Lecture 76 Prostaglandin Pharm

Question 1

Pharm uses of Prostaglandins (3)

Answer 1

1. Long lasting analogs
2. Inhibition of PG synthesis (mainly COX-2)
3. Dietary manipulation

Question 2

Alprostadil

chem, route, MOA, effects, clinical use, adverse effect

Answer 2

Chem: PGE1
Route: Penile, Intraurethral, IV- wide distribution, metabolized lungs (mainly)
MOA: GPCP stimulates cAMP prod
Effects:Relaxation of arterial smooth m., vasodilation, enhance erection
Use: Erectile dysfx, patency of fetal ductus arteriosus
Black Box: Potential apnea risk for neonates

Question 3

Bimatoprost

chem, route, MOA, effects, clinical use, adverse effect

Answer 3

Chem: PGF-2alpha analog
Route: eye drops, as a pro-drug
MOA: FP (prostaglandin F) receptor agonist
Effect: Lowers intraocular press by increasing outflow of aqueous humor. Increases eyelash length
Use: Eyelash hypotrichosis, open-angle glaucoma, ocular HTN
Side Effects: Conjunctival hyperemia, increase in iris pigmentation

Question 4

Carboprost Tromethamine

chem, route, MOA, effects, clinical use, adverse effect

Answer 4

Chem: PGF- 2alpha analog
Route: IM (diff from bimatoprost)
MOA: EP1 receptor agonist
Effects: stimulates uterine contractions, stops uterine bleeding
Uses: Induction of 2nd trimester abortion, refractory postpartum uterine bleeding
Side effects: diarrhea, nausea, vomiting

Question 5

Dinoprostone

chem, route, MOA, effects, clinical use, adverse effect

Answer 5

Chem: Synthetic preparation of PGE2
Route: Vaginal
MOA: EP2 receptor agonist
Effect: Stimulates induction of uterine contractions, effects cervical collagenase activity
Use: ripening of cervix for induction of labor, induction of 2nd trimester abortion, miss abortion, evacuation of uterus in intrauterine death, benign hydatiform mole

Question 6

Lantanoprost

route, MOA, effects, clinical use, adverse effect

Answer 6

Route: ophthalmic, stable long acting, prodrug, half-life 17 min
MOA: FP receptor agonist
Effect: lowers intraocular press by increasing outflow of aqueous humor
Use: open angle glaucoma, ocular HTN
Side effects: brown pigemtation of iris, blurred vision, burning/stinging

Question 7

Tafluprost

chem, route, MOA, effects, clinical use, adverse effect

Answer 7

Chem: PGF- 2alpha analog
Route: ophthalmic as pro drug
MOA: FP receptor agonist (12x higher affinity than latanoprost)
Effect: lowers intraocular press by increasing outflow of aqueous humor
Use: open angle glaucoma, ocular HTN
Side effect: conjuctival hyperemia

Question 8

Travoprost

chem, route, MOA, effects, clinical use, adverse effect

Answer 8

Chem: PGF 2alpha analog
Route: Ophthalmic as pro-drug
MOA: FP receptor agonist
Effect:lowers intraocular press by increasing outflow of aqueous humor
Use: Open angle glaucoma, ocular HTN (after other drugs didnt work)

Question 9

Epoprostenol

Answer 9

Used for pulmonary arterial HTN

Question 10

Misoprostol

Answer 10

Prevention of NSAID- induced gastric ulcers