Anticonvulsants and anti-epileptic drugs Flashcards
Define epilepsy
Tendency for recurrent, unprovoked seizures
Define seizure
sudden changes in behaviors characterised by electrical hyperchronisation of neuronal networks in the cerebral cortex
Types of seizures
Generalised
Partial/Focal
Define generlaised seizure
a seizure manifesting itself in both hemispheres
Define partial/focal seizure
a seizure originating from a discrete brain area in one hemisphere, has the potential to spread and develop into a global seizure
State the types of global seizures and what they’re charcterised by
Tonic-clonic = loss of consciousness -> muscle stiffening -> rapid jerky/twitching movements -> deep sleep -> awakes (with no recollection)
Absence = brief staring episodes and behavioural arrest
Tonic/atonic = sudden muscle rigidity/relaxation
Myoclonic = sudden brief muscle contractions
Status epilepticus = state of CONTINUOUS seizure activity for >5 mins
State the types of partial seizures and what they’re charcterised by
Simple = no impairment in awareness/consciousness Complex = impaired awareness/consciousness
2 most common types of central neurotransmission
Gluatminergic = excitatory GABA = inhibitory
Describe normal glutaminergic transmission
Depolarisation of presynaptic neurone
opening of VGSC, Na+ inlfux
opening of VGKC, K+ efflux
Opening of VGCC at synapse, Ca2+ influx
Stimulation of exocytosis of gluamate-containing vesicles
Docking at presynaptic membrane by SV2A docking protein
Glutamate binds to excitatiry NMDAR and Kainate-R on postsynaptic membrane
Depolarisation of postsynaptic neurone
Describe normal GABAergic transmission
GABA synthesised from GLU
Exocytosis and binding to inhibitory GABAAR
Cl- influx and hyperpolarisation
Reuptaken by GAT (GABA transporter) by presynaptic
Reuptaken by support cells and broken down to GLU by GABA-T (?GABA transaminase)
Examples of VGSC blockers
Carbamazepine, Lamotrigine
Carbamazepine MOA, PK
Stabilises inactive state of VGSC, reducing depol
ENZYME INDUCER
fast onset <1hr
long t1/2
Lamotrigine MOA, PK
Inactivates VGSC, reduced glutaminergic transmission
fast onset <1hr
long t1/2
Principles of anticonvulsant therapy
Inhibit excitatory central Glutaminergic transmission
Stimulate inhibitoy central GABAergic transmission
Types of anticonvulsant drug groups
Inhibit excitatory central Glutaminergic transmission: VGSC blockers VGCC blockers docking protein inhiitors Glutamate receptor inhibitors
Stimulate inhibitoy central GABAergic transmission
GABAAR agonists
GABA-T inhibitors