ZAFIRLUKAST tablet, coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Major Pharmaceuticals

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 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.

Authorization status:

New Drug Application

Summary of Product characteristics

ZAFIRLUKAST- ZAFIRLUKAST TABLET, COATED
MAJOR PHARMACEUTICALS
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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