1. Clinical & Scientific Overview
Montelukast Sodium (TIP-MED-000171, Reference Code [9.7]) is classified under
Respiratory, Asthma, COPD & Allergy Medicines (Ch 09) as a Selective Cysteinyl Leukotriene (CysLT1) Receptor Antagonist (Oral Anti-Inflammatory Leukotriene Modifier).
Within the Indian regulatory and compendial framework, it is governed under Schedule H Prescription Drug (To be sold by retail on the prescription of a Registered Medical Practitioner only — Drugs Rules 1945).
Representative Indian Market Examples (Edition 2.7 Ch 09 [9.7], p. 117): Singulair (MSD), Montair (Cipla), Romilast (Sun Pharma), Telekast (Lupin), Lasma; Widely dispensed in India in FDC with Levocetirizine (Montair-LC, Telekast-L, Monticope) or Fexofenadine (Montair-FX, Allegra-M) or Acebrophylline (Telekast-A) — Strengths & Dosage Forms: Oral Film-Coated Tablets: 10 mg (Adult); Paediatric Chewable Tablets / Granules: 4 mg (6 months–5 years), 5 mg (6–14 years); Common Adult FDCs: Montelukast 10 mg + Levocetirizine 5 mg OR Montelukast 10 mg + Fexofenadine 120 mg
Oral Film-Coated Tablets: 10 mg (Adult); Paediatric Chewable Tablets / Granules: 4 mg (6 months–5 years), 5 mg (6–14 years); Common Adult FDCs: Montelukast 10 mg + Levocetirizine 5 mg OR Montelukast 10 mg + Fexofenadine 120 mg
3. Mechanism of Action & Pharmacodynamics
Selective Cysteinyl Leukotriene (CysLT1) Receptor Antagonist (Oral Anti-Inflammatory Leukotriene Modifier) acting on target receptor/enzyme pathways in Respiratory, Asthma, COPD & Allergy Medicines (Ch 09): clinical efficacy is mediated via Selective Cysteinyl Leukotriene (CysLT1) Receptor Antagonist (Oral Anti-Inflammatory Leukotriene Modifier) for Prophylaxis and chronic add-on treatment of Bronchial Asthma (particularly aspirin-exacerbated respiratory disease [AERD], exercise-induced bronchoconstriction, and comorbid allergic rhinitis + asthma); seasonal and perennial allergic rhinitis..
4. Therapeutic Indications & Evidence-Supported Uses
- Prophylaxis and chronic add-on treatment of Bronchial Asthma (particularly aspirin-exacerbated respiratory disease [AERD], exercise-induced bronchoconstriction, and comorbid allergic rhinitis + asthma)
- seasonal and perennial allergic rhinitis
🇮🇳 Jurisdiction & Indication Note: Indications and schedules reflect Indian compendial and regulatory records (CDSCO / Indian Pharmacopoeia & NFI / NLEM 2022). Where international reference labels (US FDA DailyMed / NCBI StatPearls) are cited for pharmacokinetic or mechanistic parameters, international approvals do not automatically imply CDSCO approval in India.
5. Educational Dosage Context, Formulations & Administration
Educational Dosing & Regimen Summary: General Adult Reference (≥15 years): 10 mg once daily in the evening. Follow physician prescription.
Administration & Meal Timing: With or without food. | Once daily in the evening or at bedtime (targets nocturnal/early-morning cysteinyl leukotriene surges and ensures that any Levocetirizine component in '-LC' FDCs causes drowsiness during sleep rather than daytime!).
6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment
Absorption, distribution, metabolism, and excretion follow class pharmacokinetic profile; verify patient renal/hepatic function.
Renal: Excreted almost entirely via bile/faeces; no dose adjustment required in any stage of CKD. Hepatic: No adjustment in mild-to-moderate hepatic impairment; avoid in severe cirrhosis (Child-Pugh C).
Renal: Excreted almost entirely via bile/faeces; no dose adjustment required in any stage of CKD. Hepatic: No adjustment in mild-to-moderate hepatic impairment; avoid in severe cirrhosis (Child-Pugh C).
Renal: Excreted almost entirely via bile/faeces; no dose adjustment required in any stage of CKD. Hepatic: No adjustment in mild-to-moderate hepatic impairment; avoid in severe cirrhosis (Child-Pugh C).
7. Contraindications, Precautions & High-Risk Warnings
- 1. NOT for relief of acute asthma attacks (nor is it a substitute for Inhaled Corticosteroids in persistent asthma!). 2. FDA / CDSCO Boxed Warning for Serious Neuropsychiatric Events: Montelukast crosses the blood-brain barrier and can cause vivid nightmares, insomnia, agitation, aggression, anxiety, depression, and suicidal ideation/behaviour in children, adults, and the elderly!
Key Clinical Precautions: Renal: Excreted almost entirely via bile/faeces; no dose adjustment required in any stage of CKD. Hepatic: No adjustment in mild-to-moderate hepatic impairment; avoid in severe cirrhosis (Child-Pugh C).
8. Adverse Effects Profile
- Headache, upper respiratory symptoms, mild abdominal pain; if combined with Levocetirizine (Montair-LC): morning drowsiness, dry mouth, fatigue.
- Neuropsychiatric disturbances (vivid nightmares/sleep terrors, insomnia, severe mood changes, depression, agitation, hallucinations/confusion in the elderly—resolve promptly upon stopping the drug!), Churg-Strauss syndrome / Eosinophilic Granulomatosis with Polyangiitis (rare unmasking when oral steroids are tapered), rare hepatotoxicity.
- Monitor for severe hypersensitivity, organ toxicity, or dose-limiting adverse events.
9. Major Drug–Drug, Drug–Food & Drug–Herb Interactions
- Metabolised by CYP2C8, CYP3A4, and CYP2C9: Phenytoin, phenobarbitone, and rifampicin reduce montelukast plasma AUC by ~40%
- Gemfibrozil (CYP2C8 inhibitor) increases montelukast exposure 4
- 4-fold
10. Clinical Monitoring, Patient Counselling & Storage
Clinical & Laboratory Monitoring: Monitor clinical response, baseline renal/hepatic parameters, and relevant serum biomarkers.
Pharmacist Patient Counselling Points:
- Patient Counselling Checklist: 1. Counsel every patient and caregiver about the Neuropsychiatric Warning: 'If you or your child/elderly parent experience unusual disturbing nightmares, restlessness, mood changes, anxiety, or depression after starting Montair/Telekast, stop the tablet and inform the doctor.' 2. Audit chronic use of Montelukast + Levocetirizine ('Montair-LC / Telekast-L'): in India, patients frequently take 'Montair-LC' every night for years for minor sneezing—in elderly patients, the daily Levocetirizine component causes chronic daytime drowsiness, falls, and urinary hesitancy!
- Meal & Clock Timing Instruction: With or without food. (Once daily in the evening or at bedtime (targets nocturnal/early-morning cysteinyl leukotriene surges and ensures that any Levocetirizine component in '-LC' FDCs causes drowsiness during sleep rather than daytime!).)
- Missed Dose Protocol: Skip the missed evening dose and take the next evening dose at the regular time; never double.
- Geriatric Dispensing Pearl: If an elderly CGHS asthma patient requires long-term Montelukast, dispense plain Montelukast 10 mg rather than indefinite Montair-LC (or use non-sedating Bilastine/Fexofenadine short-term if rhinitis is active), and screen for sleep disturbances or confusion.
Storage, Stability & Dispensing Safeguards: Store below 25°C–30°C in original moisture- and light-resistant packaging out of reach of children. Available forms: Oral Film-Coated Tablets: 10 mg (Adult); Paediatric Chewable Tablets / Granules: 4 mg (6 months–5 years), 5 mg (6–14 years); Common Adult FDCs: Montelukast 10 mg + Levocetirizine 5 mg OR Montelukast 10 mg + Fexofenadine 120 mg
11. Visual Pharmacology & Mechanism Diagram (svg-v339-01-adme-12-step-journey)
12. Authoritative References, Regulatory Sources & Editorial Disclaimer
Primary Compendial & Guideline Reference: Indian Pharmacist Desk Reference — Professional Edition 2.7 (2026–27) • Ch 09 [9.7] (p. 117)
Official Verification Portals: Indian Pharmacopoeia Commission (IPC) & National Formulary of India (NFI) • Central Drugs Standard Control Organization (CDSCO) • Ministry of Health & Family Welfare — NLEM 2022 • NCBI Bookshelf / StatPearls Pharmacology Reference • DailyMed (US FDA Official Prescribing Reference)
Last Medically & Pharmaceutically Reviewed: 2026-11-10 • Verification Status: HANDBOOK_SOURCE_CONTENT
Educational & Clinical Disclaimer: This reference profile is published solely for pharmacy education, academic study, and professional clinical reference. It does not substitute for patient-specific clinical judgement, qualified specialist oncology/medical supervision, or official CDSCO/IP prescribing information. Never self-medicate with prescription, Schedule H/H1/X, NDPS, or oncology medicines.
13. Related Reference Monographs, Educational Guides & Visual Concept
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