Introduction to the Pharmacology of CNS Drugs

Question 1

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

Answer 1

transmission

Question 2

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

Answer 2

ion flow through transmembrane channels of nerve cells

Question 3

Voltage-gated sodium channel that blocks from outside

Answer 3

tetrodotoxin

Question 4

Voltage-gated sodium channel that slows inactivation and shifts activation

Answer 4

batrachotoxin

Question 5

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

Answer 5

Apamin

Question 6

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

Answer 6

Charybdotoxin

Question 7

Voltage-gated calcium channel that blocks N type channel

Answer 7

omega conotoxin

Question 8

Voltage-gated calcium channel that blocks P type channel

Answer 8

Agatoxin

Question 9

Ligand-gated nicotinic Ach receptor that is an irreversible antagonist

Answer 9

a-Bungarotoxin

Question 10

Ligand-gated GABA receptor that blocks channel

Answer 10

Picrotoxin

Question 11

Ligand-gated glycine receptor that is an competitive antagonist

Answer 11

Strychnine

Question 12

Ligand-gated AMPA receptor that blocks channel

Answer 12

Philanthotoxin

Question 13

Respond to changes in membrane potential

Answer 13

VOLTAGE GATED ION CHANNELS

Question 14

Responsible for FAST action potentials

Answer 14

VOLTAGE GATED ION CHANNELS

Question 15

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

Answer 15

initial segments of the axons

Question 16

responsible for action potential
propagation

Answer 16

sodium channels

Question 17

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

Answer 17

potassium and calcium

Question 18

what are the 2 CLASSES OF NEUROTRANSMITTER RECEPTORS

Answer 18

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

Question 19

ion gated channel that are chemically gated

Answer 19

LIGAND GATED ION CHANNELS

Question 20

ligand gated ion channels respond to chemical _____

Answer 20

neurotransmitters (NTA)

Question 21

SEVEN transmembrane G protein coupled

Answer 21

METABOTROPIC RECEPTORS

Question 22

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

Answer 22

true

Question 23

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

Answer 23

SECOND messengers

Question 24

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 ________

Answer 24

membrane-delimited pathways

Question 25

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

Answer 25

G protein

Question 26

effect of G proteins interact with calcium channels

Answer 26

inhibit channel function (presynaptic metabotropic receptors are activated)

Question 27

effect of G proteins interact with potassium channels

Answer 27

activate channel (slow postsynaptic inhibition)

Question 28

Excitatory postsynaptic potentials (EPSP) ________ potential change

Answer 28

depolarize

Question 29

EPSP are generated by opening of

Answer 29

sodium or calcium channels

Question 30

EPSP are generated by closing of

Answer 30

potassium channels in some synapses

Question 31

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

Answer 31

diffusible second messengers

Question 32

flow of EPSP

Answer 32

+Na, -K, +Ca

Question 33

Inhibitory postsynaptic potential (IPSP) ________ potential change

Answer 33

hyperpolarize

Question 34

IPSP are generated by opening of

Answer 34

potassium or chloride channels

Question 35

flow of IPSP

Answer 35

+K, +Cl, -Ca

Question 36

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

Answer 36

direct

Question 37

Most drugs exert their effect mainly at the

Answer 37

synapses

Question 38

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

Answer 38

axoaxonic synapses

Question 39

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

Answer 39

(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

Question 40

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

Answer 40

presynaptic category

Question 41

This stimulant induces the release of catecholamines from adrenergic synapses

Answer 41

amphetamine

Question 42

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

Answer 42

Capsaicin

Question 43

Inhibits synthesis of serotonin

Answer 43

Parachlorophenylalanine

Question 44

Inhibits storage of catecholamines

Answer 44

Reserpine

Question 45

Inhibits degradation of Acetylcholine

Answer 45

Anticholinesterase

Question 46

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

Answer 46

hierarchical system

Question 47

this type of neuronal system control major sensory and motor functions

Answer 47

hierarchical system

Question 48

this type of neuronal system control the Excitability of the CNS

Answer 48

hierarchical system

Question 49

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

Answer 49

relay or projection neurons and local circuit neurons

Question 50

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

Answer 50

projection neurons

Question 51

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

Answer 51

Local circuit neurons

Question 52

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

Answer 52

Aspartate Glutamate

Question 53

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

Answer 53

Gamma amino butyric acid (GABA) Glycine

Question 54

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

Answer 54

Nonspecific or Diffuse Neuronal Systems

Question 55

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

Answer 55

Varicosities

Question 56

Marked effects on CNS functions

Answer 56

Attention Appetite Emotional states

Question 57

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

Answer 57

synaptic

Question 58

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

Answer 58

electrical or chemical stimulation

Question 59

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

Answer 59

Synaptic mimicry

Question 60

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

Answer 60

ACETYLCHOLINE

Question 61

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 3. Increase cAMP

Answer 61

DOPAMINE

Question 62

Activation of α 1 and β 1 receptors Decrease K conductance

Answer 62

NOREPINEPHRINE Excitatory effects

Question 63

Activation of α 2 and β 2 receptors Increase K conductance

Answer 63

NOREPINEPHRINE Inhibitory effects

Question 64

1. Multiple 5 hydroxytryptamine (5 HT) receptor subtypes 2. Metabotropic 3. Inhibitory at many CNS sites 4. Excitatory depending on the receptor subtype activated

Answer 64

SEROTONIN

Question 65

1. Excitatory for most neurons 2. N methyl D aspartate (NMDA) receptor 3. Learning and memory 4. Inhibition of adenyl cyclase

Answer 65

GLUTAMIC ACID

Question 66

primary NTA mediating IPSPs

Answer 66

GABA

Question 67

Opens Cl conductance

Answer 67

GABA A receptor activation

Question 68

Opens K + channels Closes Ca +2 channels

Answer 68

GABA B receptor activation

Question 69

more numerous in the cord inhibitory

Answer 69

Glycine

Question 70

Increases Cl conductance

Answer 70

Glycine

Question 71

Beta endorphins, dynorphins

Answer 71

OPIOID PEPTIDES

Question 72

Decrease Ca +2 conductance

Answer 72

OPIOID PEPTIDES Inhibitory (presynaptic)

Question 73

Increase K conductance

Answer 73

OPIOID PEPTIDES Inhibitory (postsynaptic)