DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet

País: Estados Unidos

Idioma: inglés

Fuente: NLM (National Library of Medicine)

Ingredientes activos:

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

Disponible desde:

Aphena Pharma Solutions - Tennessee, LLC

Vía de administración:

ORAL

tipo de receta:

PRESCRIPTION DRUG

indicaciones terapéuticas:

Diphenoxylate Hydrochloride and Atropine Sulfate Tablets USP are effective as adjunctive therapy in the management of diarrhea. Diphenoxylate hydrochloride and atropine sulfate tablets are contraindicated in patients with: Diphenoxylate hydrochloride and atropine sulfate tablets are 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

Resumen del producto:

Diphenoxylate Hydrochloride and Atropine Sulfate Tablets USP are available as round white tablets debossed ‘490’ on one side and plain on the other side. Each tablet contains 2.5 mg of diphenoxylate hydrochloride and 0.025 mg of atropine sulfate and are supplied as: NDC Number      Size 62559-490-01     Bottle of 100 tablets 62559-490-10     Bottle of 1,000 tablets Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [See USP controlled room temperature]. Manufactured by: ANI Pharmaceuticals, Inc. Baudette, MN 56623 9981 Rev 05/17

Estado de Autorización:

Abbreviated New Drug Application

Ficha técnica

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
APHENA PHARMA SOLUTIONS - TENNESSEE, LLC
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DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE TABLETS USP, CV
RX ONLY
DESCRIPTION
Each tablet, for oral administration, contains:
Diphenoxylate Hydrochloride USP…. 2.5 mg
Atropine Sulfate USP...................... 0.025 mg
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.
Each tablet contains the following inactive ingredients:
confectioner’s sugar, corn starch, lactose
monohydrate, magnesium stearate, and sodium starch glycolate.
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
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 stu