Loperamide Hcl

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® (loperamide hcl) is also indicated for reducing the volume of discharge from ileostomies.

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® (loperamide hcl) capsules are supplied in bottles of 100.

NDC 50458-400-10.........(100 CAPSULES)

Store at 15°-25°C (59°-77°F).

Janssen Pharmaceutica Inc. Revised September 1996, July 1998. FDA Rev date: 10/21/2005

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® (loperamide hcl) 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 - 14.4 hours. Plasma levels of unchanged drug remain below 2 nanograms per mL after the intake of a 2mg capsule of IMODIUM® (loperamide hcl) . 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 CYP2D6 appear to play a minor role in loperamide N-demethylation. Excretion of the unchanged loperamide and its metabolites mainly occurs through the feces. In those patients in whom biochemical and hematological parameters were monitored during clinical trials, no trends toward abnormality during IMODIUM® (loperamide hcl) therapy were noted. Similarly, urinalyses, EKG and clinical ophthalmological examinations did not show trends toward abnormality.

Patients should be advised to check with their physician if their diarrhea does not improve in 48 hours or if they note blood in their stools, develop a fever or develop abdominal distention.

Tiredness, dizziness, or drowsiness may occur in the setting of diarrheal syndromes treated with IMODIUM (loperamide hcl) . Therefore, it is advisable to use caution when driving a car or operating machinery. (see ADVERSE REACTIONS).

You should not use this medication if you are allergic to loperamide, or if you have stools that are bloody, black, or tarry, or if you have diarrhea that is caused by taking an antibiotic.

Before taking loperamide, tell your doctor if you have a fever, mucus in your stools, a history of liver disease, or if you are taking an antibiotic.

Drink plenty of liquids while you are taking loperamide.

It may take up to 48 hours before your symptoms improve. Keep using the medication as directed and tell your doctor if your symptoms do not improve after 10 days of treatment.

Loperamide may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Your pharmacist can provide more information about loperamide.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2013 Cerner Multum, Inc. Version: 5.02. Revision date: 4/18/2012.

Your use of the content provided in this service indicates that you have read,understood and agree to the End-User License Agreement,which can be accessed by clicking on this link.