Beside drug metabolizing enzymes alsogenetically variable membrane transporters may substantially contribute to the interindividual variability in pharmacokinetics and efficacy of opioids and other analgesics. The organic cation transporter OCT1 is strongly expressed in the sinusoidal membrane of the human liver. It may affect hepatic uptake and thus limit metabolic rates. OCT1 is highly genetically variable. Genetic polymorphisms lead to substantially reduced OCT1 activity in up to 9% of the Europeans and the white Americans. This review summarize the data on the effect of OCT1 polymorphisms on pharmacokinetics and efficacy of opioids like morphine, codeine, and tramadol and of anti-migraine drugs. It discuss currently possible applications and perspectives for establishing OCT1 pharmacogenetics as a useful tool in personalized pain management.
Keywords: O-desmethyltramadol; SLC22A1; morphine; organiccation transporter 1; sumatriptan; tramoadol.