Musculoskeletal, Skin, and CT Pharm Flashcards
NSAIDs Examples
Ibuprophen, naproxen, indomethacin, ketorolac, diclofenac
NSAIDs MOA
Reversibly inhibit COX 1 and 2. Block PG synthesis.
NSAIDs Clinical Use
Antipyretic, analgesic, anti-inflammatory. Indomethacin is used to close a PDA.
NSAIDs Toxicity
Interstitial nephritis, gastric ulcer (PGs protect gastric mucosa), renal ischemia (PGs vasodilate afferent arteriole)
COX-2 Inhibitors (celeCOXib) MOA
- Reversibly inhibit specifically the COX-2 isoform, 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 TXAs production is dependent on COX-1.
COX-2 Inhibitors (celeCOXib) Clinical Use
Rheumatoid arthritis and osteoarthritis; patients with gastritis or ulcers.
COX-2 Inhibitors Toxicity
Increased risk of thrombosis. Sulfa allergy.
Acetaminophen (Tylenol) MOA
Reversibly inhibits cyclooxygenase, mostly in the CNS. Inactivated peripherally.
Acetaminophen Clinical Use
Antipyretic, analgesic, but NOT anti-inflammatory. Used instead of aspirin to avoid Reye’s syndrome in children with viral infection.
Acetaminophen Toxicity
Overdose produces hepatic necrosis; acetaminophen metabolite depletes glutathione and forms toxic tissue adducts in liver
Antidote? N-acetylcysteine which regenerates glutathione
Bisphosphonates (Alendronate and other -dronates) MOA
Pyrophosphate analogs; bind hydroxyapatite in bone inhibiting osteoclast activity–> less bone resorption
Bisphosphonates (Alendronate and other -dronates) Clinical Use
Osteoporosis, hypercalcemia, Paget’s disease of bone
Bisphosphonates (Alendronate and other -dronates) Toxicity
Corrosive esophagitis, osteonecrosis of the jaw
Chronic Gout Drugs
Allopurinol, Febuxostat, Probenecid, Colchicine
Acute Gout Drugs
NSAIDs (naproxen and indomethacin)
Glucocorticoids (oral or intra-articular)