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Loperamide

IMODIUM

What it isPeripherally restricted mu agonist slowing gut transit; diarrhea.

Why this oneP-glycoprotein keeps it out of the CNS, so it controls diarrhea without euphoria or dependence at normal doses.

What limits itAt the supratherapeutic doses used for abuse it saturates P-gp and causes torsades and death. Avoid in inflammatory or invasive colitis.

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Diarrhea (OTC)Adults & children ≥12 yr2 caplets after first loose stool, then 1 after each subsequent loose stool4 caplets/24 hr
Diarrhea (OTC)Children 9–11 yr (60–95 lb)1 caplet after first loose stool, then ½ after each subsequent3 caplets/24 hr
Diarrhea (OTC)Children 6–8 yr (48–59 lb)1 caplet after first loose stool, then ½ after each subsequent2 caplets/24 hr

Renal Undefined

Hepatic Undefined

Instructions

Pregnancy Undefined

Lactation Undefined

NO BOXED WARNINGS

Principal riskTorsades at the supratherapeutic doses used for abuse

Cost, est. cash$5–$150/month

Generic entry1991

Classes and tags

Clinical profile

Therapeutic safety burden1 / 4
Overdose danger4 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades1 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk1 / 4

Legacy pregnancy categoryC

Defining liabilityTherapeutic CNS effects are minimal, but high-dose misuse can cause fatal sodium/potassium-channel cardiotoxicity.

Mechanism of action: Loperamide ballicule

Loperamide ballicule: receptor binding, kinetics and half-life diagram

Open Loperamide in the interactive console ↗

Memory aids: mascots and interaction avatars

Loperamide IMODIUM mascot mnemonic cartoon
“Loops Immobilize peristalsis”
Loperamide CYP3A4 substrate avatar
CYP3A4 substrate
Loperamide P-gp substrate avatar
P-gp substrate (sensitive)

Open Loperamide in the interactive console ↗