1.What does NSAID stand for?: Non-Steroidal Anti-Inflammatory Drug
2.What are prostaglandins?: Local (paracrine) mediators of inflammation (short half-life)
3.How are prostaglandins synthesized?: Synthesized by cyclooxygenase enzyme from arachidonic acid, makes thromboxane also
(platelet aggregation)
4.What do prostaglandins cause?: ~Increased sensitivity of pain receptors
~Increased body temperature (fever)
~Secretion of cytoprotective mucus in stomach (good)
~Uterine wall contractions
~Renal vasodilation
5.What is an effect of prostaglandins that we may want?: Secretion of cytoprotective mucus in stomach
6.What are cyclooxygenases?: Enzymes that control prostaglandin production
7.What are the two isozymes of cyclooxygenase (COX)? What do they cause?: 1.
COX1 - mainly affects stomach mucus production
2. COX2 - pain sensitivity, fever, inflammation
8. How do NSAIDs work?: Inhibiting cyclooxygenases
9. What are NSAIDs used for?: ~Baby aspirin to reduce risk of MIs and strokes
~Osteoarthritis - degeneration of the joints
~Rheumatoid arthritis - progressive inflammatory disease of joints, affects >40 million Americans, autoimmune ~Aches and pains
~Menstrual cramps (primary dysmenorrhea) - aspirin not particularly effective
10. Side-effects of NSAIDs?: ~Stomach ulceration - rare, usually caused by bacteria
~Increased risk of hemorrhage
~Renal failure
~Asthma attacks in 20% of asthma patients
~Reduced efficacy of ACE inhibitor drugs
11. What is unique about the possible renal failure side-effect of NSAIDs?: Occurs
at high dosages in predisposed patients; those with decreased circulation volume due to CHF, liver cirrhosis, renal disease, use of
diuretics, elderly
12. Analgesic, antipyretic, anti-inflammatory; inhibits thromboxane production
(lowers MI, ischemic stroke risk); gastric bleeding with prolonged use; OTC: acetylsalicylic acid (ASA, Aspirin)
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13 q 4 hours; better than aspirin for primary dysmenorrhea, less risk of gastric bleeding; OTC: ibuprofen (Advil, Motrin)
14. similar to ibuprofen, longer half-life (q 8 hours); OTC: naproxen (Aleve)
15. acetylsalicylic acid (ASA, Aspirin): Analgesic, antipyretic, anti-inflammatory; inhibits thromboxane production (lowers MI,
ischemic stroke risk); gastric bleeding with prolonged use; OTC
16. ibuprofen (Advil, Motrin): q 4 hours; better than aspirin for primary dysmenorrhea, less risk of gastric bleeding; OTC
17. naproxen (Aleve): similar to ibuprofen, longer half-life (q 8 hours); OTC
18. Ketorolac: High efficacy, not opioid (most efficacious NSAID); prescription only; used post-surgery; IM, IV, opthalmic, oral
forms (6h half-life); short-term use only (<5 days) due to risk of stomach ulcers (inhibits COX1 as well as COX2)
19. High efficacy, not opioid (most efficacious NSAID); prescription only; used post-surgery; IM, IV, opthalmic, oral forms (6h
half-life); short-term use only
(<5 days) due to risk of stomach ulcers; inhibits COX1: Ketorolac
20. NSAID with highest efficacy: Ketorolac
21. Prescription only NSAID used for short-term post-surgery: Ketorolac
22. COX2 inhibitors: Should cause pain-relief without risk of COX1-related stomach ulcers or bleeding; for long-term arthritis
use
23. celecoxib (Celebrex): COX2 inhibitor; doesn't inhibit platelet aggregation; some increase in mortality due to strokes/MIs
24. COX2 inhibitor; doesn't inhibit platelet aggregation; some increase in mortality due to strokes/MIs: celecoxib (Celebrex)
25. Two COX2 inhibitors that were discontinued due to increased mortality by strokes/MIs: Vioxx, Bextra
26. Acetaminophen (APAP, Tylenol): Not actually anti-inflammatory, analgesic and antipyretic; works via
CNS effects; does not cause stomach ulcers; OTC, but very high doses can cause liver failure
27. Tylenol 1, 2, 3, 4: Contain APAP + codeine at different doses; require prescription
28. Not actually anti-inflammatory, analgesic and antipyretic; works via CNS effects; does not cause stomach ulcers; OTC, but
very high doses can cause liver failure: Acetaminophen (APAP, Tylenol)
29. Tylenol for migraines?: Combined with butalbital (barbiturate)
30. Migraines?: Difficult to treat as cause is not well-understood
31 Triptan drugs: For migraines, serotonin agonists?, work best if taken at onset; SC injection best, nasal spray, oral pill also
available; sumatriptan (Imitrex) and others; generics all end in -triptan
32. Suffix for migraine drugs?: -triptan
33. Triptan drug for migraines?: sumatriptan (Imitrex)
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