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FPT > Intro to CNS pharmacology 2 > Flashcards

Intro to CNS pharmacology 2 Flashcards

1
Q

what are the 2 types of cholinergic receptors?

A

1- nicotinic
2- muscarinic

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2
Q

nicotinic receptors are part which types of receptors?

A

ionotropic (cholinergic)

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3
Q

where are nicotinic receptors mostly found?

A
  • mostly skeletal muscle
  • some in the CNS
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4
Q

muscarinic receptors are part of which types of receptors?

A

metabotropic (cholinergic)

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5
Q

where are muscarinic receptors found?

A

mostly in the CNS

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6
Q

Acetylcholine is synthesized from what, and by which enzyme?

A

synthesized from choline and acetyl-CoA.
By choline acetyl transferase (CAT).

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7
Q

what is the rate limiting step in acetylcholine synthesis?

A

choline uptake

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8
Q

in acetylcholine’s nicotinic effects the signal is terminated by what?

A

acetylcholine esterase and possibly an uptake mechanism.

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9
Q

acetylcholine’s nicotinic effects are linked to which type of diseases?

A

neurodegenerative diseases (eg. Parkinson’s, Alzheimer’s)

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10
Q

Loss of cholinergic neurons at the basal forebrain are a pathologic feature of which disease?

A

alzheimer’s

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11
Q

which anticholinesterase drugs provide benefit to AD patients, and how do they work?

A

Tacrine and donepezil, they work by reducing Ach degradation.

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12
Q

muscarinic receptor effect speed compared to nicotinic effects is… (faster or slower)?

A

slower effects

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13
Q

Acetylcholine muscarinic effects is responsible for mediating which behavioral effects of Ach?

A

Arousal.
Learning.
and short-term memory

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14
Q

biogenic amines is derived from what?

A

amino acids.

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15
Q

catecholamine are derived from which amino acid?

A

Tyrosine

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16
Q

give examples of catecholamine?

A

-Dopamine.
-Norepinephrine (noradrenaline).
-Epinephrine (adrenaline).

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17
Q

Norepinephrine and epinephrine binds to which type of receptor?

A

adrenergic receptors.

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18
Q

speed of response of NE and E at adrenergic receptors?

A

slow responses

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19
Q

What is the category of dopamine?

A

biogenic amine.

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20
Q

what is the postsynaptic effect of dopamine?

A

Excitatory or inhibitory.

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21
Q

dopamine receptors are bound by which type of drugs?

A

antipsychotic drugs

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22
Q

what are the 4 dopaminergic pathways in the CNS?

A

1-meso-limbic.
2-nigro-striatal.
3-hypothalamus.
4- Chemoreceptor trigger zone (CTZ).

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23
Q

What is the importance of the dopaminergic meso-limbic pathway? which disease is related to it?

A

important in emotion an reward pathway.
related to schizophrenia.

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24
Q

What is the importance of the dopaminergic nigro-striatal pathway? which disease is related to it?

A

important in motor control.
related to Parkinson’s disease.

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25
Q

What is the importance of the dopaminergic hypothalamus pathway?

A

important in some hormone regulation (eg. prolactin).

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26
Q

What is the effect of the dopaminergic Chemoreceptor trigger zone pathway?

A

emetic effect “vomiting”

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27
Q

what are the 5 subtypes for DA receptors?

A

D1
D2
D3
D4
D5

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28
Q

Which DA receptor is responsible for Parkinson’s like effect, motor side effect, and extrapyramidal symptoms (EPS)?

A

D1 (including D5)

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29
Q

which DA receptor subtype gets blocked by antipsychotic drugs?

A

D2 (Including D3 and D4)

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30
Q

which DA receptor subtype gets blocked by haloperidol and clozapine?

A

they are antipsychotic drugs.
so they block D2 (including D3 and D4)

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31
Q

which type of nerves is norepinephrine released form?

A

adrenergic nerves.

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32
Q

norepinephrine is formed from which catecholamine?

A

dopamine

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33
Q

what are norepinephrine receptors?

A

Alpha 1 and 2
Beta 1 and 2

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34
Q

which organ is epinephrine released from?

A

adrenal glands.

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35
Q

epinephrine is synthesized from which catecolamine?

A

norepinephrine

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36
Q

inhibition of noradrenaline happens through the activation of which receptor?

A

activation of beta receptors.

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37
Q

excitation of noradrenaline happens through the activation of which receptors?

A

activation of both alpha and beta receptors.

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38
Q

noradrenergic pathways are important in what?

A

1- arousal.
2- control of blood pressure.
3- mood control.

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39
Q

what is venlafaxine (effexor)?

A

antidepressants.

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40
Q

how dose venlafaxine (effexor) work?

A

it is a serotonin norepinephrine reuptake inhibitors (SNRIs).

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41
Q

how does cocaine work?

A

reuptake inhibitors.

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42
Q

amphetamine is an example of a drug which is linked to which pathway?

A

noradrenergic pathways.

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43
Q

how does amphetamine effect the noradrenergic pathway?

A

increases catecholamine in the brain, increases wakefulness, alertness and exploratory activity.

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44
Q

what are clonidine and methyldopa?

A

centrally acting antihypertensives.

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45
Q

how do clonidine and methyldopa work?

A

they are agonists to alpha 2, couples to Gi protein, decrease sympathetic discharge from the CNS.

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46
Q

which biogenic amine blocks hunger and tiredness in the brain?

A

histamine.

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47
Q

what is the postsynaptic effect of histamine?

A

excitatory.

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48
Q

all histamine receptors are which type of receptors?

A

G-protein coupled.

49
Q

what are the effects of histamine in the brain?

A

affects arousal and attention.

50
Q

what are the effects of histamine in the peripheries?

A

inflammation and vasodilation.

51
Q

what is the postsynaptic effects of serotonin?

A

excitatory.

52
Q

what is the source of 5-hydroxytryptamine (5-HT) (serotonin)?

A

tryptophan

53
Q

how does HT-5 affect the GIT?

A

Increases GIT motility.

54
Q

how does HT-5 affect platelets?

A

platelet aggregation.

55
Q

5-HT has which effect in the CTZ?

A

vomiting

56
Q

what effects does 5-HT have on the CNS?

A

control of:
- appetite,
- sleep/wakefulness,
- mood and emotion,
- behaviors “hallucinations”,
- pain perception,
- vomiting.

57
Q

antidepressants have which effects on appetite?

A

loss of appetite.

58
Q

5-HT is involved in which clinical conditions?

A
  • migraines.
  • mood disorders and anxiety.
59
Q

what type of drugs treat mood disorders and anxiety? “HINT: related to 5-HT”

A

tricyclic “TCA” and selective serotonin reuptake inhibitors “SSRI”

60
Q

What type of receptors are serotonin receptors?

A

there are 14 distinct receptor subtypes, 13 are G protein coupled receptors (GPCRs), and one (5-HT3) ligand-gated ion channel (LGIC)

61
Q

list serotonin effects? (HINT: there are 4)

A

1- involved in sleep/wakefulness cycle.
2- SSRI and depression and anxiety.
3- coagulation.
4- antiemetic effects.

62
Q

name amino acid neurotransmitters at excitatory synapses?

A

glutamate and aspartate.

63
Q

name amino acid neurotransmitters at inhibitory synapses?

A

GABA (gamma-amino butyric acid) and glycine.

64
Q

what category is glutamate?

A

small molecule

65
Q

what are glutamate neurons called?

A

glutaminergic neurons.

66
Q

where is glutamate synthesized from?

A

glutamine from glia.

67
Q

what are glutamate ionotropic receptors?

A

NMDA.
AMPA.
kainate

68
Q

where is the location of NMDA ionotropic glutamate receptors?

A

late EPSP

69
Q

which ionotropic glutamate receptor is glycine and mg+2 dependent?

A

NMDA

70
Q

Where is the AMPA ionotropic glutamate receptor located?

A

Early EPSP

71
Q

Where is the kainate ionotropic glutamate receptor located?

A

Early EPSP

72
Q

what are the metabotropic glutamate receptors?

A

mammalian metabotropic glutamate receptors. are all named mGluR

73
Q

the major EAA’s in the CNS are?

A

1- L-Glutamate (glutamic acid).
2- Aspartate.

74
Q

what is the major excitatory transmitter in the CNS?

A

L-Glutamate.

75
Q

what major excitatory transmitter is widely distributed in the CNS?

A

L-Glutamate.

76
Q

what major inhibitory transmitter is widely distributed in the CNS?

A

GABA

77
Q

what is the major inhibitory transmitter in the CNS?

A

GABA

78
Q

GABA is synthesized mainly from what?

A

glutamate via GAD (Glutamic acid decarboxylase).

79
Q

decarboxylases are vitamin ____ dependent enzymes.

A

B6

80
Q

Vitamin B6 can lead to _____ due to not enough synthesis of GABA

A

seizures

81
Q

glycine is mostly found where?

A

in the spinal cord.

82
Q

strychnine antagonist causes what?

A

convulsions

83
Q

which category is GABA from?

A

small molecule

84
Q

which type of neuron is GABA?

A

GABAergic neurons.

85
Q

what postsynaptic effect does GABA have?

A

inhibitory.

86
Q

GABA is made from what?

A

glucose.

87
Q

what is the ionotropic GABA receptor called?

A

GABA A

88
Q

what is the metabotropic GABA receptor called?

A

GABA B

89
Q

what does GABA A receptor do?

A

gates CL- channel

90
Q

what does GABA B receptor do?

A

gates K+ channel

91
Q

where is GABA A receptor located?

A

post-synaptically

92
Q

GABA A opens for what?

A

Chloride.

93
Q

GABA A chloride opening results in what?

A

decrease in membrane excitability (hyperpolarization).

94
Q

list the drugs that interact in GABA A?

A

1- Benzodiazepine.
2-Convulsants.
3-Barbiturates.

95
Q

what are the effects of benzodiazepines when they interact at GABA A?

A

reduction of anxiety, induction of sleep, muscle relaxant, and reduction of convulsion.

96
Q

_________ are GABA A antagonist.

A

Convulsants.

97
Q

give an example for barbiturates that interact at GABA A?

A

phenobarbital

98
Q

GABA B is which type of receptor?

A

GPCR

99
Q

what is the effect of GABA B?

A

inhibits cAMP production.

100
Q

short chains of amino acids

A

neuropeptides.

101
Q

give the 2 examples of neuropeptides, and where are they found.

A
  • endogenous opiates (endorphins - in the brain)
  • morphine - like (vasopressin - antidiuretic hormone - found in the posterior pituitary).
102
Q

which purine is an NT?

A

ATP

103
Q

what is the effect of the ionotropic ATP receptor?

A

Fast excitatory NT

104
Q

what is the effect of the metabotropic ATP receptor?

A

neuromodulation

105
Q

which type of purine is involved in neuronal toxicity?

A

ATP cytosol

106
Q

list the effects of adenosine (A receptors)?

A
  • sedative.
  • anticonvulsant.
  • neuroprotective.
  • methylxanthines, (increase wakefulness).
107
Q

give examples of methylxanthines?

A

caffeine and theophylline, which are A2 antagonists.

108
Q

nitric oxide is synthesized by which enzyme?

A

nitric oxide synthase

109
Q

____ increases NO production

A

CA +2

110
Q

NO increases the production of ________

A

cGMP

111
Q

excessive NO production causes what?

A

neurotoxicity.

112
Q

NO is important in what?

A
  • LTP — Memory.
  • protect against ischemic brain damage.
113
Q

list the 3 CNS barriers?

A

1- Blood - brain barrier.
2- Blood - CSF barrier.
3- the arachnoid barrier.

114
Q

what is the favoured route for global delivery of drugs to all brain cells?

A

BBB

115
Q

Which barrier is created at the level of cerebral capillary endothelial cells by tight junction formation?

A

BBB

116
Q

what is the largest area for exchange to the brain in humans?

A

BBB

117
Q

which CNS barrier is NOT an important route for the entry of solutes into brain?

A

arachnoid barrier.

118
Q

which medical condition causes the BBB to be leaky

A

Bacterial meningitis.

119
Q

what are the factors that influence drug entry through BBB? “hint: there are 7”

A

1- size.
2- molecular conformation.
3-lipophilicity.
4-charge.
5- enzymatic stability.
6- affinity to transporter.
7- plasma protein binding.

FPT (17 decks)

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