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Accolate: profile and news
Everyday Asthma Control Secrets Mar 5, 2006 SECURSTAR WINS INTERNATIONAL SECURITY AWARD Feb 23, 2006 AstraZeneca Provides Additional Support to Hurricane Victims Nov 17, 2005 AstraZeneca Provides Additional Support to Hurricane Victims Nov 17, 2005 Comprehensive eicosanoid profiling becomes reality Oct 26, 2005 Lipomics Technologies to Offer Comprehensive Eicosanoid Profiling ... Oct 24, 2005 Healthy price Screenings galore, and they're all free Oct 10, 2005 Healthy price Screenings galore, and they're all free 11 Oct 2005 Book Review - The PDR Family Guide to Prescription Drugs Sep 17, 2005 AstraZeneca Pledges More Than $1 Million in Contributions and ... Sep 1, 2005 AstraZeneca Pledges More Than $1 Million in Contributions and ... Sep 1, 2005 CAUSE OF CHRONIC HIVES OFTEN NOT FOUND Aug 11, 2005 Some Asthma Sufferers May Not Need Daily Steroids Aug 28, 2005 Science Center Management Team Strengthened; The Science Center ... Jul 28, 2005 Allergy medications: Know your options Jun 25, 2005 Allergy medications: Know your options Jun 25, 2005 Daily steroids for asthma may not be necessary Apr 21, 2005 Study: Asthma Sufferers Can Limit Steroid Use Apr 13, 2005 Study calls into question daily treatment for mild asthma Apr 13, 2005 Study: Lessen asthma drug use Apr 16, 2005 Asthma drug routine challenged Apr 13, 2005 New study examines asthma patients taking steroids Apr 18, 2005 Medicare reform and the pharmaceutical industry Feb 21, 2005 Other information Indication For the prophylaxis and chronic treatment of asthma Pharmacology Zafirlukast is a synthetic, selective peptide leukotriene receptor antagonist (LTRA) indicated for the prophylaxis and chronic treatment 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. in vitro studies demonstrated that Zafirlukast antagonized the contractile activity of three leukotrienes (LTC4, LTD4 and LTE4) in conducting airway smooth muscle from laboratory animals and humans. Zafirlukast prevented intradermal LTD4-induced increases in cutaneous vascular permeability and inhibited inhaled LTD4-induced influx of eosinophils into animal lungs. 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. Drug Category Anti-Asthmatic Agents; Leukotriene Antagonists; ATC:R03DC01 Brand Names/Synonyms Accolate; CHEMBANK1613; Zafirlukast; Zafirlukast [Usan:Ban:Inn] Dosage Forms TABLET Absorption Rapidly absorbed following oral administration, reduced following a high-fat or high-protein meal Interactions Interactions for Zafirlukast: In a drug interaction study in 16 healthy male volunteers, coadministration of multiple doses of zafirlukast (160 mg/day) to steady-state with a single 25 mg dose of warfarin resulted in a significant increase in the mean AUC (+63%) and half-life (+36%) of S-warfarin. The mean prothrombin time (PT) increased by approximately 35%. This interaction is probably due to an inhibition by zafirlukast of the cytochrome P450 2C9 isoenzyme system. Patients on oral warfarin anticoagulant therapy and ACCOLATE should have their prothrombin times monitored closely and anticoagulant dose adjusted accordingly. No formal drug-drug interaction studies with ACCOLATE and other drugs known to be metabolized by the cytochrome P450 2C9 isoenzyme (eg, tolbu-tamide, phenytoin, carbamazepine) have been conducted; however, care should be exercised when ACCOLATE is coadministered with these drugs. In a drug interaction study in 11 asthmatic patients, coadministration of a single dose of zafirlukast (40 mg) with erythromycin (500 mg three times daily for 5 days) to steady-state resulted in decreased mean plasma levels of zafirlukast by approximately 40% due to a decrease in zafirlukast bioavailability. Coadministration of zafirlukast (20 mg/day) or placebo at steady-state with a single dose of sustained release theophylline preparation (16 mg/kg) in 16 healthy boys and girls (6 through 11 years of age) resulted in no significant differences in the pharmacokinetic parameters of theophylline. Coadministration of zafirlukast (80 mg/day) at steady-state with a single dose of a liquid theophylline preparation (6 mg/kg) in 13 asthmatic patients, 18 to 44 years of age, resulted in decreased mean plasma levels of zafirlukast by approximately 30%, but no effect on plasma theophylline levels was observed. Rare cases of patients experiencing increased theophylline levels with or without clinical signs or symptoms of theophylline toxicity after the addition of ACCOLATE to an existing theophylline regimen have been reported. The mechanism of the interaction between ACCOLATE and theophylline in these patients is unknown (see ADVERSE REACTIONS). Coadministration of zafirlukast (40 mg/day) with aspirin (650 mg four times daily) resulted in mean increased plasma levels of zafirlukast by approximately 45%. In a single-blind, parallel-group, 3-week study in 39 healthy female subjects taking oral contraceptives, 40 mg twice daily of zafirlukast had no significant effect on ethinyl estradiol plasma concentrations or contraceptive efficacy. No formal drug-drug interaction studies between ACCOLATE and marketed drugs known to be metabolized by the P450 3A4 (CYP3A4) isoenzyme (eg, dihydropyridine calcium-channel blockers, cyclosporin, cisapride) have been conducted. As ACCOLATE is known to be an inhibitor of CYP3A4 in vitro, it is reasonable to employ appropriate clinical monitoring when these drugs are coadministered with ACCOLATE. Chemical IUPAC Name cyclopentyl [3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methyl-indol-5-yl]aminoformate Chemical Formula C31H33N3O6S Half Life 10 hours Drug Type Approved Drug # Accession No APRD00377 CAS Registry Number 107753-78-6 |
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