DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

NuCare Pharmaceuticals,Inc.

INN (International Name):

DIPHENOXYLATE HYDROCHLORIDE

Composition:

DIPHENOXYLATE HYDROCHLORIDE 2.5 mg

Administration route:

ORAL

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

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: - Known hypersensitivity to diphenoxylate or atropine. - Obstructive jaundice. - Diarrhea associated with pseudomembranous enterocolitis or enterotoxin-producing bacteria. 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

Product summary:

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 68071-4063-1 Bottles of 10 NDC 68071-4063-5 Bottles of 15 NDC 68071-4063-2 Bottles of 20 NDC 68071-4063-3 Bottles ofs 30 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

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
NUCARE PHARMACEUTICALS,INC.
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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 study
the bioava