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Department of Pharmacy & Pharmacology, Unit Catalogue 2008/09


PA20242 Drug metabolism, pharmacokinetics, natural products and analysis

Credits: 12
Level: Intermediate
Academic Year
Assessment: CW 10%, EX 90%
Requisites:
Aims: To develop the student's understanding of drug metabolism at a molecular level, to introduce more advanced concepts in pharmacokinetics in order to explain, interpret, and contrast medicines and their pharmacokinetic data, to develop the student's understanding of biosynthetic sources of pharmaceutical materials and introduce a biosynthetic approach to natural products, with all aspects underpinned by analysis; to undertake an analytical mini-project.
Learning Outcomes:
After completion of this unit the student should be able to: demonstrate an outline understanding of drug metabolism and the enzymes which cause these biotransformations, their structure-activity relationships (SAR) and their significance; examine advanced pharmacokinetic data in order to elucidate key clinical factors about medicines; demonstrate an awareness of natural sources of pharmaceutical materials and an outline understanding (at the level of chemical structures and mechanisms) of major pathways of biosynthesis; demonstrate an understanding of the value of spectroscopic data in stereochemical and conformational analysis; follow biosynthetic pathways mechanistically, understanding the limits of their knowledge; carry out and write-up an analytical mini-project.
Skills:
Practical skills (T/F)
Data handling and analysis (T/F/A)
Problem solving (T/F/A).
Content:
General introduction to drug metabolism. Definitions of the two phases of drug metabolism. The importance of enzymes as catalysts and structure-activity relationships (SAR) across drug metabolising enzymes. Examples of hydrolysis and oxidation, para-hydroxylation, epoxide hydrolase. General introduction of more advanced pharmacokinetic models and examples. The process of medicines development. Pharmacokinetics in clinical trials across Phases I to IV. Regulatory agencies. Bioavailability. Bioequivalence and generic formulations. The Biopharmaceutical Classification System. Introduction to analysis in the BP monographs, sample preparation, radioactivity, and associated calculations in metabolism, pharmacokinetics, and radioactivity. Plant and animal sources of pharmaceutical materials. Molecular aspects of biosynthetic pathways. Problem-solving workshops in stereochemical analysis using spectroscopy. Calculations of natural product concentrations and serial dilutions. Mini-project.