ZAFIRLUKAST tablet, coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

ZAFIRLUKAST (UNII: XZ629S5L50) (ZAFIRLUKAST - UNII:XZ629S5L50)

Available from:

Par Pharmaceutical, Inc.

INN (International Name):

ZAFIRLUKAST

Composition:

ZAFIRLUKAST 10 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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.

Product summary:

Zafirlukast 10 mg Tablets, (NDC 49884-549-02) 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. Zafirlukast 20 mg Tablets, (NDC 49884-554-02) white, round, biconvex, film-coated tablets debossed with “P” on one side and “20” on the other, are supplied in opaque HDPE bottles of 60 tablets. 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.

Authorization status:

New Drug Application

Summary of Product characteristics

ZAFIRLUKAST- ZAFIRLUKAST TABLET, COATED
PAR PHARMACEUTICAL, INC.
----------
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:
31
33
3
6
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.
_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 incl