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Most clinicians are aware that cytochrome P450 (CYP) enzymes affect pharmacokinetics. Also, the efflux pump P-glycoprotein affects drug disposition and activity in the brain and elsewhere. These processes are balanced by influx transporters — i.e., organic cation and organic anion transporters. Three recent studies elucidate potential effects on drug efficacy of these transporters.
Urban et al. studied gabapentin, a drug used frequently in psychiatry. Gabapentin is not bound to plasma protein and is eliminated by the kidneys without being metabolized. Kidney cells transfected with genetic material for the novel organic cation transporter OCTN1 or for a common variant had, respectively, two and four times the gabapentin uptake of nontransfect…