Overview
DESCRIPTION Loperamide hydrochloride, 4-(p-chlorophenyl)-4-hydroxy-N, N-dimethyl-α,α-diphenyl-piperidinebutyramide monohydrochloride, is a synthetic antidiarrheal for oral use. Loperamide hydrochloride is available in 2 mg capsules. The inactive ingredients are: Lactose monohydrate, microcrystalline cellulose, sodium starch glycolate, colloidal silicon dioxide, magnesium stearate gelatin,...
Mechanism of Action
CLINICAL PHARMACOLOGY Mechanism of Action In vitro and animal studies show that loperamide hydrochloride capsules act 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 propulsive peristalsis, and increasing intestinal transit time. Loperamide increases the tone of the anal sphincter, thereby reducing incontinence and urgency. Pharmacodynamics Loperamide 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.
Indications
- INDICATIONS AND USAGE Loperamide hydrochloride capsules are indicated for the control and symptomatic relief of acute nonspecific diarrhea in patients 2 years of age and older and of chronic diarrhea in adults associated with inflammatory bowel disease. Loperamide hydrochloride capsules are also indicated for reducing the volume of discharge from ileostomies.
Common Doses
- 2 mg
- 4 mg
- 16 mg
- 1 mg
Dosage
DOSAGE AND ADMINISTRATION Loperamide hydrochloride capsules USP are contraindicated in pediatric patients less than 2 years of age due to the risks of respiratory depression and serious cardiac adverse reactions (see CONTRAINDICATIONS ). Avoid loperamide hydrochloride capsules dosages higher than recommended in adult or pediatric patients 2 years of age and older due to the risk of serious cardiac adverse reactions (see WARNINGS , OVERDOSAGE ). (1 capsule = 2 mg) Patients should receive appropriate fluid and electrolyte replacement as needed.
Black Box Warning
WARNING: TORSADES DE POINTES AND SUDDEN DEATH Cases of Torsades de Pointes, cardiac arrest, and death have been reported with the use of a higher than recommended dosage of loperamide hydrochloride capsules (see WARNINGS and OVERDOSAGE ). Loperamide hydrochloride capsules are contraindicated in pediatric patients less than 2 years of age (see CONTRAINDICATIONS ). Avoid loperamide hydrochloride capsules dosages higher than recommended in adults and pediatric patients 2 years of age and older due to the risk of serious cardiac adverse reactions (see DOSAGE AND ADMINISTRATION ).
Contraindications
- CONTRAINDICATIONS Loperamide hydrochloride capsules are contraindicated in: pediatric patients less than 2 years of age due to the risks of respiratory depression and serious cardiac adverse reactions (see WARNINGS ). patients with a known hypersensitivity to loperamide hydrochloride or to any of the excipients. patients with abdominal pain in the absence of diarrhea. patients with acute dysentery, which is characterized by blood in stools and high fever. patients with acute ulcerative colitis.
Side Effects
- ADVERSE REACTIONS Clinical Trial Experience The adverse effects reported during clinical investigations of loperamide hydrochloride capsules are difficult to distinguish from symptoms associated with the diarrheal syndrome. Adverse experiences recorded during clinical studies with loperamide hydrochloride capsules were generally of a minor and self-limiting nature. They were more commonly observed during the treatment of chronic diarrhea. The adverse events reported are summarized irrespective of the causality assessment of the investigators.
Interactions
- Drug Interactions Effects of Other Drugs on Loperamide Concomitant use of loperamide hydrochloride capsules with inhibitors of CYP3A4 (e.g., itraconazole) or CYP2C8 (e.g., gemfibrozil) or inhibitors of P-glycoprotein (e.g., quinidine, ritonavir) can increase exposure to loperamide. The increased systemic exposure to loperamide may increase a risk for cardiac adverse reactions especially in patients who are taking multiple CYP enzyme inhibitors, or in patients with underlying cardiac conditions (see WARNINGS ). Monitor patients for cardiac adverse reactions.