ZAFIRLUKAST tablet ZAFIRLUKAST- zafirlukast tablets tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Rising Pharmaceuticals, Inc.

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. The safety of Zafirlukast Tablets 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 in this age range participating in 52 weeks of treatment in an open label extension. The effectiveness of Zafirlukast Tablets for the prophylaxis and chronic treatment of asthma in pediatric patients 5 through 11 years of age is based on an extrapolation of the demonstrated efficacy of Zafirlukast Tablets in adults with asthma and the likelihood that the disease course, and pathophysiology and the drug’s effect are substantially similar betw

Product summary:

Zafirlukast Tablets 10 mg: (NDC 16571-654-06) Pink colored, round, biconvex tablets debossed with “654” on one side and “P” on the other side, and are supplied in opaque HDPE bottles of 60 tablets. Zafirlukast Tablets 20 mg: (NDC 16571-655-06) Pink colored, round, biconvex tablets debossed with “655” on one side and “P” on the other side, and 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. Manufactured by: RA Chem Pharma Ltd. Hyderabad, India 500076 Manufactured for: Rising Pharma Holdings, Inc. East Brunswick, NJ 08816 PIR65506-00 Issued: 09/2022

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

ZAFIRLUKAST- ZAFIRLUKAST TABLET
RISING PHARMACEUTICALS, INC.
----------
ZAFIRLUKAST 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-3ylmethyl)-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, an off white to light pink color powder, is practically
insoluble in water. It is
freely soluble in tetrahydrofuran, dimethylsulfoxide and acetone.
Zafirlukast Tablets are supplied as 10 and 20 mg tablets for oral
administration.
INACTIVE INGREDIENTS: Film-coated tablets containing Colloidal silicon
Dioxide,
Croscarmellose Sodium, Ferric Oxide Red, Hypromellose, Lactose
Anhydrous, Macrogol
400, Magnesium Stearate, Microcrystalline Cellulose, Polyvinyl
Pyrrolidone, 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 25-100 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
laboratory animals and humans. Zafirlukast prevented intradermal LTD
-induced
31
33
3
6
4
4
4
4
4
4
4
4
4
increases in cutaneous vascular permeability and inhibited inhaled LTD
-induced influx of
eosinophils into animal lungs. Inhalational challenge studies in
sensitized sheep showed
th