MSK Pharm Flashcards
Neutrophil Chemotactic Agent
LTB4
Leukotrienes that function in bronchoconstriction, vasoconstriction, contraction of smooth muscle, and increased vascular permeability.
LTC4, D4 and E4
Prostaglandin that inhibits platelet aggregation and promotes vasodilation
PGI2
Irreversibly inhibits cyclooxygenase (COX1 and 2) by acetylation, which decreases synthesis of both thromboxane A2 and prostaglandins. Increases bleeding time with no effect on PT or PTT. NSAID
Aspirin
Reversibly inhibit COX 1 and 2. Block prostaglandin synthesis.
NSAIDS
NSAIDS
Ibuprofen, naproxen, indomethacin, ketorolac, and diclofenac.
Reversibly inhibit COX2, found in inflammatory cells and vascular endothelium and mediates inflammation/pain; spares COX1 which helps maintain the gastric mucosa. Spares platelet function as TXA2 production is dependent on COX1.
COX-2 Inhibitors (Celecoxib)
Reversibly inhibits COX, mostly in the CNS but peripherally inactivated.
Acetaminophen
Pyrophosphate analogs; bind hydroxyapatite in bone to inhibit osteoclast activity.
Bisphosphonates (Alendronate, other -dronates)
Used for osteoporosis, hypercalcemia, Paget’s disease of bone
Bisphosphonates (Alendronate, other -dronates)
Used as antipyretic, analgesic, but not anti-inflammatory. Used instead of aspirin to avoid Reye’s Syndrome in children with viral infection.
Acetaminophen
Used for RA and OA, pts with gastritis or ulcers.
COX2 Inhibitors (Celecoxib)
Used as antipyretic, analgesic, anti-inflammatory. One of which can be used to close a PDA
NSAIDS (Ibuprofen, naproxen, indomethacin, ketorolac, and diclofenac),
- Indomethacin to close PDA
- Low Dose (<300 mg/day): decreases platelet aggregation.
- Intermediate Dose (300-2400 mg/day): antipyretic and analgesic
- High Dose (2400-4000 mg/day): anti-inflammatory.
Aspirin
SE: Gastric ulceration, tinnitus (CN VIII). Chronic use –> acute renal failure, interstitial nephritis, and upper GI bleeding. Risk of Reye’s syndrome in kids treated for viral infection. Also stimulates resp centers, causing hyperventilation and resp alkalosis.
Aspirin
SE: Interstitial nephritis, gastric ulcer (PGs protect gastric mucosa), renal ischemia (PGs vasodilate afferent arteriole)
NSAIDS (Ibuprofen, naproxen, indomethacin, ketorolac, and diclofenac)
SE: Increased risk of thrombosis, sulfa allergy
COX-2 Inhibitors (Celecoxib)
SE: Overdose produces hepatic necrosis, metabolite depletes glutathione and forms toxic tissue adducts in liver. N-acetylcystein is antidote (regulates glutathione)
Acetaminophen
SE: Corrosive esophagitis, osteonecrosis of jaw
Bisphosphonates (Alendronate, other -dronates)
(For Gout) Inhibits Xanthine Oxidase to decrease conversion of xanthine to uric acid.
Allopurinol, Febuxostat
Also used in lymphoma and leukemia to prevent tumor lysis-associated irate nephropathy. Increases concentrations of azathioprine and 6-MP (both normally oxidized by xanthine oxidase)
Allopurinol
Do not give with salicylates; all but the highest doses depress uric acid clearance. Even high doses have only minor uricosuric activity.
Allopurinol.
(For Gout) Inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)
Probenecid
(For Gout) Binds and stabilizes tubulin to inhibit polymerization, impairing leukocyte chemotaxis and degranulation. GI Side effects if given orally.
Colchicine
