Averkaz

Chewable tab: Montelukast (Averkaz) 5 mg is a pink coloured round semi biconvex tablets engraved with 'ACME' on one face and other face being plain.
Each Chewable Tablet contains: Montelukast (as Sodium) 5 mg.
FC tab: Montelukast (Averkaz) 10 mg is a white round semi biconvex film coated tablets engraved with 'ACME' on one face and other face being plain.
Each Film-Coated Tablet contains: Montelukast (as Sodium) 10 mg.

Pharmacology: Pharmacodynamics: Montelukast is an orally active compound which binds with high affinity and selectivity to the CysLT₁ receptor. In clinical studies, montelukast inhibits bronchoconstriction due to inhaled LTD₄ at doses as low as 5 mg. Bronchodilation was observed within 2 hours of oral administration. The bronchodilation effect caused by a β agonist was additive to that caused by montelukast. Treatment with montelukast inhibited both early- and late phase bronchoconstriction due to antigen challenge. Montelukast, compared with placebo, decreased peripheral blood eosinophils in adult and paediatric patients. In a separate study, treatment with montelukast significantly decreased eosinophils in the airways (as measured in sputum) and in peripheral blood while improving clinical asthma control.
Pharmacokinetics: Absorption: Montelukast is rapidly absorbed following oral administration. For the 10 mg film-coated tablet, the mean peak plasma concentration (Cmax) is achieved 3 hours (Tmax) after administration in adults in the fasted state. The mean oral bioavailability is 64%. The oral bioavailability and Cmax are not influenced by a standard meal. Safety and efficacy were demonstrated in clinical trials where the 10 mg film-coated tablet was administered without regard to the timing of food ingestion. For the 5 mg chewable tablet, the Cmax is achieved in 2 hours after administration in adults in the fasted state. The mean oral bioavailability is 73% and is decreased to 63% by a standard meal.
Distribution: Montelukast is more than 99% bound to plasma proteins. The steady-state volume of distribution of montelukast averages 8-11 litres. Studies in rats with radiolabelled montelukast indicate minimal distribution across the blood-brain barrier. In addition, concentrations of radiolabelled material at 24 hours post-dose were minimal in all other tissues.
Biotransformation: Montelukast is extensively metabolised. In studies with therapeutic doses, plasma concentrations of metabolites of montelukast are undetectable at steady state in adults and children. Cytochrome P450 2C8 is the major enzyme in the metabolism of montelukast. Additionally, CYP 3A4 and 2C9 may have a minor contribution, although itraconazole, an inhibitor of CYP 3A4, was shown not to change pharmacokinetic variables of montelukast in healthy subjects that received 10 mg montelukast daily. Based on in vitro results in human liver microsomes, therapeutic plasma concentrations of montelukast do not inhibit cytochromes P450 3A4, 2C9, 1A2, 2A6, 2C19, or 2D6. The contribution of metabolites to the therapeutic effect of montelukast is minimal.
Elimination: The plasma clearance of montelukast averages 45 mL/min in healthy adults. Following an oral dose of radiolabelled montelukast, 86% of the radioactivity was recovered in 5-day faecal collections and <0.2% was recovered in urine. Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.

It is used in the management of chronic asthma, allergic rhinitis, and as prophylaxis for exercised-induced asthma.

Adults 15 years of age and older: One tablet (10 mg) once daily at bed time.
Children 6 to 14 years of age: One chewable tablet (5 mg) once daily at bed time.
Children 2 to 5 years of age: One chewable tablet (4 mg) once daily at bed time.
Safety and effectiveness in children younger than 2 years of age have not been established.
Montelukast may be taken with or without food.
Or as directed by the physician.

In chronic asthma studies, montelukast has been administered at doses up to 200 mg/day to adult patients for 22 weeks and in short term studies, up to 900 mg/day to patients for approximately one week without clinically important adverse experiences. There have been reports of acute overdose in post-marketing experience and clinical studies with montelukast. These include reports in adults and children with a dose as high as 1000 mg (approximately 61 mg/kg in a 42 month old child). The clinical and laboratory findings observed were consistent with the safety profile in adults and paediatric patients.
Symptoms of overdose: There were no adverse experiences in the majority of overdose reports. The most frequently occurring adverse experiences were consistent with the safety profile of montelukast and included abdominal pain, somnolence, thirst, headache, vomiting and psychomotor hyperactivity.
Management of overdose: No specific information is available on the treatment of overdose with montelukast. It is not known whether montelukast is dialysable by peritoneal- or haemo-dialysis.

Montelukast is contraindicated in patients who are hypersensitive to any component of this product and to those patients with hepatic impairment or cirrhosis.

Montelukast is not indicated for use in acute asthma attacks. Therapy with montelukast can be continued during acute exacerbations of asthma. Montelukast should not be used as monotherapy for the treatment and management of exercise induced bronchospasm. There are no adequate and well controlled studies in pregnant women. Montelukast should be used during pregnancy only if clearly needed. Montelukast is excreted in milk. So caution should be exercised when montelukast is given to a nursing mother.

Pregnancy and Lactation: Animal studies do not indicate harmful effects with respect to effects on pregnancy or embryonal/foetal development. Available data from published prospective and retrospective cohort studies with montelukast use in pregnant women evaluating major birth defects have not established a drug-associated risk. Available studies have methodologic limitations, including small sample size, in some cases retrospective data collection, and inconsistent comparator groups. Montelukast 10 mg film-coated tablets may be used during pregnancy only if it is considered to be clearly essential.
Breastfeeding: It is unknown whether montelukast is excreted in human milk. Studies in rats have shown that montelukast is excreted in milk. Montelukast 10 mg film-coated tablets may be used in breast-feeding only if it is considered to be clearly essential.

Montelukast has been generally well tolerated. Side effects, which usually are mild, including gastro-intestinal disturbances, dry mouth, thirst; hypersensitivity reactions including anaphylaxis, angioedema and skin reactions; asthenia, dizziness, irritability, restlessness, headache, sleep disorders (insomnia, drowsiness, nightmares); upper respiratory tract infection, fever, arthralgia, myalgia. The overall incidence of side effects reported with montelukast was comparable to placebo.

It is reasonable to employ appropriate clinical monitoring when potent cytochrome P450 enzyme inducers, such as phenobarbital or rifampin, are co-administered with montelukast.

Store at temperatures not exceeding 30°C. Protect from light.

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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