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food allergies common 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 food allergies common. The molecular weight of zafirlukast is 575.7 and the structural formula is:
Zafirlukast, a fine white to pale yellow amorphous powder, is practically insolublein water food allergies common. It is slightly soluble in methanol and freely soluble in tetrahydrofuran,dimethylsulfoxide, and acetone food allergies common. ACCOLATE is supplied as 10 and 20 mg tablets for oral administration food allergies common. Inactive Ingredients: Film-coated tablets containing croscarmellose sodium,lactose, magnesium stearate, microcrystalline cellulose, povidone, hypromellose,and titanium dioxide food allergies common.
In vitro studies demonstrated that zafirlukast antagonized the contractileactivity of three leukotrienes (LTC 4 , LTD 4 and LTE 4 ) in conducting airwaysmooth muscle from laboratory animals and humans food allergies common. Zafirlukast prevented intradermalLTD 4 -induced increases in cutaneous vascular permeability and inhibited inhaledLTD 4 -induced influx of eosinophils into animal lungs food allergies common. Inhalational challengestudies in sensitized sheep showed that zafirlukast suppressed the airway responsesto antigen; this included both the early- and late-phase response and the nonspecifichyperresponsiveness food allergies common. In humans, zafirlukast inhibited bronchoconstriction caused by several kindsof inhalational challenges food allergies common. Pretreatment with single oral doses of zafirlukastinhibited the bronchoconstriction caused by sulfur dioxide and cold air in patientswith asthma food allergies common. Pretreatment with single doses of zafirlukast attenuated the early-and late-phase reaction caused by inhalation of various antigens such as grass,cat dander, ragweed, and mixed antigens in patients with asthma food allergies common. Zafirlukastalso attenuated the increase in bronchial hyperresponsiveness to inhaled histaminethat followed inhaled allergen challenge food allergies common. Clinical Pharmacokinetics and Bioavailability: Distribution Metabolism Excretion In the pivotal bioequivalence study, the mean terminal half-life of zafirlukastis approximately 10 hours in both normal adult subjects and patients with asthma food allergies common. In other studies, the mean plasma half-life of zafirlukast ranged from approximately8 to 16 hours in both normal subjects and patients with asthma food allergies common. The pharmacokineticsof zafirlukast are approximately linear over the range from 5 mg to 80 mg food allergies common. Steady-stateplasma concentrations of zafirlukast are proportional to the dose and predictablefrom single-dose pharmacokinetic data food allergies common. Accumulation of zafirlukast in the plasmafollowing twice-daily dosing is approximately 45% food allergies common. The pharmacokinetic parameters of zafirlukast 20 mg administered as a singledose to 36 male volunteers are shown with the table below food allergies common. Mean (% Coefficient of Variation) pharmacokinetic
Race: No differences in the pharmacokinetics of zafirlukast due to race havebeen observed food allergies common. Elderly: The apparent oral clearance of zafirlukast decreases with age food allergies common. Inpatients above 65 years of age, there is an approximately 2-3 fold greater Cmax and AUC compared to young adult patients food allergies common. Children: Following administration of a single 20 mg dose of zafirlukast to20 boys and girls between 7 and 11 years of age, and in a second study, to 29boys and girls between 5 and 6 years of age, the following pharmacokinetic parameterswere obtained: Parameter Children age
Zafirlukast disposition was unchanged after multiple dosing (20 mg twice daily)in children and the degree of accumulation in plasma was similar to that observedin adults food allergies common. Hepatic Insufficiency: In a study of patients with hepatic impairment (biopsy-provencirrhosis), there was a reduced clearance of zafirlukast resulting in a 50-60%greater C max and AUC compared to normal subjects food allergies common. Renal Insufficiency: Based on a cross-study comparison, there are no apparentdifferences in the pharmacokinetics of zafirlukast between renally-impairedpatients and normal subjects food allergies common. Drug-Drug Interactions
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| ffood allergies common foood allergies common foood allergies common foodd allergies common food allergies common food aallergies common food alllergies common food alllergies common food alleergies common food allerrgies common food allerggies common food allergiies common food allergiees common food allergiess common food allergies common food allergies ccommon food allergies coommon food allergies commmon food allergies commmon food allergies commoon food allergies commonn ood allergies common fod allergies common fod allergies common foo allergies common foodallergies common food llergies common food alergies common food alergies common food allrgies common food allegies common food alleries common food allerges common food allergis common food allergie common food allergiescommon food allergies ommon food allergies cmmon food allergies comon food allergies comon food allergies commn food allergies commo f ood allergies common fo od allergies common foo d allergies common food allergies common food allergies common food a llergies common food al lergies common food all ergies common food alle rgies common food aller gies common food allerg ies common food allergi es common food allergie s common food allergies common food allergies common food allergies c ommon food allergies co mmon food allergies com mon food allergies comm on food allergies commo n food allergies common ofod allergies common food allergies common fodo allergies common foo dallergies common fooda llergies common food lalergies common food allergies common food alelrgies common food allregies common food allegries common food alleriges common food allergeis common food allergise common food allergie scommon food allergiesc ommon food allergies ocmmon food allergies cmomon food allergies common food allergies comomn food allergies commno afood allergies common thefood allergies common food allergies common | |||
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Copyright 2005 D-S LTD. |
