2011 Pharm 3170 Accel Week 2 Part 1 BB With Sound

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  • 8/3/2019 2011 Pharm 3170 Accel Week 2 Part 1 BB With Sound

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    Pharmacology 3170 Accelerated

    Week Two Peripheral Nervous System

    Part 1 with sound

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    Basic Principles of

    Neuropharmacology

    Multiple receptor types and selectivity of

    drug actions

    An approach to learning about peripheralnervous 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

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    Review of

    Neuropharmacology

    Figure 12-01. 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.)

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    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 cellAnother neuron, muscle cell, or cell within a secretory

    gland

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    Basic Mechanisms of

    Neuropharmacologic Agents

    Sites of action: axons versus synapsesAxonal conduction

    Synaptic transmission

    Receptors

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    Basic Mechanisms

    Steps insynaptic

    transmission:

    1.Transmittersynthesis

    2.Transmitter

    storage

    3.Transmitter

    release

    4.

    Receptorbinding

    5.Termination

    oftransmission

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    Steps in synaptic transmission

    Figure 12-02. Steps in synaptic transmission.Step 1, Synthesis of transmitter (T) from precursor molecules (Q, R, and S). Step 2, Storage of transmitter in vesicles. Step 3, Release of

    transmitter: In response to an action potential, vesicles fuse with the terminal membrane and discharge their contents into the synaptic gap.Step 4,Action at receptor: Transmitter binds (reversibly) to its receptor on the postsynaptic cell, causing a response in that cell. Step 5,

    Termination of transmission: Transmitter dissociates from its receptor and is then removed from the synaptic gap by (a) reuptake into the nerve

    terminal, (b) enzymatic degradation, or (c) diffusion away from the gap.

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    Basic Mechanisms of

    Neuropharmacologic Drugs

    Effects of drugs on the steps of synaptic

    transmission:

    1. Transmitter synthesis

    a) Increase transmitter synthesisb) Decrease transmitter synthesis

    c) Cause the synthesis of transmitter

    molecules

    2. Transmitter storage

    a) Cause receptor activation to decrease

    3. Transmitter release

    a) Promote or inhibit release

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    Basic Mechanisms of

    Neuropharmacologic Drugs, Contd

    4. Effects of drugs on the steps of synaptic

    transmission:

    5. Receptor bindinga) Cause activationb) Block activation

    c) Enhance activation

    6. Termination of transmissiona) Block transmitter reuptake

    b) Inhibit transmitter degradation

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    Multiple Receptor Types and

    Selectivity of Drug Action

    SelectivityMost desirable quality a drug can have

    Able to alter a disease process while leaving

    other physiologic processes largely unaffected

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    Mort and Merv

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    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