FA MSK Pharm Flashcards
Reversibly inhibit COX 1&2. Block PG synthesis. Indomethacin closes PDA
SE: interstitial nephritis, gastric ulcer, renal ischemia
NSAIDs.
Reversibly inhibit COX2 (spares COX-1, wh/ helps maintain the gastric mucosa; spares platelet function as TXA2 production is dependent on COX1);
SE: increased risk of thrombosis (through PGI2?), sulfa allergy
COX-2 inhibitors (celecoxib)
Reversibly inhibits COX, mostly in CNS; inactivated peripherally.
SE: centrilobular hepatic necrosis, NAPQI depletes glutathione (NAC regenerates)
Acetaminophen
Pyrophosphate analogs; bind hydroxyapatite in bone, inhibiting osteoclast activity
SE: corrosive esophagitis, osteonecrosis of jaw
Bisphosphonates
Inhibits xanthine oxidase. Used to prevent chronic gout and tumor lysis, increases conc of azathioprine and 6-MP. Do not give salicylates, which depress uric acid clearance.
Allopurinol, febuxostat
Inhibits reabsorption of uric acid in PCT (also inhibits secretion of PCN). Don’t use in renal failure or tumor lysis.
Probenecid
Binds and stabilizes tubulin to inhibit microtubule polymerization, impairing leukocyte chemotaxis and degranulation.
SE: GI
Colchicine
Fusion protein (receptor for TNF-alpha and IG1 Fx), produced by recombinant DNA. CU: RA, psoriasis, ankylosing spondylitis
Etanercept
Anti-TNF-alpha monoclonal antibody.
CU: IBD, RA, ank spond, psoriasis
SE: reactivates TB
Infliximab, adalimumab
Irreversibly inhibits COX-1 and COX-2 by covalent acetylation, which decreases TXA2 and PGs. Increased BT for >7 days.
SE: gastric ulcers, tinnitis, Reyes (microvesicular hepatic steatosis - mitrochondrial dysfxn) in kids, OD: resp alkalosis then met acidosis (combo)
ASA