Loperamide

Information about Loperamide

Loperamide is synthetic opioid that primarily affects opiate receptors in the intestine and is used to treat diarrhea.

Liver safety of Loperamide

Loperamide has not been linked to serum enzyme elevations during therapy or to clinically apparent liver injury.

Mechanism of action of Loperamide

Loperamide (loe per’ a mide) is a synthetic piperidine derivative that acts as a mild opiate receptor agonist (predominant µ type receptors), but is used largely for the treatment of diarrhea rather than pain. Loperamide is not structurally related to morphine or codeine and has minimal or no euphoric or analgesic effects, apparently because it is poorly absorbed orally and is actively transported out of the central nervous system. Loperamide acts as a potent opiate agonist in the intestine and reduces intestinal motility, causing a slowing of intestinal transport and increased resorption of water and electrolytes, actions that are helpful in treating diarrhea.

FDA approval information for Loperamide

Loperamide was approved for use in the United States in 1976 and is still widely used to treat acute diarrhea caused by gastroenteritis, as well as the chronic diarrhea of inflammatory bowel disease.

FDA approval information for Loperamide

Loperamide is available as tablets and capsules of 2 mg and solution of 1 mg/5 mL generically and under the brand name Imodium. The usual dose of loperamide in adults is 4 mg initially, followed by 2 mg after each unformed stool, not to exceed 16 mg daily.

Side effects of Loperamide

Side effects of loperamide include abdominal bloating and pain, nausea and vomiting and constipation. Rare side effects include hypersensitivity reactions and paralytic ileus.

DEA controlled substance classification of Loperamide

Loperamide is not classified as a controlled substance and several formulations are available without prescription.

Full and partial opiod agonists:

• Alfentanil
• Butorphanol
• Codeine
• Diphenoxylate
• Fentanyl
• Heroin
• Hydrocodone
• Hydromorphone
• Levorphanol
• Loperamide
• Meperidine
• Methadone
• Morphine
• Opium
• Oxycodone
• Oxymorphone
• Pentazocine
• Remifentanil
• Sufentanil
• Tramadol

Opiate antagonists:

• Nalmefene
• Naloxegol
• Naloxone
• Naltrexone

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