Anticonvulsants Flashcards
What is an epileptic seizure?
Manifestation of an abnormal or excessive synchronised discharge of a set of cerebral neurones
What is epilepsy?
A tendency to recurrent, unprovoked seizures
Diagnosis of epilepsy?
Brain activity can be measured using:
- Electroencephalography (EEG)
- Magnetic resonance imaging (MRI)
What are the two main types of epilepsy?
Partial/Focal seizures– the excess discharge is localised to one area of the brain (and may spread out)
Generalised seizures – the synchronised discharge affects both hemispheres of brain
List the five types of general seizures
Tonic-clonic seizures Absence seizures Tonic/atonic seizures Myoclonic seizures Status epilepticus
State the symptoms associated with each the five types of general seizure
Tonic-clonic seizures: loss of consciousness => muscle stiffening => jerking/twitching => deep sleep => wakes up
Absence seizures: brief staring episodes with behavioural arrest
Tonic/atonic seizures: sudden muscle stiffening/sudden loss of muscle control
Myoclonic seizures: sudden, brief muscle contractions
Status epilepticus: > 5 min of continuous seizure activity
State and describe the two different types of partial/focal seizures
Simple: retained awareness/consciousness
Complex: impaired awareness/consciousness
Briefly describe the neurotransmission at the glutamatergic synapse
- Voltage-gated Na+ channel (VGSC) opens => membrane depolarisation
- Voltage-gated K+ channel (VGKC) opens => membrane repolarisation
- Ca2+ influx through voltage-gated calcium channels (VGCCs) => vesicle exocytosis; Synaptic vesicle associated (SV2A) protein allows vesicle attachment/docking to presynaptic membrane
- Glutamate activates excitatory post-synaptic receptors (e.g. NMDA, AMPA & kainate receptors)
State two Voltage-gated Na+ channel blockers
Carbamazepine
Lamotrigine
State any important details on the pharmacodynamics and pharmacokinetics of carbamazepine
Pharmacodynamics:
- Stabilises inactive state of Na+ channel, reducing neuronal activity
Pharmacokinetics:
- Enzyme inducer
- Onset of activity within 1 hour
- 16-30 hour half-life
Potential severe side-effects in using carbamazepine in individuals with what?
potential severe side-effects (SJS & TEN) in individuals with HLA-B*1502 allele
State any important details on the pharmacodynamics and pharmacokinetics of Lamotrigine
Pharmacodynamics:
- Inactivates Na+ channels, reducing glutamate neuronal activity
Pharmacokinetics
- Onset of activity within 1 hour
- 24-34 hour half-life
Name a Voltage-gated Ca2+ channel blocker
Ethosuximide
State any important details on the pharmacodynamics and pharmacokinetics of Ethosuximide
Pharmacodynamics
- T-type Ca2+ channel antagonist; reduces activity in relay thalamic neurones
Pharmacokinetics
- Long half-life (50 hours)
State two drugs which interfere with glutamate exocytosis and/or receptors
Levetiracetam
Topiramate