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Pharmacology

Department of Pharmacology

Pharm 271/272 Introductory Pharmacology

Introduction

Pharmacology is the basis of clinical therapeutic and thus forms a core part of the programme. In the course emphasis is laid on basic mechanisms of drug action in relation both to drug-receptor interaction and to the operation of physiological and biochemical systems. The section also provides an introduction to the pharmacology of neuro effector systems.

Objectives

By the end of the course, students should:

  1. Attain a core knowledge in basic pharmacology and so laid a secure foundation in the principles of drug action to support courses in clinical pharmacy and other course in pharmacy.
  2. Be able a broad knowledge of modern pharmacology, from the molecular basis of receptors and cell signaling, to the effect of drugs on whole body systems
  3. Identify the major classes of drug receptors and sites of drug action within the body;

i.)  Pharmacological mechanisms by which drugs of various classes may alter biochemical, physiological or pathophysiological parameters to produce theraoeutic or unwanted effects.

Course Content

Principles of Drug Action

  • Introduction to pharmacology
  • Targets of Drug-Action-receptors, enzymes, ion channel, carrier systems
  • Action via specific receptors.
  • Relationship between binding and response. Forces involved in drug-receptor interaction.
  • Affinity, Efficacy. Agonist. Antagonists.
  • Structure- activity relations (receptor identification).
  • Competitive anatagonism. Quantitative methods for assessing atagonist binding from dose-ratio to produce a given level of effects. Schild plot.
  • Radioligand binding. Specific and non-specific binding. Displacement.
  • Non-competitive antagonism. Reversible v. irreversible antagonist.
  • Spare receptors, partial agonists. Cooperativity (Hill plot).Functional or “physiological” antagonism.
  • Receptor superfamilies
  • Receptor mechanisms. Intracellular receptors regulating gene expression. Ligand-regulated transmemberane tyrosine kinases. Ligand gated ion channels. G-protein coupled receptors.
  • Family of channels gated by accetycholine, -amino butyric acid (GABA), glycine on 5th .
  • Family of voltage gated ion channels, sodium, calcium and potassium. Introduction to selective blockers. Local anaesthetics.
  • G-protein coupled receptors. Basic structure. Pertussis toxin, cholera toxin. Activation and inhibition of adenylyl cyclase. Modulation of ion channels. Activation of phospholipase C. diacylcylcerol, IP3, protein kinase C.
  • Intracellular receptors mediating gene expression. Glucocorticoids, Mineralocorticoids, Oestrogens, Progestogens.
  • Ligand regulated transmembrane kinases. Insulin, epidermal growth factor, platelet derived growth factor.
  • Example of integrated action. Drugs affecting insulin release.
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