Inflammation drugs

Question 1

Acetylsalicylic acid

Mech
Tx
Side eff

Answer 1

irreversibly acetylates COX-1 and -2; metabolite (salicylic acid) reversibly inhibits COX-1 and -2

Tx: 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

Question 2

Diflunisal

Mech
Tx
Side eff

Answer 2

Difluorophenyl derivitive of salicylic acid, which reversibly inhibits COX-1 and -2

Tx: Osteoarthritis, musculoskeletal strains/sprains, pain after dental extraction, and postepisiotomy pain

Fewer GI side effects and less effect on platelets than aspirin

Question 3

Acetaminophen

Mech
Tx
Side eff

Answer 3

Reversibly inhibits COX-1 and -2 (favors COX-1)

Tx: 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

Question 4

Indomethacin

Mech
Tx
Side eff

Answer 4

Reversibly inhibits COX-1 and -2 (favors COX-1)

Tx: 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

Sulindac

Mech
Tx
Side eff

Answer 5

Reversibly inhibits COX-1 and -2 (favors COX-1)

tx: Rhematoid arthritis, ankylosing spondylitis, osteoarthritis, acute gout

At times, thrombocytopenia, aplastic anemia, and severe frontal headaches
Nephrotoxicity in elderly or hypovolemic patients

Question 6

Ibuprofen

Mech
Tx
Side eff

Answer 6

Reversibly inhibits COX-1 and -2 (favors COX-1)

Tx: Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

GI irritation; hepatotoxicity (less frequent than aspirin)

Question 7

Flurbiprofen

Mech
Tx
Side eff

Answer 7

Reversibly inhibits COX-1 and -2 (favors COX-1)

Tx: Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

GI irritation; hepatotoxicity (less frequent than aspirin)

Question 8

Naproxen

Mech
Tx
Side eff

Answer 8

Reversibly inhibits COX-1 and -2 (favors COX-1)

Tx: Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

GI irritation; hepatotoxicity (less frequent than aspirin)

Question 9

Oxaprozin

Mech
Tx
Side eff

Answer 9

Reversibly inhibits COX-1 and -2 (favors COX-1)

Tx: Rheumatic disorders, osteoarthritis, ankylosing spondylitis, postpartum pain, dysmenorrheal pain, and many types of surgeries

GI irritation; hepatotoxicity (less frequent than aspirin)

Question 10

Piroxicam

Mech
Tx
Side eff

Answer 10

Reversibly inhibits COX-1 and -2 (favors COX-1)
Very long half-life (45 hours) permits single daily dose

Tx: Long-term treatment of rheumatoid arthritis or osteoarthritis; also, ankylosing spondylitis, acute musculoskeletal disorders, acute gout

Same as aspirin

Question 11

Ketorolac

Mech
Tx
Side eff

Answer 11

Reversibly inhibits COX-1 and -2 (favors COX-1)
Injectable (one of few NSAIDs available for this)

Post-operative pain; inflammatory eye conditions

Same as aspirin; relatively nonirritating

Question 12

Celocoxib

Mech
Tx
Side eff

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

Etoricoxib

Mech
Tx
Side eff

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