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270193 VO Pharmaceutical and solution chemistry of (metallo)drugs (2017S)

1.50 ECTS (1.00 SWS), SPL 27 - Chemie

Details

Language: English

Examination dates

Lecturers

Classes

13.6. 14-16 Seminarraum 4
14.6. 11-13 Seminarraum 4
20.6. 14-16 Seminarraum 4
21.6. 11-13 Seminarraum 4
22.6. 14-16 Seminarraum 4
23.6. 12-14 Seminarraum 4
27.6. 14-16 Seminarraum 4
28.6. 10-12 Seminarraum 4
29.6. 11.30-13.30 Seminarraum 4


Information

Aims, contents and method of the course

Basic definitions of pharmaceutical (medicinal) chemistry; classification of drugs; introduction to pharmacodynamics and pharmacokinetics; therapeutic index; side effects; drug development steps; clinical trials.
Factors affecting pharmacokinetics (LADME properties: liberation, absorption, distribution, metabolism, excretion), bioavailability, accumulation, biofluids; routes of drug administration. Acid-base properties: macroconstants and microscopic proton dissociation constants. Lipophilicity, solubility and their modifications. Experimental determination of pKa and logP values. Biological pH-buffers.
Metal containing drugs (anticancer/-bacterial/-diabetic; chelate therapy). Solution stability of metal complexes, complex formation equilibrium processes. Conditional stability constants. Concentration distribution. Experimental determination of stability constants. Lipophilicity of metal complexes. Redox properties of metal complexes.
Prodrugs (metallic, nonmetallic).
Effect of interaction with biological macromolecules (proteins, DNA) on pharmacokinetics. Plasma protein binding. Experimental determination of binding sites and binding constants of protein-ligand adducts.

Assessment and permitted materials

Minimum requirements and assessment criteria

Examination topics

Reading list

Medicinal Chemistry: Principles and Practice (Ed. F.D. King), Royal Society of Chemistry, 2002.; M.T. Beck; I. Nagypál; Chemistry of Complex Equilibria, Ellis Horwood, Chichester, UK, 1990; Metallotherapeutic Drugs and Metal-based Diagnostic Agents (Eds, M. Gielen, E.R.T. Tiekink), Wiley, Chichester, 2005.

Association in the course directory

EF-1, EF-2, EF-3

Last modified: Mo 07.09.2020 15:42