Anticonvulsant drugs

Question 1

What substance synthesises glutamine to glutamate?

Answer 1

glutiminase

Question 2

What substance synthesises glutamate to GABA?

Answer 2

glutamic acid dehydrogenase (GAD)

Question 3

where are glutiminase and GAD found?

Answer 3

the neuron pre-synaptic terminal

Question 4

How is GABA taken up into the glia cells?

Answer 4

Via the GABA transporter (GAT)

Question 5

What substance causes the degredation of GABA to succinic semialdehyde?

Answer 5

GABA transminase

Question 6

What substance causes the degredation of succinic semialdehyde to succinate?

Answer 6

SSA dehydrogenase

Question 7

Where does the degredation of GABA take place?

Answer 7

In the glia cell

Question 8

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

Answer 8

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

sodium valproate

phenobarbitone

felbamate

Question 9

Give examples of drugs that InhibitGABA transaminase?

Answer 9

vigabatrin

sodium valproate

Question 10

Give examples of drugs that Inhibit SSA dehydrogenase?

Answer 10

sodium valproate

Question 11

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

Answer 11

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

Question 12

Give an example of a drug that inhibits GABA reuptake

Answer 12

Tiagabine

Question 13

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

Answer 13

perampanel

Question 14

what are the side effects of perampanel

Answer 14

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

Question 15

What is perampanel potentially useful for treating?

Answer 15

useful for treatment-resistant focal seizures?

Question 16

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

Answer 16

Felbamate

Question 17

How could you reduce glutamate release

Answer 17

metabotropic glutamate receptor agonists – future drugs?

Question 18

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

Answer 18

psychosis

memory impairment

motor function

Question 19

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

Answer 19

carbamazepine

oxcarbazepine,

phenytoin

sodium valproate

lamotrigine

Question 20

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

Answer 20

Low voltage activated T-type

Question 21

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

Answer 21

ethosuximide

sodium valproate

Question 22

How does gabapentin prevent voltage gated calcium influx?

Answer 22

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.

Question 23

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

Answer 23

lamotrigine

phenytoin

Question 24

How does Topiramate function as an anti-epileptic?

Answer 24

block Na+ channels

block Ca2+ channels

enhance GABA transmission

block AMPA receptors

Question 25

How does Levetiracetam function as an anti-epileptic?

Answer 25

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

Question 26

How does Felbamate function as an anti-epileptic?

Answer 26

inhibits NMDA | potentiates GABAA responses

Question 27

How does Retigabine function as an anti-epileptic?

Answer 27

activates KCNQ potassium channels leading to hyperpolarisation and neuron inhibiton also active against some forms of pain

Question 28

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

Answer 28

carbamazepine lamotrigine sodium valproate levetiracetam oxcarbazepine

Question 29

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

Answer 29

carbamazepine lamotrigine oxcarbazepine sodium valproate

Question 30

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

Answer 30

diazepam lorazepam midazolam

Question 31

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

Answer 31

ethosuximide lamotrigine sodium valproate

Question 32

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

Answer 32

sodium valproate

Question 33

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

Answer 33

levetiracetam sodium valproate, topiramate

Question 34

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

Answer 34

carbamazepine phenytoin

Question 35

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

Answer 35

clobazam and topimarate