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pharmacology Neuro > Anticonvulsant drugs > Flashcards

Anticonvulsant drugs Flashcards

1
Q

What substance synthesises glutamine to glutamate?

A

glutiminase

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2
Q

What substance synthesises glutamate to GABA?

A

glutamic acid dehydrogenase (GAD)

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3
Q

where are glutiminase and GAD found?

A

the neuron pre-synaptic terminal

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4
Q

How is GABA taken up into the glia cells?

A

Via the GABA transporter (GAT)

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5
Q

What substance causes the degredation of GABA to succinic semialdehyde?

A

GABA transminase

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6
Q

What substance causes the degredation of succinic semialdehyde to succinate?

A

SSA dehydrogenase

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7
Q

Where does the degredation of GABA take place?

A

In the glia cell

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8
Q

Give examples of drugs that potentiate GABA actions at GABAA receptors on the post-synaptic terminals?

A

benzodiazepines (e.g. clobazam, midazolam, diazepam, lorazepam)

sodium valproate

phenobarbitone

felbamate

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9
Q

Give examples of drugs that InhibitGABA transaminase?

A

vigabatrin

sodium valproate

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10
Q

Give examples of drugs that Inhibit SSA dehydrogenase?

A

sodium valproate

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11
Q

Describe how sodium valproate reduces GABA degredation by inhibiting SSA dehydrogenase?

A

It prevents the degredation of succinic semialdehyde so that its concentration remains high, which means that GABA will not break down as there is no downhill concentration gradient

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12
Q

Give an example of a drug that inhibits GABA reuptake

A

Tiagabine

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13
Q

Give an example of a AMPA antagonist which reduces the activity of glutumate?

A

perampanel

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14
Q

what are the side effects of perampanel

A

increased insidence of falls due to AMPA receptors being blocked in the cerebellum

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15
Q

What is perampanel potentially useful for treating?

A

useful for treatment-resistant focal seizures?

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16
Q

Give an example of a NMDA antagonist which reduces the activity of glutumate?

17
Q

How could you reduce glutamate release

A

metabotropic glutamate receptor agonists – future drugs?

18
Q

What are the problems with drugs that block glutamate release/actions?

A

psychosis

memory impairment

motor function

19
Q

Give examples of drugs used to Block of voltage-activated sodium channels?

A

carbamazepine

oxcarbazepine,

phenytoin

sodium valproate

lamotrigine

20
Q

What voltage-activated calcium channels may be involved in abscence seizures?

A

Low voltage activated T-type

21
Q

Give an example of a drug that blocks voltage-activated T-type calcium channels?

A

ethosuximide

sodium valproate

22
Q

How does gabapentin prevent voltage gated calcium influx?

A

gabapentin binds to the a2 and gamma subunit interface in the Q and P-type channels preventing their trafficking to the plasma membrane, ad thus preventing the amount of calcium flowing into the neurone following a voltage activation.

23
Q

Give examples of drugs that block voltage-activated calcium channels?

A

lamotrigine

phenytoin

24
Q

How does Topiramate function as an anti-epileptic?

A

block Na+ channels

block Ca2+ channels

enhance GABA transmission

block AMPA receptors

25
Q

How does Levetiracetam function as an anti-epileptic?

A

binds to synaptic vesicle protein 2A (SV2A) reducing neurotransmitter release

26
Q

How does Felbamate function as an anti-epileptic?

A

inhibits NMDA

potentiates GABAA responses

27
Q

How does Retigabine function as an anti-epileptic?

A

activates KCNQ potassium channels leading to hyperpolarisation and neuron inhibiton

also active against some forms of pain

28
Q

What are the First-line anti-epileptic drugs (AEDs) used to treat partial (focal) siezures

A

carbamazepine

lamotrigine

sodium valproate

levetiracetam

oxcarbazepine

29
Q

What are the First-line anti-epileptic drugs (AEDs) used to treat General tonic-clonic seizures (GTCS)

A

carbamazepine

lamotrigine

oxcarbazepine

sodium valproate

30
Q

What are the First-line anti-epileptic drugs (AEDs) used to treat Status epilepticus

A

diazepam

lorazepam

midazolam

31
Q

What are the First-line anti-epileptic drugs (AEDs) used to treat Absence seizures

A

ethosuximide

lamotrigine

sodium valproate

32
Q

What are the First-line anti-epileptic drugs (AEDs) used to treat Tonic or atonic siezures

A

sodium valproate

33
Q

What are the First-line anti-epileptic drugs (AEDs) used to treat Myoclonic seizures

A

levetiracetam

sodium valproate,

topiramate

34
Q

Give two examples of treatments that can exacerbate and worsen absence or myoclonic seizures

A

carbamazepine

phenytoin

35
Q

Adjunctive therapies may be required for generalised tonic-clonic seizures, give an example of two drugs

A

clobazam and topimarate

pharmacology Neuro (14 decks)

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