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Med Chem modules > Neuropharmacy I > Flashcards

Neuropharmacy I Flashcards

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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
Q

What type of receptors are opiate and substance P metabotropic receptors

A

GPCRs

26
Q

Write down the 5 criteria used to define a substance as a NT?

A

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
Q

What are the main symptoms of Parkinson’s disease

A

Muscle rigidity
Akinesia
Tremor at rest

28
Q

What neuronal pathway is the brain degenerates to lead to Parkinson’s disease?

A

The nigrostriatal pathway

29
Q

How is the balance of outputs from stratum to the thalamus in the direct pathway affected in Parkinson’s?

A

In the direct pathway, dopamine is excitatory.

A loss of dopamine gives an inhibited direct pathway

30
Q

How is the balance of outputs from the stratum to the thalamus via the indirect pathway affected in Parkinson’s.

A

In the indirect pathway, dopamine is inhibitory. A loss of dopamine here causes the indirect pathway to be excited.

31
Q

What’s happening to the basal ganglia in Parkinson’s

A

It’s malfunctioning, hence the rigidity

32
Q

Which NT is in deficit as a result of neuronal degeneration?

A

DA

33
Q

Which receptor does DA activate to control the direct pathway?

A

D1- to activate AC

34
Q

What receptor does DA activate to control the indirect pathway?

A

D2- couples of IP(3)

35
Q

What is the drug used to replenish the DA deficit in Parkinson’s?

A

L-DOPA

36
Q

How does carbidopa enhance the concentration of L-DOPA reaching the brain?

A

Inhibitor of DOPA decarboxylase
Stops the conversion of L-DOPA to dopamine in the periphery
Cannot cross the BBB

37
Q

How does selegiline enhance the concentration of L-DOPA reaching the brain?

A

MAO inhibitor
Reduced the breakdown of dopamine in the CNS
reduced neuronal degeneration to some extent

38
Q

Describe a drug used to for Parkinson’s in older patients.

A

Bromocriptine:
Useful where L-DOPA is no longer useful
D2 agonist

39
Q

Describe a drug used for Parkinson’s in younger patients.

A

Ropinirole:
D2 agonist
Used as a monotherapy

40
Q

What are the side effects of drugs used in Parkinson’s treatment.

A

Dyskinesia
Psychotic effects
Reduction in prolactin release

Hypotension
Nausea

41
Q

What are the type (I) symptoms of Schizophrenia?

A

Auditory hallucinations
Thought disorders
Delusions
Thought broadcasting

42
Q

What are the negative type (II) symptoms of schizophrenia?

A

Lack of drive
Social withdrawal
Motor disturbance (catatonia)

43
Q

How are D2 receptors targeted in schizophrenia treatment?

A

They are antagonised in the mesolimbic and mesocortical pathways

44
Q

How are 5HT(1A) receptors targeted in treatment of schizophrenia?

A

Agonised for the increase of the release of dopamine form mesocortical neurones to frontal cortex

45
Q

How are 5HT(2) receptors targeted in treatment of schizophrenia?

A

Antagonised- contribute to antipsychotic effects

46
Q

Give 2 examples of typical antipsychotic drugs.

A

Phenothianes- chlorpromazine

Butyrophenones- haloperidol

47
Q

What are the symptoms of typical antipsychotic drugs

A 
EPS (induced Parkinson's)
Dystonia
Akathisia
Hyperprolactinaemia 
Aplastic anaemia
48
Q

Give an example of an atypical antipsychotic

A

Clozapine

49
Q

Why is an atypical drug termed so

A

They bind weakly to the D2 receptor. Antipsychotics are made on the premise that D2 receptors need to be antagonised

50
Q

Which two monoamine NTs are targeted to treat depression?

A

5HT and NA

51
Q

How could you increase the concentration of monoamine in the synapse?

A

Inhibit NET
Inhibit MOA
Increases synaptic NA

52
Q

Name a tricyclic antidepressant

A

Imipramine

53
Q

How do tricyclic antidepressants work

A

They block the uptake of NA into the presynaptic neurone

54
Q

Name a selective NA uptake blocker

A

Maprotiline

55
Q

Name a selective serotonin reuptake blocker

A

Fluoxetine

56
Q

How have antidepressants been improved from tricyclics

A

Been made to be safer in overdose by fewer side effects by making them more selective.

57
Q

Name a reversible MAO inhibitor

A

Maclobemide

58
Q

Name an irreversible MAO inhibitor

A

Phenelzine

59
Q

What are the side effects of MAO inhibitors?

A

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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