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Med Chem modules > Neuropharmacy I > Flashcards

Neuropharmacy I Flashcards

1
Q

List 3 amino acids that are NTs.

A

GABA- major inhibitory
Glutamate- major excitatory
Glycine- an inhibitory NT

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2
Q

Name 3 monoamines that are found in the brain

A

NA
5HT
DA

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3
Q

How is 5HT formed?

A

1) L-tryptophan to 5-hydroxy-L-tryptophan by tryptophan hydroxylase
2) 5-hydroxy-L-tryptophan to 5HT by aromatic L-amino acid decarboxylase

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4
Q

How is dopamine formed?

A

L-tyrosine to L-DOPA by tyrosine hydroxylase

L-DOPA to dopamine by DOPA decarboxylase

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5
Q

Which monoamines are catecholamines?

A

NA

DA

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6
Q

Which monoamine is an indolamine?

A

5HT

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7
Q

Which peptides act as NTs?

A

Opioids:
Enkephalins, dynorphin, endorphin

Tachykinins:
Substance P, neurokinin A &B

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8
Q

Is glycine stimulatory or inhibitory?

A

Always inhibitory

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9
Q

Is NA stimulatory or inhibitory?

A

Depends on the receptor. Can be either

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10
Q

Is 5HT stimulatory or inhibitory?

A

Depends on the receptor

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11
Q

Is endorphin stimulatory or inhibitory?

A

Inhibitory (as will all opioids)

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12
Q

Is substance P stimulatory or inhibitory?

A

Stimulatory

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13
Q

Give an example of an ionotropic GABA receptor

A

GABA(A)-R for Cl

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14
Q

Give an example of an metabotropic GABA receptor

A

GABA(B)-R (linked to G protein for K)

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15
Q

Give examples of an ionotropic GluR

A

AMPA (Na)

NMDA (Ca, Na)

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16
Q

Give an example of a metabotropic GluR

A

mGluR ( linked to G proteins)

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17
Q

Give an example of an ionotropic NA receptor.

A

There are none

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18
Q

Give examples of metabotropic NA receptors

A

Alpha 1-2

Beta 1-3

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19
Q

Give an example of an ionotropic serotonin receptor.

A

5HT(3)

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20
Q

Give examples of metabotropic serotonin receptors

A

5HT (1,2 & 4-7)

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21
Q

Give examples of ionotropic substance P receptors

A

-

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22
Q

Give examples of ionotropic opiate receptors

A

-

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23
Q

Give examples of ionotropic dopamine receptors

A

-

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24
Q

Give examples of metabotropic DA receptors.

A

D1 & D2 (GPCRs)

25
What type of receptors are opiate and substance P metabotropic receptors
GPCRs
26
Write down the 5 criteria used to define a substance as a NT?
1) must be present in the presynaptic nerve terminal 2) they must be stored in vesicles 3) they must be released upon stimulation 4) an effect must be shown with the existence of a specific receptor 5) a mechanism of effect of termination must be evident
27
What are the main symptoms of Parkinson's disease
Muscle rigidity Akinesia Tremor at rest
28
What neuronal pathway is the brain degenerates to lead to Parkinson's disease?
The nigrostriatal pathway
29
How is the balance of outputs from stratum to the thalamus in the direct pathway affected in Parkinson's?
In the direct pathway, dopamine is excitatory. | A loss of dopamine gives an inhibited direct pathway
30
How is the balance of outputs from the stratum to the thalamus via the indirect pathway affected in Parkinson's.
In the indirect pathway, dopamine is inhibitory. A loss of dopamine here causes the indirect pathway to be excited.
31
What's happening to the basal ganglia in Parkinson's
It's malfunctioning, hence the rigidity
32
Which NT is in deficit as a result of neuronal degeneration?
DA
33
Which receptor does DA activate to control the direct pathway?
D1- to activate AC
34
What receptor does DA activate to control the indirect pathway?
D2- couples of IP(3)
35
What is the drug used to replenish the DA deficit in Parkinson's?
L-DOPA
36
How does carbidopa enhance the concentration of L-DOPA reaching the brain?
Inhibitor of DOPA decarboxylase Stops the conversion of L-DOPA to dopamine in the periphery Cannot cross the BBB
37
How does selegiline enhance the concentration of L-DOPA reaching the brain?
MAO inhibitor Reduced the breakdown of dopamine in the CNS reduced neuronal degeneration to some extent
38
Describe a drug used to for Parkinson's in older patients.
Bromocriptine: Useful where L-DOPA is no longer useful D2 agonist
39
Describe a drug used for Parkinson's in younger patients.
Ropinirole: D2 agonist Used as a monotherapy
40
What are the side effects of drugs used in Parkinson's treatment.
Dyskinesia Psychotic effects Reduction in prolactin release Hypotension Nausea
41
What are the type (I) symptoms of Schizophrenia?
Auditory hallucinations Thought disorders Delusions Thought broadcasting
42
What are the negative type (II) symptoms of schizophrenia?
Lack of drive Social withdrawal Motor disturbance (catatonia)
43
How are D2 receptors targeted in schizophrenia treatment?
They are antagonised in the mesolimbic and mesocortical pathways
44
How are 5HT(1A) receptors targeted in treatment of schizophrenia?
Agonised for the increase of the release of dopamine form mesocortical neurones to frontal cortex
45
How are 5HT(2) receptors targeted in treatment of schizophrenia?
Antagonised- contribute to antipsychotic effects
46
Give 2 examples of typical antipsychotic drugs.
Phenothianes- chlorpromazine | Butyrophenones- haloperidol
47
What are the symptoms of typical antipsychotic drugs
``` EPS (induced Parkinson's) Dystonia Akathisia Hyperprolactinaemia Aplastic anaemia ```
48
Give an example of an atypical antipsychotic
Clozapine
49
Why is an atypical drug termed so
They bind weakly to the D2 receptor. Antipsychotics are made on the premise that D2 receptors need to be antagonised
50
Which two monoamine NTs are targeted to treat depression?
5HT and NA
51
How could you increase the concentration of monoamine in the synapse?
Inhibit NET Inhibit MOA Increases synaptic NA
52
Name a tricyclic antidepressant
Imipramine
53
How do tricyclic antidepressants work
They block the uptake of NA into the presynaptic neurone
54
Name a selective NA uptake blocker
Maprotiline
55
Name a selective serotonin reuptake blocker
Fluoxetine
56
How have antidepressants been improved from tricyclics
Been made to be safer in overdose by fewer side effects by making them more selective.
57
Name a reversible MAO inhibitor
Maclobemide
58
Name an irreversible MAO inhibitor
Phenelzine
59
What are the side effects of MAO inhibitors?
Hepatotoxicity Insomnia Convulsions Postural hypotension Irreversible MAO inhibitors can also interact with dietary tyramine which can lead to fatal hypertension

Med Chem modules (8 decks)

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