ملوكاست    - اطلاعات ملوكاست برای بیمار   -    اطلاعات ملوكاست برای پزشکان   -   سؤال در مورد ملوكاست

 Melukast^®

Generic Name: Montelukast

Category: Antiasthmatic, leukotriene receptor antagonist

Composition:

  Melukast^® 5:   Each chewable tablet contains Montelukast 5mg.

  Melukast^® 10: Each film coated tablet contains Montelukast 10 mg.

Actions and Pharmacokinetics:

    Melukast is a leukotriene (loo-koe-try-een) inhibitor. Leukotrienes are substances in the body that are associated with the inflammation and constriction of airway muscles and the accumulation of fluid in the lungs, all of which occur during an asthma attack.Melukast inhibits bronchoconstriction due to antigen challenge. Melukast is a selective leukotriene receptor antagonist of the cysteinyl leukotriene CysLT1 receptor. The cysteinyl leukotrienes (LTC4, LTD4, LTE4) are products of arachidonic acid metabolism that are released from various cells, including mast cells and eosinophils. They bind to cysteinyl leukotriene receptors (CysLT) found in the human airway. 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. Melukast binding to the CysLT1 receptor is high-affinity and selective, preferring the CysLT1 receptor to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or beta-adrenergic receptor. Melukast inhibits physiologic actions of LTD4 at the CysLT1 receptors, without any agonist activity. Absorption: Rapid. Bioavailability is not affected by a standard meal in the morning. Distribution: Steady-state volume of distribution averages 8 to 11 liters. Protein binding: Very high (more than 99%). Biotransformation: Hepatic, extensive, involves cytochrome P450 3A4 and 2C9. Half-life: Range, 2.7 to 5.5 hours in healthy young adults. Elimination: Biliary/fecal( 86%), Renal:( Less than 0.2%).

Indications:

    Melukast is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 12 months of age and older.

Melukast is indicated for the relief of symptoms of allergic rhinitis (seasonal allergic rhinitis in adults and pediatric patients 2 years of age and older, and perennial allergic rhinitis in adults and pediatric patients 6 months of age and older).

Contraindications:

Hypersensitivity to any component of this product.

Precautions:

    Melukast is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus.

Patients should be advised to have appropriate rescue medication available. Therapy with Melukast can be continued during acute exacerbations of asthma.

While the dose of inhaled corticosteroid may be re-duced gradually under medical supervision, Melukast should not be abruptly substituted for inhaled or oral corticosteroids.

Melukast should not be used as monotherapy for the treatment and management of exercise-induced bronchospasm. Patients who have exacerbations of asthma after exercise should continue to use their usual regimen of inhaled (beta)-agonists as prophylaxis and have available for rescue a short-acting inhaled (beta)-agonist.

Patients with known aspirin sensitivity should continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking Melukast. Although Melukast is effective in improving airway function in asthmatics with documented aspirin sensitivity, it has not been shown to truncate bronchoconstrictor response to aspirin and other non-steroidal anti-inflammatory drugs in aspirin-sensitive asthmatic patients.

In rare cases, patients with asthma on therapy with Melukast may present with systemic eosinophilia, sometimes presenting with

clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic

corticosteroid therapy. These events usually, but not always, have been associated with the reduction of oral corticosteroid therapy. Physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. A causal association between Melukast and these underlying conditions has not been established

 Pregnancy:

    Adequate and well-controlled studies in humans have not been done. Studies in animals found no evidence of teratogenicity. Risk-benefit should be considered before use of melukast during pregnancy.

FDA Pregnancy Category B.

Breast-feeding:

    It is not known whether melukast is distributed into breast milk in humans. Risk-benefit should be considered before breast-feeding during treatment with melukast.

 Drug interactions:

    Phenobarbital (concurrent use results in significant decreases [approximately 40%] in the area under the curve [AUC] for melukast, as a result of induction of hepatic metabolism; however, no dosage adjustment is necessary). melukast has been administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma with no apparent increase in adverse reactions. In drug-interaction studies, the recommended clinical dose of melukast did not have clinically important effects on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (norethindrone 1 mg/ethinyl estradiol 35 mcg), terfenadine, digoxin, and warfarin. Although additional specific interaction studies were not performed, melukast was used concomitantly with a wide range of commonly prescribed drugs in clinical studies without evidence of clinical adverse interactions. These medications included thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, and decongestants.

 Adverse Effects:

The frequency of less common adverse events was comparable between melukast and placebo.

The most common side effects with melukast include:

stomach pain, stomach or intestinal upset, heartburn, tiredness, fever , stuffy nose, cough, flu, upper respiratory infection, dizziness, headache , rash .

Administration and Dosage:

    For Asthma (Take in the evening):

·   One 10-mg tablet for adults and adolescents 15 years of age and older,

·   One 5-mg chewable tablet for children 6 to 14 years of age,

·   One 4-mg chewable tablet for children 2 to 5 years of age, or

·   4-mg for children 12 to 23 months of age.

    For Allergic Rhinitis (Take at about the same time each day):

·   One 10-mg tablet for adults and adolescents 15 years of age and older,

·   One 5-mg chewable tablet for children 6 to 14 years of age,

·   4-mg chewable tablet for children 2 to 5 years of age, or

·   4-mg for children 2 to 5 years of age with seasonal allergic rhinitis, or for children 6 months to 5 years of age with perennial allergic rhinitis.

Storage: Store below 30 °C. Protect from light and moisture.

 How Supplied:

    Melukast^® 5:  Box of 5 blisters of 10 chewable tablets.

    Melukast^® 10: Box of 4 blisters of 15 scored tablets.