosis
Definition
primarily AF; placement of mechanicla heart valve; prolonged bed rest; protein C deficiency
Term
Heparin
Definition
parenteral anticoagulant; glycosaminoglycan made of D-glucosamine and iduronic acid; accelterates activity of ATIII to inactivate thrombin, Xa, and IXa
Term
Heparin used to treat:
Definition
DVT, PE, arterial and cerebral thromboembolism
Term
heparin contraindicated with:
Definition
bovine protein hypersensitivity; patients with HIT
Term
AEs of heparin
Definition
bleeding, bleeds from gums
Term
types of LMWH
Definition
enoxaparin, dalteparin, tinzaparin
Term
advantages of LMWH
Definition
doesn't require as rigorous medical monitoring of aPTT
Term
LMWH treats
Definition
DVT; lower chance of miscarriage; improve preganncy outcomes in women with APS
Term
2 classes of direct thrombin inhibitors
Definition
bivalent DTI and monovalent DTI
Term
Hirudin is:
Definition
a specific irreversible thrombin inhibitor; a 65 AA compound made in trace amounts by European medicinal leech
Term
Hirudin's action
Definition
anticoagulant; not inhibited by platelet factor IV; thrombin times exceed 200 seconds
Term
hirudin is used for
Definition
anticoagulation in patients with HIT
Term
Lepirudin (Refludan) is:
Definition
yeast-derived recombinant form of natural anticoagulant hirudin; identical to hirudin except leucine is substituted for isoleucine at N-terminal and sulfate group on tyrosine portion 63 is deleted
Term
action of Lepirudin (refludan)
Definition
direct inhibitor of free thrombin or thrombin entrapped w/in clots; trhombin times exceed 200 seconds, not inhibited by platlet factor IV
Term
Lepirudin (refludan) used for
Definition
anticoagulation in pts w/ HIT
Term
Lepirudin contraindicated:
Definition
in pts with hirudin hypersensitivity
Term
AE of lepiruding (refludan)
Definition
bleeding major risk! monitor aPTT
Term
Bivalirudin (angiomax)
Definition
specific reversible direct thrombin inhibitor; blocks circulating thrombin and clot-bound thrombin
Term
bivalirudin (angiomax) used for:
Definition
tx of pts with unstable angina undergoing percutaneous transluminal coronary angioplasty (PTCA)
Term
Bivalirudin (angiomax) is contraindicated in:
Definition
not be initiated in patients with baseline aPTT ratio of 2.5 more
Term
AEs of bivalirudin (angiomax)
Definition
bleeding major risk; discontinue breast-feeding
Term
examples of drugs that block thrombin-induced platelet activation:
Definition
Lepirudin and Eptifibatide
Term
Argatroban is:
Definition
a N2-substituted derivative of arginine
Term
Action of Argatroban
Definition
selective direct thrombin inhibitor, reversibly inhibits catalytic site of circulating thrombin adn clot-bound thrombin
Term
examples of selective thrombin inhibitors:
Definition
argatroban, bivalirudin, desirudin, lepirudin
Term
Use of argatroban:
Definition
HIT, end-stage renal disease, coronary artery thrombosis prophylaxis; percutaneous coronary intervention (PCI)in patients with or risk of HIT
Term
contraindication of argatroban
Definition
aPTT shouldn't exceed 100 seconds; hepatic impairment; breast feeding
Term
Melagatran and Ximelegatran (Exanta) is:
Definition
new anticoagulant molecules that directly inhibit thrombin
Term
Melagatran and Ximelegatran (Exanta) used for:
Definition
prevention of DVT and PE in patients going for surgery; prevention of stroke in pts with AF; secondary prevention of venous thromboembolism
Term
Melagatran and Ximelegatran (Exanta) AE:
Definition
increases liver enzymes
Term
Warfarin (coumadin) is:
Definition
oral coumarin anticoagulant; VitK is co-factor for carboxylation of glutamate residues to gamma-carboxyglutamates on N-terminal regions of VitK-dependent proteins; anticoagulant effects are steroselective; S-isomer of warfarin is 3-5x more potent than R-isomer
Term
Use of Warfarin:
Definition
prevent or treat thromboembolic disease
Term
contraindication for warfarin:
Definition
crosses placenta, so not in pregnancy!
Term
AE of warfarin:
Definition
fatal bleeding, necrosis of skin
Term
Mech of Action for Coumadin
Definition
inhibits syntesis of vitK-dependent coagulation factors II, VIII, IX, and C and antigoagulant proteins C and S; inhibits C1 subunit of vitK epoxide reductase which reduces regeneration of VitK epoxide; carboxylation allows coagulation proteins to have conformational change needed for activation
Term
INR
Definition
International normalized ration; PT ratio of test/control
Term
dosing of warfarin contingent upon:
Definition
INR; liver and kidney dysfunction; frequent blood tests to measure PT are taken to avoid risk of excessive thinning and bleeding
Term
drugs enhancing action of coumadin:
Definition
aspirin, tylenol, alcohol, ibuprofen, oxendrolone, vitamins, antibiotics
Term
drugs inhibiting coumadin:
Definition
metronidazole; fluconazole, tmp-smx; amiodarone, disulfiram; cimetidine
Term
types/locations of anti-platelet agents:
Definition
platelet membrane receptors; generated w/in platelet to interact with membrane receptor; generated w/in platelet to act w/in platelet
Term
this drug blocks the ADP receptor on teh platelet membrane:
Definition
clopidogrel
Term
Gp IIb/IIIa inhibitors at clinical trials:
Definition
tirofiban, eptifibatide, lambifiban, abciximab
Term
tirofiban
Definition
GP IIb/IIIa inhibitor that blocks ligand binding
Term
eptifibatide
Definition
GP IIb/IIIa inhibitor that blocks ligand binding
Term
Tirofiban (aggrastat)
Definition
a peptidomimetic, platelt GP IIB/IIIA inhibitor, IV form
Term
MA of tirofiban (aggrastat)
Definition
competitive inhibitor of GP IIb/IIIa; blocks cross-linking of activated platelets; inhibits ex vivo platelet aggregation induced by ADP
Term
Use of Tirofiban (aggrastat)
Definition
tirofiban plus heparin more effective than heparin alone for acute coronary syndromes; reduces ischemic complications associated with PCI
Term
CIs of tirofiban (aggrastat)
Definition
prolonged bleed time; inhibition of platelet aggregation
Term
AE of tirofiban (aggrastat)
Definition
bleeding secondary to drug-induced platelet dysfunction
Term
Epitifibatide (integrilin)
Definition
cyclic peptide; platelet GP IIb/IIIa inhibitor; given IV
Term
Epitifibatide (integrilin) action
Definition
blocks binding to VWF, fibrinogen, and other adhesion molecules to activated platelets; prevents platelet aggregation regardless of agonist involved
Term
Epitifibatide (integrilin) use
Definition
pts undergoing PCI; tx of unstable angina; non-Q-wave MI
Term
Epitifibatide (integrilin) contraindications and AEs
Definition
bleed time prolongation; ex vivo aggregation induced by ADP and other agonists; bleeding secondary to induced platelet dysfunction
Term
Lamifiban
Definition
blocks platelt GP RECEPTOR of Ib/IIIA; used for unstale angina, prolongs bleeding, investigational
Term
abciximab (reopro)
Definition
1st FDA approved platelet GP IIb/IIIa inhibitor, IV injection
Term
abciximab (reopro) action:
Definition
blocks binding of VWF, fibrinogen, and other adhesion molecules to activated platelets
Term
abciximab (reopro) use:
Definition
PCI (like angioplasty, atherectomy, stent placement); use with aspirin and heparin lowers acute MI
Term
abciximab (reopro) AE and CI:
Definition
bolus dose is rapidly bound to platelet receptors and increases mediab bleeding time for 5-30 minutes; 2 hours after bolus dose over 80% of GP IIb/IIIA receptors are blocked and platelelt aggregation is nonexistent; increased risk of bleeding secondary to drug-nduced platelet dysfunction
Term
abciximab (reopro) AE and CI:
Definition
bolus dose is rapidly bound to platelet receptors and increases mediab bleeding time for 5-30 minutes; 2 hours after bolus dose over 80% of GP IIb/IIIA receptors are blocked and platelelt aggregation is nonexistent; increased risk of bleeding secondary to drug-nduced platelet dysfunction
Term
phosphodiesterase inhibitors:
Definition
dipyridamole (persantine) and cilostazol (pletal)
Term
dipyridamole (persantine)
Definition
vasodilator and blocks adenosine uptake and cGMP phosphodiesterase activity
Term
cilostazol (pletal)
Definition
promotes vasodilation adn blocks platelet aggregation
Term
dipyridamole (persantine)
Definition
non-titrate coronary vasodilator that also inhibits platelet aggregation
Term
dipyridamole (persantine) action
Definition
increases coronary blood flow by selectively dilating small resistance vessles that supply the heart; does not dilate coronary blood vessels in ischemic area
Term
dipyridamole (persantine) use:
Definition
ineffective as antithrombotic for patients with acute MI, DVT, or TIAs; combo with warfarin prevents thrombosis in patients with valve disorders; combo with aspirin is approved for stroke prophylaxis
Term
dipyridamole (persantine)CI:
Definition
not use in pts with hypotension; induces orthostatic hypotension, may exacerbate angina due to vasodilatory effects, elevated hepatic enzymes
Term
Cilostazol (Pletal)
Definition
platelet aggregation inhinitor with vasodilating activity; has antithrombotic, antiplatelelt, and vasodilatory actions
Term
Cilostazol (Pletal) use
Definition
peripheral arterial disease in pts with diabetic neruopathy; redces leg pain due to poor circulation (intermittent claudication)
Term
Cilostazol (Pletal) CIs:
Definition
hemostatic disorders; active pathologic disorders - GI bleeding, retinal bleeding, retroperitoneal bleeding, intracranial bleeding
Term
1-fibrinolytic activators
Definition
thrombolytic agents that lyse thrombi; examples are the "plase"es and tPA and streptokinase and urokinase
Term
anistreplase
Definition
parenteral thrombolytic agent, complex consisting of streptokinase and human lysplasminogen
Term
anistreplase action
Definition
acylation of this complex inhibits its lyses coronary arterial thrombi; degradation by endogenous fibrinolysis inhibitors BUT its fibrin-binding activity is unaffected
Term
anistreplase use:
Definition
reduces infarct size; improves ventricular funtion post-AMI; reduces mortality associated with AMI
Term
anistreplase CIs
Definition
bleeding; hazardous in patients with AFib, Atrial flutter, cardiac disease (increases cerebral embolism)
Term
Alteplase (Activase)
Definition
parenteral thrombolytic agent that exerts action on endogenous fibrinolytic system to convert plasminogen to plasmin
Term
Alteplase (Activase) use:
Definition
lysis of PTE; lysis of acute coronary arterial thromboembolism; for tx of AMI with ST-elevation
Term
Alteplase (Activase) CI and AE
Definition
hazardous in patients with AFib, atrial flutter, cardiac disease; minor bleeding or major internal bleeding
Term
Reteplase (retavase)
Definition
recombinant plasminogen activator (r-PA) that is a fibrin-selective thrombolytic agent
Term
Reteplase (retavase) use:
Definition
tx of AMI; improvement of ventricular fonction post-AMI; reduction of incidence of CHF; reduction of mortality associated with AMI
Term
Reteplase (retavase) CI:
Definition
bleed; AFib; atrial flutter; cardiac disease;
Term
Reteplase (retavase) AE:
Definition
N/V; hypotension; fever
Term
Tenecteplase (TNKase)
Definition
modified form of tPA that binds to fibrin and converts plasminogen to plasmin; has increased resistance to PTA-1
Term
Tenecteplase (TNKase) use:
Definition
tx of AMI; thrombolytic agent
Term
Tenecteplase (TNKase) CI and AE:
Definition
Afib, Aflutter, cardiac disease, hypersensitivity to alteplase variants; causes bleeding
Term
Tenecteplase (TNKase) CI and AE
Definition
Afib, Aflutter, cardiac disease, hypersensitivity to alteplase variants; causes bleeding
Term
2-fibrinolytic inhibitors:
Definition
aminocaproic acid (EACA) and Tranexamic acid
Term
Aminocaproic acid (EACA)
Definition
similar to amino acid lysine; synthetic inhibitor of fibrinolysis; competitively inhibits plasminogen activation; don't use with patients iwth DIC
Term
tranexamic acid:
Definition
analog of aminocaproic acid; not present in USA, shoudln't be used with patients with DIC
Term
Aminocaproic acid (Amicar)
Definition
inhibits fibrinolysis by binding to lysine-binding sites w/in plasminogen/plasmin molecule blocking the plasmin's activity; decreases tuberculin reaction in pts sensitivie to tuberculin
Term
Aminocaproic acid (Amicar) use:
Definition
tx of hemorrhage caused by hyperfirinolysis; tx of systemic and urinary hyperfibrinolysis
Term
Aminocaproic acid (Amicar) CI and AE
Definition
not for pts with DIC or active intravascular clotting; hypotension and sinus bradycardia
Term
Tranexamic acid (cyklokapron)
Definition
10x more potent than aminocaproic acid; cometitive inhibitor of plasminogen activation
Term
Tranexamic acid (cyklokapron) use:
Definition
tx of primary menorrhagia; reduce or prevent hemorrhage in pts with hemophelia A or B; bleeding prophylaxis; dysfunctional uterine bleeding
Term
Tranexamic acid (cyklokapron) CI and AE:
Definition
renal insufficiency, subarachnoid hemorrhage, acquired defective color vision; increased risk of clot formation when adminitered with clotting factors (rFVIIa)
Term
Aprotinin (Trasylol)
Definition
serin protease inhibitor discontinued in US; affects finrinolysis in 2 steps by inhiiting kallikrein-kinin system and inhibiting plasmin-induced lysis of fibrin by reducing conversion of plasminogen to plasmin
Term
Aprotinin (Trasylol) use
Definition
reduces surgical bleeding; for pts non-responsive to thrombolytic therapy; during repeat CABGs
Term
Aprotinin (Trasylol) CI and AE
Definition
increased risk for renal toxicity and dialysis perioperatively; may increase mortality
Term
Therapeutic strategies & mechanisms of actions of NSAIDs:
Definition
anti-inflammatory, analgesic, antipyretic, antiplatelet
Term
Aspirin use
Definition
tx moderate pain; inhiits COX, inhibits platelet aggregation prevents arterial and venous thormbosis
Term
Aspirin AE
Definition
GI disturbance, platelet dysfunction
Term
Acetaminophen (Acephen)
Definition
para-aminophenol analgesic, active metabolite of phenacetin, weak COX1 and COX2 inhibitor in peripheral tissues and COX3 in CNS, interacts with NOS2 gene
Term
Acetaminophen (Acephen) use:
Definition
weak anti-inflammatory properties, relieves pain, reduces fever, does not relieve redness, stiffnes, or swelling form RA, does tx mild arthritis
Term
Acetaminophen (Acephen) AE:
Definition
metabolite, N-acetyl-para-benzoquinoneimine (NAPQI) is hepatotoxic
Term
Aspirin AE:
Definition
renal and resp. failure, vasomotor collapse; hypoprothrombinemia; fever, dehydration, metabolic acidosis, tinnitus, central hyperventilation; gastic intolerance, bleeding, hypersensitivity; impaired homeostasis
Term
NSAIDS inhibit:
Definition
biosynthesis of prostaglandins
Term
nonselective NSAID inhibitors of prostaglandin synthesis:
Definition
ibuprofen, meclofenamate
Term
selective inhinitors of prostaglandin biosynthesis:
Definition
piroxicam, sulindac, NSAIDS like aspirin andindomethacin, -coxibs
Term
Sulindac (clinoril)
Definition
sulfinylindene is prodrug form converted by liver to sulfide and irreversible oxidation of sulfone metabolite
Term
Sulindac (clinoril) use
Definition
regress colorectal polyps in FAP, analgesic and antipyretic properties
Term
Sulindac (clinoril)AEs
Definition
GI, platelet dysfunction; vaginal bleeding
Term
Celecoxib (celebrex)
Definition
selective COX2 inhibitor for rheumatoid arthritis, juvenile rheumatoid arthritis, acute moderate pain, or dysmenorrhea, interacts with gene PTGS2
Term
Celecoxib (celebrex) AE:
Definition
serious CV thrombotic events, MI, stroke, GI dysfunction, bleed
Term
Rofecoxib (Vioxx)
Definition
discontinued in US, lacks sulfonamide chain and behaves like ibuprofen, for osteoarthritis or acute pain, anti-inflammatory analgesic and antipyretic, doesn't block platelet aggregation, interacts with PTGS2, gauses adverse GI reactions and elevations of ALT or AST
Term
a patient on HCTZ and rofecoxib develops gradual increase in BP due to
Definition
inhibition of COX2 by rofecoxib which leads to decreased renal blood flow
Term
Etoricoxib (arcoxia)
Definition
not approved. potent and selective, orally active COX-2 inhibitor for dental pain, dysmenorrhia, RA but causes CV risks
Term
Meloxicam *mobic)
Definition
an oxicam derivative structurally related to piroxicam used for RA but causes GI bleedin gand ulceration and serious CV problems like MI, stroke, and thrombotic events that may increase with duration of use
Term
valdecoxib (bextra)
Definition
selective COX2 discontinued due to SJS, but FDA made interim recommendations for using it, but not for those ewith GI bleeds. anti-inflammatory, analgesic, antipyretic bu causes back pain, dizziness, flu-like symptoms, and overuse perpetuates episodic migraine.
Term
Etanercept produces antirheumatic effects by:
Definition
reducing circulating TNF-a levels
Term
diclofenac (cataflam)
Definition
NSAID of acetic acid derivative; analgesic/antipyretic; tablet topical or opthalmic forms; severe GI AEs like bleeding and ulceration) and cardiovascular thormbotic events like MI and stroke
Term
Diflunisal (dolobid)
Definition
difluorophenyl dreivative of salicylic acid so not metabolized by salicylic acid, has analgesic porperties for osteoarthritis and RA; given orally with water, milk, or fod; AEs are HA, blurred vision, and rash
Term
Etodolac (Lodine)
Definition
NSAID of indole and indene acetic acid derivative for osteoarthritis, RA, acute pain (even post-op), supresses expression of adhesion molecules and induces apoptosis; causes rash, blurred vision, dysuria
Term
Fenoprofen (Nalfon)
Definition
NSAID of propionic acid derivative used as antipyretid and analgesic for osteoarthritis and RA administered orally with water, milk, food, AEs are mild GI, dyspepsia, consitpation, and NV
Term
flurbiprofen (ansaid)
Definition
NSAID of the propionic acid derivative used as anti-inflammatory, analgesic and antipyretic for osteoarthritis and RA; reduces bone resporption in peridontal disleas by inhibiting carbonic anhydrase; oral or topical application to eyes; AEs are mild GI, pyspepsia, constipation and NV
Term
Ibuprofen (advil)
Definition
NSAID of porpionic acid derivative with analgesic proerties for rheumatism and arthritis; interacts with genes PTGS2 and Cyp19A1; AEs are serios GI effects and cardiovascular thrombotic events like MI and stroke
Term
Indomethacin (indocin)
Definition
NSAID of indole and indene acetic acid derivative; inhiits COX to generate ptostaglandins, inhibits motility of polymorphonuclear leukocytes; analgesi and antipyretic of osteoarthritis and RA; multi-drug resistance is limiting factor in application of drug, modulated ABCCA and PTGS1; AEs are NV, dyspepsia, pyrosis, and epigastric pain
Term
Ketoprofen (orudis)
Definition
NSAID propionic acid derivative; inhibits COX 1 and 2; analgesic and antipyretic used to tx RA and osteoarthritis; interacts with gene SLC22A11; AEs dyspepsia, retinal hemorrhage, bleeding, ulceration of stomach and intestines
Term
Methotrexate (Methotrexate LPF, Rheumatrex)
Definition
DMARD, analog of aminopterin which is derived from folic acid. used for malignant and non-malignant conditions; tx TA and prevents graft-vs-host disease; oral and parenteral forms
Term
Methotrexate (Methotrexate LPF, Rheumatrex) action:
Definition
folate antimetabolite. Methotrexate competitively inhibits dihydrofolate reductase, which is the enzyme responsible for converting folic acid to reduced folate cofactors
Term
Methotrexate AE
Definition
supresses hematopoiesis and causes anemia, aplastic anemia, andleukopenia
Term
Chlorambucil (Leukeran)
Definition
cell cycle-phase nonspecific antineoplastic agent; N mustard adn member of alkylating-agent class; for tx of CLL
Term
Chlorambucil (Leukeran) action and AE
Definition
it substitutes alkyl groups for hydrogen ions in both DNA & protein. DNA-DNA interstrand crosslink and DNA-protein crosslink occur, leading to interference in DNA replication, transcription of RNA, and nucleic acid function; causes bone marrow suppression!
Term
Cyclophosphamide (Cytoxan)
Definition
is an alkylating agent & is a prodrug that requires hepatic activation to become cytotoxic. given orally or intermittent IV cyclophosphamide
Term
Cyclophosphamide (Cytoxan) use:
Definition
tx RA; tx standard for proliferative lupus nephritis; tx of lymphoma and leukemia; activity against neoplastic disease
Term
Cyclophosphamide (Cytoxan) AE:
Definition
sterility, birth defects, mutations, cancer
Term
cyclosporine (Gengraf)
Definition
oral and parenteral immunosuppressive agent interacts with gene ABCB1 and CYP3A4, inhibit first phase of T-cell activation but can cause nephrotoxicity
Term
Cyclosporine (Gengraf) use:
Definition
tx during transplantation to improve survival, tx various autoimmune conditions, IBS, RA, iveitis, psoriasis, RA
Term
Azathioprine (Azasan)
Definition
immunosuppressive agent analog of endogenous purines adenine, ganine, adn hypoxanthine metabolized to 6-mercaptopurine; given orally adn IV
Term
Azathioprine (Azasan) use:
Definition
tx transplant patients, RA, lupus nephritis, and psoriatic arthritis. when combined with hydroxychloroquine can be used for RA; decreases metabolism of purines; causes bone marrow depression
Term
Mycophenolate Mofetil (CellCept)
Definition
prodrug for mycophenolic acid (MPA); immunosuppressive drug; myfortic is delayed-release tablet of it; used in conjunction with cyclosporine and corticosteroids in renal allograft and for RA and pts resistant to methotrexate
Term
Mycophenolate Mofetil (CellCept) action:
Definition
blocks T-cell proliferation & blocks leukocyte adhesion to E-selectin, p-selectin, & ICAM.
inhibits lymphocyte purine synthesis by reversibly.
It noncompetitively inhibits inosine monophosphate dehydrogenase (IMPDH). IMPDH is an important enzyme in the de novo synthesis of purines
Term
Mycophenolate Mofetil (CellCept) AE
Definition
gastrointestinal (GI) tract
constipation,
diarrhea, dyspepsia
nausea/vomiting
Term
Chloroquine (Aralen)
Definition
synthetic antimalarial agent to tx RA,systemic lupus erythematosus, systemic therapy of amebic liver abscesses, interacts with gene TP53, may interfere with lysosomal degradation of hemoglobin. Oral and IM, causes visual impairment.
Term
Chloroquine (Aralen)
Definition
synthetic antimalarial agent to tx RA,systemic lupus erythematosus, systemic therapy of amebic liver abscesses, interacts with gene TP53, may interfere with lysosomal degradation of hemoglobin. Oral and IM, causes visual impairment.
Term
Gold; Aurothiomalate (aurolate) and aurothioglucose
Definition
DMARDs; uset for RA, juvenile RA, given with salicylates or othe rNSAIDs in initial stage, interacts iwth albumin, administered IM, causes facial flushing, diaphoresis, dizziness, N/V, hypotension, metallic taste.
Term
Pencillamine
Definition
oral chelating agent used to tx Wilson's disease, cystinuria, resistant RA by chelating heavy metals like Cu, Fe, Pb, and Hg adn forming stable complexes that are excreted by kidneys; may cause adverse hematologic toxicity, bone marrow depression, leukopenia, thrombocytopenia, mortality
Term
Sulfasalazine (Azulfidine)
Definition
PRODRUG! used to treat ulcerative colitis and RA; a combination of sulfapyridine and 5-aminosalicylic acid (mesalamine). metabolized to its active components, sulfapyridine and mesalamine, by bacteria in the colon
Term
Sulfasalazine (Azulfidine) action and AE:
Definition
beneficial effects primarily from antiinflammatory properties; mesalamine inhibits leukotriene synthesis and arachidonic acid metabolism by inhibitng COX and reducing colonic inflammation. AE anorexia, diarrhea, GI distress
Term
TNF-a blocking agents
Definition
adalimumab; infliximab; etanercept
Term
Adalimumab (Humira)
Definition
recombinant human IgG1 monoclonal antibody; specific for TNF-a; tx RA - reduces disease progression; SC injection; AEs are HA and rash at injection site
Term
Infliximab (Remicade)
Definition
first monoclonal antibody; chimeric IgG1k monoclonal antibody targeted against TNF-a; tx Chron's disease, RA, ankylosing spondylitis, psoriatic arthritis; combo of infliximab and methotrexate; IV admin; causes elevated hepatic enzymes
Term
Etanercept (Enbrel)
Definition
dimeric fusion protein produced by recombinant DNA technology in Chinese hamster ovary cell systems; extracellular ligand-binding portion of the human 75 kD (p75) TNF-a receptor; tx RA; prevents TNF binding to receptor; SC admin; AE pain at injection and bleeding bruising at injection
Term
Colchicine
Definition
antiinflammatory properties; tx articular pain, treatment of acute gouty arthritis, & amyloidosis and biliary and hepatic cirrhosis; interferes with the inflammatory response to urate crystal deposition by binding to proteins in microtubules of neutrophils and inhibits migration of neutrophils inot area of inflammation; prevents release of inflammatory glycoprotein from phagocytes; causes N/V and diarrhea
Term
Probenecid
Definition
oral uricosuric; tx hyperuricemia assoc with gout; not effective for acute attacks of gout and can aggravate inflammation during initial stages; interferes with tubular handling of organic acids within the nephron; causes HA and N/V
Term
Sulfinpyrazone (Anturane)
Definition
uricosuric agent; tx chronic or intermittent gouty arthritis but LACKS analgesic or antiinflammatory effects; inhibits COX; dose should be slowly titrated to prevent kidney stones; oral and IV; may dispose urate stores and cause N/V/dairrhea
Term
Allopurinol (Aloprim)
Definition
structural analog of the natural purine base, hypoxanthine; prevention of gout, renal calculi due to either uric acid or calcium oxalate and in prophylaxis and tx of uric acid nephropathy; tx S/S of primary or secondary gout
Term
Allopurinol (Aloprim) action and AE
Definition
inhibits the enzyme xanthine oxidase, which blocks the metabolism of hypoxanthine and xanthine (oxypurines) to uric acid; interferes with catabolism of purines; oral and IV; AE hypersensitivity and should be discontinued at first sign of rash
Term
types of nutritional anemia
Definition
iron deficiency anemia; cobalamin deficiency; folic acid deficiency; megaloblastic anemia
Term
clinical manifestations of anemia
Definition
oxygen-carrying capacity of blood; whole volume of blood; rate at which reduction in oxygen-carrying capacity adn change in blood volume developed; manifestations of underlying illness causing anemia
Term
CBC
Definition
complete blood count or automated blood count; covers seven values relating to RBCs including Hb, Hct, RBC count, MCV (100 fL), MCH (29 picog/RBC), and MCHC (32-36dL)
Term
megaloblastic anemia
Definition
a type of macrocytic anemia caused by vitamin B12 deficiency or folate deficiency
Term
Etiology of iron deficiency anemia (need more iron):
Definition
physiologic stress (growth, pregnancy), pathologic causes (blood loss), inadequate iron supply (low iron consumption, impaired absorption, abnormal transferrin)
Term
Causes of anemia
Definition
inadequate erythropoiesis or hemoglobin synthesis; inadequate B12; lack of intrinsic factor; iron-deficiency; kidney failure and insufficient erythropoietin hormone; loss of blood; RBC destruction
Term
Pernicious anemia
Definition
lack of intrinsic factor from glands of stomach
Term
aplastic anemia
Definition
complete cessation of RBC production from unknown causes
Term
hemorrhagic anemia
Definition
from loss of blood
Term
hemolytic anemia
Definition
from RBC destruction
Term
anemia causes:
Definition
hypoxia, necrosis, low blood osmolarity (tissue edema) and low blood viscosity (heart races and pressure drops)
Term
Hemopoiesis
Definition
blood cell production; stimulated by erythropoietin, thrombopoietin, and CSFs
Term
formation of an erythrocyte
Definition
proertythoblast to erythroblast to normoblast to reticulocyte to erythrocyte
Term
nutrients needed for RBC production
Definition
iron, B12, 2, 6, folic acid, niacin, VitC, A, E, Copper, Cobalt, AAs, calories, proteins
Term
how to treat iron deficiency anemia
Definition
oral iron replacement (ferrous sulfate) or parenteral (iron dextran, Iron gluconate)
Term
complications of parenteral tx for iron deficient anemia
Definition
allergic reactions and anaphylaxis limit tx to specific health conditions like inability to absorb iron from GI tract or inability to tolerate oral iron
Term
Folic acid precursor
Definition
tetrahydrofolate
Term
tetrahydrofolate
Definition
active forms of folic acid are derived from this. acts as methyl donor for purine and pyrimidine synthesis; converts deoxyuridine monophosphate to deoxythymidine monophosphate for DNA synth.
Term
causes of cobalamin deficiency
Definition
nutritional; abnormal intragastric events; deficient or defective IF; abnormal events in small bowel; disordered mucosa
Term
tx of B12 deficiency
Definition
goal is to replenish total body stores by administering cyanocobalamin IM or oral use of pancreatic extract
Term
monitoring tx of anemia is done by:
Definition
reversion of megaloblastic hematopoiesis to normal hematopoiesis; reticulocyte counts; methylmalonic acid and homocysteine levels return to normal; RBC count, hemoglobin and hematocrit
Term
folic acid is absorbed:
Definition
in the small intestine
Term
from the small intestine, folic acid goes:
Definition
to the serum where it is free or loosely and nonspecifically bound to serum proteins
Term
in tissues other than the liver, folic acid:
Definition
enters and remains within cell through its lifespan
Term
stored folic acid in liver:
Definition
can be released into biliary circulation
Term
biliary drainage does what to serum folate levels?
Definition
dramatically decreases serum folate levels
Term
causes of folic acid deficiency:
Definition
inadequate intake; increased requirements due to pregnancy, lactation, psoriasis, hemolysis; intestinal malabsorption; drug interactions; defective cellular uptake
Term
causes of intestinal malabsorption of folic acid:
Definition
spure, drugs like methotrexate or phenytoin, chron's disease, HIV-related enteropathy
Term
Drugs causing folic acid deficiency
Definition
methotrexate, phenytoin, ethanol, sulfa drugs, barbiturates
Term
folic acid deficiency is determined by:
Definition
low serum folic acid level; measurement of RBC folic acid; serum homocysteine and methylmalonic acid levels. TOtal serum homocysteine level is elevated in deficient patients, but methylmalonic acid levels are normal in patients with folic acid deficiencies
Term
tx of folic acid deficiency is done by:
Definition
oral folic acid 1-5 mg/day even when intestinal malabsorption of food folate exists
Term
prophylactic folic acid should be given to:
Definition
women contemplating pregnancy, pregnant or lactating women, patients with chronic hemolysis and increased erythropoiesis
Term
folic acid supplements decrease:
Definition
homocysteine levels
Term
hematopoietic growth factors
Definition
M-CSF, G-CSF, GM-CSF
Term
myeloid growth factors:
Definition
G-CSF, GM-CSF
Term
recombinant myeloid growth factors
Definition
Filgrastim (neupogen), sargramostim (leukine), pegfilgrastim (neulasta)
Term
megakaryocyte growth factors
Definition
thrombopoietin and interleukin-11; recombinant IL-11 is Oprelvekin (Neumega)
Term
uses of thrombopoietin
Definition
post-chemo, post-radiotherapy, alastic anemia, thromboctopenia purpura, prenatal thormbocytopenia, and more!
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