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Pilocarpine

Common Name: Jaborandi alkaloid Brands: Salagen, Isopto Carpine

Medicinal Chemistry

Molecular Weight 208.26
Molecular Formula C11H16N2O2
IUPAC Name
(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]dihydrofuran-2(3H)-one

Pharmacognosy

Biological Source

Pilocarpus jaborandi, P. microphyllus

Active Constituents

Pilocarpine

Pharmacology & Synthesis

Mechanism of Action

Direct-acting cholinergic agonist; specifically stimulates muscarinic receptors (M3).

Pharmacokinetics (ADME)

A: Good topical/oral absorption.
D: Localized in eye or systemic if oral.
M: Plasma esterases and hepatic.
E: Renal.

Pharmacodynamics

Causes miosis, contraction of ciliary muscle, and intensely stimulates sweating/salivation.

Synthesis Pathway

Derived from histidine.

Safety, Warnings & Interactions

Adverse Effects

Sweating, salivation, brow ache (topical), bradycardia.

Contraindications

Narrow-angle glaucoma (paradoxical block), acute iritis.

Drug Interactions

Anticholinergics (antagonism).

Pharmaceutics & Compendia

Dosage Forms Ophthalmic drops, Tablets
Official Compendia IP, BP, USP
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