Anti-epileptics Flashcards
What are (6) important AEDs?
Phenytoin, valproate, ethosuximide, carbamazepine, diazepam, phenobarbitone
What two key things do AEDs do?
Decrease excitation
Increase inhibition
How is excitation decreased?
Decrease efficacy at excitatory synapses, inhibiting VG cation channels - Na+, Ca2+
How is an increase in inhibition achieved?
Increase efficacy at inhibitory synapses, increase K+ channel activity
What drugs are used to reduce activity of Na+ channels?
Volproate, carbamazepine, phenytoin (block high frequency discharge without affecting low frequency firing)
What drugs are used to decrease activity at excitatory synapses?
Ethosuximide (generation of normal thalamocortico rhythms)
What drug blocks GABA metabolism? i.e. blocks GABA-transaminase
Valproate - increases GABA (inhibitory NT) in the brain
What drugs potentiate GABA action?
PAM of GABA-a receptors - BDZs, barbiturates
What newer drugs inhibit Na channels?
lamotrigine, topiramate
What blocks NMDA-type GluRs?
Felbamate - This is effective EXPERIMENTALLY.
What drug inhibits GABA uptake?
Tiagabine - inhibits GABA uptake membrane transporters thus increasing spread and duration of GABA
What is a key side effect of AEDs?
Teratogenicity - a substance that disturbs the development of an embryo/foetus
Valproate should not be used on women of child-bearing potential
Other side effects?
Changes in anticoagulant metabolism and oral contraceptive metabolism that could lead to prolonged bleeding (blood won’t clot normally) and unwanted pregnancies.
Epilepsy - could fall during a seizure –> loss of blood
Drugs used for partial seizures?
carbamazepine, valproate, phenytoin
Generalised tonic-clonic drugs?
Valproate, carbamazepine