Loperamide Hydrochloride

• Loperamide Hydrochloride acts on gut opioid receptors without CNS effects, ensuring safe action.
• It controls acute and chronic diarrhea by slowing intestinal movement.

Chemical Formula:

• C₂₉H₃₃ClN₂O₂·HCl

Mechanism of Action:

• Peripheral μ-opioid receptor agonist
• Acts on myenteric plexus of GI tract → inhibits peristalsis
• No CNS penetration (substrate of P-glycoprotein efflux pump)

Uses of Loperamide Hydrochloride:

• Antidiarrheal
• Traveler’s diarrhea, chronic diarrhea (IBS-D)

Side Effects of Loperamide Hydrochloride:

• Constipation
• Abdominal cramping
• CNS toxicity only at very high doses or when abused with P-gp inhibitors (e.g. quinidine)

Notes:

• Over-the-counter (Imodium)
• Abuse at high doses (“poor man’s methadone”) can cause QT prolongation, cardiac arrest

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