Pharmacology: MSK/Rheum

Question 1

Aspirin

Answer 1

Anti-platelet (low dose), anti-pyretic and analgesic (med dose), anti-inflammatory (high dose)
- Acetylates and irreversibly inhibits COX-1 and -2
- Prevents AA –> TXA2 conversion (which normally mediates plt aggregation) and AA –> PGs
- Increases BT
- No effect on PT/PTT
SEs:
- GI: gastric ulcers, bleeding
- Renal: RF, AIN
- Hyperventilation, tinnitus (CN VIII)
- Reye’s syndrome in kids (rash, encephalitis, fatty liver)

Question 2

Ibuprofen

Answer 2

NSAID
- Reversibly inhibit COX-1 and -2
SEs: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers

Question 3

Naproxen

Answer 3

NSAID
- Reversibly inhibit COX-1 and -2
SEs: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers

Question 4

Indomethacin

Answer 4

NSAID
- Reversibly inhibit COX-1 and -2
- CLOSE PDA
SEs: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers

Question 5

Ketorolac

Answer 5

NSAID
- Reversibly inhibit COX-1 and -2
SEs: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers

Question 6

Celecoxib

Answer 6

Selective COX-2 inhibitor
- Spares COX-1, should decr risk of GI irritation/ulceration/bleeding
SE: incr risk of thrombosis, sulfa allergy

Question 7

Acetaminophen

Answer 7

Reversibly inhibits COX, mostly in CNS. Inactivated peripherally
SE: Heptatic necrosis!! (depletes glutathione and forms toxic tissue adducts)

Question 8

Etidronate

Answer 8

Bisphosphonate
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: corrosive esophagitis, osteonecrosis of the jaw

Question 9

Pamidronate

Answer 9

Bisphosphonate
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: corrosive esophagitis, osteonecrosis of the jaw

Question 10

Alendronate

Answer 10

Bisphosphonate
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: corrosive esophagitis, osteonecrosis of the jaw

Question 11

Risdedronate

Answer 11

Bisphosphonate
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: corrosive esophagitis, osteonecrosis of the jaw

Question 12

Zoledronate

Answer 12

Bisphosphonate (IV form)
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: IV so no sophagitis, osteonecrosis of the jaw

Question 13

Probenicid

Answer 13

Uricosuric agent, for chronic gout

• Inhibit reabsorption of uric acid in PCT (also inhibits secretion of PCN)
• *MUST HAVE GOOD RENAL FUNCTION. e.g. not in a patient with no UOP! Do not use in pts at risk for nephrolithiasis or uric acid nephropathy

Question 14

Allopurinol

Answer 14

Anti-gout, chronic

• Inhibit xanthine oxidase, decr conversion of xanthine to uric acid
• Also used to prevent tumor lysis-associated urate nephropathy
• Increases concentrations of azathioprine and 6-MP
• Also don’t give diruetics or salicylates! They will decr tubular secretion of urate

Question 15

Febuxostat

Answer 15

Anti-gout, chronic

- Inhibitis xanthine oxidase

Question 16

Colchicine

Answer 16

Anti-inflammatory, for acute gout

- Binds and stabilizes tubulin to inhibit polymerization and impairs leukocyte chemotaxis and degranulation

Question 17

Drugs to use in acute gout

Answer 17

Colchicine
Indomethacin
Naproxen/NSAIDs

Question 18

Etanercept

Answer 18

TNF-alpha inhibitor
Recombinant TNF receptor decoy
- Prevents leukocyte recruitment, activation of macrophages, destruction of phagocytosed microbes
SE: increased risk of infections, eg. reactivation TB

Question 19

Infliximab

Answer 19

Anti-TNF antibody
Tx: Crohn’s, RA, AS
Increased risk of infection (reactivation of TB), fever, hypotension

Question 20

Adalimumab

Answer 20

Anti-TNF antibody
Tx: Crohn’s, RA, AS, psoriasis
Increased risk of infection (reactivation of TB), fever, hypotension

Question 21

Calcipotene

Answer 21

Topical Vit D analog

• Binds and activates Vit D receptor, inhibits keratinocyte proliferation and stimulates differentiation
• Inhibits T cell proliferation and inflammation

Question 22

Calcitriol

Answer 22

Topical Vit D analog

• Binds and activates Vit D receptor, inhibits keratinocyte proliferation and stimulates differentiation
• Inhibits T cell proliferation and inflammation

Question 23

Tacalcitol

Answer 23

Topical Vit D analog

• Binds and activates Vit D receptor, inhibits keratinocyte proliferation and stimulates differentiation
• Inhibits T cell proliferation and inflammation

Question 24

Cyclosporine

Answer 24

Immunosuppressant
- Inhibits calcineurin, which normally activates NFAT
- Prevents IL-2 and IL-2 receptor synthesis
(IL-2 produced by Th2 cells)
Tx: psoriasis, prevent transplant rejection
SE: nephrotoxic, ppx wit mannitol diuresis

Question 25

Ustekinumab

Answer 25

Anti-IL-12 and IL-23
Inhibits differentiation and activation of CD4+ Th1 and Th17
Tx: Psoriasis

Question 26

Rasburicase

Answer 26

Recombinant urate oxidase (an enzyme in many other mammals, but not humans)
- Converts uric acid to allantoin (5-10x more soluble than uric acid)
Prevent and tx hyperuricemia and the resulting renal manifestations of tumor lysis syndrome (incr uric acid ppt in kidney causing obstructive uropathy and ARF; hyperK from lysing cells causing arrhythmia)