DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE tablet

国: アメリカ合衆国

言語: 英語

ソース: NLM (National Library of Medicine)

有効成分:

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

から入手可能:

Mylan Pharmaceuticals Inc.

INN（国際名）:

DIPHENOXYLATE HYDROCHLORIDE

構図:

DIPHENOXYLATE HYDROCHLORIDE 2.5 mg

投与経路:

ORAL

処方タイプ:

PRESCRIPTION DRUG

適応症:

Diphenoxylate hydrochloride and atropine sulfate tablets 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 equi

製品概要:

Diphenoxylate Hydrochloride and Atropine Sulfate Tablets, USP are available containing 2.5 mg of diphenoxylate hydrochloride, USP (Warning: May be habit forming) and 0.025 mg of atropine sulfate, USP. The tablets are white, round, unscored tablets debossed with M over 15 on one side of the tablet and blank on the other side. They are available as follows: NDC 0378-0415-77 bottles of 90 tablets NDC 0378-0415-01 bottles of 100 tablets NDC 0378-0415-10 bottles of 1000 tablets Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Protect from light. Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure. Pharmacist:  Dispense with a child-resistant closure only. Mylan Pharmaceuticals Inc. Morgantown, WV 26505 U.S.A. Revised: 2/2018 DPXAS:R14

認証ステータス:

Abbreviated New Drug Application

製品の特徴

DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE
HYDROCHLORIDE AND ATROPINE SULFATE TABLET
MYLAN PHARMACEUTICALS INC.
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DESCRIPTION
Each diphenoxylate hydrochloride and atropine sulfate tablet, USP
contains:
2.5 mg of diphenoxylate hydrochloride, USP (Warning: May be habit
forming) (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-(±)-alpha-(hydroxymethyl) benzeneacetic acid 8-methyl-8-
azabicylo[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 diphenoxylate hydrochloride and atropine
sulfate tablets include colloidal
silicon dioxide, microcrystalline cellulose, pregelatinized starch
(corn) 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 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 the plasma concentration-time
curve, and the amount o