Montelukast


Full Prescribing Info
Dosage/Direction for Use

Oral
Chronic asthma
Adult: As film-coated tab: 10 mg once daily in the evening.
Child: 6 months-<2 years
As granules: 4 mg once daily; 2-5 years As granules or chewable tab: 4 mg once daily; 6-14 years As chewable tab: 5 mg once daily; ≥15 years Same as adult dose. All doses to be taken in the evening. Evaluate patient after 2-4 weeks of treatment.

Oral
Allergic rhinitis
Adult:
As film-coated tab: 10 mg once daily (taken in the evening for asthmatic patients; for nonasthmatic patient, doses may be taken either in the morning or evening).
Child: ≥15 years
Same as adult dose.

Oral
Prophylaxis of exercise-induced asthma
Adult: As film-coated tab: 10 mg to be taken 2 hours prior to exercise; no additional doses to be taken within 24 hours.
Child: 2-5 years
As granules or chewable tab: 4 mg; 6-14 years As chewable tab: 5 mg; ≥15 years Same as adult dose. Doses to be taken 2 hours prior to exercise; no additional doses to be taken within 24 hours. Evaluate patient after 2-4 weeks of treatment.
Special Precautions
Aspirin-sensitive asthmatic patient must continue avoiding aspirin and other NSAIDs. Not intended for treatment of acute asthma attacks. Not recommended as monotherapy in treatment of moderate chronic asthma. Avoid abrupt substitution to oral or inhaled corticosteroids. Children. Pregnancy and lactation. Patient Counselling This drug may cause dizziness or drowsiness, if affected, do not drive or operate machinery. Monitoring Parameters Monitor for signs and symptoms of behavioural changes.
Adverse Reactions
Significant: Behavioural changes (e.g. agitation, anxiety, depression, dream abnormalities, obsessive-compulsive disorder). Rarely, systemic eosinophilia, vasculitis with eosinophilic granulomatosis with polyangiitis (Churg-Strauss syndrome). Ear and labyrinth disorders: Otalgia, otitis media. Eye disorders: Myopia, conjunctivitis. Gastrointestinal disorders: Diarrhoea, nausea, vomiting, abdominal pain, dyspepsia, gastroenteritis. General disorders and administration site conditions: Pyrexia. Infections and infestations: Viral infection, tooth infection. Investigations: Elevated serum transaminase levels (ALT, AST). Nervous system disorders: Headache, drowsiness, dizziness. Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection, cough, acute bronchitis, influenza, laryngitis, pharyngitis, rhinorrhoea, sinusitis, sinus headache, pneumonia. Skin and subcutaneous tissue disorders: Rash, eczema or atopic dermatitis, skin infection, urticaria. Vascular disorders: Epistaxis.
Overdosage
Symptoms: Abdominal pain, somnolence, thirst, headache, vomiting, psychomotor hyperactivity. Management: Supportive treatment.
Drug Interactions
Decreased plasma concentration with CYP450 inducers (e.g. phenytoin, phenobarbital, rifampicin). Gemfibrozil may increase montelukast serum concentration.
Action
Montelukast is a selective leukotriene receptor antagonist with a long duration of action. It inhibits cysteinyl leukotriene type-1 (CysLT1) receptor found in the human airway and on pro-inflammatory cells. The binding of CysLTs in leukotriene receptors are involved in the pathophysiology of asthma, including smooth muscle contraction, airway oedema and inflammation; CysLTs are released from the nasal mucosa after allergen exposure which is associated with symptoms of allergic rhinitis.
Onset: Asthma control: Within a day.
Duration: >24 hours.
Absorption: Rapidly absorbed. Bioavailability: 64% (conventional tab); 73% (chewable tab), 63% (with standard meal). Time to peak plasma concentration: 3-4 hours (conventional tab, fasting); 2 hours (4 mg chewable tab, fasting); 2-2.5 hours (5 mg chewable tab, fasting); 2.3±1 hour (granules, fasting); 6.4±2.9 hours (with high-fat meal).
Distribution: Present in breast milk. Volume of distribution: 8-11 L. Plasma protein binding: >99%.
Metabolism: Extensively metabolised in the liver by CYP3A4, CYP2C8 and CYP2C9.
Excretion: Mainly via faeces (86%); via urine (<0.2%). Elimination half-life: 2.7-5.5 hours.
Storage
Oral: Store below 30°C. Protect from light and moisture.
ATC Classification
R03DC03 - montelukast ; Belongs to the class of leukotriene receptor antagonists. Used in the systemic treatment of obstructive airway diseases.
Disclaimer: This information is independently developed by CIMS 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 CIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, CIMS 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 © 2020 CIMS. All rights reserved. Powered by CIMSAsia.com
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