Getz Pharma


Getz Bros
Full Prescribing Info
Montelukast sodium.
Montelukast sodium is a selective and orally active leukotriene receptor antagonist that inhibits the cysteinyl leukotriene CysLT1 receptor, stimulation of which by circulating leukotrienes is thought to play a role in the pathogenesis of asthma. It supresses both early and late bronchoconstrictor responses to inhaled antigens or irritations, but is not suitable for the management of acute attacks of asthma.
Montelukast sodium is [R-(E)]-1-[[[1-[3-[2-(7-chloro-2 quinolinyl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic acid, monosodium salt. The molecular formula is C35H35CINNaO3S.
Pharmacology: Mechanism of Action: Montelukast sodium is a competitive selective and orally active leukotriene D4 (cysteinyl leukotriene CysLT1) receptor antagonist. The cysteinyl leukotrienes (LTC4, LTD4 and LTE4) are products of arachidonic acid metabolism and are released from various cells, including mast cells and eosinophils. These eicosanoids bind to cysteinyl leukotriene (CysLT) receptors. Binding of cysteinyl leukotrienes to leukotriene receptors has been correlated with the pathophysiology of asthma, including airway edema, smooth muscle contraction and altered cellular activity associated with the inflammatory process, factors that contribute to the signs and symptoms of asthma. Thus, montelukast sodium inhibits physiologic actions of LTD4 at the CysLT1 receptors, without any agonist activity.
Pharmacokinetics: Absorption: Montelukast sodium is rapidly absorbed following oral administration. Peak plasma concentrations of montelukast sodium are achieved in 2-4 hrs after oral administration. The mean oral bioavailability is 64%.
Distribution: Montelukast sodium is >99% bound to plasma proteins. The mean plasma t½ of montelukast sodium ranged from 2.7-5.5 hrs in healthy young adults. The pharmacokinetics of montelukast sodium is nearly linear for oral doses up to 50 mg.
Metabolism: Montelukast sodium is extensively metabolized in the liver by cytochrome P-450 isoenzymes CYP3A4, CYP2A6 and CYP2C9. Therapeutic plasma concentrations of montelukast sodium do not inhibit cytochromes P-450, 3A4, 2C9, 1A2, 2A6, 2C19 or 2D6.
Elimination: The plasma clearance of montelukast sodium averages 45 mL/min in healthy adults. Montelukast sodium and its metabolites are excreted principally in the feces via the bile.
Special Populations: Elderly, pediatric, males, females and patients with renal insufficiency have similar plasma pharmacokinetic profiles as young adults.
Hepatic Insuficiency: Patients with mild-to-moderate hepatic insufficiency and clinical evidence of cirrhosis had evidence of decreased metabolism and prolonged elimination t½ of montelukast sodium resulting in 41% higher mean area under the plasma concentration curve (AUC) following a single 10 mg dose. No dosage adjustment is required in patients with mild-to-moderate hepatic insufficiency.
Pediatric patients: In children 6-11 months, the systemic exposure to montelukast and the variability of plasma montelukast concentrations were higher than those observed in adults. Safety and tolerability of montelukast in a single-dose pharmacokinetic study in children 6-23 months were similar to that of patients ≥2 years.
Prophylaxis and chronic treatment of asthma including prevention of day and night time symptoms, treatment of aspirin-sensitive asthmatic patients and prevention of exercise-induced bronchoconstriction.
Relief of symptoms of seasonal allergic rhinitis in adults and pediatric patients ≥2 years.
Dosage/Direction for Use
The therapeutic effect of montelukast sodium on parameters of asthma control occurs within 1 day. Montiget tablets and chewable tablets can be taken with or without food. Patients should be advised to continue taking the drug while their asthma is controlled as well as during periods of worsened asthma.
Montiget should be taken once daily. For asthma, the dose should be taken in the evening. For seasonal allergic rhinitis, the time of administration may be individualized to suit patient needs. Patients with both asthma and seasonal allergic rhinitis should take only 1 tab or 1 sachet daily in the evening.
Asthma and Seasonal Allergic Rhinitis: Adults and adolescents ≥15 years: One 10 mg tab daily.
Pediatric Patients 6-14 years: One 5 mg chewable tab daily.
Pediatric Patients 2-5 years: One 4 mg chewable tab or one 4 mg sachet of pediatric granules daily.
Use of Montiget in Relation to Other Treatment for Asthma: Montiget can be added to a patient's existing treatment regimen: Bronchodilator: Montiget can be added to the treatment of patients who are not adequately controlled on bronchodilator alone. When a clinical response is evident (usually after the 1st dose), the patient's bronchodilator therapy can be reduced as tolerated.
Inhaled Corticosteroids: Treatment with Montiget provides additional clinical benefit to patients treated with inhaled corticosteroids. A reduction in the corticosteroid dose can be made as tolerated. The dose should be reduced gradually with medical supervision. In some patients, the dose of the inhaled corticosteroids can be tapered off completely. Montiget should not be abruptly substituted for inhaled corticosteroids.
Administration: Montiget Pediatric Granules: Montiget 4 mg pediatric granules can be administered either directly in the mouth or mixed with a spoonful of cold or warm temperature soft foods. The sachet should not be opened until ready to use. After opening the sachet, the full dose (with or without food) must be administered within 15 min. If mixed with food, Montiget pediatric granules must not be stored for future use. Discard any unused portion. Montiget pediatric granules are not intended to be dissolved in liquid for administration. However, liquids may be taken subsequent to administration.
Patients who has shown hypersensitivity to montelukast sodium or any of its components.
Montelukast sodium is not indicated for use in acute asthma attacks including status asthmaticus.
Special Precautions
General: Montelukast sodium should not be abruptly substituted for inhaled or oral corticosteroids. However, the dose of inhaled corticosteroid may be reduced gradually under medical supervision.
Although a casual relationship with leukotriene receptor antagonism has not been established, caution and appropriate clinical monitoring is recommended when systemic corticosteroid reduction is considered in patients receiving montelukast sodium.
Montelukast sodium should not be used as monotherapy for the treatment and management of exercise-induced asthma. Patients who have exacerbations of asthma after exercise should continue to use their usual regimen of inhaled β-agonists as prophylaxis and should have it available as and when required.
Montelukast sodium does not block bronchoconstrictor response to aspirin or NSAIDs in aspirin-sensitive asthmatic patients. Such patients should continue to avoid aspirin and other NSAIDs.
Caution should be exercised when using montelukast sodium with bronchodilator therapy. When clinical response is apparent, the bronchodilator therapy should be reduced.
Use in pregnancy: Montelukast sodium has not been studied in pregnant women. It should be used during pregnancy only if clearly needed.
Use in lactation: It is not known if montelukast sodium is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when montelukast sodium is given to a nursing mother.
Use In Pregnancy & Lactation
Use in pregnancy: Montelukast sodium has not been studied in pregnant women. It should be used during pregnancy only if clearly needed.
Use in lactation: It is not known if montelukast sodium is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when montelukast sodium is given to a nursing mother.
Adverse Reactions
Montelukast sodium is generally well tolerated. However, following are the adverse effects reported which usually were mild and did not require discontinuation of therapy. Hypersensitivity reactions (including anaphylaxis, angioedema, rash, pruritus, urticaria and very rarely, hepatic eosinophillic infiltration).
Dream abnormalities, hallucinations, palpitations, drowsiness, irritability, restlessness, insomnia, increased sweating and headache.
Other adverse effects include nausea, vomiting, dyspepsia, diarrhea, abdominal pain, myalgia including muscle cramps, increased bleeding tendency, bruising edema, tremor, dry mouth, vertigo and arthralgia.
Drug Interactions
It is recommended that clinical monitoring be conducted when potent hepatic enzyme inducers eg, phenytoin, phenobarbital or rifampicin are given with montelukast sodium. No dosage adjustment for montiget is recommended.
Store at temperature <30°C. Protect from sunlight and moisture.
MIMS Class
Antiasthmatic & COPD Preparations
ATC Classification
R03DC03 - montelukast ; Belongs to the class of leukotriene receptor antagonists. Used in the systemic treatment of obstructive airway diseases.
FC tab 10 mg x 14's. Chewable tab 4 mg x 14's, 5 mg x 14's. Granules for oral soln (sachet) 4 mg x 14's.
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