Drugdrug Interactions Involving Transportermediated Hepatic

UPTAKE Transporter-mediated hepatic uptake can cause drug-drug interactions among drugs that are actively taken up into the liver and metabolized and/or excreted in the bile. When an inhibitor of drug-metabolizing enzymes is highly concentrated in hepatocytes by active transport,

FIGURE 2-6 Transporters in the hepatocyte that function in the uptake and efflux of drugs across the sinusoidal membrane and efflux of drugs into the bile across the canalicular membrane. See text for details of the transporters pictured.

extensive inhibition of the drug-metabolizing enzymes may be observed because of the high concentration of the inhibitor in the vicinity of the drug-metabolizing enzymes.

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