Syllabus
Topics of lectures definition of basic pharmacokinetic parameters, linear/nonlinear pharmacokinetics, drug dosage pharmacokinetic drug-drug interactions (DDI), role of biotransformation enzymes in pharmacokinetic DDI, examples of clinically important DDI on biotransformation enzymes role of drug transporters in pharmacokinetic DDi, examples of clinically important DDI on drug transporters preclinical experimental methods (in vitro, in vivo, in silico) used for quantification of the role biotransformation enzymes play in pharmacokinetics; their advantages and disadvantages, extrapolation of experimental results to humans, available options for testing in clinical settings. preclinical experimental methods (in vitro, in vivo, in silico) used for evaluation of drug absorption, distribution and excretion and involvement of drug transporters in these processes; their advantages and disadvantages, extrapolation of experimental results to humans, available options for testing in clinical settings. factors affecting pharmacokinetics with a focus on specific groups of patients (e.g. in children, in older people, in pregnancy) gene polymorphisms, their effect on pharmacokinetics, examples of gene mutations leading to affected pharmacokinetics
Topics for practical lessons evaluation of functional activity of selected biotransformation enzymes, testing of drug-drug interactions (inhibition) on selected cytochrome P450 isoenzymes evaluation of drug absorption in vitro, comparison of transcellular transport of hydrophilic and lipophilic drug using Caco-2 cell monolayers, evaluation of drug interaction with drug transporters (MDCKII cells) evaluation of selected cytochrome P450 isoenzyme induction in vitro using qRT-PCR technique
Annotation
Understanding pharmacokinetic principles and mechanisms of pharmacokinetic drug-drug interactions is essential for choosing effective and safe pharmacotherapy. Knowledge on pharmacokinetics and drug interactions is exploited throughout all the pharmaceutical disciplines, particularly in clinical pharmacy, hospital as well as public pharmacies and it is further reflected in the area drug research and development.
In the subject Pharmacokinetics students will (i) gain an overview of the molecular basis of pharmacokinetics, the causative mechanisms of pharmacokinetic drug-drug interactions and its clinical aspects, (ii) learn about current methods that are used to evaluate pharmacokinetic interactions and are recommended by drug regulatory agencies and (iii) will take the advantage of trying some of the crucial in vitro methods during practical laboratory lessons.