NSAIDs

Question 1

Aspirin (acetylsalicylic acid, ASA)

Answer 1

Class: NSAID
Apps: alagesic, antiinflammatory, antipyretic, antithrombotic
Mech: irreversibly inhibit COX (inhibits COX-1 170x more than COX-2). Its metabolite, salicylic acid, inhibits prostaglandin synthesis. Does not suppress leukotriene synthesis by lipoxygenase
Side effects: GI, nausea, etc. Inhibit uric acid secretion by renal tubule. Bleeding, Salicylate toxicity– hyperthermia, hearing loss, tinnitus.

Question 2

Celecoxib

Answer 2

Class: NSAID, selective COX-2 inhibitor
Apps: analgesic, esp. hyperalgesia.
Mech: selective COX-2 inhibitor, does not inhibit platelet aggregation. Inhibits PGI2 production, but not thrombaxane A2 (made by COX-1).
Effects: GI effects. Increased risk of CV events.

Question 3

Diclofenac

Answer 3

Class: NSAID
Apps: nonselective COX inhibitor. rapid onset of action, well absorbed with i.m. injection
Mech: blocks both COX by blocking arachidonate binding.
Effects: similar to other NSAIDs. hepatotoxicity

Question 4

Ibuprofen

Answer 4

Class: NSAID
Apps: mild to moderate pain
Mech: nonselective COX inhibitor. For OA, RA, dysmenorrhea. antipyretic
Effects: similar to other NSAIDs. GI effects less than those for ASA

Question 5

Indomethacin

Answer 5

Class: NSAID
Apps: potent NSAID, serious side effects. Used for RA, OA, AS, gout.
Mech: nonselective COX inhibitor. oral, rectal or IV. rapid absorption.
Adverse: similar to other NSAIDs.

Question 6

Ketorolac

Answer 6

Class: NSAID
Apps: analgesia onset & efficacy with systemic administration similar to morphine, but less drowsiness/nausea. For MSK pain, IM ketolorac is no better than oral ibuprofen. Can be given IV.
Mech: nonselective COX inhibitor. rapid bioavailability
Effects: more GI problems than other NSAIDs. Can only be given for up to 5 consecutive days

Question 7

Naproxen (Aleve, Naprosyn)

Answer 7

Class: NSAID
Apps: similar to other NSAIDs. Better tolerated than aspirin or indomethacin
Mech: nonselective COX inhibitor. Longer half life than ibuprofen.
Effects: like other NSAIDs.

Question 8

Sulindac

Answer 8

Class: NSAID
Apps: used for OA, RA, AS, bursitis/tendonitis, acute gouty arthritis. Sulindac & celecoxib are only NSAIDs effective for regression of colorectal polyps in patients with familial adenomatous polyposis.
Mech: Nonselective NSAID
Effects: CV events, GI events

Question 9

Meloxicam

Answer 9

Class: NSAID
Apps: arthritis, reduce pain, swelling and joint stiffness. analgesic and antipyretic.
Mech: COX-1 and COX-2 inhibitor. Somewhat selective for COX-2
Effects: GI, tinnitus, headache, rash

Question 10

Acetaminophen

Answer 10

Class: Non-opioid analgesic (NOT and NSAID)
Apps: Analgesic & antipyretic. to treat episodic pain in patients w/ renal disease. May be preferred for elderly with OA b/c of fewer GI & renal effects
Effects: excess dosing = hepatotoxicity.