Pharmacology of Prostaglandin Analogues

Table of Contents

I. Introduction

Prostaglandins are autacoids derived from arachidonic acid via the cyclooxygenase pathway and modulate numerous physiological processes—vascular tone, inflammation, gastric cytoprotection, uterine contraction, and intraocular pressure. Prostaglandin analogues are synthetic structural or functional mimetics designed to replicate or enhance one or more actions of natural prostaglandins, often with improved pharmacokinetics and receptor selectivity. Their clinical applications span from glaucoma and obstetric indications to peptic ulcer protection and pulmonary arterial hypertension.

II. Classification and Examples

Subtype	Key Drugs	Primary Use
PGF2α analogues	Latanoprost, Bimatoprost, Travoprost, Tafluprost	Glaucoma
PGE1 analogues	Misoprostol, Alprostadil	Gastric protection, ED, ductus arteriosus patency
PGE2 analogues	Dinoprostone	Labor induction, cervical ripening
PGI2 analogues	Epoprostenol, Iloprost, Treprostinil, Beraprost	Pulmonary HTN, antiplatelet

III. Mechanisms of Action

Prostaglandin receptors are G-protein-coupled receptors (GPCRs) selectively activated by PG analogues, resulting in diverse tissue-specific effects:

PGF2α analogues: Lower intraocular pressure via increased uveoscleral outflow (glaucoma therapy).
PGE1/PGE2 analogues: Relax smooth muscle, modulate gastric mucosal protection, contract/relax uterine tissue depending on site/receptor.
PGI2 analogues: Potent vasodilation in pulmonary vasculature; inhibit platelet aggregation.

IV. Pharmacological Profiles and Clinical Uses

A. PGF2α Analogue Eye Drops (Glaucoma)

Latanoprost, Bimatoprost, Travoprost, Tafluprost

Action: Topical application increases uveoscleral outflow of aqueous humor, lowering intraocular pressure (IOP).
Therapeutic use: Primary open-angle glaucoma; ocular hypertension
Pharmacokinetics: Administered once daily, well-absorbed into anterior segment.
Adverse effects: Iris pigment darkening, eyelash growth (hypertrichosis), conjunctival hyperemia, rare uveitis, cystoid macular edema.

Bimatoprost is also used for cosmetic eyelash enhancement.

B. PGE1 and PGE2 Analogues

1. Misoprostol (PGE1 analogue)

Action: Increases gastric mucus and bicarbonate production, reduces acid secretion.
Therapeutic use: Prevention of NSAID-induced gastric ulcers (co-prescribed with long-term NSAIDs), abortifacient use (with mifepristone).
Adverse effects: Diarrhea, abdominal cramps, uterine contractions, contraindicated in pregnancy (unless for medical abortion).

2. Alprostadil (PGE1 analogue)

Use:

Maintains ductus arteriosus patency in neonates with congenital heart defects until surgery
Erectile dysfunction (intracavernosal, intraurethral use)

Adverse effects: Penile pain, hypotension, flushing.

3. Dinoprostone (PGE2 analogue)

Use:

Cervical ripening, induction of labor, pregnancy termination

Adverse effects: Uterine hyperstimulation, GI upset, fever.

C. PGI2 (Prostacyclin) Analogues

Epoprostenol, Iloprost, Treprostinil, Beraprost

Action: Induce pulmonary/prostacyclin receptor-mediated vasodilation, inhibit platelet aggregation
Therapeutic use: Pulmonary arterial hypertension, Raynaud’s phenomenon, off-label for PVD
Pharmacokinetics: Epoprostenol (IV, short half-life), iloprost/treprostinil (inhaled, oral, subcutaneous, longer action)
Adverse effects: Flushing, headache, hypotension, jaw pain, limb pain

V. Other Indications

Gemeprost and carboprost: Synthetic PGE1, PGF2α analogues, respectively; used in medical abortion and postpartum hemorrhage.
Lubiprostone (PGE1 derivative): Activates ClC-2 chloride channels in gut, approved for chronic constipation and irritable bowel syndrome with constipation.

VI. Adverse Effects and Contraindications

Drug/Class	Major Adverse Effects	Contraindications
Glaucoma agents	Iris/skin pigmentation, eyelash changes	Macular edema, uveitis risk
Misoprostol	Diarrhea, cramps, abortion risk	Pregnancy (unless intended)
Labor inducers	Uterine rupture, hyperstimulation	Prior C-section, uncontrolled asthma
Pulmonary HTN agents	Flushing, hypotension, bleeding	Cardiac decompensation, bleeding

VII. Summary Table

Analogue	Structure Base	Main Uses	Notable AE
Latanoprost	PGF2α	Glaucoma	Iris pigment, lashes
Misoprostol	PGE1	Ulcer prevention, abortion	Diarrhea
Dinoprostone	PGE2	Labor, cervical ripening	Uterine hyperstim
Epoprostenol	PGI2	Pulmonary hypertension	Flushing, headache

Prostanoid receptors: transduction and functional cues

Receptor	Endogenous agonist	Primary G protein	Main second messenger	Representative effects
EP1	PGE2	Gq/11	↑IP3/DAG, ↑Ca2+	Smooth muscle contraction context‑dependently in select tissues
EP2	PGE2	Gs	↑cAMP	Smooth muscle relaxation and anti‑inflammatory signaling in many beds
EP3	PGE2	Gi (±Gq/11 splice variants)	↓cAMP (±↑Ca2+)	Uterine contraction and diverse tissue‑specific effects by isoform
EP4	PGE2	Gs	↑cAMP	Vasodilation, tissue protection, and immunomodulation pathways
FP	PGF2α	Gq/11	↑IP3/DAG, ↑Ca2+	Uterine contraction and ciliary muscle remodeling for IOP reduction
IP	PGI2	Gs	↑cAMP	Vasodilation, anti‑platelet, anti‑proliferative vascular actions
TP	TXA2	Gq/11	↑IP3/DAG, ↑Ca2+	Platelet activation and vasoconstriction balance to PGI2
DP1	PGD2	Gs	↑cAMP	Vasodilation and neuromodulatory roles in select contexts
DP2 (CRTH2)	PGD2	Gi‑biased	↓cAMP and chemotaxis signals	Leukocyte chemotaxis and Th2‑linked responses

Therapeutic prostaglandin analogs: routes, uses, and key cautions

Class	Examples	Route	Key indications	Prominent cautions
PGE1	Alprostadil	Intracavernosal, intraurethral, IV	Erectile dysfunction and ductus arteriosus patency	Priapism in hematologic risk, fibrosis in Peyronie disease
PGE1	Misoprostol	Oral, vaginal, buccal, sublingual, rectal	NSAID‑ulcer prevention and obstetric uses off‑label	Teratogenic for ulcer prophylaxis during pregnancy
PGE2	Dinoprostone	Vaginal insert	Cervical ripening and induction	Hyperstimulation risk with inadequate spacing or monitoring
PGF2α	Carboprost	IM	Postpartum hemorrhage and abortion induction	Bronchospasm and GI intolerance
FP agonists	Latanoprost, Travoprost, Tafluprost	Topical ophthalmic	Glaucoma and ocular hypertension	Hyperemia, pigment changes, lash growth
FP/prostamide	Bimatoprost	Topical ophthalmic/dermal	Glaucoma and eyelash hypotrichosis	Eyelash prominence and periocular pigmentation
FP + NO donor	Latanoprostene bunod	Topical ophthalmic	Glaucoma with dual outflow mechanism	As with class, plus NO‑mediated effects
IP agonists	Epoprostenol	IV continuous	Pulmonary arterial hypertension	Vasodilation, thrombocytopenia, line dependence
IP agonists	Treprostinil	IV, SC, inhaled, oral	Pulmonary arterial hypertension	Site pain (SC), cough (inhaled), hypotension
IP agonists	Iloprost	Inhaled	Pulmonary arterial hypertension	Hypotension, headache, cough

VIII. Key Learning Points

Prostaglandin analogues are powerful and targeted modulators of smooth muscle and other tissues, harnessed in a range of therapies: glaucoma, GI protection, obstetrics, pulmonary hypertension, and more.
Class and receptor selectivity defines both their main clinical utility and adverse effect profile.
They have strict contraindications, especially in pregnancy and certain cardiovascular/eye conditions.

IX. References

Brunton LL, Hilal-Dandan R, Knollmann BC. Goodman & Gilman’s The Pharmacological Basis of Therapeutics. 13th Edition. “Prostaglandins and Leukotrienes.”
Katzung BG, Trevor AJ, eds. Basic & Clinical Pharmacology. 15th Edition. Chapters: Eicosanoids, Uterine relaxants/stimulants, Glaucoma pharmacology.
Ritter JM, Flower RJ, Henderson G, et al. Rang & Dale’s Pharmacology. 10th Edition. GPCR ligands, glaucoma drugs, eicosanoid drugs.

How to cite this page - Vancouver Style

Bharatha, Dr. Ambadasu. Pharmacology of Prostaglandin Analogues. Pharmacology Mentor. Available from: https://pharmacologymentor.com/pharmacology-of-prostaglandin-analogues/. Accessed on January 26, 2026 at 02:30.

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