Pilocarpine


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Dry mouth after radiotherapy for malignant neoplasms of the head and neck Initial: 5 mg tid. Increase gradually after 4 wk if needed. Max: 10 mg tid. Sjoren's syndrome For dry eyes and mouth: 5 mg 4 times/day. Max: 30 mg/day. Stop treatment if no improvement after 3 mth. Ophth Open-angle glaucoma As pilocarpine HCl or pilocarpine nitrate: Instill a 0.5-4% soln into affected eye/s 4 times/day, adjusted according to response.
Dosage Details
Ophthalmic
Open-angle glaucoma
Adult: As pilocarpine HCl or pilocarpine nitrate: Instill a 0.5-4% soln into affected eye/s up to 4 times daily, adjusted according to response.

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

Oral
Sjogren's syndrome
Adult: For dry eyes and mouth: 5 mg 4 times daily. Max: 30 mg daily. Stop treatment if no improvement after 3 mth.
Hepatic Impairment
Oral:
Reduce dose in moderate to severe cirrhosis.
Administration
May be taken with or without food.
Contraindications
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.
Special Precautions
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.
Adverse Reactions
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.
Patient Counseling Information
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.
MonitoringParameters
Monitor intraocular pressure. Perform funduscopic exam, visual field testing when necessary.
Overdosage
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.
Drug Interactions
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.
Food Interaction
Decreased rate of absorption w/ high fat meal.
Action
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.
Chemical Structure

Chemical Structure Image
Pilocarpine

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

Storage
Store between 15-30°C.
ATC Classification
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.
References
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.

Disclaimer: This information is independently developed by MIMS based on Pilocarpine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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