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Neurology > Applied Neuro-Pharmacology > Flashcards

Applied Neuro-Pharmacology Flashcards

1
Q

What approaches ca be used to reduce synaptic transmission?

A

Blocking the voltage gated sodium channels
Blocking the voltage gated calcium channels
Inhibiting the packagaing mechanism
Blocking the release machinery
Blocking the postsynaptic receptors
Activating presynaptic inhibitory receptors

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2
Q

How do local anaesthetics manipulate synaptic transmission

A

Reduce transmission by blocking the voltage gated sodium channels and thereby blocking any sodium from entering the neuron post AP, therefore blocking all release

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3
Q

How do substances such as spider toxins manipulate synaptic transmission?

A

Reduce it by blocking voltage gated calcium channels, thereby blocking all transmitter release

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4
Q

How does Botox manipulate synaptic transmission?

A

Reducing it by blocking the presynaptic release machinery

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5
Q

How do receptor antagonists manipulate synaptic transmission?

A

They reduce it by blocking the postsynaptic receptors

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6
Q

What approaches can be used to increase synaptic transmission?

A

Increasing synthesis by flooding the cells with appropriate precursor
Blocking breakdown of the transmitter
Blocking uptake of the transmitter
Activating the postsynaptic receptors

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7
Q

How do benzodiazepines and barbituates acting on GABA receptors manipulate synaptic transmission?

A

THey increase it by activating the postsynaptic receptor whilst potentiating the effects of the endogenous transmitter

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8
Q

How do anticholinesterases acting on ACh manipulate synaptic transmission?

A

Increase it by blocking breakdown of the transmitter

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9
Q

Name the monoamine class of neurotransmitter

A

Noradrenaline
Dopamine
Serotonin (5-HT)

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10
Q

Name the amino acid class of neurotransmitter

A

Glutamate
GABA
Glycine

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11
Q

Name the purine class of neurotransmitter

A

ATP

Adenosine

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12
Q

Name the neuropeptide class of neurotransmitter

A

Endorphins
CCK
Substance P

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13
Q

Name the two neurotransmitter which do not belong to a class or group

A

Acetylcholine

NO

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14
Q

Does each neurotransmitter have only one specific function?

A

No, each have multiple different functions in different areas

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15
Q

What separates the brain from the peripheral nervous system?

A

BBB

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16
Q

Where is dopamine distributed in the brain?

A

Brain stem
Basal ganglia
Limbic system/frontal cortex

17
Q

What physiological functions are affected by dopamine?

A

Vomiting
Voluntary movements
Emotions

18
Q

What happens to DA in Parkinson’s disease?

A

Degeneration of DA cells in the SN (nigrostriatal pathway)

Leads to DA deficiency in the basal ganglia. Leads to stiffness, slow movements, change in posture, tremor

19
Q

Can in theory both selective agonists and selective antagonists produce a beneficial effect with respect to dopamine?

A

Yes in theory either could

20
Q

What are the key enzymes in dopamine breakdown?

A

MAO-B

COMT

21
Q

Give a dopaminergic DA precursor drug

A

Levodopa

22
Q

Give some dopaminergic DA agonist drugs

A

Bromocriptine, pergolide
Ropinirole
Pramipexole
Apomorphine

23
Q

What are some enzyme inhibitors used in the treatment of Parkinson’s?

A

Peripheral AAAD inhibitors - carbidopa, benserazide. Reduce peripheral side-effects of levodopa to allow a greater proportion of the dose to reach the CNS

MAOB inhibitors - selegiline. Reduce the metabolism of dopamine so increase the effectiveness of levodopa.

COMT inhibitors - entacapone. Same effect as MAOB inhibitors

24
Q

What are the pros and cons of dopaminergic drugs?

A

Pros - Parkinson’s e.g. rigidity and bradykinesia in the limbs

Cons - nausea, vomiting, psychosis

Cannot help - ‘midline’ features such as dysathria, balance, cognition

25
Q

Describe the relationship between the BBB and vomiting

A

DA antagonist aniemetics will generally worsen PD and should therefore be avoided in patients with PD. This only applies because the antiemtic will cross the BBB. This is not necessary in theory, however, as the area postrema/vomiting centre us functionally outside the BBB in the medulla. For this reason domperidone is used, - a DA antagonist antiemtic which does not cross the BBB

26
Q

What are the features of domperidone?

A 
DA antagonist
Anti-emtic
Does not cross BBB
No antipsychotic properties
Relatively safe for use in PD
Has permitted the therapeutic use of apomorphine (powerful antiemetic)
27
Q

What are dyskinesias?

A

Abnormal involuntary movements

28
Q

Should anti-emetic DA antagonists be used long term?

A

No, long term vomiting doesn’t happen

29
Q

Should anytipsychotic DA antagonists be used long term?

A

Yes, there is often no alternative

30
Q

What is the major side effect of long term DA use?

A

Often cause parkinsonism

Neurology (42 decks)

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