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Chapter 12 Basic Principles of Neuropharmacology Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. Basic Principles of Neuropharmacology Neuropharmacology can be defined as “the study of drugs that alter processes controlled by the nervous system.” These drugs are used to treat conditions ranging from depression to epilepsy to hypertension to asthma. Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 2 Basic Principles of Neuropharmacology How neurons regulate physiologic processes Basic mechanisms by which neuropharmacologic agents act: Sites of action: axons vs. synapses Steps in synaptic transmission Effects of drugs on the steps of synaptic transmission Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 3 Fig. 12-1. How neurons regulate other cells. There are two basic steps in the process by which neurons elicit responses from other cells: (1) axonal conduction and (2) synaptic transmission. (T = neurotransmitter.) Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 4 Basic Mechanisms of Neuropharmacologic Agents Sites of action: axons vs. synapses Axonal conduction Synaptic transmission Receptors Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 5 How Neurons Regulate Physiologic Processes in Two Basic Steps Axonal conduction Action potential down the axon Synaptic transmission Information carried across the neuron gap and the postsynaptic cell Postsynaptic cell • Another neuron, muscle cell, or cell within a secretory gland Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 6 Basic Mechanisms: Steps in Synaptic Transmission 1. Transmitter synthesis 5. Termination of transmission 2. Transmitter storage Steps in synaptic transmission: 4. Receptor binding 3. Transmitter release Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 7 Fig. 12-2. Steps in synaptic transmission. Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 8 Basic Mechanisms of Neuropharmacologic Agents Effects of drugs on the steps of synaptic transmission Transmitter synthesis Transmitter storage Increase transmitter synthesis Decrease transmitter synthesis Cause synthesis of transmitter molecules Cause receptor activation to decrease Transmitter release Promote or inhibit release Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 9 Basic Mechanisms of Neuropharmacologic Agents Effects of drugs on the steps of synaptic transmission Receptor binding Cause activation Block activation Enhance activation Termination of transmission Block transmitter reuptake Inhibit transmitter degradation Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 10 Multiple Receptor Types and Selectivity of Drug Action Selectivity Most desirable quality a drug can have Able to alter a disease process while leaving other physiologic processes largely unaffected Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 11 Meet Mort and Merv Fig. 12-3. Multiple drug receptors and selective drug action. Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 12 An Approach to Learning About Peripheral Nervous System Drugs Three types of information needed Type (or types) of receptor through which the drug acts (alpha1, alpha2, beta1, etc) Normal response to activation of those receptors (agonist versus antagonist) What the drug in question does to receptor function Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 13 Basic Principles of Neuropharmacology An approach to learning about peripheral nervous system drugs Knowing the receptors that the drug affects Knowing the normal responses to activation of those receptors Knowing whether the drug in question increases or decreases receptor activation Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc. 14