Schedule H

Ophthalmic (topical), Oral

• Ophthalmic solution: 1%, 2%, 4% (as pilocarpine nitrate or hydrochloride)

• Ophthalmic gel: 4% (for night-time use)

• Oral tablets: 5 mg

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Chronic Simple Glaucoma / Primary Open-Angle Glaucoma

ADULTS — Ophthalmic:

Parameter Recommendation

Starting dose 1–2% solution, 1 drop in affected eye(s) 2–4 times daily

Titration Increase to 4% solution if inadequate response after 1 week

Usual maintenance dose 1–2 drops of 2% solution 2–4 times daily

Maximum dose 1 drop of 4% solution up to 6 times daily (specialist discretion)

Clinical Notes:

• Often used adjunctively with beta-blockers or prostaglandin analogues

• Evaluate fundus before initiating long-term therapy (retinal detachment risk)

• Warn patients about miosis-induced visual effects, especially night vision impairment

1. Acute Angle-Closure Glaucoma (Initial Emergency Management Prior to Surgery)

ADULTS — Ophthalmic:

Parameter Recommendation

Starting dose 1–2 drops of 1–2% solution every 5–10 minutes × 3 doses

Titration Then 1 drop every 15–30 minutes until surgery

Usual maintenance dose Not applicable (emergency/pre-surgical use only)

Maximum dose As per ophthalmologist discretion

Clinical Notes:

• Ophthalmologist emergency use only

• Adjunctive therapy with systemic acetazolamide indicated

• Use pilocarpine only after IOP is reduced with systemic medications to avoid ischaemic miosis block

1. Induced Miosis (Pre-operative or During Diagnostic Procedures)

ADULTS — Ophthalmic:

Parameter Recommendation

Starting dose 1 drop of 1% solution in eye 30–60 minutes prior to procedure

Titration Not applicable

Usual maintenance dose Not applicable (single-dose use)

Maximum dose 1 drop of 2% if stronger effect required

Clinical Notes:

• Short-acting miotic effect

• Used under specialist supervision only

1. Xerostomia (Post-radiotherapy or Sjögren's Syndrome)

ADULTS — Oral:

Parameter Recommendation

Starting dose 5 mg orally three times daily (TDS)

Titration Increase to 10 mg QID if tolerated and clinically needed; allow 2–4 weeks between dose increases

Usual maintenance dose 5–10 mg orally three to four times daily

Maximum dose 30 mg/day in divided doses

Clinical Notes:

• Duration: Chronic use guided by symptom response and tolerability

• Counsel patients about cholinergic side effects (sweating, salivation, flushing)

• Take with meals to reduce GI side effects

Secondary Indications – Adults (Off-label)

Indication Dose Duration Specialist Only Evidence Basis

Night vision difficulties due to iris atrophy/pupil dilation — OFF-LABEL 1 drop of 1% solution once at night As needed Yes — Ophthalmology Case series from Indian tertiary centres

Primary Indication: Paediatric Glaucoma (e.g., Congenital Glaucoma — Adjunctive or When Surgery Not Feasible)

Children >2 years — Ophthalmic:

Parameter Recommendation

Starting dose 1% solution, 1 drop in affected eye(s) 2–4 times daily

Titration Increase to 2% solution if inadequate response after 1 week

Usual maintenance dose 1–2% solution, 1 drop every 6–12 hours

Maximum dose 4% solution up to 6 times daily (specialist discretion)

Clinical Notes:

• Use in congenital glaucoma is specialist-only; often temporary bridge to surgery

• Monitor for excessive miosis and visual field effects

• Ensure careful cholinergic side effect monitoring

Secondary Indications – Paediatrics (Off-label)

Indication Recommendation

Xerostomia Not routinely used in children due to limited safety data; specialist supervision required if considered

⚠️ Not recommended in children <2 years of age except under paediatric ophthalmologist supervision.

Route Recommendation

Ophthalmic (topical) No adjustment required

Severity Ophthalmic Use Oral Use

Mild impairment (Child-Pugh A) No adjustment required Use with caution; start at lower end of dose range (5 mg BID)

Moderate impairment (Child-Pugh B) No adjustment required Use with caution; start at lower end of dose range (5 mg BID)

Severe impairment (Child-Pugh C) No adjustment required Avoid or initiate only with specialist input

• Known hypersensitivity to pilocarpine or formulation excipients

• Uveitis or iritis (increases inflammation)

• Acute iridocyclitis

• Uncontrolled asthma (oral use)

• Severe cardiac disease including uncontrolled heart failure, recent MI, or significant bradycardia (oral use)

• Narrow-angle glaucoma (for oral use — may worsen angle closure)

• Conditions where miosis is undesirable

• Retinal detachment risk — evaluate fundus before initiating chronic topical therapy

• Asthma or chronic respiratory disease (especially with oral form)

• Peptic ulcer disease — oral use may increase gastric secretions

• Parkinsonism or seizure disorders — theoretical risk with oral use

• Cholelithiasis or biliary tract disease

• In paediatric ocular use — monitor for excessive miosis and visual field effects

• Operating machinery or driving — affects night vision; warn patients

• Corneal damage or abrasion — increased systemic absorption from topical us

Parameter Recommendation

Overall safety Limited human data; animal studies suggest minimal risk

Preferred alternatives For xerostomia: artificial saliva substitutes; For glaucoma: beta-blockers (timolol) may be preferred

When to use Topical ophthalmic: May be used for glaucoma under ophthalmologist guidance; Oral: Avoid unless clearly indicated

Monitoring Intraocular pressure monitoring; fetal monitoring not routinely needed for eye drops

Parameter Recommendation

Breastfeeding compatibility Topical ophthalmic: Compatible — minimal systemic absorption; Oral: Avoid if feasible

Preferred alternatives Artificial saliva for xerostomia

Expected drug levels in milk Low (minimal systemic absorption with topical use)

Infant monitoring If oral formulation used: excessive salivation, diarrhoea, feeding difficulties

Parameter Recommendation

Starting dose (Oral) 5 mg twice daily (BID) initially

Starting dose (Ophthalmic) Standard adult dosing

Titration Slower titration recommended due to increased cholinergic sensitivity

Extra risks Increased miosis-induced vision problems (night driving, visual field limitation); falls risk due to blurred or dim vision; increased cholinergic sensitivity; bradycardia and hypotension with oral use

Interacting Drug Mechanism/Effect Recommendation

Beta-blockers (topical ophthalmic — timolol) Additive bradycardia or hypotension, especially with concurrent oral pilocarpine Monitor heart rate and BP; use with caution

Anticholinergic drugs (atropine, antihistamines, TCAs) Antagonistic effects → reduced efficacy of pilocarpine Avoid concurrent use if possible; may negate therapeutic effect

Parasympathomimetics (bethanechol, neostigmine) Additive cholinergic effects → potential cholinergic overdose Avoid combination; monitor for excessive cholinergic symptoms

Interacting Drug Effect Recommendation

Antihypertensives Oral pilocarpine may enhance hypotensive effects Monitor blood pressure

Digoxin Theoretical vagal tone alteration affecting cardiac conduction Monitor cardiac function and ECG

Antihistamines (first-generation) May reduce pilocarpine efficacy by opposing muscarinic action Monitor for reduced therapeutic effect

Opioids May have additive miotic effects (ophthalmic use) Monitor pupil size if clinically relevant

Topical Ophthalmic:

• Blurred vision

• Brow ache / headache

• Eye irritation or lacrimation

• Miosis / light sensitivity

• Accommodative spasm

• Reduced night vision

Oral:

• Sweating (most common)

• Increased salivation

• Nausea

• Flushing

• Urinary frequency

• Diarrhoea

• Retinal detachment — rare but vision-threatening; requires urgent cessation and ophthalmology referral

• Bronchospasm — with oral use; may be severe in asthmatics

• Bradycardia or hypotension — oral route, especially at high doses

• Severe GI hypermotility / cramping

• Visual field restriction — may affect driving or mobility safety

• Cholinergic crisis — with overdose or excessive systemic absorption

⚠️ Retinal detachment, severe bronchospasm, or cholinergic crisis require immediate discontinuation and emergency management.

Phase Parameters

Baseline Ophthalmic: Fundoscopic examination before long-term therapy (retinal detachment risk); IOP measurement; Oral: Heart rate, blood pressure, respiratory history, GI history

After initiation/dose change IOP monitoring (every 4–6 weeks initially for glaucoma); Heart rate and BP if oral form started (especially in elderly or cardiac patients); Eye exam for miosis-induced visual limitation

Long-term Periodic visual field testing; regular IOP monitoring (every 6–12 weeks for glaucoma); reassessment of xerostomia symptoms if oral form continued chronically

• Pilocar (Sun Pharma) — Eye drops 1%, 2%, 4%

• Pilomax — Eye drops

• Pilopine HS — Ophthalmic gel 4%

• Salagen — Oral 5 mg tablet (imported; limited availability)

Note: Not listed under NLEM; not NPPA price-controlled

• Often not first-line for open-angle glaucoma due to poor compliance with frequent dosing and visual side effects — best used adjunctively or when prostaglandin analogues are contraindicated

• Topical pilocarpine significantly reduces night vision — warn elderly patients and those who drive at night

• In acute angle-closure glaucoma, always use pilocarpine only after IOP is reduced with systemic medications (acetazolamide, mannitol) to avoid ischaemic miosis block

• Oral formulation is useful in radiation-induced xerostomia; counsel patients extensively about cholinergic side effects (sweating is very common)

• Miotic effect may reduce accuracy of gonioscopy or pupillary examination — time doses accordingly before assessments

• For glaucoma, consider prostaglandin analogues or beta-blockers as first-line; reserve pilocarpine for adjunctive use or specific indications

Pilocarpine; glaucoma; miotic; xerostomia; parasympathomimetic; cholinergic agonist; ophthalmic; Sjögren's syndrome; radiotherapy xerostomia; pregnancy-caution; Schedule H

RxIndia v1.0 — 30 Jan 2026

• CDSCO product inserts

• Indian Pharmacopoeia

• AIIMS Ophthalmology Drug List

• NCDC Glaucoma Management Modules

• API Textbook of Medicine — Xerostomia Management

• Goodman & Gilman's The Pharmacological Basis of Therapeutics

• Indian specialist ophthalmology practice protocols