Department of Pharmacy & Pharmacology, Unit Catalogue 2009/10 |
PA40280: Quantitative pharmacology and the development of modern medicines |
 Credits:
| 6 |
| Level:
| Masters |
| Period: | Semester 2 |
| Assessment:
| CW20EX80 |
| Supplementary Assessment: | Supplementary assessment information not currently available (this will be added shortly) |
| Requisites:
| |
| Description: | Aims: To provide an in depth understanding of how pharmacological theory is applied to the development of modern medicines in the industrial setting. Learning Outcomes: After completing this unit, students should be able to: * Demonstrate understanding of pharmacological principles used in the in vitro characterisation of agonists and antagonists; * Discuss the pros and cons of such assays in drug discovery; * Demonstrate knowledge of how the above principles have been used in the development of medicines: inhaled beta 2 adrenoceptor agonists for asthma and oral angiotensin II inhibitors for hypertension; * Demonstrate an appreciation of how the discovery of such drugs extended our knowledge of how molecules interact with receptors and how this influenced receptor theory and subsequent drug design. Skills: Communication : Problem solving: Decision making : All these skills are taught, facilitated and assessed. Content: This unit will be delivered via a blend of web-based learning, using Moodle, and face-to-face seminars. Several drug examples will be used to illustrate how pharmacology translates into the practice of discovering medicines: * Assumptions when conducting assays * Assays used in assessing agonist and antagonist pharmacology - pros and cons * Using agonists and antagonists in receptor classification * How do agonists and antagonists achieve receptor selectivity * How many receptors do you need to occupy to get agonist and antagonist effects in vivo * Design principles to achieve agonists with a long duration of action (example will be salmeterol) * Design principles to achieve antagonists with a long duration of action (example will be tiotropium and losartan-candesartan) * How the discovery of salbutamol and salmeterol uncovered new mechanisms to activate the beta 2 adrenoceptor * How the recently described structure of the beta 2 adrenoceptor can aid drug design * How the discovery of losartan-candesartan aided the concept that duration of effect in vivo can be controlled by receptor kinetics which can be independent of pharmacokinetics. |