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LCRS Pharmacology and Therapeutics > Anticonvulsants > Flashcards

Anticonvulsants Flashcards

1
Q

What is an epileptic seizure?

A

Manifestation of an abnormal or excessive synchronised discharge of a set of cerebral neurones

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2
Q

What is epilepsy?

A

A tendency to recurrent, unprovoked seizures

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3
Q

What is the clinical manifestation of epilepsy?

A

Seizures

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4
Q

What is epilepsy classified based on?

A

Part of the brain that is affected:
Focal epilepsy- Excess discharge being localised to one part of brain
Generalised epilepsy- synchronised discharge affects all areas

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5
Q

When does epilepsy develop?

A

At any stage but there are two distinct peaks:
Early adulthood- where genetic predispositions begin to manifest
Later years- when patients start getting brain injuries e.g. stroke

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6
Q

What percentage of epilepsy is caused by genetics?

A

70%

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7
Q

What sort of acquired factors can lead to epilepsy

A

Tumour
Stroke
Infection
Head injury

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8
Q

What can be used to measure brain activity?

A

Electroencepahlography
Magnetoencephalography
Functional MRI

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9
Q

What are the distinctive firing patterns and what are they associated with?

A 
Gamma: awareness - hyperactive 
Beta: awareness - thinking
Alpha: awareness - relaxed
Theta: drowsiness, meditation
Delta: deep-sleep
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10
Q

Give a brief summary of glutamergic synapse activity?

A

Voltage gated NA+ channel opens- membrane depolarisation
Voltage gated K+ channel opens - membrane repolarisation
Ca2+ influx through voltage gated calcium channels - vesicle exocytosis
Glutamate activates excitatory post-synaptic receptors

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11
Q

What is carbamazepine?

A

Voltage gated Na+ channel blocker that is the drug of choice for partial seizures and tonic-clonic seizures. Stabilises inactive state of channel

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12
Q

What are the pharmacokinetics of carbamazepine?

A

Induces the expression of hepatic enzymes
16-30 hour half-life
Dangerous in individuals with HLA-B 1502 allele

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13
Q

What is phenytoin?

A

Voltage gated Na+ channel blocker that is indicated for most forms of epilepsy. It is a class 1b channel blocker.

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14
Q

What are the pharmacokinetics of phenytoin?

A

Fast onset (10 mins) and long half-life (10-20 hours)

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15
Q

What is retigabine?

A

VGKC enhancer- potassium channel opener specific for Kv7 alpha subunit. Only licensed for adjunctive treatment. Fast onset (30 mins) and long (10 hour) half life

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16
Q

What is ethosuximide?

A

T-type Ca channel antagonist

17
Q

When is ethosuximide mainly used?

A

For absence seizures- long half life (50 hours)

18
Q

What is gabapentin?

A

Thought to inhibit a2d subunit. Indicated for partial seizures

19
Q

What does levetiracetam do?

A

It binds to synaptic vesicle associated protein preventing glutamate release. Monotherapy for focal seizures. It has a fast onset (1 hour) and long half life of 10 hours

20
Q

What does topiramate do?

A

It inhibits GluK5 subunit of kainate receptor. Also affects VGSCs and GABA receptors. It is indicated for most types of epilepsy
Fast-onset (1 hour), long half life (24 hours)

21
Q

What does perampanel do?

A

It is a selective inhibitor of AMPA receptor. Adjunct for partial seizures. Fast onset (1 hour) long half life (24 hours)

22
Q

List the different types of drugs that affect glutamergic synapses and what they affect?

A

VGSC antagonist - phenytoin, carbamazepine
VGKC enhancer -retigabine
VGCC antagonist- ethosuximide and gabapentin
SV2a inhibitor- levetiracetam
Glutamate receptor antagonist- perampanel and topiramate

23
Q

Explain how a GABAergic synapse works?

A

GABA can be released tonically and also following neuronal stimulation
GABA activates inhibitory post-synaptic GABAa receptors
GABAa receptors are chloride channels - membrane hyper polarisation
GABA is taken up by GAT
GABA is metabolised by GABA transaminase (GABA-T)

24
Q

When are benzodiazepines used in epilepsy?

A

All forms of epilepsy- Fast onset and long half life

25
Q

When are barbiturates (phenobarbital) used?

A

For most forms of epilepsy except absent seizures

26
Q

What do benzodiazepines and barbiturates target?

A

GABA receptors

27
Q

What effect do barbiturates have in adults and children?

A

In adults, they act as a sedative but in children may be the cause of behavioural disturbances.

28
Q

What drugs target the GABAergic synapse?

A

Tiagabine
Sodium valproate
Vigabatrin

29
Q

What does tiagabine do?

A 
It is a selective inhibitor of GAT-1. It used for adjunctive treatment for partial seizures
Fast onset (45 mins) short half life (6h)
30
Q

What does sodium valproate do?

A

It is indicated for all forms of epilepsy and inhibits GABA transaminase. It has fast onset (1h) and has a half life (12 hours)

31
Q

What does vigabatrin do?

A

It irreversibly inhibits GABA transaminase enzyme. Monotherapy for infantile spasm or an adjunct for partial seizures

LCRS Pharmacology and Therapeutics (33 decks)

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