ACCOLATE Coated tablet (2015)
Βιβλιογραφική αναφορά
Συγγραφείς
Par Pharmaceutical, Inc.
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1. 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. ...
2. Clinical Pharmacology
Mechanism of Action Zafirlukast is a selective and competitive receptor antagonist of leukotriene D<sub>4</sub> and E<sub>4</sub> (LTD<sub>4</sub> and LTE<sub>4</sub>), components of slow-reacting substance ...
3. Indications and Usage
ACCOLATE is contraindicated in patients who are hypersensitive to zafirlukast or any of its inactive ingredients. ACCOLATE is contraindicated in patients with hepatic impairment including hepatic cirrhosis. ...
5. Warnings
Hepatotoxicity Cases of life-threatening hepatic failure have been reported in patients treated with ACCOLATE. Cases of liver injury without other attributable cause have been reported from post-marketing ...
6.1. General
Eosinophilic Conditions In rare cases, patients with asthma on ACCOLATE may present with systemic eosinophilia, eosinophilic pneumonia, or clinical features of vasculitis consistent with Churg-Strauss ...
6.2. Information for Patients
Patients should be told that a rare side effect of ACCOLATE is hepatic dysfunction, and to contact their physician immediately if they experience symptoms of hepatic dysfunction (eg. right upper quadrant ...
6.4. Drug Interactions
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 ...
6.6. Carcinogenesis, Mutagenesis, Impairment of Fertility
In two-year carcinogenicity studies, zafirlukast was administered at dietary doses of 10, 100, and 300 mg/kg to mice and 40, 400, and 2000 mg/kg to rats. Male mice at an oral dose of 300 mg/kg/day (approximately ...
6.7. Pregnancy
Pregnancy Category B. No teratogenicity was observed at oral doses up to 1600 mg/kg/day in mice (approximately 160 times the maximum recommended daily oral dose in adults on a mg/m² basis), up to 2000 ...
6.9. Nursing Mothers
Zafirlukast is excreted in breast milk. Following repeated 40 mg twice-a-day dosing in healthy women, average steady-state concentrations of zafirlukast in breast milk were 50 ng/mL compared to 255 ng/mL ...
6.10. Pediatric Use
The safety of ACCOLATE at doses of 10 mg twice daily has been demonstrated in 205 pediatric patients 5 through 11 years of age in placebo-controlled trials lasting up to six weeks and with 179 patients ...
6.11. Geriatric Use
Based on cross-study comparison, the clearance of zafirlukast is reduced in patients 65 years of age and older such that C<sub>max</sub> and AUC are approximately 2- to 3-fold greater than those of younger ...
7. Adverse Reactions
Adults and Children 12 years of age and older The safety database for ACCOLATE consists of more than 4000 healthy volunteers and patients who received ACCOLATE, of which 1723 were asthmatics enrolled in ...
9. Overdosage
No deaths occurred at oral zafirlukast doses of 2000 mg/kg in mice (approximately 210 times the maximum recommended daily oral dose in adults and children on a mg/m <sup>2</sup> basis), 2000 mg/kg in rats ...
10. Dosage and Administration
Because food can reduce the bioavailability of zafirlukast, ACCOLATE should be taken at least 1 hour before or 2 hours after meals. Adults and Children 12 years of age and older The recommended dose of ...
11. How Supplied
<u>ACCOLATE 10 mg Tablets,</u> (NDC 49884-589-02) white, round, biconvex, film-coated tablets debossed with P on one side and 10 on the other, are supplied in opaque HDPE bottles of 60 tablets. <u>ACCOLATE ...
12. Storage and Handling
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.
13. Clinical Studies
Three U.S. double-blind, randomized, placebo-controlled, 13-week clinical trials in 1380 adults and children 12 years of age and older with mild-to-moderate asthma demonstrated that ACCOLATE improved daytime ...