anticonvulsants Flashcards
What is the primary mechanism of action of lamotrigine?
- Blocks voltage gated Na+ channels preventing Na+ influx
- Prevents depolarisation of glutamatergic neurones and reduces glutamate excitotoxicity
What is the drug target of lamotrigine?
Voltage gated Na+ channels
What are the main common side effects of lamotrigine?
- Rash
- Drowsiness
What are the less common but serious side effects of lamotrigine?
- Steven-Johnson’s syndrome
- Suicidal thoughts
Why is lamotrigine introduced gradually?
Introduction of lamotrigine is gradual to reduce frequency and severity of allergic skin reactions
What is the primary mechanism of action of sodium valproate?
- Inhibition of GABA transaminase prevents breakdown of GABA
- Increases GABA conc directly in synapse presynaptically
- Also indirectly prolongs GABA in synapse since extraneuronal GABA metabolism is slowed which also slows GABA removal from synapse
What is the drug target of sodium valproate?
GABA transaminase
What are the main common side effects of sodium valproate?
- Diarrhoea
- Drowsiness
- Weight gain
- Hair loss
What are the main serious side effects of sodium valproate?
- Hepatotoxicity
- Teratogenicity
- Pancreatitis
What else does sodium valproate act as?
It’s a broad CYP enzyme inhibitor: increases serum concentration of many co-administered drugs
What is the primary mechanism of action of diazepam?
- Increases Cl- influx in response to GABA binding at GABA A receptor
- This hyperpolarises the excitatory neurones
What is the drug target of diazepam?
Benzodiazepine site on GABA A receptor
What are the main common side effects of diazepam?
- Drowsiness
- Respiratory depression (if IV or at high dose)
What are uncommon but serious side effects of diazepam?
- Haemolytic anaemia
- Jaundice
Why is diazepam not used long term for suppression of seizures?
Tolerance develops, and it is also an addictive drug