Research Institute for 

Pharmacy & Biochemistry

25 May 2019
Course description

Analysis of chiral drugs

At present 99% of all used drugs are represented by organic compound molecules that can be obtained synthetically, semisynthetically or by isolation from products of nature. It is stated that 60% of all available drugs are chiral, i.e. optically active. 75% of that number are used as racemates, and 25% are formed by one enantiomer. The reason is that preparation of individual enantiomers is much more expensive and time-consuming; however, the existing legislation requires that all probable stereochemic entities were addressed, their biological effects were evaluated, and their presence was quantified.

The chirality is considered to be one of the most interesting and important stereochemical phenomena in the drug R&D. A drug with chiral atoms that is not divided into individual enantiomers (racemate) can be an equimolar mixture of enantiomers that can have different pharmacological and toxicological properties. In an organism representing chiral enviromnement the enantiomers interact with enzymes or receptors differently. This is caused by their different disposition at stereospecific reactions with organism's biomolecules. Different interactions lead to pharmacodynamic and pharmacokinetic differences, so also differences in absorption, distribution, metabolism and elimination can appear.

Stereodifferentiation of pharmacokinetic processes is significant mainly in cases when a drug interacts with an enzyme complex (metabolic systems or selective membrane transport systems).The course deals with the chirality phenomenon and acquaints with differences in metabolization of chiral drugs and their different behaviour in an organism. Also the problematics of chirality in the legislation and guidelines relating to pharmacy and drug R&D is discussed. The key part of the course is devoted to approaches and possibilities of chiral compound analysis by the classical liquid chromatography technique and electromigration separation methods. The special part of the course is dedicated to chiroptical spectroscopy methods: electronic circular dichroism, vibrational circular dichroism and Raman optical activity.

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Location: Brno

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