DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet

Država: Združene države Amerike

Jezik: angleščina

Source: NLM (National Library of Medicine)

Aktivna sestavina:

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

Dostopno od:

McKesson Contract Packaging

INN (mednarodno ime):

DIPHENOXYLATE HYDROCHLORIDE

Sestava:

DIPHENOXYLATE HYDROCHLORIDE 2.5 mg

Tip zastaranja:

PRESCRIPTION DRUG

Status dovoljenje:

Abbreviated New Drug Application

Lastnosti izdelka

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
MCKESSON CONTRACT PACKAGING
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DESCRIPTION
Each tablet for oral administration contains:
diphenoxylate
hydrochloride, USP 2.5 mg
(Warning – May be habit forming)
atropine
sulfate, USP 0.025 mg
Diphenoxylate hydrochloride, an antidiarrheal, is ethyl 1-(3-cyano-3,
3-diphenylpropyl)-4-phenyl-
isonipecotate monohydrochloride and has the following structure:
Atropine sulfate, an anticholinergic, is
endo-(±)-alpha-(hydroxymethyl) benzeneacetic acid 8-methyl-8-
azabicylo[3.2.1] oct-3-yl ester sulfate (2:1)] (salt) monohydrate and
has the following structure:
A subtherapeutic amount of atropine sulfate is present to discourage
deliberate overdosage.
Each tablet for oral administration contains the following inactive
ingredients: colloidal silicon dioxide,
microcrystalline cellulose, pregelatinized starch and stearic acid.
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 4-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 16
subject cross-over bioavailability study, a linear relationship in the
dose range of 2.5 mg to 10 mg was
found between the dose of diphenoxylate hydrochloride (given as
Diphenoxylate Hydrochloride and
Atropine Sulfate Oral Solution) and the peak plasma concentration, the
area under the plasma
concentration-time curve, and the amount of diphenoxylic acid excreted
in the urine. In the same study
the bioavailability of the tablet compared with an equal dose of the
liqui