ZAFIRLUKAST tablet, film coated

Χώρα: Ηνωμένες Πολιτείες

Γλώσσα: Αγγλικά

Πηγή: NLM (National Library of Medicine)

Δραστική ουσία:

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

Διαθέσιμο από:

Aurobindo Pharma Limited

Οδός χορήγησης:

ORAL

Τρόπος διάθεσης:

PRESCRIPTION DRUG

Θεραπευτικές ενδείξεις:

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.

Περίληψη προϊόντος:

Zafirlukast Tablets 10 mg , are white, round, biconvex, film-coated tablets debossed with “1” on one side and “B” on other side.                                                              Bottles of 60     NDC 59651-291-60 Zafirlukast Tablets 20 mg , are white, round, biconvex, film-coated tablets debossed with “2” on one side and “B” on other side.                                                             Bottles of 60    NDC 59651-292-60 Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature]. Protect from light and moisture. Dispense in the original air-tight container.  Distributed by: Aurobindo Pharma USA, Inc. 279 Princeton-Hightstown Road East Windsor, NJ 08520 Manufactured by: Aurobindo Pharma Limited Hyderabad-500 032, India Issued: June 2023

Καθεστώς αδειοδότησης:

Abbreviated New Drug Application

Αρχείο Π.Χ.Π.

ZAFIRLUKAST - ZAFIRLUKAST TABLET, FILM COATED
AUROBINDO PHARMA LIMITED
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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-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, off-white to light pink color powder, is practically
insoluble in water, 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,
hypromellose, lactose monohydrate, magnesium stearate,
microcrystalline cellulose,
povidone 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
31
33
3
6
4
4
4
4
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
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 both the
ear