Xenobiochemistry

Xenobiochemistry studies metabolic conversion of xenobiotics, especially drugs and environmental contaminants. Xenobiochemistry explains causes of pharmacological and toxicological consequences of presence of xenobiotics in living organism. Simultaneously creates sciential basis for qualified activity of pharmacists and bioanalytics in the field of laboratory monitoring of drug levels.

Syllabus

  • Introduction , history, overview – definition of xenobiochemistry, explanation of necessity of biotransformation’s enzymes for organisms, fate of xenobiotics in organism, distribution of xenobiotic-biotransforming enzymes
  • Experimental approaches to the study of metabolism – techniques for studying metabolic processes from whole organisms to cultured cells and organelles isolated by ultracentrifugation
  • Cytochrome P450s – chemical structure of P450´s, nomenclature, significance of drug oxidative reactions, mechanisms of catalytic activity, substrate specificity, the multiplicity of P450
  • Flavin-containing monooxygenases (FMO) and other oxidative enzymes – catalytic activity, substrate specificity, multiplicity, examples, classification
  • Reductases – major reducing enzymes, nomenclature, superfamilies classification, reductive metabolic pathways
  • Conjugation pathways – importance for organism, classification, mechanisms, glucuronidation, sulfation, acetylation, methylation, conjugation with glutathione, conjugation with amino acids
  • Induction of drug metabolism – molecular mechanism of induction of multiple forms of P450 , role of other oxidative enzymes in induction, induction of extrahepatic drug metabolism, biological significance of induction
  • Inhibition of drug metabolism – molecular mechanism of inhibition, drugs and xenobiotics inhibiting drug metabolism, biological significance
  • Factors affecting drug metabolism – introduction, internal and external factors
  • Chiral aspects of drug metabolism – history, fate of xenobiotics in organism, stereochemistry of metabolism, utilization of stereochemistry in drug research….., examples
  • Drug metabolizing enzymes in human placenta, fetuses and newborns – expression an inducibility of biotransformation enzymes in human fetal placenta and liver, neonatal hepatic drug elimination, pediatric significance
  • Pharmacological and toxicological aspects of drug metabolism – activation and deactivation of drugs, contribution of drug metabolizing enzymes to mutagenesis, carcinogenesis, teratogenesis….., examples
  • The clinical relevance of drug metabolism – effect of different activity of biotransformation enzymes under physiological and pathological state in man. Examples. Genetic polymorphism in human drug metabolism
  • Summary

Literature

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