Montelukast: Indication, Dosage, Side Effect, Precaution

Generic Medicine Info Patient Medicine Information

This information is not country-specific. Please refer to the Myanmar prescribing information.

Generic Medicine Info

Indications and Dosage

Oral
Perennial allergic rhinitis

Adult: As conventional tab: 10 mg once daily.
Child: 6-23 months As granules: 1 sachet (4 mg) once daily in the evening; 2-5 years As 4 mg chewable tab or granules: 1 tab or sachet once daily in the evening; 6-14 years As 5 mg chewable tab: 1 tab once daily in the evening; ≥15 years As conventional tab: Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Oral
Seasonal allergic rhinitis

Adult: As conventional tab: 10 mg once daily.
Child: 2-5 years As 4 mg chewable tab or granules: 1 tab or sachet once daily in the evening; 6-14 years As 5 mg chewable tab: 1 tab once daily in the evening; ≥15 years As conventional tab: Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Oral
Chronic asthma

Adult: As conventional tab: 10 mg once daily in the evening.
Child: 6-23 months As granules: 1 sachet (4 mg) once daily in the evening; 2-5 years As 4 mg chewable tab or granules: 1 tab or sachet once daily in the evening; 6-14 years As 5 mg chewable tab: 1 tab once daily in the evening; ≥15 years As conventional tab: Same as adult dose. Dosage recommendations may vary among countries or individual products. Refer to specific product guidelines.

Oral
Prophylaxis of exercise-induced asthma

Adult: As conventional tab: 10 mg given at least 2 hours before exercise; limit to 1 dose every 24 hours.
Child: 2-5 years As 4 mg chewable tab or granules: 1 tab or sachet once daily in the evening; 6-14 years As 5 mg chewable tab: 1 tab once daily in the evening; ≥15 years As conventional tab: Same as adult dose.

Special Precautions

Patient with known aspirin sensitivity (continue avoidance of aspirin or NSAIDs during treatment with montelukast). Not indicated for the treatment of acute asthma attacks, including status asthmaticus. Not recommended as monotherapy in patients with moderate persistent asthma. Avoid abrupt substitution to inhaled or oral corticosteroids. Children. Pregnancy and lactation.

Adverse Reactions

Significant: Neuropsychiatric events (e.g. agitation, depression, hallucinations, suicidal thoughts and behaviour, dream abnormalities, aggressive behaviour or hostility, anxiety, disorientation, disturbance in attention, dysphemia, insomnia, irritability, memory impairment, obsessive-compulsive symptoms, restlessness, somnambulism, tic, tremor). Rarely, systemic eosinophilia (sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome).
Blood and lymphatic system disorders: Rarely, increased bleeding tendency, thrombocytopenia.
Cardiac disorders: Rarely, palpitations.
Ear and labyrinth disorders: Otitis media.
Gastrointestinal disorders: Abdominal pain, diarrhoea, nausea, vomiting, thirst, dry mouth, dyspepsia.
General disorders and administration site conditions: Pyrexia, asthenia, malaise, oedema.
Immune system disorders: Hypersensitivity reactions including anaphylaxis.
Investigations: Elevated ALT/AST levels.
Musculoskeletal and connective tissue disorders: Myalgia, arthralgia, muscle cramps.
Nervous system disorders: Headache, dizziness, drowsiness, paraesthesia, hypoaesthesia, seizure.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection, pharyngitis, cough, influenza, rhinorrhea, sinusitis, epistaxis.
Skin and subcutaneous tissue disorders: Rash, pruritus, urticaria, bruising.

Pregnancy Category (US FDA)

PO: B

Monitoring Parameters

Monitor for neuropsychiatric symptoms, including changes in behaviour and suicidal thoughts.

Drug Interactions

Decreased plasma concentration with CYP inducers (e.g. phenobarbital, phenytoin, rifampicin). Increased systemic exposure with gemfibrozil.

Action

Description: Montelukast is a selective leukotriene receptor antagonist. It inhibits cysteinyl leukotriene type-1 (CysLT₁) receptor found in the human airway and on other pro-inflammatory cells. The binding of CysLTs in leukotriene receptors is involved in the pathophysiology of asthma, including bronchoconstriction, mucous secretion, vascular permeability, and eosinophil recruitment. Additionally, CysLTs are released from the nasal mucosa after allergen exposure which is associated with symptoms of allergic rhinitis.
Duration: >24 hours.
Pharmacokinetics:
Absorption: Rapidly absorbed. Bioavailability: 64% (conventional tab); 73% (5 mg chewable tab). Time to peak plasma concentration: 3-4 hours (conventional tab); 2 hours (chewable tab).
Distribution: Volume of distribution: 8-11 L. Plasma protein binding: >99%.
Metabolism: Extensively metabolised in the liver, mainly by CYP2C8, and to a lesser extent by CYP3A4 and CYP2C9 enzymes.
Excretion: Mainly via faeces (86%); urine (<0.2%). Elimination half-life: 2.7-5.5 hours.

Chemical Structure

Storage

Store between 15-30°C. Protect from light and moisture.

MIMS Class

Antiasthmatic & COPD Preparations / Antihistamines & Antiallergics

ATC Classification

R03DC03 - montelukast ; Belongs to the class of leukotriene receptor antagonists. Used in the systemic treatment of obstructive airway diseases.

References

Anon. Montelukast Sodium. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 12/05/2022.

Anon. Montelukast. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 12/05/2022.

Apotex NZ Ltd. Apo-Montelukast 10 mg Tablets, 4 mg & 5 mg Chewable Tablets data sheet 27 November 2018. Medsafe. http://www.medsafe.govt.nz. Accessed 12/05/2022.

Asthator Tablet 4 mg, 5 mg and 10 mg (Laboratories Torrent [Malaysia] Sdn Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 12/05/2022.

Buckingham R (ed). Montelukast Sodium. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/05/2022.

Joint Formulary Committee. Montelukast. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/05/2022.

Montelukast 10 mg Tablets (Torrent Pharma UK Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 12/05/2022.

Montelukast 4 mg Chewable Tablets (Torrent Pharma UK Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 12/05/2022.

Montelukast 4 mg Granules (Torrent Pharma UK Ltd.). MHRA. https://products.mhra.gov.uk. Accessed 12/05/2022.

Montelukast 5 mg Chewable Tablets (Milpharm Limited). MHRA. https://products.mhra.gov.uk. Accessed 12/05/2022.

Singulair 4 mg Oral Granules, 4 mg Chewable Tablets, 5 mg Chewable Tablets, 10 mg Film-coated Tablets (Merck Sharp & Dohme [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 12/05/2022.

Singulair Granule; Tablet, Chewable; Tablet, Film Coated (Organon LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 12/05/2022.

Singulair Tablets/Chewable Tablets/Oral Granules (Organon Malaysia Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 16/06/2022.

Disclaimer: This information is independently developed by MIMS based on Montelukast from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2024 MIMS. All rights reserved. Powered by MIMS.com