Montair

Chewable tablet: Each chewable tablet contains: Montelukast (as sodium) 4 mg and 5 mg.
Film-coated tablet: Each film-coated tablet contains: Montelukast (as sodium) 10 mg.
Montelukast is a selective leukotriene receptor antagonist. It works by blocking the reaction of substance that causes the inflammation, fluid retention, mucous secretion and constriction in the lungs.

Pharmacology: Pharmacodynamics: Montelukast causes potent inhibition of airway cysteinyl leukotriene receptors as demonstrated by the ability to inhibit bronchoconstriction due to inhaled LTD4 in asthmatic patients. Doses as low as 5 mg cause substantial blockage of LTD4-induced bronchoconstriction.
Montelukast is a selective leukotriene-receptor antagonist that specifically inhibits the cysteinyl leukotriene CysLT1 receptor. The cysteinyl leukotrienes [CysLT (LTC4, LTD4, and LTE4)] are potent inflammatory eicosanoids released from various cells including mast cell and eosinophils that bind to CysLT receptors. The CysLT type 1 (CysLT1) receptor is present in the human airway (including airway smooth muscle cells and airway macrophages). CysLT contribute to the pathophysiology of asthma and allergic rhinitis. In asthma, CysLT are found to increase mucus secretion, vascular permeability, and bronchoconstriction. In allergic rhinitis, CysLT are released from the nasal mucosa after exposure to allergens and are associated with symptoms of allergic rhinitis. Montelukast inhibits bronchoconstriction and reduces inflammation of the nasal mucosa induced by exposure to known precipitants.
Pharmacokinetics: Peak plasma concentrations of Montelukast are achieved in 2 to 4 hours after oral administrations. The mean oral bioavailability is 64%. Montelukast is more than 99% bound to plasma proteins. It is extensively metabolized in the liver by cytochrome P450 isoenzymes CYP3A4, CYP2A6 and CYP2C9, and excreted principally in the feces via the bile. Metabolism was reduced and the elimination half-life prolonged in patients with mild to moderate hepatic impairment.

For the treatment of bronchial asthma and allergic rhinitis.

Adults more than 15 years old: 10 mg tablet daily.
6-14 years old: 5 mg tablet.
2-5 years old: 4 mg tablet.
To be taken once daily at bed time or as prescribed by the physician.

No specific information is available on the treatment of overdosage with montelukast. In chronic asthma studies, montelukast has been administered at doses up to 200 mg per days to adult patients for 22 weeks and in short-term studies, up to 900 mg per day to patients for approximately one week to without clinically important adverse experiences. There have been reports of acute overdosage in postmarketing experience and clinical studies with montelukast. These includes reports in adults and children with a dose as high as 1000 mg. the clinical and laboratory findings observed were consistent with the safety profile in adults and pediatric patients. There were no adverse experiences reported in the majority of overdosage reports. The most frequent occurring adverse experiences were consistent with the safety profile of montelukast and included abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity. It is not known whether montelukast is dialyzable by peritoneal or hemodialysis.

It is contraindicated in patients with known hypersensitivity to montelukast.

Montelukast sodium and other leukotriene receptor antagonists should not be used for the treatment of acute asthma attack. They are contraindicated in patients with hepatic impairment or cirrhosis.

Pregnancy: Pregnancy category B: There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, montelukast should be used during pregnancy only if clearly needed.
Lactation: Studies in rats have shown that montelukast is excreted in milk. It is not known if montelukast is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercise when montelukast is given to lactating mother.

Adverse effects include headache, increased incidence of respiratory tract infection (in the elderly), and gastrointestinal disturbances. Other adverse effects have included generalized pain, arthralgia and myalgia, fever and dizziness. Hypersensitivity reactions including urticaria and angioedema has been reported. There have been also rare reports of agranulocytosis, bleeding, bruising and edema.

No dose adjustment is needed when montelukast is co-administered with theophylline, prednisone, prednisolone, oral contraceptives, fexofenadine, digoxin, warfarin, gemfibrozil, itraconazole, thyroid hormones, sedative hypnotics, non-steroidal inflammatory agents, benzodiazepines, decongestants and Cytochrome P450 (CYP) enzyme inducers.
Theophylline, Prednisone, and Prednisolone: Montelukast has been administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma with no apparent increase in adverse reaction.
Oral contraceptives, Fexofenadine, Digoxin, and Warfarin: In drug interaction studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of oral contraceptive (norethindrone 1mg/ethinyl estradiol 35 mcg), digoxin, and warfarin.
Thyroid hormones, sedative hypnotics, Non-Steroidal Anti-Inflammatory Agents (NSAIDs), Benzodiazepine, and Decongestant: Although additional specific interaction studies were not performed, montelukast was used concomitantly with a wide range of commonly prescribed drugs in clinical studies without evidence of clinical adverse interactions with thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory drugs, benzodiazepines, and decongestant.
Cytochrome P450 (CYP) Enzyme Inducers: Phenobarbital, which induces hepatic metabolism, decreased the area under the plasma concentration curve (AUC) of montelukast approximately 40% following a single 10 mg-dose of montelukast. No dosage adjustment for montelukast is recommended.

Store at temperatures not exceeding 30°C.

Antiasthmatic & COPD Preparations

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

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