Musculoskeletal Pharm EC Flashcards
LTB4 function
Neutrophil chemotaxis
LTC4, LTB4, LTE4 functions
Bronchoconstriction
Vasoconstriction
SM contraction
Increased vascular permeability
PGI2 functions
Inhibits platelet aggregation
Vasodilation
PGE2, PGF2 functions
Increase uterine tone
Increase vascular tone
Decrease bronchial tone
TXA2 functions
Increase platelet aggregation
Increase vascular tone
Increase bronchial tone
Aspirin (MOA, Use, Tox)
Irreversibly inhibit COX1&2 by acetylation
Increased bleeding time with no change in PT or PTT
Low dose=inhibit platelet aggregation
Medium dose=antipyretic/analgesic
High dose=anti-inflammatory
Gastric ulceration, tinnitus, acute renal failure, interstitial nephritis, upper GI bleed.
Risk of Reye’s syndrome in children with viral infection.
Stimulates respiratory centers (hyperventilation/respiratory alkalosis)
Ibuprofen, Naproxen, Indomethacin, Ketorolac, Diclofenac (MOA, Use, Tox)
NSAIDS
Reversibly inhibit COX 1&2
Antipyretic, analgesic, anti-inflammatory.
Indomethacin used to close PDA
Interstitial nephritis, Gastric ulcer (PG’s protect gastric mucosa), Renal ischemia (PGs vasodilate afferent arteriole)
Celecoxib (MOA, Use, Tox)
COX 2 inhibitor (spares COX1 which helps maintain gastric mucosa and spares platelet function as TXA2 is dependent on COX 1)
RA and osteoarthritis, patients with gastritis or ulcers
Increased risk of thrombosis
Sulfa allergy
Acetaminophen (MOA, Use, Tox)
Reversibly inhibits cyclooxygenase, MOSTLY IN CNS (inactivated peripherally)
Antipyretic, analgesic, NOT ANTI-INFLAMMATORY
Used instead of aspirin to avoid Reye’s syndrome in children with viral infection
Overdose produces hepatic necrosis
(acetaminophen metabolite depletes glutathione and forms toxic tissue adducts in liver)
*Antidote=N-acetylcysteine (regenerates glutathione)
Alendronate (MOA, Use, Tox)
Bisphosphonate Pyrophosphate analog (bind hydroxyapatite in bone, inhibiting osteoclasts)
Osteoporosis
Hypercalcemia
Paget’s
Corrosive esophagitis, osteonecrosis of jaw
Allopurinol (MOA, Use, Drug-interaction)
Inhibits Xanthine oxidase (decrease conversion of xanthine to uric acid)
Chronic Gout, lymphoma/leukemia (prevent tumor lysis)
Increases Azathioprine and 6-MP (met. by XO)
Febuxostat (MOA, Use, Tox)
Inhibits Xanthine oxidase (decrease conversion of xanthine to uric acid)
Chronic Gout
Probenecid (MOA, Use, Drug-interaction)
Inhibit reabsorption of uric acid in proximal convoluted tubule
Chronic Gout
Inhibits secretion of penicillin
Colchicine (MOA, Use, Tox)
Stabilize tubulin to inhibit polymerization (impairing leukocyte chemotaxis and degranulation)
Chronic Gout
GI side effects
Acute gout drugs
Naproxen, Indomethacin (NSAIDS)
Glucocorticoids