Abc Transporters In Drug Absorption And Elimination

Systemic exposure to orally administered digoxin is increased by coadministration of MDR1 inducers and negatively correlated with MDR1 protein expression in the intestine. MDR1 is also expressed on the brush-border membrane of renal epithelia, and its function can be monitored using digoxin (>70% excreted in the urine). MDR1 inhibitors (e.g., quinidine, verapamil, vaspo-dar, spironolactone, clarithromycin, and ritonavir) all markedly reduce renal digoxin excretion. In view of this, drugs with narrow therapeutic windows (e.g., digoxin) should be used with great care if MDR1-based drug-drug interactions are likely.

ABC Transporters Involved in Drug Absorption, Distribution, and Excretion

Transporter Name Tissue Distribution

Physiological Function

Substrates

MDR1 (ABCB1)

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