Adult: As 1%, 2% or 4% pilocarpine hydrochloride drops: Instil 1-2 drops into the affected eye(s) up to 4 times daily. Treatment and dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).
Ophthalmic Miosis
Adult: To antagonise the effects of cycloplegic or mydriatic eye drops: As 1%, 2% or 4% pilocarpine hydrochloride drops: Instil 1 drop into the affected eye(s) every 5 minutes until the effect is counteracted. As 2% pilocarpine nitrate drops: Instil 1-2 drop(s) into the affected eye(s). Treatment and dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).
Ophthalmic Acute closed-angle glaucoma
Adult: Alone or in combination with other agents to reduce IOP prior to surgery: As 1%, 2% or 4% pilocarpine hydrochloride drops: Instil 1 drop into the affected eye(s) every 5 minutes until miosis is achieved. Treatment and dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).
Oral Dry mouth from salivary gland hypofunction caused by radiotherapy for head and neck cancer
Adult: As treatment of symptoms: Initially, 5 mg tid; may increase to a Max of 30 mg daily according to patient's clinical response and tolerability. Dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).
Oral Dry eyes associated with Sjogren's syndrome, Dry mouth associated with Sjogren’s syndrome
Adult: As treatment of symptoms: 5 mg 4 times daily; may increase to a Max of 30 mg daily in divided doses, if needed. Treatment and dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).
What are the brands available for Pilocarpine in Singapore?
Oral:
Dose reduction may be required. Dosage recommendations may vary among individual products and between countries (refer to specific product guidelines).
Administration
Pilocarpine Should be taken with food. Avoid taking w/ high-fat meals.
Contraindications
Conditions when miosis is undesirable (e.g. acute iritis, anterior uveitis). Oral: Uncontrolled asthma, uncontrolled cardiorenal disease.
Special Precautions
Patient with controlled asthma, chronic bronchitis, COPD, significant CV disease, peptic ulceration; nephrolithiasis, known or suspected cholelithiasis or biliary tract disease, cognitive or psychiatric disturbances, Parkinson's disease; pre-existing retinal disease (ophthalmic). Renal and hepatic impairment (oral). Pregnancy and lactation.
Adverse Reactions
Significant: Hypotension, hypertension, bradycardia, tachycardia. Rarely, retinal detachment and retinal tear (ophthalmic). Cardiac disorders: Palpitations. Eye disorders: Lacrimation, conjunctivitis, eye pain, blurred vision, abnormal vision; decreased visual acuity in poor illumination, sensitisation of the lids and conjunctival vascular congestion, superficial keratitis, ciliary spasm, induced myopia, transient myopia, lens changes, increased pupillary block, vitreous haemorrhage (ophthalmic). Gastrointestinal disorders: Dyspepsia, diarrhoea, abdominal pain, nausea, vomiting, constipation, increased salivation. General disorders and administration site conditions: Flu syndrome, asthenia, chills. Nervous system disorders: Headache, dizziness. Renal and urinary disorders: Increased urinary frequency, urinary urgency. Respiratory, thoracic and mediastinal disorders: Rhinitis. Skin and subcutaneous tissue disorders: Rash, pruritus, sweating. Vascular disorders: Flushing.
This drug may cause impairment of depth perception, blurred vision or other visual disturbances, if affected, do not drive or operate machinery. Remove contact lenses before administration and reinsert after 10 minutes (ophthalmic). Maintain adequate fluid intake (oral).
Monitoring Parameters
Ophthalmic: Perform fundus examination before treatment initiation. Monitor IOP and visual fields regularly.
Overdosage
Symptoms: Muscarinic effects (e.g. abdominal cramps, diarrhoea, nausea, vomiting, involuntary defaecation and urination, sweating, salivation, increased bronchial secretions, miosis, bradycardia, hypotension); nicotinic effects (e.g. involuntary twitching, fasciculations, generalised weakness). Management: Supportive treatment. May administer parenteral atropine as an antidote for the muscarinic effects; epinephrine (IM or SC) for severe CV depression or bronchoconstriction. Artificial respiration may be instituted for severe respiratory depression.
Drug Interactions
Increased risk of conduction disturbances with β-blockers. Concomitant use with other drugs which have parasympathomimetic effects may result in additive pharmacologic effects. May antagonise the anticholinergic effects of atropine and inhaled ipratropium bromide.
Food Interaction
May decrease the rate of absorption with a high-fat meal (oral).
Action
Description: Mechanism of Action: Pilocarpine is a direct-acting tertiary amine parasympathomimetic agent. It binds to cholinergic receptors, thereby increasing the secretion in the exocrine glands (e.g. salivary, lacrimal and sweat glands) and increasing smooth muscle tone in the gastrointestinal and urinary tract. Onset: Oral: 20 minutes. Ophthalmic: 10-30 minutes (miosis); 1 hour (IOP reduction). Duration: Oral: 3-5 hours. Ophthalmic: 4-8 hours (miosis); 4-14 hours (IOP reduction). Pharmacokinetics: Absorption: Oral: May decrease the rate of absorption with a high-fat meal. Time to peak plasma concentration: 0.85-1.25 hours; increased to 1.47 hours with a high-fat meal. Excretion: Oral: Via urine (approx 30% as unchanged drug and inactive metabolites). Elimination half-life: 0.76-1.35 hours.
Chemical Structure
Pilocarpine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5910, Pilocarpine. https://pubchem.ncbi.nlm.nih.gov/compound/Pilocarpine. Accessed Oct. 28, 2024.
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 Hydrochloride. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 10/06/2024.Anon. Pilocarpine, Pilocarpine Hydrochloride, Pilocarpine Nitrate. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 10/06/2024.Bausch & Lomb (NZ) Ltd. Minims Pilocarpine Nitrate Eye Drops, Solution data sheet 31 July 2018. Medsafe. http://www.medsafe.govt.nz. Accessed 10/06/2024.Brayfield A, Cadart C (eds). Pilocarpine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/06/2024.Isopto Carpine 2% Ophthalmic Solution (Novartis Corporation [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 10/06/2024.Joint Formulary Committee. Pilocarpine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/06/2024.Minims Pilocarpine Nitrate 2% w/v Eye Drops, Solution (Bausch & Lomb UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 10/06/2024.Novartis New Zealand Limited. Isopto Carpine Eye Drops, Solution data sheet 14 September 2021. Medsafe. http://www.medsafe.govt.nz. Accessed 10/06/2024.Pilocarpine (Ophthalmic). UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/06/2024.Pilocarpine (Systemic). UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 10/06/2024.Pilocarpine Eye Drops 1.0% w/v (Martindale Pharmaceuticals Ltd). MHRA. https://products.mhra.gov.uk. Accessed 10/06/2024.Pilocarpine Hydrochloride 5 mg Film-coated Tablets (Strandhaven Limited t/a Somex Pharma). MHRA. https://products.mhra.gov.uk. Accessed 10/06/2024.Pilocarpine Hydrochloride Ophthalmic Solution/Drops (Somerset Therapeutics, LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 10/06/2024.Pilocarpine Hydrochloride Tablet, Film Coated (Bryant Ranch Prepack). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 10/06/2024.Pilocarpine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 14/08/2024.Salagen (Advanz Pharma). MIMS Singapore. http://www.mims.com/singapore. Accessed 10/06/2024.
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