Loperamide--an opiate receptor agonist with gastrointestinal motility effects.

Article Details

Citation

Mellstrand T

Loperamide--an opiate receptor agonist with gastrointestinal motility effects.

Scand J Gastroenterol Suppl. 1987;130:65-6.

PubMed ID
2820051 [ View in PubMed
]
Abstract

Loperamide is an opiate agonist, also exerting activity by inhibiting the action of calmodulin. The mode of action in the clinic is probably mainly due to its action on opiate receptors, since the effects of loperamide can be reversed by naloxone. The exclusive action in the gut is explained by the specific distribution of loperamide with extensive distribution to the gut and minimal influence on opiate receptors in CNS. Loperamide is well absorbed after oral administration and extensively metabolized. The pharmacokinetic properties are linear over a wide dose range.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
LoperamideCalmodulinProteinHumans
Unknown
Inhibitor
Details