Download Week 2 - New antiepileptics

NEW ANTIEPILEPTIC DRUGS
Name
Brivaracetam
Carisbamate
2-Deoxy-d-glucose
Eslicarbazepine acetate
Ganaxolone
Mode of Action
Binds to SV2A (synaptic vesicle protein)
Inhibits voltage-dependent Na channels
Inhibits voltage-gated Na channels
Modest inhibition of high-voltage
activated Ca channels
Analogue of glucose – cannot undergo
metabolism
Inhibitor of glycolysis suppresses
discharges in the hippocampus
Interacts with site II of inactivated
voltage-gated Na channel  prevents
repetitive firing
Inhibits release of GABA, glutamate,
aspartate and DA
Modulator of GABA receptors – activates
receptor
GABA – inhibitory neurotransmitter
Huperzine A
JZP-4
Inhibits NMDA receptors – reduced
glutamate toxicity
Inhibits acetycholinesterases (is also used
in Alzheimer’s disease)
Na channel blocker
Ca channel blocker
Lacosamide
NAX-5055
Propylisopropyl acetamide
Retigabine
5,5-diphenylbarbituric acid
Tonabersat
Valrocemide
YKP3089
Raises seizure threshold
Selectively enhances the slow
inactivation of voltage gated Na channels
Modulates activity of collapsing response
mediator protein- 2 (CRMP-2)  is a part
of the signal transduction pathway
{neuroprotective)
Enhances galanin receptor
neurotransmission – galanin is a
anticonvulsant peptide produced in the
hippocampus
Seizures are caused when there is a shift
in the balance between glutamate
(excitation) and galanin (inhibition);
fatigue of galanergic neurones  seizures
Unknown mechanism
Opens K channels – enhances voltage
gated M current  opposes depolarising
inputs
Suppresses high frequency neurone firing
at motor terminals
Enhances slow outward currents
Neuronal gap junction inhibitor – inhibits
connexion cell-mediated coupling 
prevents hypersynchonicity
Connexion – forms gap junctions
Unknown
Unknown
Treatment for...
Partial epilepsy
Generalised epilepsy
Disease modifying effects
Status epilepticus – reduced neuron loss
in cortex, hippocampus, amygdale and
thalamus
Delay/prevent development of
spontaneous recurrent seizures
Chronic - Protective against kindling
progression
Acute - Broadly suppressive against many
cellular and membrane processes to
prevent network synchronisation
Tonic seizures
Limbic seizures
Partial seizures
Clonic seizures
Retard development of recurrent seizures
Paediatrics – infantile spasms
Unknown
Tonic-clonic seizures
Partial seziures
Partial seizures
Primary generalised seizures
Secondary generalized seizures
Status epilepticus
Partial epilepsy
Secondary generalised seizures
Generalised seizures
Partial epilepsy
Clonic seizures
Tonic seizures
Broad spectrum
Broad spectrum