Eoiliepsy Flashcards
1
Q
4 classical drug target sites
A
Receptors
Enzymes
Ion channels
Transport proteins
2
Q
Receptors example
A
GABAA receptor,AMPA receptor,NMDA receptor
3
Q
Enzymes example
A
GABA transaminase
4
Q
Ion channels examples
A
Voltage gated sodium and calcium ion channels
5
Q
Transport proteins
A
GABA transporter
6
Q
Diazepam
A
- Binds to GABAA receptor (alpha subunit) on the post-synaptic membrane in the temporal lobe
- Treats for complex, partial focal seizures
- Increases effectiveness of GABA activation of receptor- leads to Cl- influx in presence of GABA which hyperpolarises temporal lobe neurone and decreases febrile seizures
7
Q
Lamotrigine
A
- Binds to and blocks voltage gated sodium channels on glutamatergic neurones in temporal lobe
- This reduces neuronal depolarisation which would lead to glutamate NT release- so this is decreased and there is less excitatory stimulation of the post-synaptic neurone
- Produces anti-epileptic effect
8
Q
Pregablin
A
- Binds to and blocks voltage gated calcium channels on glutamatergic neurones in temporal lobe
- This prevents calcium influx into neurone which is required to promote vesicle exocytosis and NT release so less glutamate is released and there’s less excitatory stimulation of the post-synaptic neurones
- Produces anti-epileptic effect
9
Q
Levetiracetam
A
- Binds to synaptic vesicle protein SV2A in glutamatergic neurones in the temporal lobe
- It interferes with vesicle fusion and reduces exocytosis of glutamate thus decreasing excitatory activation of the post-synaptic neurone
10
Q
Sodium valproate
A
Non selective
Acts on multiple targets
Teratogenic-avoided in females of child bearing age
