País: Estados Unidos
Língua: inglês
Origem: NLM (National Library of Medicine)
ZAFIRLUKAST (UNII: XZ629S5L50) (ZAFIRLUKAST - UNII:XZ629S5L50)
Major Pharmaceuticals
ORAL
PRESCRIPTION DRUG
Zafirlukast is indicated for the prophylaxis and chronic treatment of asthma in adults and children 5 years of age and older. Zafirlukast is contraindicated in patients who are hypersensitive to zafirlukast or any of its inactive ingredients. Zafirlukast is contraindicated in patients with hepatic impairment including hepatic cirrhosis.
Zafirlukast 20 mg Tablets, white, round, biconvex, film-coated tablets debossed with “P” on one side and “20” on the other, are supplied as follows: Carton of 30 tablets (10 tablets each blister pack x 3) NDC 0904-6646-04 Store at controlled room temperature, 20-25°C (68-77°F) [see USP]. Protect from light and moisture. Dispense in the original air-tight container.
New Drug Application
ZAFIRLUKAST- ZAFIRLUKAST TABLET, COATED MAJOR PHARMACEUTICALS ---------- ZAFIRLUKAST TABLETS DESCRIPTION Zafirlukast is a synthetic, selective peptide leukotriene receptor antagonist (LTRA), with the chemical name 4-(5-cyclopentyloxy-carbonylamino-1-methyl-indol-3-ylmethyl)-3-methoxy-N-o- tolylsulfonylbenzamide. The molecular weight of zafirlukast is 575.7 and the structural formula is: The empirical formula is: C H N O S Zafirlukast, a fine white to pale yellow amorphous powder, is practically insoluble in water. It is slightly soluble in methanol and freely soluble in tetrahydrofuran, dimethylsulfoxide, and acetone. Zafirlukast is supplied as 10 and 20 mg tablets for oral administration. INACTIVE INGREDIENTS: Film-coated tablets containing croscarmellose sodium, lactose, magnesium stearate, microcrystalline cellulose, povidone, hypromellose, and titanium dioxide. CLINICAL PHARMACOLOGY MECHANISM OF ACTION: Zafirlukast is a selective and competitive receptor antagonist of leukotriene D4 and E4 (LTD4 and LTE4), components of slow-reacting substance of anaphylaxis (SRSA). Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma. Patients with asthma were found in one study to be 25-100 times more sensitive to the bronchoconstricting activity of inhaled LTD4 than nonasthmatic subjects. 31 33 3 6 _In vitro_ studies demonstrated that zafirlukast antagonized the contractile activity of three leukotrienes (LTC , LTD and LTE ) in conducting airway smooth muscle from laboratory animals and humans. Zafirlukast prevented intradermal LTD -induced increases in cutaneous vascular permeability and inhibited inhaled LTD -induced influx of eosinophils into animal lungs. Inhalational challenge studies in sensitized sheep showed that zafirlukast suppressed the airway responses to antigen; this included Leia o documento completo