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Y2 Pharm (LCRS1) > Anticonvulsants for Pharmacology and Therapeutics > Flashcards

Anticonvulsants for Pharmacology and Therapeutics Flashcards

1
Q

What is an epileptic seizure?

A

Seizures are “sudden changes in behaviour caused by electrical hypersynchronization of neuronal networks in the cerebral cortex”

Either too much glutamate or too little GABA

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2
Q

What is epilepsy?

A

A neurological condition causing frequent seizures

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3
Q

What are the two main types of epilepsy?

A

Partial/Focal – the excess discharge is localised to one area of the brain Generalised – the synchronised discharge affects all brain areas

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4
Q

When are the two peaks in incidence of epilepsy and what are they usually caused by?

A

Young adults – where genetic predispositions begin to manifest Later years – when patients start getting brain injuries e.g. stroke

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5
Q

What are the main mechanisms of anti-epileptic drugs?

A

Enhancing GABA-mediated inhibition Inhibiting glutamate-mediated excitation Na+ channel blockade (blocking nerve conduction) Calcium channel blockade

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6
Q

Give an example of a group of drugs that enhance GABA-mediated inhibition.

A

Benzodiazepines

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7
Q

What does Levatiracetam bind to in order to inhibit glutamate release?

A

SV2A

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8
Q

What are the 3 main excitatory receptors?

A

AMPA and Kainate (Na+/Ca2+ channel) NMDA

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9
Q

Describe the effects of important AEDs on hepatic enzymes.

A

Phenytoin and Carbamazepine – hepatic enzyme INDUCERS Valproate – hepatic enzyme INHIBITORS

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10
Q

What are the 2 ways of diagnosing epilepsy?

A

Electroencephalography (EEG) Magnetic resonance imaging (MRI)

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11
Q

What are the different types of general seizure?

A

Tonic-clonic Absence Tonic/atonic Myoclonic Status epilepticus

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12
Q

What are the features of a tonic clonic seizure?

A

loss of consciousness -> muscle stiffening -> jerking/twitching -> deep sleep -> wakes up

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13
Q

What are the features of a absence seizures?

A

brief staring episodes with behavioural arrest can lead to loss of muscle tone and falling over

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14
Q

What are the features of a tonic/atonic seizures?

A

sudden muscle stiffening/sudden loss of muscle control

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15
Q

What are the features of a myoclonic seizures?

A

sudden, brief muscle contractions similar to tonic by less severe

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16
Q

What are the features of a status epilepticus?

A

> 5 min of continuous seizure activity Doesn’t necessarily manifest of any of the 4 but can have parts of each or just be one

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17
Q

Describe the types of focal seizure

A

Simple: retained awareness/consciousness Complex: impaired awareness/consciousness

18
Q

How does the glutamatergic synapse work?

A
  • 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
  • Glutamate activates excitatory post-synaptic receptors
19
Q

What receptors does glutamate act on at the post synaptic membrane?

A

NMDA, AMPA & kainate receptors

20
Q

What protein allows vesicle attachment to the presynaptic terminal in glutamernergic synapses?

A

Synaptic vesicle associated (SV2A) protein

21
Q

What are 2 drugs that act on VGSC?

A

Carbamazepine

Lamotrigine

22
Q

What are the pharmacodynamics and pharmacokinetics of carbamazepine?

A

Pharmacodynamics

  • Stabilises inactive state of Na+ channel
  • Reduces neuronal activity

Pharmacokinetics

  • Enzyme inducer
  • Onset of activity within 1 hour
  • 16-30 hour half-life
23
Q

What are the potential consequences of carbamazepine treatment?

A
  1. Potential severe side-effects
  • SJS & TEN - potentially fatal skin conditions
  • in individuals with HLA-B*1502 allele
24
Q

What are the pharmacodynamics and pharmacokinetics of lamotrigine?

A

Pharmacodynamics:

  • Inactivates Na+ channels -> reducing glutamate neuronal activity

Pharmacokinetics:

  • Onset of activity within 1 hour
  • 24-34 hour half-life
25
Q

What drug blocks VGCC?

A

Ethosuximide

26
Q

What are the pharmacodynamics and pharmacokinetics of ethosuximide?

A

Pharmacodynamics

  • T-type Ca2+ channel antagonist
  • Reduces activity in relay thalamic neurones

Pharmacokinetics

  • Long half-life (50 hours)
27
Q

What drugs target glutamate exocytosis?

A

Levetricetam

28
Q

What are the pharmacodynamics and pharmacokinetics of levetiracetam?

A

Pharmacodynamics

  • Binds to synaptic vesicle associated protein (SV2A)
  • Preventing glutamate release

Pharmacokinetics

  • Fast-onset (1 hour); half-life (10 hours)
29
Q

What drug targets glutamate receptors?

A

Topiramate

30
Q

What are the pharmacodynamics and pharmacokinetics of topiramate?

A

Pharmacodynamics

  • Inhibits NMDA & kainate receptors
  • Also affects VGSCs & GABA receptors

Pharmacokinetics

  • Fast-onset (1 hour); long half-life (20 hours
31
Q

What is topiramate used for?

A
  • Mainly neuropathic pain
  • Also epilepsy
32
Q

Summarise the sites of action for drugs effecting the Glutamatergic Synapse

A
  1. VGSC antagonist: e.g Carbamazepine
  2. VGCC antagonist: Ethosuximide (T-type antagonist);
  3. SV2A inhibitor: Levetiracetam
  4. Glutamate receptor antagonist: Topiramate
33
Q

Describe the GABA synapse

A
  1. GABA can be released tonically & also following neuronal stimulation
  2. GABA activates inhibitory post-synaptic GABAA receptors
  3. GABAA receptors are chloride (Cl-) channels -> membrane hyperpolarisation
  4. GABA is taken up by GAT & metabolised by GABA transaminase (GABA-T)
34
Q

What epilepsy drugs target the GABA synapse?

A
  • Diazepam
  • Sodium valoprate
35
Q

What are the pharmacodynamics and pharmacokinetics of diazepam?

A

Pharmacodynamics

  • GABA receptor, PAM
  • Increases GABA-mediated inhibition - positive allosteric action

Pharmacokinetics

  • Rectal gel - Fast-onset (within 15 min); half-life (2 hours)
36
Q

What are the pharmacodynamics and pharmacokinetics of sodium valporate?

A

Pharmacodynamics

  • Inhibits GABA transaminase ® increases GABA-mediated inhibition

Pharmacokinetics

  • Fast onset (1h); half-life (12h
37
Q

What drugs should you use for the treatment of absence seizures?

A
  • Ethosuximide
  • Lamotrigine
  • Valproate
38
Q

What drugs should you use for the treatment of tonic clonic seizures?

A
  • Carbamazepine
  • Lamotrigine
  • Valproate
39
Q

What drugs should you use for the treatment of tonic/atonic seizures?

A

Sodium valporate

40
Q

What drugs should you use for the treatment of myoclonic seizures?

A
  • Levetiracetam
  • Topiramate
  • Valproate
41
Q

What drugs should you use for the treatment of status epilepticus?

A
  • Diazepam
42
Q

What drugs should you use for the treatment of Focal seizures?

A
  • Carbamazepine
  • Levetiracetam
  • Lamotrigine
  • Valproate

Y2 Pharm (LCRS1) (34 decks)

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