Pilocarpine

Indications
 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 wk 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 mth.
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/hr 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.
Contraindications
 Angle-closure glaucoma; acute iritis, anterior uveitis; hypersensitivity. Pregnancy.
Warnings / 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.
Adverse Reactions
 Ocular: Pain and irritation, blurred vision, lachrymation, browache, conjunctival vascular congestion, superficial keratitis, vitreous haemorrhage, increased pupillary block.
Overdose Reactions
 May lead to "cholinergic crisis".
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.
See Below for More pilocarpine Drug Interactions
Mechanism of Actions
 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 min (ophthalmic).
Duration: Miosis: 4-8 hr, IOP reduction: 4-14 hr (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 hr (10 mg).
Administration
 May be taken with or without food.
Storage Conditions
 Ophthalmic: Store <8°C. Do not freeze. Oral: Store at 2-27°C.
ATC Classification
 N07AX01 - pilocarpine ; Belongs to the class of other parasympathomimetics.
S01EB01 - pilocarpine ; Belongs to the class of parasympathomimetics. Used in the treatment of glaucoma and miosis.
Storage
 Ophthalmic: Store <8°C. Do not freeze. Oral: Store at 2-27°C.
Available As
  • Pilocarpine Nitrate 0.2%
  • Pilocarpine 0.2%
  • Pilocarpine Nitrate 0.5%
  • Pilocarpine Nitrate 0.5% w/v
  • Pilocarpine Nitrate 1%
  • Pilocarpine Nitrate 1% w/v
  • Pilocarpine Nitrate 2%
  • Pilocarpine 2%
  • Pilocarpine Nitrate 2% w/v
  • Pilocarpine 20 mg
  • Pilocarpine Nitrate 4%
  • Pilocarpine Nitrate 4% w/v
  • Pilocarpine Nitrate 4% w/w
  • Pilocarpine 5 mg

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