ACCOLATE zafirlukast tablet film coated

Nchi: Marekani

Lugha: Kiingereza

Chanzo: NLM (National Library of Medicine)

Viambatanisho vya kazi:

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

Inapatikana kutoka:

AstraZeneca Pharmaceuticals LP

INN (Jina la Kimataifa):

ZAFIRLUKAST

Tungo:

ZAFIRLUKAST 10 mg

Dawa ya aina:

PRESCRIPTION DRUG

Idhini hali ya:

New Drug Application

Tabia za bidhaa

ACCOLATE- ZAFIRLUKAST TABLET, FILM COATED
ASTRAZENECA PHARMACEUTICALS LP
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ACCOLATE®
(_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 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.
ACCOLATE 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 25-100 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