1. Participation at seminary lessons 100% . In case of absence (max. 3 times) at a seminary lesson it is necessary to present the topic in the form of seminar work next week or in the credit week. 2. To obtain at least the evaluation of mark E from average of otained points in 8 written tests.

In this subject student will obtain knowledge in biotransformation of endogenous and exogenous xenobiotics. Study subject improves the obligatory subjects Pharmacology and Toxicology in biotransformation reactions some drugs which are converted into non-toxic products eliminated by living organism.

Xenobiotics, their biotransformation, detoxification,

mechanism of biotransformation reactions,

biotransformation of endogenous xenobiotics,

sources of free radicals in living organism and their function,

oxidative stress,

factors influencing the biotransformation of xenobiotíics,

regulation of biotransformation of xenobiotics,

biotransformation of antibiotics,

biotransformation of sulfonamides,

biotransformation of nitrofurans,

biotransformation of chinolones.

1. Organization of study subject Xenobiochemistry.

Evaluation of students.

Xenobiotics, their biotransformation, detoxification.

Endogenous and exogenous xenobiotics.

Two phases of biotransforamation reactions.

2. Mechanism of biotransformation reactions.

Mechanism of first phase reactions (oxygenation, hydoxylation, reduction, dealkylation, desulfuration, hydrolysis).

Mechanism of second phase reactions (conjugation enzyme systems).

3. Biotransformation of endogenous xenobiotics.

Biotransformation of bile pigments.

Biotransformation of steroid hormones.

4. Sources of free radicals in living organism and their functions.

Free radicals, reactive oxygen species, reactive nitrogen species, their physiological function.

Antioxidants, pro-oxidants.

5. Oxidative stress.

Antioxidative enzyme system.

Antioxidative non-enzyme system.

6. Factors influencing of biotransformation of xenobiotics.

Animal species, genetics, age, diseases.

Diet, chemical exposure factors.

7. Regulation of biotransformation of xenobiotics.

Enzyme induction.

Inhibition of biotransformation reactions.

Chemical reactivity, bioactivation, new drug development.

Toxicity of intermediates, metabolites (alergy, cancer, cell death).

8. Biotransformation of penicilin and cephalosporin antibiotics.

9. Biotransformation of tetracycline antibiotics.

10. Biotransformation of macrolide antibiotics.

11. Biotransformation of sulphonamides, nitrofurans.

12. Biotransformation of chinolones.

13. Presentation of seminar works.

Student evaluation, credits.

Harvey, R.A., Ferrier, D.R.: Lippincott´s Illustrated Reviews: Biochemistry. 5th Edition. Baltimore, Lippincott Wiliams and Wilkins, 2011, 521pp. Nelson, D. L., Cox, M. M.: Lehninger Principles of Biochemistry. 4th Edition. New York : W. H. Freeman and Company, 2005. 1119 pp.

Content prerequisite:

Biochemistry

Continuous assessment:

continuous tests (on seminary lessons from actually tought topics)

Conditions for completion of course:

1. Participation at seminary lessons 100% . In case of absence (max. 3 times) at a seminary lesson it is necessary to present the topic in the form of seminar work next week or in the credit week. 2. To obtain at least the evaluation of mark E from average of otained points in 8 written tests.

Final assessment:

written exam