Pharmacology: MSK/Rheum Flashcards
Aspirin
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)
Ibuprofen
NSAID
- Reversibly inhibit COX-1 and -2
SEs: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers
Naproxen
NSAID
- Reversibly inhibit COX-1 and -2
SEs: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers
Indomethacin
NSAID
- Reversibly inhibit COX-1 and -2
- CLOSE PDA
SEs: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers
Ketorolac
NSAID
- Reversibly inhibit COX-1 and -2
SEs: Renal damage, fluid retention, aplastic anemia, GI distress, ulcers
Celecoxib
Selective COX-2 inhibitor
- Spares COX-1, should decr risk of GI irritation/ulceration/bleeding
SE: incr risk of thrombosis, sulfa allergy
Acetaminophen
Reversibly inhibits COX, mostly in CNS. Inactivated peripherally
SE: Heptatic necrosis!! (depletes glutathione and forms toxic tissue adducts)
Etidronate
Bisphosphonate
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: corrosive esophagitis, osteonecrosis of the jaw
Pamidronate
Bisphosphonate
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: corrosive esophagitis, osteonecrosis of the jaw
Alendronate
Bisphosphonate
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: corrosive esophagitis, osteonecrosis of the jaw
Risdedronate
Bisphosphonate
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: corrosive esophagitis, osteonecrosis of the jaw
Zoledronate
Bisphosphonate (IV form)
- Inhibit osteoclast activity, reduce both formation and resorption of hydroxyapatite
SEs: IV so no sophagitis, osteonecrosis of the jaw
Probenicid
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
Allopurinol
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
Febuxostat
Anti-gout, chronic
- Inhibitis xanthine oxidase
Colchicine
Anti-inflammatory, for acute gout
- Binds and stabilizes tubulin to inhibit polymerization and impairs leukocyte chemotaxis and degranulation
Drugs to use in acute gout
Colchicine
Indomethacin
Naproxen/NSAIDs
Etanercept
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
Infliximab
Anti-TNF antibody
Tx: Crohn’s, RA, AS
Increased risk of infection (reactivation of TB), fever, hypotension
Adalimumab
Anti-TNF antibody
Tx: Crohn’s, RA, AS, psoriasis
Increased risk of infection (reactivation of TB), fever, hypotension
Calcipotene
Topical Vit D analog
- Binds and activates Vit D receptor, inhibits keratinocyte proliferation and stimulates differentiation
- Inhibits T cell proliferation and inflammation
Calcitriol
Topical Vit D analog
- Binds and activates Vit D receptor, inhibits keratinocyte proliferation and stimulates differentiation
- Inhibits T cell proliferation and inflammation
Tacalcitol
Topical Vit D analog
- Binds and activates Vit D receptor, inhibits keratinocyte proliferation and stimulates differentiation
- Inhibits T cell proliferation and inflammation
Cyclosporine
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
Ustekinumab
Anti-IL-12 and IL-23
Inhibits differentiation and activation of CD4+ Th1 and Th17
Tx: Psoriasis
Rasburicase
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)