The ability to predict drug interactions mediated by active drug transport systems can help optimise pharmacotherapy

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Although most drug interactions result from inhibition or induction of cytochrome P450 isozymes, recent evidence suggests that active transmembrane drug transporting systems also have a role in pharmacokinetic drug interactions. P-glycoprotein is involved in cellular efflux of drugs, while human organic anion-transporting polypeptide is involved in cellular influx. The bioavailability of substrate drugs can be affected by other drugs or food that act as inhibitors or inducers of these systems

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