| CODE | PHR2026 | ||||||||||||||||
| TITLE | Medicinal Chemistry 1 | ||||||||||||||||
| UM LEVEL | 02 - Years 2, 3 in Modular Undergraduate Course | ||||||||||||||||
| MQF LEVEL | 5 | ||||||||||||||||
| ECTS CREDITS | 6 | ||||||||||||||||
| DEPARTMENT | Pharmacy | ||||||||||||||||
| DESCRIPTION | - Review of organic functional groups with examples of biological and pharmaceutical importance. - The effect of geometric isomerism and stereochemistry, chirality on drug formulation, disposition, activity and toxicity. - The correlation of structure to biological activity. - Photosensitising drugs. - Rational drug design based on ionisation studies of H2-antagonists. - Bioisosterism. - The Pro-drug concept and rationale. - Historical development and applications of QSAR: methods of drug design, computer aided drug design. - Drug profile: Introduction to Structure Activity Relationship (SAR) studies of various drug classes, through formal lectures, group and individual research, presentation and discussion. Drug classes include: Sympathomimetics and anticholinergic drugs; beta-lactam antibiotics and their subclasses. - The pro-drug approach to antibiotics. - Ligand based drug design. - Pharmacophore based drug design. - X-ray Crystallography. - Reading and understanding the information contained in Protein Data Bank files. - Practical aspects: Calibration of glassware. - Chemical analysis in water for injections: analysis of sulphates, pH testing, conductivity testing. - Moisture content in grains: comparison of two different methods. - Analysis of active content in Calcium lactate tablets. - Determination of shelf life. - Methodology researching. - Stability testing. - Application of kinetic principles of pharmacy: shelf-life and the Q10 method. - Stability concerns in dosage forms: physical, chemical, therapeutical and microbiological changes in a dosage form, hydrolysis and oxidation as the major reactions providing stability concerns. - Methods for determining the stability of a dosage form: isothermal and nonisothermal accelerated stability studies, handling and plotting of data from an isothermal accelerated stability study to extract the shelf-life of a product. Study-unit Aims: - To present an introduction to medicinal chemistry by reviewing the properties of the major organic functional groups and their influences on the water and lipid solubility; in vitro and in vivo stability; and on the molecular geometry, biological activity of molecules. - To proceed to understand the various principles applied to drug design with emphasis on qualitative and quantitative structure-activity and structure property relationships as exemplified by specific drugs, classified pharmacologically and/or chemically. Emphasis will also be made on the importance of pharmaceutical nomenclature. - To introduce basic principles in chemical analysis, in particular with reference to analysis of foods and pharmaceuticals. - To introduce the student to the concept of kinetics as representing a time-dependent change in a parameter. The student will become familiar with the basic concepts of kinetic processes, and the various factors that can affect the kinetics of a particular process. - To demonstrate the applications of kinetics in pharmaceutics, particularly the concept of stability of dosage forms and the methods used to monitor stability. Learning Outcomes: 1. Knowledge & Understanding: By the end of the study-unit the student will be able to: - understand principles of geometric isomerism; - understand the rationale behind the pro-drug approach; - understand the difference between ligand and pharmacophore based approaches to drug design; - understand the theory behind X-Ray crystallography; - understand how X-Ray crystallographic data is stored within the Protein Data Bank; - acquire a clear understanding of those factor that influence the kinetics of a reaction; - comprehend the influence these factors have when formulating a drug delivery system with that particular format. 2. Skills: By the end of the study-unit the student will be able to: - appreciate the functional groups most important in eliciting biological activity; - correlate notions of isomerism and stereochemistry with biological activity; - read Protein Data Bank Files and generate computational representations of their contents; - identify the characteristics of those factors which influence the kinetics of drug delivery systems; - acquire mathematical skills needed in calculating the kinetic factors being sought. Main Text/s and any supplementary readings: - Lemke TL. Review of organic Functional Groups: Introduction to Medicinal Organic Chemistry. USA:Williams & Wilkins. 1992. ISBN 0-7817-4381-8. - Foye WO. Principles of Medicinal Chemistry. USA: Lippincott, Williams & Wilkins 2008, ISBN 978-0-7817-6870-5. - Smith HJ and Williams H. Eds. Introduction to the Principles of Drug Design, UK: Harwood Academic Publishers. 2005. ISBN 90-5702-037-8. - Adrien Albert. Selective Toxicity: The Physico-Chemical Basis of Therapy. USA: Springer. 1985. ISBN 9870-4122-6020-9. - Souidijn W. The Role of Medicinal Chemistry in Drug Research, Pharmaceutische Weekblad, Scientific Edition 1991; 13(4): 161-6. - Burger’s Medicinal Chemistry & Drug Discovery. USA: John Wiley and Sons, ISBN 9780-4712-6694-5. - The British Pharmacopoeia Vols I & II. The Stationery Office. - Ansel, H., Allen, L., Popovich, N. Pharmaceutical Dosage Forms and Drug Delivery Systems. 1999. Williams & Wilkins. (7th edition). - Sinko PJ. Martin's physical pharmacy and pharmaceutical sciences. USA: Lippincott Williams and Wilkins. 2006 ISBN 978 0 7817 5027. |
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| RULES/CONDITIONS | Before TAKING THIS UNIT YOU MUST TAKE PHR1027 | ||||||||||||||||
| ADDITIONAL NOTES | Please note that a pass in the Practical component is obligatory for an overall pass mark to be awarded. | ||||||||||||||||
| STUDY-UNIT TYPE | Lectures, Practical and Tutorials | ||||||||||||||||
| METHOD OF ASSESSMENT |
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| LECTURER/S | Nicolette Sammut Bartolo Claire Shoemake |
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The University makes every effort to ensure that the published Courses Plans, Programmes of Study and Study-Unit information are complete and up-to-date at the time of publication. The University reserves the right to make changes in case errors are detected after publication.
The availability of optional units may be subject to timetabling constraints. Units not attracting a sufficient number of registrations may be withdrawn without notice. It should be noted that all the information in the description above applies to study-units available during the academic year 2023/4. It may be subject to change in subsequent years. |
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