Schedule H

Oral

• Film-coated tablet: Montelukast 10 mg + Formoterol fumarate 6 mcg (Modified Release)

• Chewable tablet: Montelukast 5 mg + Formoterol fumarate 6 mcg (Modified Release)

• Chewable tablet: Montelukast 4 mg + Formoterol fumarate 6 mcg (Modified Release)

Note: Formoterol in these oral FDCs is formulated as sustained-release microparticles for systemic absorption — distinct from inhaled formoterol preparations.

INDICATIONS + DOSING — FOR CLINICIAN USE ONLY

Primary Indications (Approved / Standard in India)

1. Mild to Moderate Persistent Bronchial Asthma

Indication criteria: When inhaled ICS-LABA therapy is not feasible due to poor technique, non-adherence, or lack of access to inhalers

Adults and Adolescents ≥15 years:

Parameter Recommendation

Starting dose Montelukast 10 mg + Formoterol SR 6 mcg — 1 tablet once daily in the evening

Titration Not required

Usual maintenance dose 1 tablet once daily

Maximum dose Montelukast 10 mg + Formoterol 12 mcg per day (oral)

Clinical Notes:

• Reserved for patients where inhaled therapy is unsuitable or persistently refused

• Oral LABA has slower onset and greater systemic exposure than inhaled route

• Not appropriate for acute bronchospasm — always ensure access to SABA rescue inhaler

• Evening dosing preferred for optimal circadian efficacy of montelukast

• Reassess inhaler feasibility periodically; transition to inhaled therapy when possible

1. Exercise-Induced Bronchospasm (Prophylaxis)

Adults and Adolescents ≥15 years (select cases with poor inhaler access):

Parameter Recommendation

Starting dose Montelukast 10 mg + Formoterol SR 6 mcg — 1 tablet once daily

Titration Not applicable

Usual maintenance dose 1 tablet once daily, taken 1–2 hours before anticipated exercise

Maximum dose 1 tablet per day

Clinical Notes:

• This indication is uncommon for oral FDC; inhaled SABA or LABA before exercise is preferred

• Use only in selected patients under specialist supervision where inhalers are unavailable

Secondary Indications — Adults Only (Off-label)

Indication Dose Duration Notes Evidence Basis

COPD with asthma overlap (OFF-LABEL) Montelukast 10 mg + Formoterol SR 6 mcg once daily Long-term if beneficial Specialist only; when inhaled therapy poorly tolerated Weak evidence; select use in Indian chest physician practice; not routinely recommended

PAEDIATRIC DOSING (Specialist Only)

Primary Indications (Approved / Standard in India)

Mild to Moderate Persistent Bronchial Asthma (When Inhalers Not Feasible)

6–14 years Montelukast 5 mg + Formoterol SR 6 mcg chewable tablet 1 tablet once daily in evening Once daily

≥15 years Montelukast 10 mg + Formoterol SR 6 mcg tablet 1 tablet once daily in evening Once daily

Dosing Parameters (Children 6–14 years):

Parameter Recommendation

Starting dose 1 chewable tablet (Montelukast 5 mg + Formoterol SR 6 mcg) once daily

Titration Not required

Usual maintenance dose 1 tablet once daily in the evening

Maximum dose 1 tablet per day

Safety Monitoring:

• Monitor for tremors, tachycardia, and headache

• Observe for neuropsychiatric symptoms: nightmares, irritability, aggression, mood changes

• Counsel caregivers to report any behavioural disturbances promptly

Age Restriction: Not recommended below 6 years of age

Secondary Indications — Paediatrics (Off-label)

Indication Dose Duration Notes Evidence Basis

Allergic Rhinitis with co-existing asthma (OFF-LABEL) Age-appropriate tablet once daily Short-term seasonal use (8–12 weeks maximum) Specialist only Extrapolated from montelukast monotherapy data; Indian paediatric specialist practice

Clear Statement: Off-label paediatric use should be under paediatric pulmonologist or allergist supervision only. Not recommended below 6 years except under exceptional specialist guidance.

• No dose adjustment required in mild to moderate renal impairment

• Severe renal impairment (eGFR <30 mL/min): Use with caution; limited pharmacokinetic data for oral sustained-release formoterol

• Haemodialysis/Peritoneal dialysis: No specific data available; use cautiously with monitoring

• Known hypersensitivity to montelukast, formoterol, or any excipient

• Severe hepatic impairment (Child-Pugh C)

• Known arrhythmogenic conditions or congenital/acquired long QT syndrome

• Acute asthma exacerbation or status asthmaticus (not a rescue medication)

• Concurrent use with other long-acting beta-agonists

• Cardiovascular disease (coronary artery disease, heart failure) — increased risk of tachycardia, palpitations

• Thyrotoxicosis — LABA component may exacerbate sympathomimetic symptoms

• Diabetes mellitus — formoterol may elevate blood glucose levels

• Hypokalaemia or conditions predisposing to electrolyte imbalance

• Seizure disorders — formoterol may lower seizure threshold

• History of neuropsychiatric illness — montelukast associated with behavioural changes

• Concurrent corticosteroid therapy — do not abruptly discontinue steroids when initiating this FDC

Aspect Recommendation

Safety category Montelukast: No formal contraindication; considered relatively safe (Category B-equivalent profile). Formoterol (oral SR): Limited human data; avoid if possible

Preferred alternatives Inhaled ICS ± inhaled LABA; inhaled salbutamol for rescue

When it may be used Only when inhaled therapy not feasible and maternal benefit clearly outweighs fetal risk; specialist consultation required

Monitoring Maternal heart rate, blood pressure; fetal growth; uterine tone (oral LABA may inhibit labour contractions)

Aspect Recommendation

Compatibility Limited data; short-term use acceptable with caution under specialist supervision

Preferred alternatives Inhaled ICS ± inhaled LABA

Drug levels in milk Montelukast: Low levels expected. Formoterol (oral): Unknown; potential for systemic effects in infant

Infant monitoring Observe for restlessness, tachycardia, irritability, poor feeding, tremors

Aspect Recommendation

Starting dose Montelukast 10 mg + Formoterol SR 6 mcg — 1 tablet once daily

Titration Not required; however, initiate with careful observation

Special risks Increased susceptibility to cardiovascular effects (palpitations, tachycardia); higher risk of hypokalaemia; potential for CNS effects (tremors, insomnia); QT prolongation risk with concurrent medications

Additional considerations Assess baseline cardiac status and electrolytes; consider ECG in patients with cardiac history

Interacting Drug/Class Mechanism/Effect Clinical Action

Strong CYP3A4 inhibitors (ketoconazole, itraconazole, ritonavir) Increased formoterol plasma levels Avoid combination; increased risk of QT prolongation, tremors, cardiovascular effects

Non-selective beta-blockers (propranolol, carvedilol) Antagonise bronchodilatory effect of formoterol Avoid; use cardioselective beta-blockers if essential

Loop and thiazide diuretics (furosemide, hydrochlorothiazide) Additive hypokalaemia with LABA Monitor potassium; correct hypokalaemia before and during therapy

QT-prolonging drugs (sotalol, amiodarone, haloperidol, ondansetron) Additive QT prolongation risk Avoid combination or monitor ECG closely

MAO inhibitors / tricyclic antidepressants Enhanced adrenergic effects of formoterol Avoid concurrent use or use with extreme caution

Interacting Drug/Class Clinical Consideration

Theophylline/Aminophylline Additive sympathomimetic effects; increased risk of tachycardia, insomnia; monitor heart rate

Rifampicin CYP induction may reduce montelukast levels; monitor clinical efficacy

Phenobarbital, Phenytoin, Carbamazepine CYP inducers; potential reduction in montelukast efficacy

Fluoroquinolones (levofloxacin, moxifloxacin) Additive QT prolongation risk with formoterol; use with caution

Systemic corticosteroids No direct interaction; additive benefit in asthma control; do not abruptly withdraw steroids

Xanthine derivatives Additive stimulatory effects; monitor for CNS adverse effects

• Headache

• Tremors

• Palpitations

• Tachycardia

• Insomnia

• Nausea

• Abdominal discomfort

• Myalgia

• Dizziness

• Upper respiratory tract infection symptoms

• Behavioural disturbances in children (nightmares, irritability, restlessness)

Adverse Effect Clinical Action

QT prolongation and ventricular arrhythmias Discontinue immediately; obtain ECG; cardiology consultation

Neuropsychiatric events (agitation, aggression, depression, hallucinations, suicidal ideation) — montelukast component Discontinue promptly; psychiatric evaluation; report to pharmacovigilance

Anaphylaxis or severe hypersensitivity Discontinue permanently; emergency management

Eosinophilic granulomatosis with polyangiitis (Churg-Strauss syndrome) Rare; may occur with steroid dose reduction; discontinue and investigate

Stevens-Johnson Syndrome / Toxic Epidermal Necrolysis Extremely rare; discontinue immediately; hospitalisation required

Severe hypokalaemia Correct electrolytes; ECG monitoring

After initiation (1–2 weeks) Heart rate; blood pressure; tremors; CNS effects; behavioural changes in children

Long-term (every 6–12 months) LFTs if prolonged therapy; serum potassium; ongoing neuropsychiatric symptom surveillance; reassessment of inhaler feasibility

• Montair-F (Cipla)

• Montemac-F (Macleods)

• Monticope-F (Aristo)

• Lukan-F (Lupin)

• Montelin-F (Elder)

• Odimont-F (Mankind)

Note: Verify formulation contains sustained-release formoterol; product names may vary by manufacturer.

Notes:

• Not included in NLEM; not under NPPA price control

• Primarily available through private retail pharmacies

• Limited availability in government supply chains; may be stocked at select tertiary care centres

• This oral FDC is a fallback option when inhaled ICS-LABA therapy is genuinely not feasible — not a first-line choice for asthma management

• Oral formoterol has slower onset of action and higher systemic side effect burden compared to inhaled formoterol

• Never use for acute asthma exacerbations — always ensure patient has access to SABA rescue inhaler

• Neuropsychiatric monitoring is essential, particularly in children — caregivers must be counselled to report behavioural changes immediately

• Periodically reassess inhaler technique and compliance; transition to inhaled therapy when patient becomes capable

• Consider de-prescribing this FDC once stable control achieved with inhalers

Montelukast + Formoterol; asthma; LTRA; LABA; oral FDC; non-inhaler asthma therapy; paediatric asthma; neuropsychiatric monitoring; exercise-induced bronchospasm; Schedule H

RxIndia v1.0 — 22 May 2025

• CDSCO Fixed-Dose Combination Approval Listings

• Indian Pharmacopoeia / National Formulary of India

• API Textbook of Medicine

• ICMR Guidelines for Asthma Management

• AIIMS Paediatric Asthma Management Protocol

• IAP Guidelines for Childhood Asthma

• Indian Chest Society Consensus Statements

• Cipla and Lupin Product Inserts (India-specific)

• Off-label use references: Based on documented Indian pulmonology and paediatric specialist practices