País: Estados Unidos
Idioma: inglés
Fuente: NLM (National Library of Medicine)
Loperamide Hydrochloride (UNII: 77TI35393C) (Loperamide - UNII:6X9OC3H4II)
McNeil Consumer Healthcare
Loperamide Hydrochloride
CAPSULE
2 mg
ORAL
PRESCRIPTION DRUG
IMODIUM® (loperamide hydrochloride) is indicated for the control and symptomatic relief of acute nonspecific diarrhea and of chronic diarrhea associated with inflammatory bowel disease. IMODIUM® is also indicated for reducing the volume of discharge from ileostomies. IMODIUM is contraindicated in patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients. IMODIUM is contraindicated in patients with abdominal pain in the absence of diarrhea. IMODIUM is not recommended in infants below 24 months of age. IMODIUM should not be used as the primary therapy: A specific clinical study designed to assess the abuse potential of loperamide at high doses resulted in a finding of extremely low abuse potential. Studies in morphine-dependent monkeys demonstrated that loperamide hydrochloride at doses above those recommended for humans prevented signs of morphine withdrawal. However, in humans, the naloxone challenge pupil test, which when positive indicates opiate-like effects, performed
Capsules - each capsule contains 2 mg of loperamide hydrochloride. The capsules have a light green body and a dark green cap with "JANSSEN" imprinted on one segment and "IMODIUM" on the other segment. IMODIUM® capsules are supplied in bottles of 100. NDC 50458-400-10 (100 CAPSULES) Store at 15°-25°C (59°-77°F).
IMODIUM- LOPERAMIDE HYDROCHLORIDE CAPSULE MCNEIL CONSUMER HEALTHCARE ---------- IMODIUM CAPSULES DESCRIPTION IMODIUM® (loperamide hydrochloride), 4-(p-chlorophenyl)-4-hydroxy-N,N-dimethyl-_a,a_-diphenyl- 1-piperidinebutyramide monohydrochloride, is a synthetic antidiarrheal for oral use. IMODIUM® is available in 2mg capsules. The inactive ingredients are: Lactose, cornstarch, talc, and magnesium stearate. IMODIUM® capsules contain FD&C Yellow No. 6. CLINICAL PHARMACOLOGY _IN VITRO_ and animal studies show that IMODIUM® (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, IMODIUM® prolongs the transit time of the intestinal contents. It reduces 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 - 14.4 hours. Plasma levels of unchanged drug remain below 2 nanograms per mL after the intake of a 2mg capsule of IMODIUM®. Plasma levels are highest approximately five 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 ketoconazole (CYP3A4 inhibitor) significantly inhibited the N- demethylation process _in vitro_ by 40% and 90%, respectively. In addition, CYP2B6 and Leer el documento completo