ZAFIRLUKAST tablet, coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

AvKARE

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 42291-970-60) 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 42291-971-60) 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 to 25°C (68 to 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
AVKARE
----------
ZAFIRLULKAST TABLETS
RX ONLY
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 D
and E
(LTD
and LTE
), 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
to 100 times more sensitive to the bronchoconstricting activity of
inhaled LTD
than
nonasthmatic subjects.
31
33
3
6
4
4
4
4
4
_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 inclu