PHARMACOLOGY OF CHEMICAL MEDIATORS

SHE Level 3
SCQF Credit Points 20.00
ECTS Credit Points 10.00
Module Code M3B223437
Module Leader Yvonne Dempsie
School School of Health and Life Sciences
Subject Biological and Biomedical Sciences
Trimester
  • B (January start)

Pre-Requisite Knowledge

Fundamentals of Pharmacology, Physiology 1 & 2

Summary of Content

This module provides an in-depth understanding of the basic principles of drug action and applies this to the analysis of drug receptor interactions. The content highlights the actions of selected endogenous chemical mediators as a framework for studying drug actions. A laboratory programme enhances and underpins lecture material and provides experience of practical pharmacology with emphasis on collection, analysis and interpretation of pharmacological experimental data.

Syllabus

Types of chemical mediators. Drug targets: Enzymes, transporters, ion channels, receptors. Quantitative aspects of drug receptor interaction. Affinity, efficacy, agonist, partial agonist, inverse agonist. Calculation of agonist affinity (K D ), relationship between occupancy and response. Relationship between concentration/dose- response relationship and EC 50 . Types of antagonism, antagonist affinity, fractional occupancy, Schild Equation, Schild plot (pK B /pA 2 ). Receptors and receptor superfamilies- classification :- Ionotropic receptors, G-coupled receptors (metabotropic), examples with transduction pathways for Gs, Gi Gq, therapeutic drugs. Kinase-linked receptors including (structure, transduction, therapeutic examples):- Receptor tyrosine kinases, Cytokine receptors, Serine/threonine kinases, Guanylyl cyclase-linked receptors. Nuclear receptors classes. Ion channels as drug targets , Ligand-gated, voltage-gated (Na + , Ca 2+ , K + ), calcium-release, store-operated. Ion channel structure, ion selectivity, voltage sensor and gating mechanisms and pharmacology. Pharmacology of cellular mechanisms: excitation, contraction and secretion. Mechanisms of calcium regulation, ion channels and membrane potential, voltage-gated Na + channel, cardiac action potentials, inactivation peptide and refractory period, drugs affecting the voltage-gated Na + channel and use-dependence. Potassium channels:- Voltage-gated, including HERG and LQT channels, role in cardiac dysrhythmias. Inwardly rectifying K ATP, therapeutic example in pancreatic ?-cells. Ryanodine receptor. Mediators of the autonomic nervous system/ motor nerves. Drugs affecting noradrenergic transmission. Adrenoceptors: subtypes and transduction mechanisms. Drugs acting on adrenoceptors. Drugs affecting cholinergic transmission. Cholinoceptors: subtypes and transduction mechanisms. Drugs acting on cholinoceptors. Pharmacology of nitric oxide. Receptors and pharmacology of 5-hydroxytryptamine. Receptors and pharmacology of histamine. Amino acid neurotransmitters: excitatory amino acids; inhibitory amino acids. Inflammation: the acute inflammatory reaction; inflammatory mediators; anti-inflammatory drugs; specific immunological response. Laboratories The aim of the laboratory programme is to enhance and underpin the lectures and to give the student experience of practical pharmacology. The practical classes will allow the student to become familiar with techniques for the analysis of drug-receptor interactions and will provide experience of collection, analysis and interpretation of pharmacological experimental data. Techniques for studying mechanisms of drug action will include measurement of functional responses in a variety of isolated smooth muscle preparations, including stimulated preparations to investigate effects on endogenous mediators and radio-ligand binding measurements in membrane preparations.

Learning Outcomes

On successful completion of this module, the student should be able to:a) understand the roles of chemical mediators and receptors in cell communicationb) understand the mechanisms involved in activation of the four major receptor classesc) understand the actions of therapeutic drugs at the four major receptor classes d) apply the basic principles of drug action to the analysis of drug receptor interactions.e) appreciate how selective manipulation of the production or effects of endogenous chemical mediators can lead to the development of therapeutic agents.f) analyse and interpret data from pharmacological experiments.

Teaching / Learning Strategy

A variety of teaching and learning modes will be used including lectures, tutorials, practical laboratory sessions, and GCU-learn. The module lecture material utilizes a convergent teaching approach in order to ensure that each of the different student groups taking the module quickly achieves the required background. The emphasis however, in both lectures and tutorials, will be on participative modes of learning and this together with evidence-based learning gleaned through the practical laboratory programme aims to promote a divergent thought process . Analytical skills that are an inherent component of the practical work are further developed in data analysis component of the module. The subject areas covered in the module provide the student with an indepth understanding, which together with analytical and communications skills develops broad and deeper learning , promoting long-term retention of knowledge and students who are confident in their chosen field . The lecture material, laboratory work and data analysis is challenging, relative to the real world, requires substantial self-input and is engaging and generative producing engaged learners that have developed strategic learning skills and the ability to transfer these skills to solve pharmacological problems creatively. The module therefore promotes knowledgeable, confident and engaged learners who are able to make professional judgement and take responsibility in order to solve real world scientific and medical problems .

Indicative Reading

i ) Essential texts Rang and Dale's Pharmacology. Rang, H.P., Dale, M.M. & Ritter, J.M. & Flower, R.J. Henderson, G. 7th Edition. Churchill Livingstone. Page,C., Curtis,M., Sutter,M., Walker,M. and Hoffman,B. 2006 Integrated Pharmacology, 3rd Edition. Mosby. Spina D. 2008 Medical Pharmacology Mosby Elsevier Robbins, S.L., et al.. (2003) Basic Pathology, 7 th ed. Saunders.

Transferrable Skills

The students' transferable skills should be extended in the following areas: -360 1. Knowledge of pharmacology. -360 2. The analysis and interpretation of scientific data (laboratory work and data analysis). 3. Communication by the written and spoken word (poster presentation). -360 4. The student will also be able to acquire a number of transferable skills such as: - use of graph drawing software; - laboratory skills, safe laboratory practice, logical planning and undertaking experiments; - independent study skills; - teamwork

Module Structure

Activity Total Hours
Tutorials (FT) 6.00
Practicals (FT) 18.00
Independent Learning (FT) 134.00
Assessment (FT) 20.00
Lectures (FT) 22.00

Assessment Methods

Component Duration Weighting Threshold Description
Exam (Exams Office) 3.00 50.00 35% Unseen written exam (MCQ + Essay questions)
Coursework 1 3.00 20.00 35% Data Analysis/group poster presentation or oral presentation
Coursework 2 n/a 30.00 35% Laboratory Reports