Inflammation

Question 1

Acetylsalicylic acid (ASA, Aspirin)

Answer 1

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

Question 2

Diflunisal (Dolobid)

Answer 2

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

Question 3

Acetaminophen (Tylenol)

Answer 3

Class: Para-amino phenol
MOA: Reversibly inhibits COX-1 and -2 (favors COX-1)
Uses: Analgesic and antipyretic effect similar to aspirin, but weak anti-inflammatory effects
SE: Renal tubular necrosis if chronically abused with other NSAIDs; hepatic necrosis with overdose; GI irritation (less than aspirin)
Misc: 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

Indomethacin (Indocin)

Answer 4

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

Question 5

Sulindac (Clinoril)

Answer 5

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

Question 6

Ibuprofen (Advil, Motrin)

Answer 6

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

Question 7

Flurbiprofen (Ocufen)

Answer 7

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

Question 8

Naproxen (Aleve)

Answer 8

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

Question 9

Oxaprozin (Daypro)

Answer 9

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

Question 10

Piroxicam (Feldene)

Answer 10

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

Question 11

Ketorolac (Toradol)

Answer 11

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

Question 12

Celocoxib (Celebrex)

Answer 12

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

Question 13

Etoricoxib (Arcoxia)

Answer 13

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