Many drugs undergo reversible metabolism. The basis of our understanding of this process is the reversible metabolism of prednisone (PD)-prednisolone (PL). The pharmacokinetics of reversible metabolism requires the use of four area under the curve values integrated into four equations for clearance (CL). Other variables, such as linear versus non-linear disposition, can play important roles in reversible metabolism. Of recent interest is the reversible metabolism of haloperidol which consists of an interconversion process between the parent drug haloperidol (HL) and its reduced metabolite (RH). However, the interconversion of HL-RH differs from the PD-PL model in that, whereas PD and PL are both active, RH is considered to be a therapeutically inactive, possibly toxic, metabolite. This article reviews the pharmacodynamic and pharmacokinetic properties of HL and RH and the possible clinical effects that can result from this reversible metabolism.