DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet

Ülke: ABD

Dil: İngilizce

Kaynak: NLM (National Library of Medicine)

Aktif bileşen:

DIPHENOXYLATE HYDROCHLORIDE (UNII: W24OD7YW48) (DIPHENOXYLATE - UNII:73312P173G)

Mevcut itibaren:

Bryant Ranch Prepack

INN (International Adı):

DIPHENOXYLATE HYDROCHLORIDE

Kompozisyon:

DIPHENOXYLATE HYDROCHLORIDE 2.5 mg

Reçete türü:

PRESCRIPTION DRUG

Yetkilendirme durumu:

Abbreviated New Drug Application

Ürün özellikleri

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
BRYANT RANCH PREPACK
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DESCRIPTION
Each diphenoxylate hydrochloride and atropine sulfate tablet for oral
use contains:
Diphenoxylate Hydrochloride
........................................... 2.5 mg
Atropine Sulfate.....................................................
0.025 mg
In addition, each tablet contains the following inactive ingredients:
colloidal silicon dioxide, lactose
monohydrate, microcrystalline cellulose, pregelatinized starch, and
stearic acid.
Diphenoxylate hydrochloride, an antidiarrheal, is ethyl
1-(3-cyano-3,3-diphenyl-propyl)-4-
phenylisonipecotate monohydrochloride and has the following structural
formula:
Molecular formula C
H N O •HCl
M.W. = 489.05
Atropine sulfate, an anticholinergic, is
1αH,5αH-Tropan-3-α-ol(±)-tropate (ester), sulfate (2:1) (salt)
monohydrate and has the following structural formula:
Molecular formula (C
H NO ) •H SO •H O M.W. = 694.83
A subtherapeutic amount of atropine sulfate is present to discourage
deliberate overdosage.
CLINICAL PHARMACOLOGY
Diphenoxylate is rapidly and extensively metabolized in man by ester
hydrolysis to diphenoxylic acid
(difenoxine), which is biologically active and the major metabolite in
the blood. After a 5 mg oral dose
of carbon-14 labeled diphenoxylate hydrochloride in ethanolic solution
was given to three healthy
volunteers, an average of 14% of the drug plus its metabolites was
excreted in the urine and 49% in the
feces over a four-day period. Urinary excretion of the unmetabolized
drug constituted less than 1% of
the dose, and diphenoxylic acid plus its glucuronide conjugate
constituted about 6% of the dose. In a
sixteen-subject cross-over bioavailability study, a linear
relationship in the dose range of 2.5 to 10 mg
was found between the dose of diphenoxylate hydrochloride (given as
Diphenoxylate HCl and Atropine
Sulfate Oral Solution) and the peak plasma concentration, the area
under the plasma concentration-tim