epilepsy Flashcards

1
Q

what are the 4 classical drug target sites

A

receptors
enzymes
ion channels
transport proteins

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2
Q

examples of receptors

A

GABAA receptor, AMPA receptor, NMDA receptor

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3
Q

examples of enzymes

A

GABA transaminase

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4
Q

examples of ion channels

A

voltage gated Na and Ca channel

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5
Q

examples of transport proteins

A

GABA transporter

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6
Q

what is the drug target for diazepam

A

GABAa receptor (alpha subunit)

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7
Q

where is the diazepam drug target

A

postsynaptic neurones in the temporal lobe (for complex, partial focal seizures)

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8
Q

what is the result of diazepam

A

diazepam binds and increases the effectiveness of GABA activation of this receptor (it does not activate the receptor itself) > leads to Cl- influx in the presence of GABA which hyperpolarises the temporal lobe neurone and decreases the effects observed

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9
Q

what are some drugs used to treat epilepsy (3)

A

lamotrigine
pregabalin
levetiracetam

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10
Q

drug target for lamotrigine

A

voltage gated sodium channel

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11
Q

drug target for pregabalin

A

voltage gated calcium channel

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12
Q

drug target for levetiracetam

A

synaptic vesicle protein SV2A

glutamatergic neurones in the temporal lobes

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13
Q

how does lamotrigine cause an antiepileptic effect

A

blocking the sodium channels reduces neuronal depolarisation which would eventually lead to NT release
glutamate neurotransmission is decreased and there is less excitatory stimulation of the postsynaptic neurone

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14
Q

how does pregabalin cause an antiepileptic effect

A

blocking the Ca channels prevents Ca influx into the neruone which is required to promote vesicle exocytosis and NT release
glutamate neurotransmission is decreased and there is less excitatory stimulation of the post synaptic neurone

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15
Q

how does levetiracetam cause an antiepileptic effect

A

drug interferes with vesicle fusion and therefore reduces exocytosis of glutamate > decreasing the excitatory activation of the postsynaptic neurone

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16
Q

what is the name of an antiepileptic drug that should not be used in female patients with childbearing potential

A

sodium valproate

17
Q

what does sodium valproate have in terms of selectivity

A

low selectivity - acts on multiple targets (eg VGSCs , GABA-T, VGCCs, NMDA receptor blockade and even enhances GABA production)
many side effects