ZAFIRLUKAST tablet, film coated

País: Estados Unidos

Língua: inglês

Origem: NLM (National Library of Medicine)

Ingredientes ativos:

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

Disponível em:

Carilion Materials Management

DCI (Denominação Comum Internacional):

Zafirlukast

Composição:

Zafirlukast 20 mg

Via de administração:

ORAL

Tipo de prescrição:

PRESCRIPTION DRUG

Indicações terapêuticas:

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.

Resumo do produto:

Product: 68151-1977 NDC: 68151-1977-6 1 TABLET, FILM COATED in a PACKAGE

Status de autorização:

Abbreviated New Drug Application

Características técnicas

ZAFIRLUKAST- ZAFIRLUKAST TABLET, FILM COATED
CARILION MATERIALS MANAGEMENT
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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 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 25-100 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 i