Pharmacology of Drug Stereoisomers (eBook)

The book is devoted to an important aspect of pharmacology and pharmaceutical chemistry, i.e. the significance of stereoisomerism of drugs for their biological effect from the point of view of their pharmacokinetics, pharmacodynamics and toxicology. The authors review the landmarks in the development of stereochemistry and stereopharmacology. Present-day IUPAC terminology is discussed; general issues of stereoisomerism are considered including separation of racemic mixtures and asymmetric synthesis of isomers, methods of quantifying the isomers of a drug in biological material. The authors put special emphasis on general problems of the influence of stereoisomerism on pharmacological and adverse effects of drugs. A classification of drugs based on stereochemical properties of their isomers is proposed. Possibilities of interaction of stereoisomers in racemic mixtures are discussed. A considerable portion of the book is devoted to pharmacological action of the main groups of drugs whose structure includes asymmetric atoms (that is, drugs with several isomers). Detailed attention is paid to advisability of developing single isomer drugs and to the specifics of their study at the stage of preclinical and clinical trials.

Dr. Alexander Alexeyevich Spasov, Doctor of Medicine, Professor, Corresponding Member of Russian Academy of Medical Sciences, Head of the Department of Pharmacology at the Volgograd State Medical University, Vice-Director of the Volgograd Medical Research Center (Russian Federation).

Dr. Igor Nikolayevich Iezhitsa, Doctor of Biological Sciences, Professor at Department of Pharmacology & Therapeutics, School of Medicine, International Medical University (Malaysia) and Department of Pharmacology and Bioinformatics at the Volgograd State Medical University (Russian Federation). 

Dr. Pavel Mikhailovich Vassiliev, Doctor of Biological Sciences, Head of Laboratory for Information Technology in Pharmacology and Computer Modeling of Drugs for Research Center of Innovative Medicines, Professor of the Department of Pharmacology and Bioinformatics, Volgograd State Medical University (Russian Federation), Vice-Chairman of Russian section of the Cheminformatics and QSAR Society

Dr. Alexander Alexandrovich Ozerov, Doctor of Chemistry, Professor, head of Department of Pharmaceutical and Toxicological Chemistry at the Volgograd State Medical University, vice-director for research at the Research Institute for Pharmacology at the Volgograd State Medical University

Dr. Renu Agarwal, Doctor of Pharmacology, Professor, Professor at Department of Pharmacology & Therapeutics, School of Medicine, International Medical University (Malaysia).

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The book is devoted to an important aspect of pharmacology and pharmaceutical chemistry, i.e. the significance of stereoisomerism of drugs for their biological effect from the point of view of their pharmacokinetics, pharmacodynamics and toxicology. The authors review the landmarks in the development of stereochemistry and stereopharmacology. Present-day IUPAC terminology is discussed; general issues of stereoisomerism are considered including separation of racemic mixtures and asymmetric synthesis of isomers, methods of quantifying the isomers of a drug in biological material. The authors put special emphasis on general problems of the influence of stereoisomerism on pharmacological and adverse effects of drugs. A classification of drugs based on stereochemical properties of their isomers is proposed. Possibilities of interaction of stereoisomers in racemic mixtures are discussed. A considerable portion of the book is devoted to pharmacological action of the main groups of drugs whose structure includes asymmetric atoms (that is, drugs with several isomers). Detailed attention is paid to advisability of developing single isomer drugs and to the specifics of their study at the stage of preclinical and clinical trials.