Cocaine and cocaethylene binding to human tissues: a preliminary study.

The tissue binding of cocaine (COC) and cocaethylene (CE) was investigated by equilibrium dialysis of homogenates of whole human tissue supplemented with either COC or CE at concentrations of 10 and 50 microM for each drug. Concentrations of COC and CE were measured by high-pressure liquid chromatography. Kidney bound COC predominantly whereas serum bound it the least (about one tenth as much). In contrast, for CE, most binding was noted to brain with the least to serum (about one twentieth as much). Heart, placenta, and liver showed intermediate binding overall. The binding of COC and CE to these tissues may be important in understanding specific target-organ activity of both compounds.