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Description

Generic Name

Pilocarpine, pilocarpine nitrate

Chemical names

(+)-Pilocarpine hydrochloride, Pilocarpal, Pilocar

Brand names

Pilorin, pilomax, pilopress, pilomin, pilodrop, locarp

IUPAC name

(3S,4R)-3-ethyl-4-[(1-methyl-1H-imidazol-5-yl)methyl]oxolan-2-one

Pharmacokinetics

Metabolism: Inactivated at neuronal synapses and in plasma.

Excretion: urine

Actions

Pilocarpine is a cholinergic parasympathomimetic agent. It increases secretion by the exocrine glands, and produces contraction of the iris sphincter muscle and ciliary muscle (when given topically to the eyes) by mainly stimulating muscarinic receptors.

Dosage/Dosage form

  • Pilocarpine hydrochloride 5 and 7.5 mg oral tablets
  • Eye drops 5 ml

Therapeutic uses

Glaucoma

Adverse effects/Side effects

Lachrimation, blurred vision, vitreous haemorrhage, browache, pain and irritation

Interaction

  • Aminoglycosides, colistin, clindamycin, cyclopropane and halogenated inhalational anaesthetics, procainamide, quinine, β-blockers and lithium may reduce the efficacy of pilacarpine.
  • Concomitant admin of 2 miotics may increase risk of toxic reactions.
  • Concurrent use with β-blockers may lead to bradycardia.

Contraindications

Lactation, Angle-closure glaucoma, anterior uveitis, acute iritis, hypersensitivity, Pregnancy.

Storage

  • Oral: Store at 2-27°C.
  • Ophthalmic: Store <8°C. Do not freeze. 

Information

Molecular weight

244.719 g/mol

Molecular formula

C11H16N2O2

CAS number

92-13-7

Precautions

Prolonged use may lead to lens opacities. Patients with renal impairment, cognitive or psychiatric disorders, biliary tract disorders.