Brimonidine Schedule (India)

Schedule H

Brimonidine Routes

Ophthalmic (topical)

Brimonidine Formulations

Ophthalmic solution: 0.1% w/v (5 mL bottle)

Ophthalmic solution: 0.15% w/v (5 mL bottle)

Ophthalmic solution: 0.2% w/v (5 mL bottle)

Brimonidine Adult indications

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

▶ 1. Primary Open-Angle Glaucoma (POAG)

Parameter Recommendation

Starting dose 1 drop of 0.15% or 0.2% solution in affected eye(s) twice daily (approximately 12 hours apart)

Titration May increase to three times daily if IOP control inadequate after 2–4 weeks

Usual maintenance dose 1 drop twice daily

Maximum dose 1 drop three times daily per eye

Key Clinical Notes:

Onset of IOP-lowering effect: 1–2 hours; peak effect at 2–3 hours

Duration of effect: approximately 12 hours

May be used as monotherapy or adjunctive to other antiglaucoma agents (beta-blockers, prostaglandin analogues, carbonic anhydrase inhibitors)

Lower concentration (0.1%, 0.15%) may have better tolerability with similar efficacy to 0.2%

Apply nasolacrimal occlusion for 1–2 minutes after instillation to minimise systemic absorption

▶ 2. Ocular Hypertension

Parameter Recommendation

Starting dose 1 drop of 0.15% or 0.2% solution in affected eye(s) twice daily

Titration May increase to three times daily if target IOP not achieved

Usual maintenance dose 1 drop twice daily

Maximum dose 1 drop three times daily per eye

Key Clinical Notes:

Treatment decision based on baseline IOP and individual risk assessment

Monitor for progression to glaucoma

Reassess IOP at 2–4 weeks after initiation

Secondary Indications — Adults (Off-label)

Indication Dose Duration Notes

Prevention of IOP Spike Post-Laser Procedures (trabeculoplasty, iridotomy) — OFF-LABEL 1 drop 0.2% 1 hour before and immediately after laser procedure Single use (perioperative) Specialist only; Evidence: Clinical studies; commonly used in Indian ophthalmology practice

Lid Retraction in Thyroid Eye Disease (mild cases) — OFF-LABEL 1 drop 0.1% or 0.15% once or twice daily Variable; assess response Specialist only; Evidence: Case series; limited use in Indian practice

Brimonidine Paediatric indications

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

⛔ Brimonidine is CONTRAINDICATED in infants and children <2 years of age due to risk of severe CNS depression, including apnoea, hypotension, bradycardia, hypothermia, and unresponsiveness.

Secondary Indications — Paediatrics (Off-label)

▶ Paediatric Glaucoma (Children ≥2 years) — OFF-LABEL

Age Group	Dose (mcg/kg/day)	Typical Total Daily Dose	Clinical Notes

2–7 years 1 drop of 0.1% solution in affected eye(s) twice daily Use with extreme caution; higher risk of CNS effects

7 years 1 drop of 0.1% or 0.15% solution in affected eye(s) twice daily Maximum: 1 drop twice daily

Key Clinical Notes:

Not a first-line agent in paediatric glaucoma

Use only when other options (surgery, prostaglandin analogues, beta-blockers) are unsuitable or have failed

Prefer lower concentration (0.1%) to minimise systemic absorption

Paediatric ophthalmology specialist supervision mandatory

Safety Monitoring (Essential in All Paediatric Use):

Monitor level of consciousness and alertness

Observe for somnolence, lethargy, hypotonia

Monitor respiratory rate (risk of respiratory depression)

Assess feeding behaviour (poor feeding may indicate toxicity)

Check heart rate and blood pressure

Parents must be counselled on warning signs

⚠️ Absolutely contraindicated in children <2 years — risk of life-threatening CNS and respiratory depression

Brimonidine Renal Adjustments

No dose adjustment required.

Brimonidine has minimal systemic absorption following ophthalmic administration; no clinically significant renal elimination.

Brimonidine Hepatic adjustment

Hepatic Impairment	Recommendation
Mild impairment (Child-Pugh A)	No dose adjustment required
Moderate impairment (Child-Pugh B)	Use with caution; brimonidine undergoes hepatic metabolism
Severe impairment (Child-Pugh C)	Use with caution; limited data; monitor for systemic effects

Brimonidine Contraindications

Known hypersensitivity to brimonidine tartrate or any component of the formulation

Neonates and infants <2 years of age (life-threatening CNS depression risk)

Concurrent use with monoamine oxidase inhibitors (MAOIs) — risk of hypertensive crisis or exaggerated CNS effects

Concurrent use with tricyclic antidepressants — may antagonise brimonidine's hypotensive effect and interfere with its IOP-lowering action

Brimonidine Cautions

Children aged 2–7 years — increased susceptibility to CNS adverse effects; use with extreme caution

Low body weight children — higher risk of systemic toxicity

Severe cardiovascular disease (coronary insufficiency, Raynaud's phenomenon, orthostatic hypotension, thromboangiitis obliterans)

Cerebrovascular insufficiency

Depression — may worsen with alpha-2 agonist therapy

Hepatic impairment — brimonidine is metabolised by the liver

Renal impairment — use with caution in severe impairment

Contact lens wear — remove lenses before instillation; wait at least 15 minutes before reinserting (benzalkonium chloride may be absorbed by soft lenses)

Dry eye disease or ocular surface disorders — preservative may exacerbate symptoms

History of vasovagal episodes

Concurrent use of CNS depressants — additive sedation risk

Brimonidine Pregnancy

Aspect Details

Risk category Limited human data; animal studies show fetal toxicity at high doses; use with caution

Safety statement Avoid during pregnancy unless benefit clearly outweighs potential risk

Preferred alternatives Timolol (more pregnancy safety data); latanoprost (limited data but commonly used); specialist ophthalmology input essential

When to use Only if no safer alternative and IOP control is critical to prevent vision loss

Monitoring Maternal blood pressure monitoring (systemic absorption may cause hypotension); fetal well-being assessment

Brimonidine Lactation

Aspect Details

Compatibility Use with caution — limited human data

Drug levels in milk Unknown; likely low due to minimal systemic absorption with proper technique

Preferred alternatives Timolol ophthalmic (more established lactation safety data)

Recommendations Use nasolacrimal occlusion technique to minimise systemic absorption; use lowest effective dose and concentration

Infant monitoring Observe for sedation, lethargy, poor feeding, respiratory depression

Brimonidine Elderly

Aspect Recommendation

Starting dose Same as younger adults — 1 drop twice daily

Titration Avoid more frequent dosing due to increased sensitivity to systemic effects

Extra risks Increased susceptibility to hypotension, bradycardia, fatigue, and drowsiness; may worsen pre-existing orthostatic hypotension; increased fall risk

Special considerations Ensure proper drop instillation technique with nasolacrimal occlusion; assess cardiovascular status before initiation; monitor blood pressure periodically

Brimonidine Major drug interactions

Interacting Drug Mechanism / Effect Management

Monoamine oxidase inhibitors (MAOIs) — phenelzine, tranylcypromine, selegiline, moclobemide Risk of hypertensive crisis; enhanced sympathomimetic effects CONTRAINDICATED — do not use concurrently

Tricyclic antidepressants (amitriptyline, imipramine, nortriptyline) May antagonise brimonidine's hypotensive and IOP-lowering effects; reduced efficacy CONTRAINDICATED — avoid concurrent use

CNS depressants (benzodiazepines, opioids, barbiturates, alcohol) Additive CNS depression; sedation, drowsiness, respiratory depression Avoid combination or use with extreme caution; warn patients about additive sedation

Other alpha-2 agonists (clonidine, tizanidine, dexmedetomidine) Additive hypotension, bradycardia, and CNS depression Avoid concurrent use if possible

Brimonidine Moderate drug interactions

Interacting Drug Mechanism / Effect Management

Antihypertensives (beta-blockers, calcium channel blockers, ACE inhibitors) Possible additive hypotension Monitor blood pressure; may need dose adjustment of antihypertensive

Cardiac glycosides (digoxin) Additive bradycardia Monitor heart rate

Other topical antiglaucoma agents Increased local ocular side effects; potential systemic additive effects with beta-blockers Stagger administration by at least 5 minutes; monitor for systemic effects

Miotic agents (pilocarpine) May have additive IOP-lowering effect but also increased miosis Can be used together with monitoring

Note: When using multiple ophthalmic medications, administer drops at least 5 minutes apart to ensure adequate absorption.

Brimonidine Common Adverse effects

Ocular (most common):

Allergic conjunctivitis (10–25%) — often delayed onset (after 3–6 months of use)

Conjunctival hyperaemia (ocular redness)

Eye pruritus (itching)

Ocular burning/stinging on instillation

Dry eye sensation

Foreign body sensation

Blurred vision (transient)

Eyelid oedema or erythema

Blepharitis

Follicular conjunctivitis

Systemic (due to absorption):

Dry mouth (xerostomia)

Fatigue/drowsiness

Headache

Brimonidine Serious Adverse effects

Adverse Effect Clinical Action

Severe allergic conjunctivitis with follicular response Discontinue brimonidine; switch to alternative antiglaucoma agent; may require topical steroids for severe inflammation

Severe CNS depression in children (somnolence, hypotonia, apnoea, unresponsiveness) MEDICAL EMERGENCY — discontinue immediately; supportive care; may require hospitalisation and intensive monitoring

Symptomatic hypotension / syncope Discontinue; assess cardiovascular status; avoid rechallenge

Severe bradycardia Discontinue; cardiology evaluation if symptomatic

Respiratory depression (especially in young children) Discontinue immediately; emergency management

Iritis / anterior uveitis (rare) Discontinue; ophthalmology evaluation

Brimonidine Monitoring requirements

Timing	Parameters
Baseline	Intraocular pressure (IOP); ocular surface assessment; cardiovascular history; medication review (especially MAOIs, TCAs, CNS depressants)

After initiation (2–4 weeks) IOP measurement to assess response; enquire about ocular symptoms (redness, itching, irritation)

Periodic (every 3–6 months) IOP; ocular surface examination; assess for signs of delayed allergic conjunctivitis (especially between 3–12 months of use)

Paediatric use Level of consciousness; respiratory rate; heart rate; feeding behaviour; blood pressure — assess at each visit and educate parents on warning signs

Brimonidine Brands in India

Brand Name Concentration Manufacturer

Alphagan P 0.15% Allergan/AbbVie

Alphagan 0.2% Allergan/AbbVie

Brimodin 0.2% Ajanta Pharma

Brimopress 0.15% Cipla

Brimolol 0.15% Sun Pharma

Glauconex B 0.2% Entod

Common FDCs:

Brand Name	Composition	Manufacturer
*	Brimonidine + Timolol (Combigan,	Brimocom, Brimotim)
*	Brimonidine + Brinzolamide (Brizagon,	Simbrinza)

Brimonidine Price range (INR)

Formulation	Approximate Price (per tablet)
Brimonidine 0.15% (5 mL) ₹100–₹350
Brimonidine 0.2% (5 mL) ₹80–₹300
Brimonidine + Timolol FDC (5 mL) ₹200–₹500
Brimonidine + Brinzolamide FDC (5 mL) ₹350–₹600

NLEM Status Brimonidine + Timolol FDC included in NLEM 2022 Price regulated by NPPA

Government Supply Available through government eye hospitals At subsidised rates

Brimonidine Clinical pearls

Nasolacrimal occlusion technique is essential: Instruct patients to press on the inner corner of the eye for 1–2 minutes after instillation to minimise systemic absorption — particularly important in children and elderly

Delayed allergic conjunctivitis is common: Typically develops after 3–6 months of continuous use; presents with itching, redness, and follicular response; may require switching to alternative agent

Absolutely avoid in children <2 years: Risk of life-threatening CNS depression (apnoea, hypotension, bradycardia, hypothermia); even accidental exposure requires medical evaluation

Lower concentrations may be better tolerated: 0.1% and 0.15% formulations (preserved with Purite instead of benzalkonium chloride in some brands) may have lower incidence of ocular allergy with similar efficacy

Excellent adjunctive agent: Combines well with prostaglandin analogues and beta-blockers; FDCs available for improved compliance

Consider in patients with asthma/COPD: Unlike beta-blockers, brimonidine is safe in patients with bronchospastic disease and can be used when topical beta-blockers are contraindicated

Brimonidine Tags

Brimonidine; alpha-2 agonist; glaucoma; ocular hypertension; ophthalmology; IOP reduction; paediatric-contraindicated-under-2-years; allergic conjunctivitis; CNS depression risk; NLEM FDC; Schedule H

Brimonidine Version

RxIndia v1.0 — 10 Apr 2025

Brimonidine Reference

CDSCO approved product information

Indian Pharmacopoeia

NLEM India 2022

API Textbook of Medicine, 11th Edition

AIIMS Ophthalmology Treatment Protocols

All India Ophthalmological Society — Glaucoma Management Guidelines

Goodman & Gilman's The Pharmacological Basis of Therapeutics

IAP Guidelines — Paediatric Glaucoma (for paediatric contraindication and off-label use context)

Indian tertiary ophthalmic institution protocols

RxIndia

The Drug Registry

Brimonidine

Brinzolamide