14 Facts About Loperamide

Loperamide, sold under the brand name Imodium, among others, is a medication used to decrease the frequency of diarrhea.

Loperamide is effective for the treatment of a number of types of diarrhea.

Loperamide treatment is not used in symptomatic C difficile infections, as it increases the risk of toxin retention and precipitation of toxic megacolon.

Loperamide should be administered with caution to people with liver failure due to reduced first-pass metabolism.

Loperamide is not recommended in the United Kingdom for use during pregnancy or by nursing mothers.

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Loperamide can be present in breast milk, and is not recommended for breast-feeding mothers.

Loperamide is a substrate of P-glycoprotein; therefore, the concentration of loperamide increases when given with a P-glycoprotein inhibitor.

Loperamide is capable of decreasing the absorption of some other drugs.

Loperamide is an opioid-receptor agonist and acts on the µ-opioid receptors in the myenteric plexus of the large intestine.

Loperamide taken with quinidine was found to produce respiratory depression, indicative of central opioid action.

Loperamide has been shown to cause a mild physical dependence during preclinical studies, specifically in mice, rats, and rhesus monkeys.

Loperamide hydrochloride was first synthesized in 1969 by Paul Janssen from Janssen Pharmaceutica in Beerse, Belgium, following previous discoveries of diphenoxylate hydrochloride and fentanyl citrate .

Loperamide was originally marketed as Imodium, and many generic brands are sold.

Loperamide has typically been deemed to have a relatively low risk of misuse.