País: Estados Unidos
Idioma: inglés
Fuente: NLM (National Library of Medicine)
DIPHENOXYLATE HYDROCHLORIDE (UNII: W24OD7YW48) (DIPHENOXYLATE - UNII:73312P173G), ATROPINE SULFATE (UNII: 03J5ZE7KA5) (ATROPINE - UNII:7C0697DR9I)
Bryant Ranch Prepack
ORAL
PRESCRIPTION DRUG
Diphenoxylate Hydrochloride and Atropine Sulfate Tablets USP are indicated as adjunctive therapy in the management of diarrhea in patients 13 years of age and older. Diphenoxylate hydrochloride and atropine sulfate tablets are contraindicated in: 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 tablets, administered to humans for 40 to 70 days, produced opiate withdrawal symptoms. Since addiction to diphenoxylate hydrochloride is possible at high doses, the recommended dosage should not be exceeded.
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 63629-1934-1 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]. Repackaged/Relabeled by: Bryant Ranch Prepack, Inc. Burbank, CA 91504
Abbreviated New Drug Application
DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE TABLET BRYANT RANCH PREPACK ---------- DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE TABLETS USP, CV RX ONLY DESCRIPTION Each Diphenoxylate Hydrochloride and Atropine Sulfate Tablet USP 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. Each diphenoxylate hydrochloride and atropine sulfate 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 liquid) and the peak plasma concentration, the area under th Leer el documento completo