MSK/DERM/CT

Question 0

Ibuprofen

Answer 0

MOA: NSAID. Reversible inhibits COX 1 and 2 and thereby blocks PG synthesis

USES: antipyretic, analgesic, anti inflammatory.

TOXICITY: interstitial nephritis, gastric ulcer, renal ischemia (PGs vasodilate renal afferent arteriole)

Question 1

Aspirin

Answer 1

MOA: NSAID. irreversibly inhibits COX 1 and 2 by covalent acetylation, which decreases synthesis of both thromboxane A2 and prostaglandins. Increases bleeding time until new platelets are produced (~7days). NO effect on PT, PTT.

USES: low dose (<300mg): decrease platelet aggregation. Intermediate dose (300-2400mg): antipyretic and analgesic. High dose (2400-4000): anti-inflammatory

TOXICITY: gastric ulceration, tinnitus (CN VIII). Chronic use can lead to acute renal failure, interstitial nephritis, and upper GI bleeding. Risk of Reye syndrome in children treated with aspirin for viral infection. Also stimulates respiratory centers, causing hyperventilation and respiratory alkalosis.

Question 2

Naproxen

Answer 2

MOA: NSAID. Reversible inhibits COX 1 and 2 and thereby blocks PG synthesis

USES: antipyretic, analgesic, anti inflammatory.

TOXICITY: interstitial nephritis, gastric ulcer, renal ischemia (PGs vasodilate renal afferent arteriole)

Question 3

Indomethacin

Answer 3

MOA: NSAID. Reversible inhibits COX 1 and 2 and thereby blocks PG synthesis

USES: antipyretic, analgesic, anti inflammatory, closure of PDA

TOXICITY: interstitial nephritis, gastric ulcer, renal ischemia (PGs vasodilate renal afferent arteriole)

Question 4

Ketorolac

Answer 4

MOA: NSAID. Reversible inhibits COX 1 and 2 and thereby blocks PG synthesis

USES: antipyretic, analgesic, anti inflammatory.

TOXICITY: interstitial nephritis, gastric ulcer, renal ischemia (PGs vasodilate renal afferent arteriole)

Question 5

Diclofenac

Answer 5

MOA: NSAID. Reversible inhibits COX 1 and 2 and thereby blocks PG synthesis

USES: antipyretic, analgesic, anti inflammatory.

TOXICITY: interstitial nephritis, gastric ulcer, renal ischemia (PGs vasodilate renal afferent arteriole)

Question 6

Celecoxib

Answer 6

MOA: COX-2 inhibitor. Reversibly inhibits COX2, which is found in inflammatory cells and vascular endothelium and mediates inflammation and pain; spares COX-1, which helps maintain the gastric mucosa. Thus, should not have the corrosive effects of other NSAIDs on the GI lining. Spares platelet function as TXA2 production is dependent on COX-1

USES: rheumatoid arthritis and osteoarthritis; patients with gastritis or ulcers.

TOXICITY: increased risk of thrombosis. Sulfa allergy.

Question 7

Acetaminophen

Answer 7

MOA: reversibly inhibits COX, mostly in CNS. Inactivated peripherally.

USES: antipyretic, analgesic, but NOT anti-inflammatory. Used instead of aspirin to avoid Reye syndrome in children with viral infection.

TOXICITY: overdose produces hepatic necrosis; acetaminophen metabolite (NAPQI) depletes glutathione and forms toxic tissue addicts in liver. N-acetylcysteine is antidote–regenerates glutathione.

Question 8

Bisohosphonates

Answer 8

MOA: pyrophosphate analog. Binds hydroxyapatite in bone, inhibiting osteoclasts activity.

USES: osteoporosis, hypercalcemia, Paget’s disease of bone.

TOXICITY: corrosive esophagitis (patients are advisrd to take with water and remain upright for 30 minutes), osteonecrosis of jaw.

Question 9

Allopurinol

Answer 9

MOA: inhibits xanthine oxidase, decreases conversion of xanthine to uric acid.

USES: gout and lymphoma and leukemia to prevent tumor lysis–associated urate nephropathy.

TOXICITY: increases concentrations of both azathioprine and 6-MP (both normally metabolized by xanthine oxidase). Do not give salicylates; all but the highest dose depress uric acid clearance. Even high doses have only minor uricosuric activity.

Question 10

Febuxostat

Answer 10

MOA: Chronic preventative gout drug. Inhibits xanthine oxidase

Question 11

Probenecid

Answer 11

MOA: chronic preventative gout drug. Inhibits reabsorption of uric acid in PCT (also inhibits secretion of penicillin)

Question 12

Colchicine

Answer 12

MOA: binds and stabilizes tubulin to inhibit microtubule polymerization, impairing leukocyte chemotaxis and degranulation.

USES: acute and prophylaxis for gout.

TOXICITY: GI side effects (nausea, abdominal pain, diarrhea)

Question 13

Etanerecept

Answer 13

MOA: TNF decoy receptor. fusion protein (receptor for TNF-alpha + IgG1 Fc), produced by recombinant DNA.

USES: rheumatoid arthritis, psoriasis, ankylosing spondylitis

TOXICITY: predisposition to infection, including re activation of latent TB, since TNF blockade prevents activation of macrophages and destruction of phagocytosed microbes

Question 14

Infliximab

Answer 14

MOA: anti-TNF alpha monoclonal antibody

USES: rheumatoid arthritis, psoriasis, ankylosing spondylitis, IBD

TOXICITY: predisposition to infection, including re activation of latent TB, since TNF blockade prevents activation of macrophages and destruction of phagocytosed microbes

Question 15

Adalimumab

Answer 15

MOA: anti-TNF alpha monoclonal antibody

USES: rheumatoid arthritis, psoriasis, ankylosing spondylitis, IBD

TOXICITY: predisposition to infection, including re activation of latent TB, since TNF blockade prevents activation of macrophages and destruction of phagocytosed microbes

Question 16

Teriparatide

Answer 16

MOA: recombinant PTH analog given subcutaneously daily to increase osteoblastic activity

USES: osteoporosis. Causes increased bone growth compared to antiresorptive therapies (e.g. Bisphosphonates)

TOXICITY: transient hypercalcemia. May increase risk of osteosarcoma

Question 17

Pegloticase

Answer 17

Chronic preventative gout drug. Recombinant uricase that catalyzes metabolism of uric acid to allantoin (a more water soluble product)