The aim and outcome of this course are the comprehension of the universally recognised notion that the study of xenobiotic metabolism is one of the milestones for the safe and efficient use of drugs, as well as of the numerous chemical substances coming in contact with the organism, such as food and cosmetic additives, agrochemicals, environmental pollutants. This knowledge contributes to the development of better drugs, since it constitutes one of the principal approaches to the Rational Drug Design. Further aim is the acquisition of knowledge for a better comprehension of biotransformations of numerous chemical compounds, synthetic or natural, to which the organism is continously exposed, through nutrition, medicins, environmental pollution. The recent great progress of science in analysing the mechanisms developed by the organism, so that lipophilic, potentially toxic compounds are transformed to more hydrophilic, thus easily eliminated metabolites (biodetoxication)is explained. It is stresses and explained to the students that biotransformation is not always beneficial for the organism, since many metabolites are very active, capable of covalently bonding to critical cell macromolecules, leadind to toxicity. The possibility for new drug development through the study of their metabolism is stressed. The new molecules could acquire the expected activity, target the desired site, be safe and selective. Furthermore, the knowledge of the molecular mechanisms of interactions (pharmaceutic, pharmacokinetic and pharmacodynamic) aims to the development of safer drugs, control of undesired interactions, and effective drug treatment. Finally, a purpose of this course is to stress the importance of molecular mechanisms of food-drug interactions.
Course Content (Syllabus)
Rekka E., Kourounakis P.N.: The following topics are analysed in relation to cytochrome P450 (Rekka E.) or other drug metabolizing systems (Kourounakis P.N.):
a) Fate of drugs in the organism (absorption, distribution, metabolism, excretion) - routes of elimination.
b) Chemical mechanisms followed in xenobiotic biotransformation. Purpose, Phases, Chemistry - Biochemistry - Molecular Biology, Enzyme inducers and inhibitors - Biodetoxication, Biotoxication.
c) Specific drug groups (prodrugs, soft drugs, hard drugs, chemical delivery systems).
d) Molecular aspects of drug interactions.
Course Bibliography (Eudoxus)
1) Σημειώσεις (Ε. Α. Ρέκκα) όπου υποδεικνύεται επιλεγμένη διεθνής βιβλιογραφία με τη σύσταση προς τους φοιτητές να την χρησιμοποιούν ως σημείο έναρξης περαιτέρω ενημέρωσης.
2) Σημειώσεις (Π.Ν. Κουρουνάκης, Ε.Α. Ρέκκα), κεφάλαια από ανάλογα βιβλία της διεθνούς βιβλιογραφίας, υποδεικνύονται οι κατάλληλες πηγές για ενημέρωση