Inflammation

Question 1

Class;Mechanism;Therapeutics;SideEffects

Acetylsalicylic acid (ASA, Aspirin)

Answer 1

Salicylate Acetyl-salicylic acid irreversibly acetylates COX-1 and -2; metabolite (salicylic acid) reversibly inhibits COX-1 and -2 Antiplatelet, analgesic and antipyretic, and anti-inflammatory (in ascending order of amount taken); often taken as a “baby aspirin” to prevent MI, CVA GI irritation, bleeding and anemia, hepatotoxicity, and salicylate toxicity Nephrotoxicity in elderly or hypovolemic patients; rare hypersensitivity reaction —

Question 2

Class;Mechanism;Therapeutics;SideEffects

Diflunisal (Dolobid)

Answer 2

Salicylate Difluorophenyl derivitive of salicylic acid, which reversibly inhibits COX-1 and -2 Osteoarthritis, musculoskeletal strains/sprains, pain after dental extraction, and postepisiotomy pain Fewer GI side effects and less effect on platelets than aspirin — —

Question 3

Class;Mechanism;Therapeutics;SideEffects

Acetaminophen (Tylenol)

Answer 3

Para-amino phenol Reversibly inhibits COX-1 and -2 (favors COX-1) Analgesic and antipyretic effect similar to aspirin, but weak anti-inflammatory effects Renal tubular necrosis if chronically abused with other NSAIDs; hepatic necrosis with overdose GI irritation (less than aspirin) Poor function in presence of peroxides (as found in sites of inflammation); mostly metabolized via conjugation, but minor pathway via P450 enzymes may lead to toxic intermediate (N-acetyl-benzoquinoneimine)

Question 4

Class;Mechanism;Therapeutics;SideEffects

Indomethacin (Indocin)

Answer 4

Indole Reversibly inhibits COX-1 and -2 (favors COX-1) Rhematoid arthritis (10X as potent as aspirin), ankylosing spondylitis, osteoarthritis, acute gout At times, thrombocytopenia, aplastic anemia, and severe frontal headaches Nephrotoxicity in elderly or hypovolemic patients —

Question 5

Class;Mechanism;Therapeutics;SideEffects

Sulindac (Clinoril)

Answer 5

Indole Reversibly inhibits COX-1 and -2 (favors COX-1) Rhematoid arthritis, ankylosing spondylitis, osteoarthritis, acute gout At times, thrombocytopenia, aplastic anemia, and severe frontal headaches Nephrotoxicity in elderly or hypovolemic patients Half as potent as indomethacin; side effects less frequent

Question 6

Class;Mechanism;Therapeutics;SideEffects

Ibuprofen (Advil, Motrin)

Answer 6

Proprionic acid dervitive Reversibly inhibits COX-1 and -2 (favors COX-1) Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries GI irritation; hepatotoxicity (less frequent than aspirin) — —

Question 7

Class;Mechanism;Therapeutics;SideEffects

Flurbiprofen (Ocufen)

Answer 7

Proprionic acid dervitive Reversibly inhibits COX-1 and -2 (favors COX-1) Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries GI irritation; hepatotoxicity (less frequent than aspirin) — —

Question 8

Class;Mechanism;Therapeutics;SideEffects

Naproxen (Aleve)

Answer 8

Proprionic acid dervitive Reversibly inhibits COX-1 and -2 (favors COX-1) Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries GI irritation; hepatotoxicity (less frequent than aspirin) — Longer half-life than most proprionic acid derivitives (13 hours vs. 1-2 hours)

Question 9

Class;Mechanism;Therapeutics;SideEffects

Oxaprozin (Daypro)

Answer 9

Proprionic acid dervitive Reversibly inhibits COX-1 and -2 (favors COX-1) Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries GI irritation; hepatotoxicity (less frequent than aspirin) — Much longer half-life than most proprionic acid derivitives (50 hours vs. 1-2 hours)

Question 10

Class;Mechanism;Therapeutics;SideEffects

Piroxicam (Feldene)

Answer 10

Enolic acid Reversibly inhibits COX-1 and -2 (favors COX-1) Long-term treatment of rheumatoid arthritis or osteoarthritis; also, ankylosing spondylitis, acute musculoskeletal disorders, acute gout — Same as aspirin Very long half-life (45 hours) permits single daily dose

Question 11

Class;Mechanism;Therapeutics;SideEffects

Ketorolac (Toradol)

Answer 11

Heteroaryl acetic acids Reversibly inhibits COX-1 and -2 (favors COX-1) Post-operative pain; inflammatory eye conditions — Same as aspirin; relatively nonirritating Injectable (one of few NSAIDs available for this)

Question 12

Class;Mechanism;Therapeutics;SideEffects

Celocoxib (Celebrex)

Answer 12

COX-2 inhibitor Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site) Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs Less GI toxicity than traditional NSAIDs — Contraindicated in patients with heart problems/pregnancy

Question 13

Class;Mechanism;Therapeutics;SideEffects

Etoricoxib (Arcoxia)

Answer 13

COX-2 inhibitor Selectively inhibits COX-2 (too bulky to reliably interact in COX-1 site) Same anti-inflammatory, antipyretic, and analgesic effects as NSAIDs Less GI toxicity than traditional NSAIDs — Contraindicated in patients with heart problems/pregnancy