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Pilocarpine information from DrugsUpdate  

See Available Brands of Pilocarpine in India

P - Contraindicated in pregnancy
L - Caution when used during lactation

Pilocarpine is a muscarinic alkaloid obtained from the leaves of tropical American shrubs from the genus Pilocarpus. It is a non-selective muscarinic receptor agonist in the parasympathetic nervous system, which acts therapeutically at the muscarinic acetylcholine receptor M3 due to its topical application, e.g., in glaucoma and xerostomia.

Pharmacodynamics

Pharmacokinetics

Pilocarpine is a tertiary parasympathomimetic that directly stimulates cholinergic receptors in the eyes causing pupillary constriction, spasm of accommodation and a transient rise in IOP followed by a fall.

Onset
Miosis: 10-30 min, IOP reduction: 75 minutes (ophthalmic).

Duration
Miosis: 4-8 hours, IOP reduction: 4-14 hours (ophthalmic).

Metabolism
Inactivated at neuronal synapses and in plasma.

Excretion
Urine (as unchanged drug and inactive metabolites). Elimination half-lives: 0.76 (5 mg), 1.35 hours (10 mg).

Pilocarpine Indications / Pilocarpine Uses

Information Not Available

Pilocarpine Adverse Reactions / Pilocarpine Side Effects

Ocular
Pain and irritation, blurred vision, lachrymation, browache, conjunctival vascular congestion, superficial keratitis, vitreous haemorrhage, increased pupillary block.

Precautions

Pilocarpine is a cholinergic parasympathomimetic agent exerting a broad spectrum of pharmacologic effects with predominant muscarinic action. Pilocarpine, in appropriate dosage, can increase secretion by the exocrine glands. The sweat, salivary, lacrimal, gastric, pancreatic, and intestinal glands and the mucous cells of the respiratory tract may be stimulated. When applied topically to the eye as a single dose it causes miosis, spasm of accommodation, and may cause a transitory rise in intraocular pressure followed by a more persistent fall. Dose-related smooth muscle stimulation of the intestinal tract may cause increased tone, increased motility, spasm, and tenesmus. Bronchial smooth muscle tone may increase. The tone and motility of urinary tract, gallbladder, and biliary duct smooth muscle may be enhanced. Pilocarpine may have paradoxical effects on the cardiovascular system. The expected effect of a muscarinic agonist is vasodepression, but administration of Pilocarpine may produce hypertension after a brief episode of hypotension. Bradycardia and tachycardia have both been reported with use of Pilocarpine.

Special Precautions

Retinal detachment; corneal or conjunctival damage. Patients with cognitive or psychiatric disorders, renal impairment, biliary tract disorders. Prolonged use may lead to lens opacities. May impair ability to drive or operate machines. Lactation.

Other Drug Interactions

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

Potentially Fatal: Miotic and ocular hypotensive effect antagonised by anticholinergics. Conduction disturbances with β-blockers.

Other Interactions

Information Not Available

Dosage

Oral
Dry mouth after radiotherapy for malignant neoplasms of the head and neck
Adult: Initial dose: 5 mg tid. If necessary, increase dose gradually after 4 weeks until adequate response is achieved. Max dose: 10 mg tid.

Oral
Sjogren's syndrome
Adult: 5 mg 4 times daily. Max: 30 mg daily. Stop treatment if no improvement after 3 months.

Hepatic impairment: Reduce dose in moderate to severe cirrhosis. Recommended dose: Child pugh category B: 5 mg bid. Child pugh category C: Avoid usage.

Ophthalmic

Open-angle glaucoma
Adult: As HCl or nitrate: Instill a 0.5-4% soln into the eye 4 times daily. As modified-release preparation: insert preparation into the conjunctival sac which releases 20-40 mcg/hour for 7 days. As 4% ophth gel: apply once nightly into the affected eye(s).

Hepatic impairment: Reduce dose in moderate to severe cirrhosis. Recommended dose: Child pugh category B: 5 mg bid. Child pugh category C: Avoid usage.

Food(before/after)

May be taken with or without food

List of Contraindications

Pilocarpine and Pregnancy

Contraindicated in pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Pilocarpine and Lactation

Caution when used during lactation

Pilocarpine and Children

Safety and efficacy not established

Pilocarpine and Geriatic

Elderly patients also may be at increased risk for certain adverse reactions during therapy, including diarrhea, urinary frequency, and dizziness.

Pilocarpine and Other Contraindications

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

Storage

Ophthalmic
Store <8°C. Do not freeze.

Oral
Store at 2-27°C.

Lab interference

Ophthalmic
Store <8°C. Do not freeze.

Oral
Store at 2-27°C.

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