[Molecular mechanisms on drug transporters in the drug absorption and disposition].

Article Details

Citation

Masuda S, Inui K

[Molecular mechanisms on drug transporters in the drug absorption and disposition].

Nihon Rinsho. 2002 Jan;60(1):65-73.

PubMed ID
11808341 [ View in PubMed
]
Abstract

The membrane transport processes of drugs are critical issues to determine their absorption, distribution and elimination. Recently, various drug transporters have been identified and characterized. The enterocyte peptide transporter PEPT1 mediates the absorption of peptide-like drugs including beta-lactam antibiotics as well as valacyclovir lacking peptide bond. In the kidney, the basolateral organic anion transporters (OAT1, OAT3) and cation transporters (OCT1, OCT2) mediate renal distribution of hydrophilic anionic and cationic drugs, respectively. The brush-border type OAT-K1/K2 were suggested to be a target transporter for methotrexate-leucovorine rescue therapy. The ATP-driven efflux pump P-glycoprotein appeared to be an interaction site between digoxin and clarithromycin or itraconazole in the kidney. In addition, the intestinal P-glycoprotein was suggested to act as an absorptive barrier for tacrolimus in recipients of liver and small bowel transplantation.

DrugBank Data that Cites this Article

Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
ItraconazoleP-glycoprotein 1ProteinHumans
Unknown
Inhibitor
Details