Cationic amphiphilic drugs (CADs), such as haloperidol, are able to translocate through biological membrane bilayers via a chemically activated degradation of the phospholipid fabric of the membrane, which may constitute a third type of drug translocation process. We present evidence that this effect is dependent on the drug formulation. The choice of drug counterion is shown to influence the rate of bilayer hydrolysis, leading either to promotion of the reaction or the drug's precipitation via a counterion condensation process.