In clinical toxicology, a better understanding of the pharmacokinetics of the drugs may be useful in both risk assessment and formulating treatment guidelines for patients. Pharmacokinetics describes the time course of drug concentrations and is a driver for the time course of drug effects. In this chapter pharmacokinetics is described from a mathematical modeling perspective as applied to clinical toxicology. The pharmacokinetics of drugs are described using a combination of input and disposition (distribution and elimination) phases. A description of the time course of the input and disposition of drugs in overdose provides a basis for understanding the time course of effects of drugs in overdose. Relevant clinical toxicology examples are provided to explain various pharmacokinetic principles. Throughout this chapter we have taken a pragmatic approach to understanding and interpreting the time course of drug effects.