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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