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PAMercer Pharm 4
Glucocorticoids, NSAIDs, Immuno, Gout
56
Pharmacology
Graduate
04/17/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
Bradykinin
Definition
Effects similar to histamine (vasodilation, pain)
Term
Complement
Definition
Series of proteins that combine together to neutralize or destroy antigens
Term
Histamine
Definition
Released by mast cells causing vasodilation, smooth muscle constriction, capillary leakage, pruritus
Term
Leukotrienes
Definition
Released by mast cells with effects similar to histamine
Term
Prostaglandins
Definition
Increase capillary permeability, attraction of leukocytes, pain
Term
Prednisone (Sterapred®) Triamcinolone (Kenalog®) Dexamethasone (Decadron®) Methylprednisolone (Depo-Medrol®)
Definition
MoA:
↑ duration of action, ↓ salt-retaining effect, better penetration of lipid barriers (topical use)
Term
Prednisone (Sterapred®) Triamcinolone (Kenalog®) Dexamethasone (Decadron®) Methylprednisolone (Depo-Medrol®)
Definition
Uses:
Adrenal disorders: Addison’s disease, Acute adrenal insufficiency
Non-adrenal disorders:
 Inflammatory/Immunologic
 Asthma, organ transplant rejection, collagen diseases
 Hematopoietic Cancers
 Neurologic Disorders
 Chemotherapy-induced N/V
Term
Prednisone (Sterapred®) Triamcinolone (Kenalog®) Dexamethasone (Decadron®) Methylprednisolone (Depo-Medrol®)
Definition
Toxicity Signs & symptoms:  Adrenal suppression (from suppression of ACTH)  Metabolic effects  Salt retention  Psychosis
Term
Ways to minimize synthetic glucocorticoid toxicity
Definition
Local application (topicals for the skin or aerosols/inhalation solution for asthma)
Alternating day therapy/ Tapering therapy
Term
Drug interactions for synthetic glucocorticoids (including Prednisone)
Definition
CYP 450
NSAIDs/Salicylates, Alcohol (cause increased risk of GI ulceration)
Term
Cautions for use of synthetic glucocorticoids (like Prednisone)
Definition
HPA suppression
 May lead to adrenal crisis, caution with high doses, prolong therapy, pediatrics, prevent by tapered withdrawal from medication
Psychiatric disturbances
 Caution with pre-existing psychiatric disorders (may cause exacerbation)
Secondary infections due to immunosuppression
May reduce effectiveness of vaccines
Other cautions:
 Thyroid disease, hepatic impairment, renal impairment, cardiovascular disease, diabetes, seizure disorders, GI diseases
Term
NSAIDs MoA
Definition
Anti-inflammatory actions
 Inhibit cyclooxygenase (enzyme that converts arachidonic acid to prostaglandins)
Analgesic actions
 Peripheral inhibition of PG production & possible inhibition of pain stimuli
Antipyretic actions
 Inhibition of PG synthesis in the thermoregulatory center
Term
NSAIDs uses
Definition
Inflammatory diseases
Mild-moderate pain
Fever
1st line treatment for inflammation & accompanying pain
Treatment of chronic inflammation requires dosages greater than doses needed for antipyresis or analgesia
 Increased dosages generally leads to more AE
 Anti-inflammatory effects may take weeks of therapy
Term
NSAIDs Adverse effects
Definition
GI complaints (most common AEs)  Nausea, dyspepsia, abdominal pain  GI ulceration/bleeding through topical & systemic effects  Risk factors: >65 yo, comorbid medical conditions, corticosteroid  Taking NSAIDs with food helps to minimize most GI adverse effects Other AEs:  Renal dysfunction, hypersensitivity reactions, rash, CNS (drowsiness, dizziness, tinnitus) Avoid late in pregnancy  Risk of premature closure of ductus arteriosus
Term
Drug interactions with NSAIDs
Definition
Anticoagulants & Antiplatelets – ↑ effects
 Higher bleeding risk
Corticosteroids, bisphosphonates – GI effects
 Higher risk of GI ulceration
Renal mechanisms/ excretion: Methotrexate, Lithium
Renal toxicity – Cyclosporin, Antibiotics (Aminoglyosides & Vancomycin)
Antihypertensives – ↓ antihypertensive effects
 ACEI, BB, Diuretics, CCBs
Term
NSAID Black Box Warnings
Definition
↑ risk of adverse cardiovascular events (including MI, CVA, HTN)
↑ risk of GI irritation, ulceration, bleeding, perforation

GI irritation/ ulceration
 May occur at anytime during therapy
 Caution with history of GI disease, concurrent aspirin use, anticoagulants, corticosteroids, smoking, alcohol, elderly
Compromise of renal function
Serious skin adverse events
 SJS, TENs
 Caution with aspirin triad (aspirin intolerance, asthma, rhinitis)
↓ hepatic function
Preoperative: discontinue 4-6 t ½ before procedures
Term
Acetylated Salicylate
Definition
Specific drug type of Aspirin
Term
Less effect on platelets
Definition
What differs in nonacetylated salicylates from acetylated salicylates
Term
Nonacetylated Salicylates
Definition
Salsalate (Amigesic®) Diflunisal (Dolobid®) Choline Salicylate Magnesium Salicylate (Doan’s®)
Term
Acetic Acids
Definition
Etodolac (Lodine®) Diclofenac (Voltaren®)  Topical gel, Ophthalmic, PO Indomethacin (Indocin®)  Indicated for PDA, inflammatory disorders, bursitis/ tendonitis, acute gouty arthritis  PO, injection
Term
Propionic Acids
Definition
Fenoprofen Flurbiprofen (Ansaid®) Ibuprofen (Motrin, Advil®) Ketoprofen (Orudis®) Naproxen Sodium (Aleve, Naprosyn®) Oxaprozin (Daypro®)
Term
Fenamates
Definition
Meclofenamate (Meclomen®)  Inflammatory disorders, mild to moderate pain, primary dysmenorrhea Mefenamic Acid (Ponstel®)  Indicated for mild to moderate pain, primary dysmenorrhea
Term
Oxicams
Definition
Piroxicam (Feldene®)
 Rheumatoid & Osteoarthritis
Term
Oxicams
Definition
Piroxicam (Feldene®)
 Rheumatoid & Osteoarthritis
Term
Preferential Cox-2
Definition
Meloxicam (Mobic®)
Term
Specific Cox-2
Definition
Celecoxib (Celebrex®) Removed from market/ unavailable – Rofecoxib (Vioxx®), Valdecoxib (Bextra®)
Term
Inhibition of T-cells
Definition
Function of: Cyclosporine (Sandimmune, Neoral®) & Tacrolimus (Prograf®)
Term
Inhibition of DNA, RNA & protein synthesis
Definition
Function of:
Azathioprine (Imuran®)
Term
Alters & decreases the formation of T-cells
Definition
Function of:
Lymphocyte immune globulin
Term
Blocks metabolism of folic acid
Definition
Function of:
Methotrexate
Term
Antibodies specific for CD3 receptors on T-cells; used for treatment of kidney transplant rejection
Definition
Function of:
Muromonab-CD3
Term
Inhibition of T-cells, B-cells, & antibody formation
Definition
Function of:
Mycophenolate mofetil (Cellcept®)
Term
Actions of Colchicine
Definition
↓ leukocyte mobility
↓ phagocytosis in joints
↓ deposition of urate crystals
Term
Uses of Colchicine
Definition
Anti-inflammatory, Anti-gout
Dosing: Prophylaxis/Maintenance
o Low doses
o Onset of acute attack: ↑ dosing
o Used with antihyperuricemic therapy in patients with significantly elevated uric acid levels to minimize the risk of acute attacks that may occur with the initiation of uric acid lowering therapy
Term
Adverse effects of Colchicine
Definition
GI: N/V/D, abdominal pain, anorexia • Alopecia • Hematologic abnormalities
Term
Caution for use of Colchicine
Definition
Serious renal, GI, hepatic disorders, hematologic abnormalities, pregnancy
Term
Drug interactions with Colchicine
Definition
CYP 450 Substrate
o Toxicity with CYP 450 inhibitors
Acid/Base
o ↓ effects with acidic agents, ↑ effects with alkaline agents
Term
Uses of Indomethacin (Indocin®)
Definition
Inhibits prostaglandin synthesis by inhibiting cyclooxygenase
Term
Uses of Indomethacin (Indocin®)
Definition
• NSAID (particularly useful for gout)
• As effective as colchicine in acute attacks for many patients (with less GI toxicity)
• Large doses x 24-48 hours then taper over 3-4 days to minimize the risk of recurrent attacks
Term
Black box warning for Indomethacin (Indocin®)
Definition
GI ulceration (like all NSAIDs)
o Decreased risk by using high doses for short-term only
Term
Adverse effects of Indomethacin (Indocin®)
Definition
CNS: headache, dizziness, tinnitus
GI: N/V, dyspepsia, abdominal pain, GI bleed
Term
Cautions/contraindications of Indomethacin (Indocin®) use
Definition
NSAID or aspirin allergy, PUD, impaired renal function, CHF, HTN, thrombocytopenia
Term
Drug interactions with Indomethacin (Indocin®)
Definition
↑ K (especially with K-sparing diuretics)
↑ concentration with probenecid
↑ nephrotoxicity with cyclosporin, other NSAIDs, ACEI, digoxin, aminoglycosides, lithium
↓ effects of anti-HTN meds
Term
General actions of uricosuric medications
Definition
↑ renal excretion of uric acid by inhibiting renal tubular reabsorption of uric acid
Term
General uses of uricosuric medications
Definition
• Started at low doses to avoid marked uricosuria & possible stone formation & ↑ over several weeks until efficacy or max dose
• Maintenance of hydration & adequate urine flow
• Alkalinization of urine (Na Bicarb or Shohl’s solution) during the 1st several days of therapy to ↓ stone formation
Term
Adverse effects & contraindications of uricosuric medications
Definition
• GI irritation, rash/hypersensitivity, precipitation of acute gouty arthritis, & stone formation
• Contraindicated in renal impairment (CrCl < 50 Ml/min)
Term
Actions of Probenecid (Benemid®)
Definition
Competitively inhibits the reabsorption of uric acid at the PCT, leading to promotion of excretion & ↓ serum uric acid levels
Term
Uses of Probenecid (Benemid®)
Definition
Prevention of gouty arthritis, hyperuricemia, also used for prolongation of antibiotic effects (beta-lactams)
Term
Drug interactions of Probenecid (Benemid®)
Definition
↑ effects of methotrexate, quinolones, beta-lactams, & NSAIDs
Term
Adverse effects of Probenecid (Benemid®)
Definition
• CNS: headache, dizziness
• Gen/Skin: flushing of face, rash pruritus, hematologic abnormalities
• GI: N/V, anorexia, gingival soreness, hepatic necrosis
• GU: dysuria, renal calculi
• May cause acute gout attack
Term
Actions of Sulfinpyrazone
Definition
↑ urinary excretion of uric acid, leading to ↓ serum uric acid
Term
Uses of Sulfinpyrazone
Definition
Uricosuric, anti-gout Chronic gouty arthritis, intermittent gouty arthritis
Term
Actions of Allopurinol (Zyloprim®)
Definition
Inhibits xanthine oxidase (the enzyme that converts xanthine to uric acid)
Term
Uses of Allopurinol (Zyloprim®)
Definition
Xanthine oxidase inhibitor, anti-gout • Prevention of acute gout • Drug of choice in history of urinary stones or impaired renal function • Used for pre-treatment in cytotoxic therapy to prevent uric acid neuropathy
Term
Adverse effects of Allopurinol (Zyloprim®)
Definition
Skin rash, N/V, Leukopenia
Term
Drug interactions with Allopurinol (Zyloprim®)
Definition
• ↑ rash when combined with certain antibiotics
• ↑ risk of bone marrow suppression when given with immunosuppressants
• ↑ effect of anticoagulants
• ↓ effect with ethanol
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