LOMOTIL- diphenoxylate hydrochloride and atropine sulfate tablet

البلد: الولايات المتحدة

اللغة: الإنجليزية

المصدر: NLM (National Library of Medicine)

العنصر النشط:

DIPHENOXYLATE HYDROCHLORIDE (UNII: W24OD7YW48) (DIPHENOXYLATE - UNII:73312P173G), ATROPINE SULFATE (UNII: 03J5ZE7KA5) (ATROPINE - UNII:7C0697DR9I)

متاح من:

Pfizer Laboratories Div Pfizer Inc

INN (الاسم الدولي):

DIPHENOXYLATE HYDROCHLORIDE

تركيب:

DIPHENOXYLATE HYDROCHLORIDE 2.5 mg

طريقة التعاطي:

ORAL

نوع الوصفة الطبية :

PRESCRIPTION DRUG

الخصائص العلاجية:

Lomotil is indicated as adjunctive therapy in the management of diarrhea in patients 13 years of age and older. Lomotil is contraindicated in: Lomotil is classified as a Schedule V controlled substance by federal regulation. Diphenoxylate hydrochloride is chemically related to the narcotic analgesic meperidine. In doses used for the treatment of diarrhea, whether acute or chronic, diphenoxylate has not produced addiction. Diphenoxylate hydrochloride is devoid of morphine-like subjective effects at therapeutic doses. At high doses it exhibits codeine-like subjective effects. The dose which produces antidiarrheal action is widely separated from the dose which causes central nervous system effects. The insolubility of diphenoxylate hydrochloride in commonly available aqueous media precludes intravenous self-administration. A dose of 100 to 300 mg/day, which is equivalent to 40 to 120 tablets, administered to humans for 40 to 70 days, produced opiate withdrawal symptoms. Since addiction to diphenoxylate hydrochlo

ملخص المنتج:

Tablets — round, white, with SEARLE debossed on one side and 61 on the other side and containing 2.5 mg of diphenoxylate hydrochloride and 0.025 mg of atropine sulfate, supplied as: 0025-0061-31 bottle of 100 Store below 25°C (77°F).

الوضع إذن:

New Drug Application

خصائص المنتج

LOMOTIL- DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE TABLET
PFIZER LABORATORIES DIV PFIZER INC
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LOMOTIL (DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE TABLETS),
FOR ORAL
USE, C-V
DESCRIPTION
Each Lomotil tablet contains:
2.5 mg of diphenoxylate hydrochloride USP (equivalent to 2.3 mg of
diphenoxylate) and
0.025 mg of atropine sulfate USP (equivalent to 0.01 mg of atropine)
Diphenoxylate hydrochloride, an antidiarrheal, is ethyl
1-(3-cyano-3,3-diphenylpropyl)-4-
phenylisonipecotate monohydrochloride and has the following structural
formula:
Atropine sulfate, an anticholinergic, is endo-(±)-α-(hydroxymethyl)
benzeneacetic acid 8-
methyl-8-azabicyclo[3.2.1] oct-3-yl ester sulfate (2:1) (salt)
monohydrate and has the
following structural formula:
A subtherapeutic amount of atropine sulfate is present to discourage
deliberate
overdosage.
Inactive ingredients of Lomotil tablets include acacia, corn starch,
magnesium stearate,
sorbitol, sucrose, and talc.
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 16-subject crossover 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 Lomotil liquid) 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 liquid
was app