Week 10 Drugs (Eicosanoids)

Week 10 OMK Block 2

Aspirin (ASA)

Irreversibly inhibits COX-1/2; low doses inhibit platelet TXA₂ → anti-thrombotic; uses: pain, fever, inflammation, MI/stroke prophylaxis; AEs: GI bleeding, renal dysfunction, Reye’s syndrome in children; overdose causes salicylate toxicity (respiratory alkalosis → metabolic acidosis).

Ibuprofen

Propionic acid NSAID; reversible nonselective COX inhibitor; uses: pain, fever, arthritis; AEs: GI upset, ulcers, renal injury.

Naproxen

Propionic acid NSAID; reversible nonselective COX inhibitor; long half-life; uses: pain, arthritis, dysmenorrhea; AEs: GI bleeding, renal toxicity.

Ketoprofen

Propionic acid NSAID; nonselective COX inhibitor; uses: pain, inflammation; AEs: GI and renal toxicity.

Flurbiprofen

Propionic acid NSAID; nonselective COX inhibitor; topical and systemic use for arthritis; AEs: GI irritation, renal dysfunction.

Oxaprozin

Propionic acid NSAID; once-daily dosing; nonselective COX inhibitor; uses: arthritis; AEs: GI upset, ulcers.

Indomethacin

Acetic acid NSAID; potent COX inhibitor; uses: acute gout, PDA closure in infants; AEs: GI/CNS toxicity; not for long-term use.

Diclofenac

Acetic acid NSAID; nonselective COX inhibitor; topical/oral use for arthritis, pain; AEs: GI, hepatic, renal toxicity.

Ketorolac

Acetic acid NSAID; strong COX inhibitor; used for acute moderate-severe pain (short term only); AEs: GI bleeding, renal toxicity.

Sulindac

Acetic acid NSAID; prodrug, COX inhibitor; uses: arthritis; AEs: GI upset, rare hepatotoxicity.

Etodolac

Acetic acid NSAID; relatively COX-2 selective; uses: arthritis, pain; AEs: GI upset, less GI toxicity than nonselective.

Piroxicam

Oxicam NSAID; very long half-life (~50h); once-daily dosing; uses: arthritis; AEs: high GI risk.

Meloxicam

Oxicam NSAID; COX-2 selective at low dose; uses: arthritis, pain; AEs: less GI risk than piroxicam, but ↑ CV risk.

Nabumetone

Ketone NSAID; prodrug; once-daily dosing; nonselective COX inhibitor; uses: arthritis; AEs: GI upset, renal toxicity.

Celecoxib

Selective COX-2 inhibitor; uses: arthritis, dysmenorrhea, pain; fewer GI effects, no platelet inhibition; AEs: ↑ CV risk, same renal toxicity as other NSAIDs.

Alprostadil (PGE₁)

Prostanoid analog; MOA: ↑ cAMP → vasodilation; uses: erectile dysfunction (intracavernosal, intraurethral), maintain PDA patency in neonates; AEs: local pain, priapism.

Misoprostol (PGE₁ analog)

Prostanoid analog; MOA: EP receptor agonist, inhibits acid secretion, ↑ mucus/bicarbonate; uses: prevent NSAID ulcers, cervical ripening, postpartum hemorrhage, abortion (w/mifepristone); AEs: diarrhea, uterine rupture; CI: pregnancy (unless for induction).

Dinoprostone (PGE₂)

Prostanoid analog; MOA: EP receptor agonist, stimulates uterine contraction/cervical softening; uses: cervical ripening, labor induction; AEs: uterine hyperstimulation; CI: asthma, glaucoma, prior uterine scar.

Epoprostenol (PGI₂)

Prostanoid analog; MOA: IP receptor agonist → vasodilation; uses: pulmonary arterial hypertension (continuous IV); AEs: flushing, hypotension, headache, nausea, diarrhea.

Latanoprost (PGF₂α analog)

Prostanoid analog; MOA: FP receptor agonist → ↑ aqueous humor outflow; uses: glaucoma (1st line); AEs: iris darkening, eyelash growth, conjunctival hyperemia, ocular irritation.

Zileuton

Leukotriene modifier; MOA: 5-lipoxygenase inhibitor; uses: persistent asthma; AEs: ↑ LFTs, headache, rare Churg-Strauss syndrome.

Montelukast

Leukotriene modifier; MOA: CysLT₁ receptor antagonist; uses: asthma, allergic rhinitis, exercise-induced bronchospasm; AEs: neuropsychiatric events (depression, suicidality), rare Churg-Strauss syndrome.

Zafirlukast

Leukotriene modifier; MOA: CysLT₁ receptor antagonist; uses: asthma; AEs: ↑ LFTs, headache, neuropsychiatric effects, Churg-Strauss syndrome.