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MT 6314 2nd Shift > 7.1: Introduction to Pharmacology of CNS Drugs > Flashcards

7.1: Introduction to Pharmacology of CNS Drugs Flashcards

1
Q

True or False

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

A

True

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2
Q

True or False

CNS DRUGS are among the most important tools for studying all aspects of CNS physiology.

A

True

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3
Q

True or False

Unraveling the actions of drugs with known clinical efficacy led to the hypotheses regarding the mechanism of disease.

A

True

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4
Q

True or False

In ion channels & neurotransmitter receptors, most drugs that act on the CNS do so by changing ion flow through transmembrane channels of nerve cells.

A

True

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5
Q

What are the two channel types defined on the basis of the mechanism controlling their gating?

A
  1. Voltage-gated channels
  2. Ligand-gated channels
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6
Q

What are the channel types found in Voltage-Gated Channels?

A
  1. Sodium channels
  2. Potassium channels
  3. Calcium channels
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7
Q

This blocks channel from outside

A

Tetradotoxin (TTX)

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8
Q

Slows inactivation, shifts activation

A

Batrachotoxin (BTX)

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9
Q

Blocks “small Ca-activated” K channel

A

Apamin

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10
Q

Blocks “big Ca-activated” K small

A

Charybdotoxin

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11
Q

Blocks N-type channel

A

Omega conotoxin (ω-CTX-GVIA)

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12
Q

Blocks P-type channel

A

Agatoxin (ω-AGAIVA)

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13
Q

Nicotinic ACh receptor:

Irreversible antagonist

A

α-Bungarotoxin

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14
Q

Blocks GABA-A receptor

A

Picrotoxin

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15
Q

Glycine receptor:
Competitive antagonist

A

Strychnine

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16
Q

Blocks AMPA receptor channel

A

Philanthotoxin

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17
Q

What are the channel types found in Ligand-Gated Channels?

A
  1. Nicotonic ACh receptor
  2. GABA-A receptor
  3. Glycine receptor
  4. AMPA receptor
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18
Q

Identify if Voltage or Ligand:

  • Respond to changes in membrane potential
  • Concentrated on the INITIAL SEGMENT of the axons in nerve cells
  • Responsible for FAST action potentials
A

Voltage-gated ion channels

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19
Q

The voltage-gated ion channels includes the sodium channels responsible for?

A

Action potential propagation

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20
Q

True or False:

The voltage-gated ion channels have cell bodies and dendrites also have voltage-sensitive ion channels for potassium and calcium.

A

True

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21
Q

What are the two classes of neurotransmitter receptor?

A
  1. Ligand-gated ion channels or Ionotropic receptors
  2. Metabotropic receptors
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22
Q

Identify if Ionotropic or Metabotropic:

  • Chemically-gated
  • Respond to chemical neurotransmitters (NTAs) that bind to receptor subunits of the channel
A

Ionotropic Receptors

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23
Q

Identify if Ionotropic or Metabotropic:

  • SEVEN transmembrane G protein coupled
  • Binding does not result in the direct gating of a channel
  • Binding engages the G-protein that results into production of SECOND messengers that modulates the voltage gated channels
A

Metabotropic Receptor

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24
Q

What are the two channels in metabotropic receptors that delimited the pathways of the membrane?

A
  • Potassium channels
  • Calcium channels
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25
Q

Types of receptor channel coupling in LIGAND GATED ion channels activation and inactivation:

A
  1. A receptor that acts directly on the channel protein
  2. A receptor that is coupled to the ion channel
    through a G protein
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26
Q

Three receptors that are coupled to a G protein that modulates the formation of diffusible second messengers:

A

A. cyclic adenosine monophosphate (cAMP)
B. inositol trisphosphate (IP3)
C. diacylglycerol (DAG)

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27
Q

What are the two types of synapse?

A
  1. Excitatory Postsynaptic Potentials (EPSPs)
  2. Inhibitory Postsynaptic Potentials (IPSPs)
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28
Q

Identify if EPSPs or IPSPs:

  • Depolarizing potential change
  • Opening of sodium or calcium channels
  • Closing of potassium channels in some synapses
A

Excitatory Postsynaptic Potentials (EPSPs)

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29
Q

Identify if EPSPs or IPSPs:

↑ Na+, ↓K+, ↑ Ca+2

A

Excitatory Postsynaptic Potentials (EPSPs)

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30
Q

Identify if EPSPs or IPSPs:

  • Hyperpolarizing potential change
  • Opening of potassium or chloride channels
A

Inhibitory Postsynaptic Potentials (IPSPs)

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31
Q

Identify if EPSPs or IPSPs:

↑ K+, ↑ Cl- at the postsynaptic, ↓Ca+2 at the presynaptic

A

Inhibitory Postsynaptic Potentials (IPSPs)

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32
Q

What are the drugs that exert their effect through direct interactions with molecular components of ion channels on axons?

A
  • Carbamazepine
  • Phenytoin
  • Local anesthetics and some drugs used for general anesthesia
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33
Q

True or False:

In sites and mechanisms of drug action, most drugs exert their effect mainly at the synapses.

A

True

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34
Q

Inhibits synthesis of serotonin

A

Parachlorophenylalanine

35
Q

Inhibits storage of cathecolamines

36
Q

Inhibits release of catecholamines

A

Amphetamine

37
Q

Inhibits degradation of Acetylcholine

A

Anticholinesterase

38
Q

What are the two types of neuronal system?

A
  1. Hierarchical system
  2. Diffused/Non-specific Neuronal System
39
Q

Identify if Hierarchical or Diffused Non-Specific:

  • Contain large myelinated, rapidly conducting fibers
  • Control major sensory and motor functions
  • Excitability of the CNS
A

Hierarchical system

40
Q

What are the two major excitatory transmitters in hierarchical system?

A
  • Aspartate
  • Glutamate
41
Q

What are the small inhibitory interneurons transmitter in the hierarchical system?

A
  • Gamma amino butyric acid (GABA)
  • Glycine
42
Q

Identify if Hierarchical or Diffused Non-Specific:

Broadly distributed, with single cells frequently sending processes to many different parts of the brain-tangential

A

Diffused Non-Specific

43
Q

Periodic enlargements that contain transmitter vesicles and is located in the axons.

A

Varicosities

44
Q

Peptides that act on metabotropic receptors and is found primarily in a compact cell group called locus caeruleus in the caudal pontine central gray matter.

A

Transmitters

45
Q

Varicosities is located in the:

46
Q

Transmitters are located in the:

A

Locus caeruleus in the caudal pontine central gray matter

47
Q

What are the marked effect on CNS functions in the diffused/non-specific neuronal system?

A
  • Attention
  • Appetite
  • Emotional states
48
Q

What are the criteria for transmitter status?

A
  1. Present in higher concentration in the synaptic area than in other areas (localized in appropriate areas)
  2. Released by electrical or chemical stimulation via a calcium-dependent mechanism
  3. Synaptic mimicry
49
Q

Identify this neurotransmitter in the CNS:

  • 5% of neurons have receptors for Ach
  • G protein-coupled muscarinic M1 receptors
  • Slow excitation
  • Decrease permeability to potassium
A

Acetylcholine (Ach)

50
Q

Identify this neurotransmitter in the CNS:

  • Inhibitory actions at synapses in specific neuronal systems
  • G protein-coupled activation of K+ channels
  • D2 receptor is the main dopamine subtype
  • Increase cAMP
51
Q

What are the excitatory effects of norepinephrine?

A
  • Activation of α1 and β1 receptors
  • Decrease K+ conductance
52
Q

What are the inhibitory effects of norepinephrine?

A
  • Activation of α2 and β2 receptors
  • Increase K+ conductance
53
Q

Identify this neurotransmitter in the CNS:

  • Multiple 5 hydroxytryptamine (5-HT) receptor subtypes
  • Metabotropic
  • Inhibitory at many CNS sites
  • Excitatory depending on the receptor subtype activated
54
Q

Identify this neurotransmitter in the CNS:

  • Excitatory for most neurons
  • N-methyl-D-aspartate (NMDA) receptor
  • Learning and memory
  • Inhibition of adenyl cyclase
A

Glutamic acid

55
Q

Identify this neurotransmitter in the CNS:

  • Primary NTA mediating IPSPs
  • GABA-A & GABA-B receptor activation
  • Glycine is more numerous in the cord
  • Glycine is inhibitory
A

GABA and Glycine

56
Q

Function of GABA-A receptor activation in GABA and Glycine:

A

Opens Cl- conductance

57
Q

Function of GABA-B receptor activation in GABA and Glycine:

A
  • Opens K+ channels
  • Closes Ca+2 channels
58
Q

Identify this neurotransmitter in the CNS:

  • Beta-endorphins, dynorphins
  • Inhibitory (presynaptic)
  • Decrease Ca+2 conductance
  • Inhibitory (postsynaptic)
  • Increase K+ conductance
A

Opioid peptides

59
Q

Identify the specific receptor antagonist/s of Acetylcholine
(Mechanisms)
Excitatory:
⬇ in K+ conductance;
⬆ IP3, DAG

A

Pirenzepine, atropine

60
Q

Identify the specific receptor antagonist/s of Acetylcholine:
(Mechanisms)

Inhibitory:
⬆in K+ conductance; ⬇ cAMP

A

Atropine, methoctramine

61
Q

Identify the specific receptor antagonist/s of Acetylcholine:
(Mechanisms)

Excitatory: ⬆ cation conductance

A

Dihydro-B-erythroidine, a-bungarotoxin

62
Q

Identify the specific receptor antagonist/s of Dopamine:

(Mechanisms)
Inhibitory (?): ⬆cAMP

A

Phenothiazines

63
Q

Identify the specific receptor antagonist/s of Dopamine (D2):

(Mechanisms)
Inhibitory (presynaptic) ⬇Ca2+;
Inhibitory (postsynaptic): ⬆in K+ conductance, ⬇ cAMP

A

Phenothiazines, butyrophenones

64
Q

Identify the specific receptor antagonist/s of GABA-A muscimol:
(Mechanisms)

Inhibitory: ⬆︎Cl- conductance

A

Bicuculline, picrotoxin

65
Q

Identify the specific receptor antagonist/s of GABA-B baclofen:
(Mechanisms)

Inhibitory (presynaptic): ⬇︎Ca2+ conductance; Inhibitory (postsynaptic): ⬆︎K+ conductance

A

2-OH saclofen

66
Q

Identify the specific receptor antagonist/s of Glutamate:
(Mechanisms)
Excitatory: ⬆︎ cation conductance, particularly Ca2+

A

2-Amino-5-phosphonovalerate, dizocilpine

67
Q

Identify the specific receptor antagonist/s of Glutamate:
(Mechanisms)
Excitatory: ⬆︎cation conductance

A

NBQX, ACET

68
Q

Identify the specific receptor antagonist/s of Glutamate:
(Mechanisms)

Inhibitory (presynaptic): ⬇︎Ca2+ conductance, ⬇︎cAMP; Excitatory: ⬇︎K+ conductance, ⬆︎IP3, DAG

69
Q

Identify the specific receptor antagonist/s of Glycine:
(Mechanisms)
Inhibitory: ⬆︎Cl- conductance

A

Strychnine

70
Q

Identify the specific receptor antagonist/s of Serotonin (5-Hydroxytryptamine):
(Mechanisms)

Inhibitory: ⬆︎K+ conductance, ⬇︎cAMP

A

Metergoline, spiperone

71
Q

Identify the specific receptor antagonist/s of Serotonin (5-Hydroxytryptamine):
(Mechanisms)

Excitatory: ⬇︎ K+ conductance, ⬆︎ IP3, DAG

A

Ketanserin

72
Q

Identify the specific receptor antagonist/s of Serotonin (5-Hydroxytryptamine):
(Mechanisms)

Excitatory: ⬆︎cation conductance

A

Ondansetron

73
Q

Identify the specific receptor antagonist/s of Serotonin (5-Hydroxytryptamine):
(Mechanisms)

Excitatory: ⬇︎ K+ conductance

74
Q

Identify the specific receptor antagonist/s of Norepinephrine:
(Mechanisms)

Excitatory: ⬇︎K+conductance, ⬆︎IP3, DAG

75
Q

Identify the specific receptor antagonist/s of Norepinephrine:
(Mechanisms)

Inhibitory (presynaptic): ⬇︎Ca2+ conductance; Inhibitory: ⬆︎K+ conductance, ⬇︎cAMP

76
Q

Identify the specific receptor antagonist/s of Norepinephrine:
(Mechanisms)

Excitatory: ⬇︎K+conductance, ⬆︎ cAMP

A

Atenolol, practolol

77
Q

Identify the specific receptor antagonist/s of Norepinephrine:
(Mechanisms)

Inhibitory: may involve ⬆︎ in electrogenic sodium pump; ⬆︎cAMP

A

Butoxamine

78
Q

Identify the specific receptor antagonist/s of Histamine:
(Mechanisms)

Excitatory: ⬇︎K+ conductance, ⬆︎IP3, DAG

A

Mepyramine

79
Q

Identify the specific receptor antagonist/s of Histamine:
(Mechanisms)

Excitatory: ⬇︎K+ conductance, ⬆︎cAMP

A

Ranitidine

80
Q

Identify the specific receptor antagonist/s of Histamine:
(Mechanisms)

Inhibitory autoreceptors

A

Thioperamide

81
Q

Identify this neurotransmitter in the CNS:

Receptor Antagonist - Naloxone
Mechanism- Inhibitory (presynaptic): ⬇︎Ca2+ conductance, ⬇︎ cAMP
Inhibitory (postsynaptic): ⬆︎K+ conductance, ⬇︎ cAMP

A

Opioid peptides

82
Q

Identify this neurotransmitter in the CNS:

Receptor Antagonist - Suvorexant
Mechanism - Excitatory, glutamate co-release

A

Suvorexant

83
Q

Identify the specific receptor antagonist/s of Tachykinins:
(Mechanisms)

Excitatory: ⬇︎K+ conductance, ⬆︎IP3, DAG

A

Aprepitant, Sardutant, Osanetant

84
Q

Identify the specific receptor antagonist/s of Endocannabinoids:
(Mechanisms)

Inhibitory (presynaptic): ⬇︎Ca+ conductance, ⬇︎ cAMP

A

Rimonabant

MT 6314 2nd Shift (8 decks)

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