1.7 Epilepsy

Question 1

Diazepam target

Answer 1

GABAa receptors (alpha subunit)

Question 2

Where is the GABAa drug target

Answer 2

Post synaptic neurones in the temporal lobe

Question 3

How does diazepam work

Answer 3

Binds and increases effectiveness of GABA activation of this receptor (doesn’t activate the receptor itself)
Leads to chloride ion influx (in the presence of GABA) which Hyperpolarisation the temporal lobe neurone and decrease the effects observed

Question 4

Drug target site examples (epilepsy tutorial)

Answer 4

Receptors - GABAA, AMPA, NMDA
Enzymes - GABA transaminase
Ion channels - VGCC, VGSC
Transport proteins - GABA reuptake transporter

Question 5

Drug target examples ( epilepsy)

Answer 5

Receptors - GABAA, AMPA, NMDA
Enzymes - GABA transaminase
Ion channels - VGCC, VGSC
Transport proteins - GABA reuptake transporter

Question 6

What is diazepam used for

Answer 6

Anxiety, muscle spasm, seizures

Question 7

Lamotrigine (works on VGSC)

Answer 7

Blocks sodium influx reducing neuronal depolarisation so NT (Glu) is not released causing less excitatory stimulation of post synaptic neuron

Question 8

Pregablin (works on VGCC)

Answer 8

Prevents calcium influx therefore decreasing vesicles exocytosis and NT release causing less excitatory stimulation of post synaptic neuron

Question 9

Lavetiracetam (works on synaptic vesicles protein)

Answer 9

Interferes with vesicles fusion reducing vesicle exocytosis and NT release causing a decrease in excitatory stimulation of post synaptic neuron

Question 10

Valproate (works on mutltiole targets)

Answer 10

Not selective