TitleMedicinal Chemistry and Biopharmaceutics for PCS
CodePY341, PY342, PY343
Level6
Credit rating40 credits
Pre-requisitesMedicine design and analysis; Pharmaceutical microbiology, immunology and biotechnology
TypeExtensive
Aims
- To consider the chemical basis of drug-receptor interactions.
- To consider approaches to rational drug design and development.
- To relate chemical structure and associated physicochemical properties to the stability, absorption, distribution, metabolism and excretion of drugs.
- To relate drug molecule chemistry to the formulation, uniformity, bioavailability and stability of pharmaceutical products.
- To consider the preformulation requirements of new drug entities.
- The objectives of formulation to meet the quality, efficacy and safety requirements for licensing and manufacture.
- The specific formulation requirements for tablets with particular reference to the way in which these affect preparation and production.
- The requirements for quality assurance and GMP in manufacturing environments.
- To examine the sources, active constituents and problems associated with natural products used as medicines.
Learning outcomesOn completion of this module the student should be able to critically review, consolidate and extend a systematic and coherent body of knowledge evidenced by the ability to:
- demonstrate an understanding of the principles underlying drug-target interactions, including bonding, complementarity and the optical and geometrical specificity of isomers.
- discuss approaches to rational drug design and development.
- show understanding of the structural aspects of:
drug-enzyme and drug-receptor interactions.
structural modification in drug development.
biopharmaceutics with respect to the physico-chemical parameters of drugs.
- show understanding of the general mechanisms of drug metabolism and transfer and apply the knowledge to recognise sites on drug molecules at which metabolic processes may occur and be able to suggest possible metabolites that may be produced and consequences of these processes on the activity of the drug.
- formulate and prepare/manufacture a range of medicinal products in a safe, controlled and reliable manner exercising significant judgement in a range of situations and accepting accountability for determining and achieving personal and/or group outcomes.
- critically assess the importance of the properties of active compounds and excipients in conjunction with the design and formulation of medicinal products and appreciate the in vivo fate of the formulated product and factors affecting this.
- relate the above to medicines prepared from crude natural sources (herbal medicines).
ContentThe content of this unit of study can be viewed as falling into three themes.
Drug discovery and development (normally 48 hours)
The drug discovery process: lead activity, structural modification.
Sources of lead-activity molecules: natural products and secondary metabolites, physiological molecules, combinatorial libraries. Structural types from diverse sources.
Chemical features of drug-receptor and drug-enzyme interactions. Molecular architecture in relation to biological activity.
Size and shape of organic molecules and functional groups, geometric and optical isomerism, isosterism and bioisosterism and their application in drug design and importance for biological activity.
Ionisation and pKa of drug molecules, the Hammett substituent constant and reaction constant and the significance of these. The steric parameter, the partition coefficients and liposolubility of molecules, the Hansch substituent constant and fragmentation constants, the application of these parameters in Hansch analysis and drug design.
The application of a knowledge of physicochemical principles to the adsorption and distribution of drug molecules. An elementary treatment of the chemistry of drug metabolism in relation to the activity, toxicity and elimination of drugs. The implications of these concepts to drug development.
The relationships between molecular structure and biological activity for various classes of therapeutic agents including analgesics, histamine receptor antagonists, beta-adrenoceptor antagonists, Angiotensin converting enzyme inhibitors, Angiotensin II receptor antagonists, 5-HT receptor agonists.
Pharmaceutical formulation and its impact on the therapeutic action of medicines (normally 48 hours)
An introduction to the techniques used in the formulation of medicinal products in order to meet specific design criteria.
Factors affecting the bioavailability of formulated products.
Preformulation procedures for new drug entities.
Pharmaceutical and chemical methods for controlling the duration and intensity of drug action, prodrugs, targeting.
An examination of the causes and mechanisms of drug and product deterioration.
The methods used for stability testing and techniques available for minimising stability problems.
Formulation techniques for pharmaceutical products; the role of adjuvants in specific dosage forms.
Natural products as medicines (normally 8 hours)
Comparison with conventional pharmaceuticals. Variability, analysis and approaches to ensuring product quality and batch-to-batch consistency.
Teaching and learning Normally 52 hours of formal lectures with 52 hours of manipulative
strategieslaboratory and interpretative exercises. Formal class contact is supported by 176 hours of guided study with 120 hours of independent study and assessment.
Learning supportCore text books
Wilson and Gisvold’s Textbook of Organic Medicinal and Pharmaceutical Chemistry, 11th edition.
John H. Block and John M. Beale. Lippincott, Williams and Wilkins, Baltimore, 2004. ISBN 0-7817-3481-9
An Introduction to Medicinal Chemistry, 3rd Edition. Graham L. Patrick, Oxford University Press, Oxford 2005. ISBN 0-19-927500-9
Fundamentals of Medicinal Chemistry. Gareth Thomas, John Wiley & Sons, Chichester, 2003. ISBN 0-470-84307-1
Medicinal Natural Products. A Biosynthetic Approach, 2nd edition.
Paul M Dewick, John Wiley and Sons, Chichester, 2002. ISBN 0-471-49640-5 (hbk) ISBN 0-471-49641-3 (pbk)
Pharmaceutics: The Science of Dosage Form Design, M.E.Aulton, 2nd edition, Churchill Livingstone, 2002. ISBN 0 433 05517 3
Martin's physical pharmacy pharmaceutical sciences, P.J Sinko,; A.N. Martin, Williams and Wilkins, 5th Edition, 2005. ISBN13: 9780781750271
The Theory and Practice of Industrial Pharmacy, 3rd Ed, L. Lachman, H. A.Lieberman and J. Kanig, Lea and Febiger, 1986.
Remmington: The Science and Practice of Pharmacy, 20th Ed., A. Gennaro et al., Lippincott, Williams and Wilkins, 2002.
Secondary textbooks
Human drug metabolism – an introduction. M.D.Coleman, John Wiley, Chichester, 2005, 978-0-470-86353-6
Smith and Williams’ Introduction to the Principles of Drug Design and Action, 3rd edition. Ed H J Smith, Harwood Academic Publishers, Amsterdam, 1998. ISBN 90-5702-205-2
Trease & Evans' Pharmacognosy, Evans, W C, 14th Ed, Saunders, 1996, ISBN 0-7020-1899-6
Medicinal Chemistry - A Biochemical Approach, T. Nogrady, D.F. Weaver,3rd Ed, Oxford University Press, 2005, ISBN 9780195104561
Pharmacognosy and Pharmacobiotechnology. J.E.Robbers, M.K. Speedie, V.E.Tyler. Williams and Wilkins, Baltimore, 1996, ISBN 0-683-08500-X
CAL packages
A number of CAL packages are available for use within this module. Appropriate ones will be identified by members of staff at the time of delivery of their lectures.
AssessmentThis unit of study will be assessed by means of:
PY341 Coursework (20 credits).
PY342 MCQ Examination (10 credits).
PY343 Examination (10 credits): end of module examination with short answer and essay questions.
Brief description of moduleThis integrated module covers issues of drug discovery and development, chemical aspects of drug action, and the consequences of product formulation on the effectiveness of drugs.
Area Examination Board MPharm Pharmaceutical Sciences
Module authorsDrs G W J Olivier, R W Daisley, A C Hunter, S M Moghimi, K J Rutt, D K Sarker, M H Sosabowski, Mr M J Ingram and Mrs J Langford
Semester offered1 & 2
Date of first approvalSeptember 2005
Date of approval of this
version
Version number1
Replacement for previous n/a
module
Course(s) for which module Compulsory for Pharmaceutical and Chemical Sciences
is acceptable and statusOptional for Biological Sciences
in course
School homeSchool of Pharmacy & Biomolecular Sciences
External examiner Dr J Lough