Importance of Stereochemistry in Pharmacy with Special attention to DrugMolecules
Introduction
The importance of stereochemistry in drug action is gaining greater attention in pharmaceuticalsciemces, and a basic knowledge of the subject will be necessary for clinicians to make informeddecisions regarding the use of single-enantiomer drugs. Many of the drugs currently used in psychiatric practice are mixtures of enantiomers. For some therapeutics, single-enantiomer formulations can provide greater selectivities for their biological targets, improved therapeuticindices, and/or better pharmacokinetics than a mixture of enantiomers. This assignment reviewsthe importance of stereochemistry with special attention to different drug molecules, thenomenclature for describing stereochemistry and enantiomers, emphasizes the potential biologicaland pharmacologic differences between the 2 enantiomers of a drug, and highlights the clinicalexperience with single enantiomers. In some cases, both a mixture of enantiomers and a single-enantiomer formulation of a drug will be available simultaneously. In these cases, familiarity withstereochemistry and its pharmacologic implications will aid the practicing physician to provideoptimal pharmacotherapy to his or her patients.
Some Basic Concepts
Before going into the depth of this discussion let us have some concepts about the basic aspects of stereochemistry which eill ultimately help us to understand the importance of stereochemistry later on.
1
This section contains the basics needed to understand chiral drugs. The most important point is thatchiral drugs have 2 structurally similar forms that can behave very differently in biological systemsdue to their different shapes in 3-dimensional space. These 2 possible forms are termed enantiomers , and the 2 enantiomers of a given chiral drug should be considered 2 different drugs.This topic is discussed further in the next section.
Chirality
is formally defined as