MSK/CT - Pharm Flashcards
Acetominophen MOA
REVERSIBLY inhibits COX, mostly in CNS
Inactivated peripherally
Acetominophen use
Antipyretic and analgesic, but NOT anti-inflammatory
use in kids with viral illnesses
Acetominophen toxicity
Zone III hepatic necrosis
NAPQI = toxic, depletes glutathione (regenerate with NAC = antidote)
Asprin MOA
IRREVERSIBLY inhibits COX-1 and COX-2 via acetylation.
Causes decrease in TXA2 (increase bleeding time via decreased platelet aggregation) and prostaglandins
Asprin use:
LD = anti-coagulant MD = antipyretic and analgesic HD = anti-inflammatory
Asprin toxicity:
- Tinitus
- Gastric ulcers
- Chronic = GI bleed, ARF, AIN
- Reyes in kids with viruses
- Early respiratory alkalosis, then mixed with metabolic acidosis
Celecoxib MOA
REVERSIBLY inhibit COX-2 - inflammatory cells and endothelium for pain and inflammation [NOT gastric mucosa or platelets]
Celecoxib Use
RA
OA
NO GI effects
Celecoxib toxicity
Thrombosis:
Block endothelium VD without blocking platelet aggregation –> pro-coagulant state
sulfa
NSAIDs
REVERSIBLY inhibit COX 1 and COX 2
NSAIDs specific use
Indomethacin closes PDA, acute gout attacks, treats DI,
NSAID toxicity
- interstitial nephritis
- gastric ulcers
- renal ischemia
Bisphosphonates:
Alendronate, other ___dronates
Bisphosphonate mechanism
PPi analog: bind hydroxyapatite in bone, and inhibit osteoclast activity
Bisphosphonates use
OP
Hypercalcemia (from malignancies)
Pagets
Bisphosphonates toxicity
- Erosive esophagitis
- Jaw osteonecrosis
Teriparatide MOA
Recombinant PTH analog: give SubQ daily to INCREASE osteoblast activity
Teriparatide use
OP: actually causes bone growth, not just stopping resorption like bisphosphonates
Teriparatide toxicity
Transient hypercalcemia
Risk of osteosarcoma
Alloputinol MOA
inhibits XO after being converted to alloxanthane:
- decreases hypoxanthane to xanthate
- decreases xanthine to uric acid
Allopurinol use
Gout
Allopurinol Toxicity
Increases levels of 6-MP and azathioprine because they are metabolized by XO
Feboxutat
Inhibits XO (like allopurinol)
Pegloticase
uric acid to allantoin (water soluble)
Rasburicase
uric acid to allantoin (water soluble)
Probenecid MOA
Inhibits uric acid reabsorption in PCT
Probenecid use
Gout
Give with cidofovir to decrease nephrotoxicity
Probenecid toxicity
prevents penicillin secretion
Uric acid crystals (urate nephropathy)
Sulfa
Drugs for chronic gout (prevention)
Allopurinol Feboxustat Pegloticase Rasburicase Probenecid Colchicine
Drugs for acute gout
NSAIDs (indomethacin and naproxen)
Glucocorticoids: oral or injections
Colchicine
Colchicine MOA
Stabilize tubulin inhibiting MT polymerization and thus PMN chemotaxis and degranulation
Colchicine AE
GI: N/V/D
Sialycilates in gout
BAD!
inhibit uric acid clearance
TNF-a inhibitor AE
increase infections and reactivation of TB (needed for granulomas)
Etanercept
Fusion protein of TNF-a-R and IgG1-Fc
Etanercept use
RA, psoriasis, ankylosing spondylitis
Infliximab
anti-TNF-a monoclonal Ab
Infliximab use
IBD, RA, ankylosing, psoriasis
Adalimumab
anti-TNF-a monoclonal Ab
Adalimumab use
IBD, RA, ankylosing, psoriasis
