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pcol > Introduction to the Pharmacology of CNS Drugs > Flashcards

Introduction to the Pharmacology of CNS Drugs Flashcards

1
Q

Nearly ALL drugs with CNS effects act on a specific receptors that modulates ______

A

transmission

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2
Q

Most drugs that act on the CNS do so by changing what?

A

ion flow through transmembrane channels of nerve cells

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3
Q

Voltage-gated sodium channel that blocks from outside

A

tetrodotoxin

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4
Q

Voltage-gated sodium channel that slows inactivation and shifts activation

A

batrachotoxin

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5
Q

Voltage-gated potassium channel that blocks small Ca-activated K channel

A

Apamin

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6
Q

Voltage-gated potassium channel that blocks big Ca-activated K channel

A

Charybdotoxin

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7
Q

Voltage-gated calcium channel that blocks N type channel

A

omega conotoxin

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8
Q

Voltage-gated calcium channel that blocks P type channel

A

Agatoxin

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9
Q

Ligand-gated nicotinic Ach receptor that is an irreversible antagonist

A

a-Bungarotoxin

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10
Q

Ligand-gated GABA receptor that blocks channel

A

Picrotoxin

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11
Q

Ligand-gated glycine receptor that is an competitive antagonist

A

Strychnine

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12
Q

Ligand-gated AMPA receptor that blocks channel

A

Philanthotoxin

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13
Q

Respond to changes in membrane potential

A

VOLTAGE GATED ION CHANNELS

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14
Q

Responsible for FAST action potentials

A

VOLTAGE GATED ION CHANNELS

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15
Q

voltage gated ion channels are concentrated on the _________ in nerve cells

A

initial segments of the axons

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16
Q

responsible for action potential
propagation

A

sodium channels

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17
Q

Cell bodies and dendrites also have voltage sensitive ion channels for _____ and _____

A

potassium and calcium

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18
Q

what are the 2 CLASSES OF NEUROTRANSMITTER RECEPTORS

A
  1. LIGAND GATED ION CHANNELS OR
    IONOTROPIC RECEPTOS
  2. METABOTROPIC RECEPTORS
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19
Q

ion gated channel that are chemically gated

A

LIGAND GATED ION CHANNELS

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20
Q

ligand gated ion channels respond to chemical _____

A

neurotransmitters (NTA)

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21
Q

SEVEN transmembrane G protein coupled

A

METABOTROPIC RECEPTORS

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22
Q

TRUE OR FALSE: in metabotropic receptors, binding does not result in the direct gating of a channel

A

true

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23
Q

Binding engages the G protein that results into production of _________ ________ that modulates the voltage gated channels

A

SECOND messengers

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24
Q

In neurons, activation of metabotropic neurotransmitter receptors often leads to the modulation of voltage-gated channels. These interactions can occur entirely within the plane of the membrane and are referred to as ________

A

membrane-delimited pathways

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25
Q

what substance interacts directly with a voltage-gated ion channel?

A

G protein

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26
Q

effect of G proteins interact with calcium channels

A

inhibit channel function (presynaptic metabotropic receptors are activated)

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27
Q

effect of G proteins interact with potassium channels

A

activate channel (slow postsynaptic inhibition)

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28
Q

Excitatory postsynaptic potentials (EPSP) ________ potential change

A

depolarize

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29
Q

EPSP are generated by opening of

A

sodium or calcium channels

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30
Q

EPSP are generated by closing of

A

potassium channels in some synapses

31
Q

Metabotropic receptors can also modulate voltage-gated channels less directly by the generation of

A

diffusible second messengers

32
Q

flow of EPSP

A

+Na, -K, +Ca

33
Q

Inhibitory postsynaptic potential (IPSP) ________ potential change

A

hyperpolarize

34
Q

IPSP are generated by opening of

A

potassium or chloride channels

35
Q

flow of IPSP

A

+K, +Cl, -Ca

36
Q

Some drugs exert their effect through _________ interaction with molecular
components of ion channels on axons

37
Q

Most drugs exert their effect mainly at the

38
Q

they reduce the amount of transmitter released from the terminals of sensory fibers

A

axoaxonic synapses

39
Q

steps at which drugs can alter synaptic transmission:
retrograde
storage
synthesis
receptor-induced increase or decrease
release
degradation
receptor for the transmitter
metabolism
reuptake
Action potential

A

(1) Action potential in presynaptic fiber;
(2) synthesis of transmitter;
(3) storage;
(4) metabolism;
(5) release;
(6) reuptake into the nerve ending or uptake into a glial cell;
(7) degradation;
(8) receptor for the transmitter;
(9) receptor-induced increase or decrease in ionic conductance;
(10) retrograde signaling

40
Q

Drugs acting on the synthesis, storage, metabolism, and release of neurotransmitters fall into the

A

presynaptic category

41
Q

This stimulant induces the release of catecholamines from adrenergic synapses

A

amphetamine

42
Q

_______ causes the release of the peptide substance P from sensory neurons

43
Q

Inhibits synthesis of serotonin

A

Parachlorophenylalanine

44
Q

Inhibits storage of catecholamines

45
Q

Inhibits degradation of Acetylcholine

A

Anticholinesterase

46
Q

this type of neuronal system contain large myelinated, rapidly conducting fibers

A

hierarchical system

47
Q

this type of neuronal system control major sensory and motor functions

A

hierarchical system

48
Q

this type of neuronal system control the Excitability of the CNS

A

hierarchical system

49
Q

Within each nucleus and in the cortex, what are the two types of cells?

A

relay or projection neurons and local circuit neurons

50
Q

what neurons form the interconnecting pathways that transmit signals over long distances

A

projection neurons

51
Q

these neurons are inhibitory, and they release either GABA or glycine

A

Local circuit neurons

52
Q

in the hierarchical system, these substances are the Major excitatory transmitters

A

Aspartate
Glutamate

53
Q

in the hierarchical system, these substances Also include numerous small inhibitory interneurons transmitter

A

Gamma amino butyric acid (GABA)
Glycine

54
Q

this type of neuronal system is broadly distributed, with single cells frequently sending processes to many different parts of the brain tangential

A

Nonspecific or Diffuse Neuronal Systems

55
Q

Periodic enlargements that contain transmitter vesicles and are located in the axon

A

Varicosities

56
Q

Marked effects on CNS functions

A

Attention
Appetite
Emotional states

57
Q

CRITERIA FOR TRANSMITTER STATUS:
Present in higher concentration in the ____ area than in other areas

58
Q

CRITERIA FOR TRANSMITTER STATUS:
Released by ______ or ______ ________ via a calcium dependent mechanism

A

electrical or chemical stimulation

59
Q

CRITERIA FOR TRANSMITTER STATUS:
Produce the same sort of postsynaptic response that is seen with physiologic activation of the synapse

A

Synaptic mimicry

60
Q
  1. 5% of neurons have receptors for this
  2. G protein coupled muscarinic M 1 receptors
  3. Slow excitation
  4. Decrease permeability to potassium
A

ACETYLCHOLINE

61
Q
  1. Inhibitory actions at synapses in specific
    neuronal systems
  2. G protein coupled activation of K
    channels
  3. D 2 receptor is the main dopamine
    subtype
  4. Increase cAMP
62
Q

Activation of α 1 and β 1 receptors
Decrease K conductance

A

NOREPINEPHRINE
Excitatory effects

63
Q

Activation of α 2 and β 2 receptors
Increase K conductance

A

NOREPINEPHRINE
Inhibitory effects

64
Q
  1. Multiple 5 hydroxytryptamine (5 HT)
    receptor subtypes
  2. Metabotropic
  3. Inhibitory at many CNS sites
  4. Excitatory depending on the receptor
    subtype activated
65
Q
  1. Excitatory for most neurons
  2. N methyl D aspartate (NMDA) receptor
  3. Learning and memory
  4. Inhibition of adenyl cyclase
A

GLUTAMIC ACID

66
Q

primary NTA mediating IPSPs

67
Q

Opens Cl conductance

A

GABA A receptor activation

68
Q

Opens K + channels
Closes Ca +2 channels

A

GABA B receptor activation

69
Q

more numerous in the cord
inhibitory

70
Q

Increases Cl conductance

71
Q

Beta endorphins, dynorphins

A

OPIOID PEPTIDES

72
Q

Decrease Ca +2 conductance

A

OPIOID PEPTIDES
Inhibitory (presynaptic)

73
Q

Increase K conductance

A

OPIOID PEPTIDES
Inhibitory (postsynaptic)

pcol (8 decks)

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