Montelukast

Oral
Perennial allergic rhinitis

Oral
Seasonal allergic rhinitis

Oral
Chronic asthma

Oral
Prophylaxis of exercise-induced asthma

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.

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.

PO: B

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

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

Description:
Mechanism of Action: 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.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5281040, Montelukast. https://pubchem.ncbi.nlm.nih.gov/compound/Montelukast. Accessed June 28, 2022.

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

Thuốc trị hen & bệnh phổi tắc nghẽn mạn tính / Thuốc kháng histamin & kháng dị ứng

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

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.