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In pharmacology the interest in the question: "what are the effects of drugs?" has shifted more and more to the basic question: "how do drugs act?" Whatever the pharmacodynamic effect of a drug may be, it can only be due to an interaction between the molecules of the drug and the molecules constituting the biological object. Taking into account the usually small doses of drugs required to obtain responses, even in large animals, only an extremely small fraction of the molecules in the biological object can be primarily involved in the drug action. An insight in the various types of molecular interactions in which the drug molecules take part in the body are an essential requisite in the rational approach to the development of new drugs. From a functional point of view the interactions of the drug molecules with all kinds of molecules in the biological object can be differentiated in different types, especially according to the molecular sites of action and the consequences of the interaction: 1. Those molecular sites of interaction which are directly and essentially involved in the induction of the effect. They usually are indicated as the sites of action for the drug. They are characteristic for the type of response, e.g. cholinergic, curariform, convulsant, antihistaminic, etc. 2. The molecular sites of interaction which are neither directly nor essentially involved in the induction of the effect, but which mainly influence the distribution of the drug over the various compartments. They are not related to the type of response involved. These sites may interact with drugs with totally different types of action. Examples are the sites of binding for drugs on plasma proteins, often indicated as silent receptors or indifferent sites of binding, and the sites of biochemical conversion on drug degrading enzymes. They are not related to the type of response involved. Drugs with totally different types of action may interact with these sites.

A molecular approach to the modulation of pharmacokinetics: Modification of metabolic conversion by molecular manipulation