Abstract
This chapter offers a comprehensive summary of drug excretion, presenting an overview of membrane transporters in terms of classification, nomenclature, and organ expression in the beginning. Membrane transporters perform a central function in drug excretion. The ATP-binding cassette (ABC) transporter superfamily consists of membrane-bound, ATP-driven transporters that pump drugs, drug metabolites, and endogenous metabolites out of cells. The renal proximal tubule of the kidney contains several organic anion transport systems that secrete a wide array of exogenous compounds. Biliary excretion of drugs and metabolites involves one of several ATP-dependent transport proteins expressed on the canalicular membrane. These proteins are members of the ABC family of transporters, and they mediate unidirectional transport of substrates uphill against a large concentration gradient. Both liver and kidney disease have been shown to affect hepatic clearance by reducing hepatic uptake, metabolism, and biliary excretion of drugs and their metabolites. In addition to altered drug metabolism, chronic liver disease alters through a number of mechanisms.
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