Learning Outcomes
The aim of this course is to act as an introduction to the specific pharmaceutical - medicinal chemistry courses, to teach the causes of pathologic conditions and general properties of drug molecules. Other aims are to present some important characteristics of drugs, such as selectivity and the role of various chemical bonds developed in drug action. An important aim is the transfer of a sound knowledge of drug metabolism and the consequences on drug action and toxicity. Also important are the issues of the pharmacodynamic and chemotherapeutic drugs as a concept, general anaesthetics, as well as the chemical and molecular aspects of drug - drug and drug - food interactions.
Skills: By the end of this course, the students should be able to:
Know the basic classification and causes of important diseases;
Know the characteristics of pharmacodynamic and chemotherapeutic drugs;
Know the characteristics of a satisfactory drug molecule, such as selectivity, potency, toxicity;
Have a good knowledge of the fate of a drug in the body, its kinetics and, most important, its metabolism, as well as the phenomenon of xenobiotic metabolism from various aspects;
Know the formation of various types of chemical bonds and the effects on the development of drug action;
Have a good knowledge of the molecular and chemical basis of drug interactions.
Course Content (Syllabus)
An introduction in chemistry of vitamins. Their classification and study of vitamins of aliphatic, alicyclic, aromatic and heterocyclic series, which include ascorbic acid, pantotenic acid, pangamic acid, choline, linetole, inositole,lipoic acid, vitamin A, D, K, PABA, dicoumarol ,rutin, nicotinic acid nicotinamide, vitamin B6, B1, B2, folic acid, biotin, B12, B13, vitamin U. All these vitamins are studied from point of view of their properties, quality and quantity evaluation as well their impact for the health and use.
Also course include a chemical introduction on drug action and xenobiotic behaviour. Impact of drugs on health and disease. Differences and similarities between food and drugs.
General characteristics of drug molecules-Xenobiotics. General anaesthetics. Chemical bonds, drug properties and drug action. Covalent, coordinated bonds, coulombic forces, hydrogen bond, van der Waals forces, lipophilic interactions.
Principles of selectivity based on differences in cytology, biochemistry and distribution.
Ways of drug loss, elements of drug absorption, distribution and excretion.
Drug metabolism. Objectives, evolution, site, chemical nature of structural changes. Oxidations, reductions, hydrolyses and other phase I biotransformations. Conjugations with glucuronic acid, glycine, sulphate, glutathione, and other phase II biotransformations. Structure and function of cytochromes P450. P450 induction and inhibition. Biodetoxication, Biotoxication. Drug metabolism and drug stereochemistry.
Molecular aspects of drug-drug and drug-food interactions. Consequences of interactions, applications in therapy, elements of drug design and development.