Country: United States
Language: English
Source: NLM (National Library of Medicine)
DIPHENOXYLATE HYDROCHLORIDE (UNII: W24OD7YW48) (DIPHENOXYLATE - UNII:73312P173G), ATROPINE SULFATE (UNII: 03J5ZE7KA5) (ATROPINE - UNII:7C0697DR9I)
Hikma Pharmaceuticals USA Inc.
DIPHENOXYLATE HYDROCHLORIDE
DIPHENOXYLATE HYDROCHLORIDE 2.5 mg in 5 mL
ORAL
PRESCRIPTION DRUG
Diphenoxylate hydrochloride and atropine sulfate is indicated as adjunctive therapy in the management of diarrhea in patients 13 years of age and older. Diphenoxylate hydrochloride and atropine sulfate is contraindicated in: Diphenoxylate hydrochloride and atropine sulfate oral solution 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
Diphenoxylate Hydrochloride 2.5 mg and Atropine Sulfate 0.025 mg per 5 mL Oral Solution, USP The 2.5 mg/0.025 mg per 5 mL oral solution is supplied as a (cherry-flavored) clear, orange-colored solution. NDC 0054-3194-46: Bottle of 60 mL Oral Solution: Dispense only in original container. A plastic oral syringe calibrated in increments of 1/2 mL (1/4 mg) with a capacity of 3 mL (1.5 mg) accompanies each 2 oz bottle of Diphenoxylate Hydrochloride and Atropine Sulfate Oral Solution, USP. Only this plastic oral syringe should be used when measuring Diphenoxylate Hydrochloride and Atropine Sulfate Oral Solution, USP for administration to children. Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] Discard open bottle after 90 days. Distributed by: Hikma Pharmaceuticals USA Inc. Berkeley Heights, NJ 07922 C50000486/01 Revised February 2023
Abbreviated New Drug Application
DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE- DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE SOLUTION HIKMA PHARMACEUTICALS USA INC. ---------- DIPHENOXYLATE HYDROCHLORIDE AND ATROPINE SULFATE ORAL SOLUTION, USP FOR ORAL USE, C-V RX ONLY DESCRIPTION Each 5 mL of oral solution contains: 2.5 mg of diphenoxylate hydrochloride (equivalent to 2.3 mg of diphenoxylate), 0.025 mg of atropine sulfate (equivalent to 0.01 mg of atropine), and 15% alcohol. Diphenoxylate hydrochloride, an antidiarrheal, is ethyl 1-(3-cyano-3,3-diphenylpropyl)-4- phenylisoni-pecotate monohydrochloride and has the following structural formula: C H N O · HCL M.W. 489.05 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: 30 32 2 2 (C H NO ) · H SO · H O M.W. 694.83 A subtherapeutic amount of atropine sulfate is present to discourage deliberate overdosage. Inactive ingredients of diphenoxylate hydrochloride and atropine sulfate oral solution include alcohol, anhydrous citric acid, FD&C Red No. 40, FD&C Yellow No. 6, glycerin, maltol, potassium sorbate, purified water, sorbitol solution and wild cherry flavor. 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 hydrochlori Read the complete document