MSK + Skin Drugs

Question 1

aspirin mechanism

Answer 1

• irreversibly inhibits COX by covalent acetylation, which decreases TXA2 and prostaglandin synthesis
• increased bleeding time, no effect on PTT and PT

Question 2

aspirin clinical use

Answer 2

< 300mg/day - decreased platelet aggregation
300mg- 2400mg/day - antipyretic and analgesic
2400-4000mg/day - anti-inflammatory

Question 3

aspirin tox

Answer 3

• gastric ulceration, tinnitus
• chronic renal failure, nephritis, upper GI bleeds
• Reye syndrome in kids
• hyperventilation and respiratory alkalosis

Question 4

NSAIDs name and mech

Answer 4

• ibuprofen, naproxen, indomethacin, ketorolac, diclofenac

- reversibly inhibit COX1 and 2, block PG synthesis

Question 5

NSAIDS clinical use and tox

Answer 5

• antipyretic, analgesic, anti-inflammatory
• indomethacin is used to close a PDA
• tox: interstitial nephritis, gastric ulcer, renal ischemia

Question 6

COX2 inhibitors (celecoxib) mech

Answer 6

• reversibly inhibit COX2 (found in inflammatory cells and vascular endothelium)
• spares TXA2/platelet function and GI side effects

Question 7

COX2 clinical use and tox

Answer 7

• RA and osteoarthritis, patients with gastritis or ulcers

- increased risk of thrombosis, sulfa allergy

Question 8

acetaminophen

Answer 8

• reversibly inhibits COX, mostly CNS, inactivated peripherally
• antipyretic, analgesic but not anti-inflammatory
• tox: hepatic necrosis, NAPQI depletes glutathione, NAC regenerates it

Question 9

bisphosphonates

Answer 9

• alendronate and other -ates
• pyrophosphate analogs, bind hydroxyapatite in bones, inhibiting osteoclast activity
• used in osteoporosis, hypercalcemia and Pagets disease
• tox: corrosive esophagitis, osteonecrosis of jaw

Question 10

allopurinol

Answer 10

xanthine oxidase inhibitor

- prevents TLS and urate nephropathy, will increase concentrations of azathioprine and 6-MP

Question 11

Rasburicase

Answer 11

recombinant urate oxidase used in TLS

Question 12

febuxostat

Answer 12

inhibits xanthine oxidase

Question 13

probenecid

Answer 13

inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)

Question 14

colchicine

Answer 14

• inhibits microtubule polymerization, impairing leukocyte chemotaxis and degranulation
• good for acute gout and prophylaxis
• GI side effects, do not use in elderly peeps with renal dysfunction

Question 15

entanercept

Answer 15

fusion protein (TNFa receptr + IgG Fc) used as decoy receptor for RA, psoriasis, ank spon