Страна: Соединенные Штаты
Язык: английский
Источник: NLM (National Library of Medicine)
LOPERAMIDE HYDROCHLORIDE (UNII: 77TI35393C) (LOPERAMIDE - UNII:6X9OC3H4II)
Physicians Total Care, Inc.
LOPERAMIDE HYDROCHLORIDE
LOPERAMIDE HYDROCHLORIDE 2 mg
ORAL
PRESCRIPTION DRUG
Loperamide hydrochloride capsules are indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. Loperamide hydrochloride capsules are also indicated for reducing the volume of discharge from ileostomies. Loperamide hydrochloride capsules are contraindicated in patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients. Loperamide hydrochloride is contraindicated in patients with abdominal pain in the absence of diarrhea. Loperamide hydrochloride is not recommended in infants below 24 months of age. Loperamide hydrochloride should not be used as the primary therapy: - in patients with acute dysentery, which is characterized by blood in stools and high fever, - in patients with acute ulcerative colitis, - in patients with bacterial enterocolitis caused by invasive organisms including Salmonella, Shigella, and Campylobacter, - in patients with pseudomembranous colitis associated with the u
Loperamide Hydrochloride Capsules, USP are available containing 2 mg of loperamide hydrochloride, USP. The capsule is a hard-shell gelatin capsule with a light brown opaque cap and a light brown opaque body filled with white to off-white powder blend. The capsule is axially printed with MYLAN over 2100 in black ink on both the cap and the body. They are available as follows: Store at 20° to 25°C (68° to 77°F). [See USP for Controlled Room Temperature.] Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure. Mylan Pharmaceuticals Inc. Morgantown, WV 26505 REVISED JULY 2006 LOP:R11 Distributed and Repackaged by: Physicians Total Care, Inc. Tulsa, Oklahoma 74146
Abbreviated New Drug Application
LOPERAMIDE HYDROCHLORIDE - LOPERAMIDE HYDROCHLORIDE CAPSULE PHYSICIANS TOTAL CARE, INC. ---------- DESCRIPTION Loperamide hydrochloride, 4-(p-chlorophenyl)-4-hydroxy-N, N-dimethyl-α,α-diphenyl-1- piperidinebutyramide monohydrochloride, is a synthetic antidiarrheal for oral use. Loperamide hydrochloride is available in 2 mg capsules. Loperamide hydrochloride capsules, USP contain the following inactive ingredients: colloidal silicon dioxide, gelatin, iron oxides, lactose (hydrous), magnesium stearate, microcrystalline cellulose, sodium starch glycolate and titanium dioxide. CLINICAL PHARMACOLOGY _In vitro_ and animal studies show that loperamide hydrochloride acts by slowing intestinal motility and by affecting water and electrolyte movement through the bowel. Loperamide binds to the opiate receptor in the gut wall. Consequently, it inhibits the release of acetylcholine and prostaglandins, thereby reducing peristalsis, and increasing intestinal transit time. Loperamide increases the tone of the anal sphincter, thereby reducing incontinence and urgency. In man, loperamide hydrochloride prolongs the transit time of the intestinal contents. It reduces the daily fecal volume, increases the viscosity and bulk density, and diminishes the loss of fluid and electrolytes. Tolerance to the antidiarrheal effect has not been observed. Clinical studies have indicated that the apparent elimination half-life of loperamide in man is 10.8 hours with a range of 9.1 to 14.4 hours. Plasma levels of unchanged drug remain below 2 nanograms per mL after the intake of a 2 mg capsule of loperamide hydrochloride. Plasma levels are highest approximately 5 hours after administration of the capsule and 2.5 hours after the liquid. The peak plasma levels of loperamide were similar for both formulations. Elimination of loperamide mainly occurs by oxidative N-demethylation. Cytochrome P450 (CYP450) isozymes, CYP2C8 and CYP3A4, are thought to play an important role in loperamide N- demethylation process since quercetin (CYP2C8 inhibitor) and ket Прочитать полный документ