Pilocarpine

Ophthalmic
Open-angle glaucoma

Oral
Dry mouth after radiotherapy for malignant neoplasms of the head and neck

Oral
Sjogren's syndrome

Oral:
Reduce dose in moderate to severe cirrhosis.

May be taken with or without food.

Conditions where pupillary constriction is undesirable (e.g. acute iritis, acute uveitis, anterior uveitis and some forms of secondary glaucoma); acute inflammatory disease of the anterior segment. Clinically significant uncontrolled cardiorenal disease, uncontrolled asthma, COPD and other chronic disease at risk for cholinergic agonists.

Patient w/ history of retinal detachment, corneal or conjunctival damage; cognitive or psychiatric disorders, epilepsy, Parkinson’s disease; cholelithiasis or biliary tract disorders, hyperthyroidism; CV disease (e.g. HTN, hypotension); GI spasm, peptic ulceration; nephrolithiasis; resp disorders (e.g. controlled asthma, chronic bronchitis). Patients who are known to sweat excessively and who cannot drink enough liq. Hepatic or renal impairment. Pregnancy and lactation.

Ophth: Blurred vision, browache, ciliary spasm, conjunctival vascular congestion, lens changes, myopia, ocular burning and itching, vitreous haemorrhage, pupillary block, smarting. Oral: Influenza-like symptoms, rhinitis, conjunctivitis, constipation, diarrhoea, nausea, vomiting, flatulence, dyspepsia, dizziness, flushing, headache, HTN, palpitation, increased urinary frequency and urgency, lacrimation, pruritus, rash, sweating.

Ophth/PO: C

Not to be used in patients wearing soft contact lenses. This drug may cause miosis which may lead to blurred vision and difficulty w/ dark adaptation, do not drive or undertake hazardous tasks in poor illumination.

Monitor intraocular pressure. Perform funduscopic exam, visual field testing when necessary.

Symptoms: Muscarinic effects (e.g. abdominal cramps, diarrhoea, nausea, vomiting, involuntary defecation and urination, sweating, salivation, increased bronchial secretions, miosis, bradycardia and hypotension); nicotinic effects (e.g. twitching, fasciculations, generalised weakness). Management: Supportive treatment. Use parenteral atropine as an antidote to muscarinic effects. If resp depression is severe, institute artificial respiration.

Conduction disturbances w/ β-blockers. Concomitant admin of 2 miotics may increase risk of toxic reactions. Concurrent admin w/ drugs w/ parasympathomimetic effects may result in additive pharmacologic effects. May antagonise anticholinergic effects of atropine, inhaled ipratropium.

Decreased rate of absorption w/ high fat meal.

Description: Pilocarpine is a tertiary amine parasympathomimetic that directly stimulates cholinergic receptors in the eyes, causing pupillary constriction, spasm of accommodation and lowering of intraocular pressure (IOP).
Onset: Ophth: miosis: 10-30 min; IOP reduction: 60 min. Systemic: 20 min.
Duration: Ophth: miosis: 4-8 hr; IOP reduction: 4-12 hr. Systemic: 3-5 hr.
Pharmacokinetics:
Absorption: Decreased rate of absorption w/ high fat meal.
Distribution: Extensively distributed. Apparent volume of distribution: 2.1 L/kg.
Metabolism: Primarily metabolised by CYP2A6 isoenzyme.
Excretion: Via urine (approx 30%) as unchanged drug and inactive metabolites. Elimination half-life: 0.76-1.35 hr.

Source: National Center for Biotechnology Information. PubChem Database. Pilocarpine, CID=5910, https://pubchem.ncbi.nlm.nih.gov/compound/Pilocarpine (accessed on Jan. 22, 2020)

Store between 15-30°C.

Antiglaucoma Preparations

S01EB01 - pilocarpine ; Belongs to the class of parasympathomimetics. Used in the treatment of glaucoma and miosis.
N07AX01 - pilocarpine ; Belongs to the class of other parasympathomimetics.

Anon. Pilocarpine (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/02/2016.

Anon. Pilocarpine (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 01/02/2016.

Buckingham R (ed). Pilocarpine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/02/2016.

Joint Formulary Committee. Pilocarpine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/02/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Pilocarpine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 01/02/2016.