ZAFIRLUKAST tablet, film coated

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

American Health Packaging

INN (International Name):

ZAFIRLUKAST

Composition:

ZAFIRLUKAST 20 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Zafirlukast tablets are indicated for the prophylaxis and chronic treatment of asthma in adults and children 5 years of age and older. Zafirlukast tablets are contraindicated in patients who are hypersensitive to zafirlukast or any of its inactive ingredients. Zafirlukast tablets are contraindicated in patients with hepatic impairment including hepatic cirrhosis.

Product summary:

Zafirlukast tablets 20 mg are white to light pink, round film coated tablets debossed with ‘R’ on one side and ‘626’ on other side. Unit dose packages of 30 (3 x 10) NDC 68084-059-21 STORAGE Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature]. Protect from light and moisture. Rx Only FOR YOUR PROTECTION: Do not use if blister is torn or broken. PACKAGING INFORMATION American Health Packaging unit dose blisters (see How Supplied section) contain drug product from Dr. Reddy's Laboratories Limited as follows: (20 mg / 30 UD) NDC 68084-059-21 packaged from NDC 55111-626 Distributed by: American Health Packaging Columbus, OH 43217 8205921/1017

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ZAFIRLUKAST- ZAFIRLUKAST TABLET, FILM COATED
AMERICAN HEALTH PACKAGING
----------
ZAFIRLUKAST TABLETS
8205921/1017
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 molecular formula is: C
H
N
O
S
Zafirlukast, white to pale yellow coloured powder, freely soluble in
tetrahydrofuran, and
dimethylsulfoxide and practically insoluble in water.
Zafirlukast is supplied as 10 and 20 mg tablets for oral
administration.
Inactive ingredients: Film coated tablets containing hydroxypropyl
cellulose,
hypromellose, lactose monohydrate, magnesium stearate,
microcrystalline cellulose,
polyethylene glycol 400, sodium starch glycolate (Type-A) 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.
_In vitro_ studies demonstrated that zafirlukast antagonized the
contractile activity of
three leukotrienes (LTC
, LTD
and LTE
) in conducting airway smooth muscle from
31
33
3
6
4
4
4
4
4
4
4
4
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 suppres