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Pharmacology (5th year) > Anti-epileptic > Flashcards

Anti-epileptic Flashcards

(41 cards)

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1
Q

Definition of epilepsy

A

Recurrent seizures unprovoked by any systemic or acute neurologic insults

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2
Q

Diagnosis of epilepsy

A
  • exclude metabolic or toxic cause
  • LP
  • EEG
  • neuroimaging
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3
Q

Pathophysiology of epilepsy

A

Imbalance between excitatory and inhibitory processes

  • decreased GABA
  • increased glutamate
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4
Q

What is GABA synthesised from?

A

Amino acid, L-Glutamic acid

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5
Q

How is GABA synthesised?

A

Glutamic acid decarboxylase (GAD) is presen in neurons

- causes removal of a-carboxyl group

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6
Q

How does GABA inhibit?

A
  • activated GABA A receptor mediates increase in conductance
  • increase influx of Cl- ions causes membrane hyperpolerisation
  • increase in threshold for generating action potential
  • inhibitory action
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7
Q

Goals of therapy in epilepsy

A
  • control seizures
  • restore quality of life
  • restore neuronal function
  • minimize drug adverse effects
  • identify and avoid precipitating factors
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8
Q

Excitation ions and neurotransmitter

A
  • inward Na+, Ca++

- glutamate, aspartate

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9
Q

Inhibition ions and neurotransmitter

A
  • inward Cl-
  • outward K+
  • GABA
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10
Q

MOA of anti-epileptics

A
  • prolong Na+ channel inactivation
  • increase Cl- channel
  • glutamate receptor antagonism
  • Inhibition of T-type Ca++ current
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11
Q

How to choose an anti-epileptic

A
  • based on seizure classification
  • patient-specific variables
  • characteristics of drug
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12
Q

Drugs that inhibit axonal transmission

A
  • phenytoin
  • carbamazepine
  • valproate
  • lamotrigine
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13
Q

Drugs that potentiate GABA receptors

A
  • benzos

- phenobarb

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14
Q

Why do therapeutic drug monitoring?

A
  • avoid toxicity
  • optimize drug/ therapeutic response
  • detect changes in pharmacokinetics
  • monitor compliance
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15
Q

Classical AEDs

A
  • phenytoin
  • phenobarb
  • carbamazepine
  • valproate
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16
Q

Newer AEDs

A
  • lamotrigine

- Levetiracetam

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17
Q

Drugs that modulate volatge dependent ion channels

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A
  • carbamazepine
  • phenytoin
  • valproid acid
18
Q

How do benzos work?

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A
  • increase the frequency of GABA-mediated chloride channel openings
19
Q

How does phenobarb work?

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A
  • prolongs GABA-mediated chloride channel openings

- block the voltage-dependent sodium channels

20
Q

Pleiotropic AEDs

Study These Flashcards
A
  • Lamotrigine

- valproate

21
Q

How does lamotrigine work?

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A
  • blocks sodium channels
  • may interfere with glutamate release
  • inhibits Ca ++ channels
22
Q

How does valproate work?

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A
  • enhances GABA transmission
  • blocks sodium channels
  • augment K+ channels
23
Q

Inducers of Cyt p450

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A
  • phenobarb
  • phenytoin
  • carbamazepine
24
Q

Inhibitor of Cyt p450

Study These Flashcards
A

Sodium valproate

25
How does phenytoin work?
- inhibits Na+ channels to inhibit generation of rapid AP
26
Adverse effects of phenytoin
- CNS sedation - gum hyperplasia - hirsuitism - skin rash hypersensitivity
27
Interactions with phenytoin
- valproate displaces phenytoin from plasma proteins | - increase cyt p450
28
Adverse effects of carbamazapine
- diplopia and ataxia - idiosyncratic skin reaction - agranulocytosis and aplastic anaemia
29
Interactions with carbamazepine
- induces microsomal enzymes | - stimulates its own metabolism
30
Adverse effects of phenobarb
- CNS sedation - skin rashes if allergic - tolerance and physical dependence
31
Interactions with phenobarb
- stimulates cyt p450 | - CNS depression with in combo with benzos
32
Adverse effects of valproate
- elevation of liver enzymes | - birth defects
33
Interactions with valproate
- displaces phenytoin from plasma proteins | - p450 inhibitor
34
Adverse effects of lamotrigine
- less CNS sedative | - potentially life-threatening dermatitis
35
Why might patient have cross-sensitivity to multiple AEDs?
- carbamazepine - phenytoin - phenobarb Are all aromatic AED - get oxidised to arene oxide (which is toxic)
36
Adverse effects of benzos
- CNS sedative | - tolerance, dependence
37
Definition of status epilepticus
5 minutes or more of continuous - clinical or electrographic seizure activity - recurrent seizure activity without recovery between
38
General measure in status epilepticus
- start treatment immediately - ABCs - blood glucose - electrolytes and anticonvulsant levels
39
Stepwise management of status epilepticus
- benzodiazepine - phenytoin (20mg/kg) - phenobarbital (20-39mg/kg) - RSI (propofol) (2-5mg/kg, then infusion)
40
Problems with AEDs in pregnancy
- sodium valproate higher teratogenic potential - folate supplementation before pregnancy considered - pharmacokinetics change, so adjust dose
41
Problems with ARVs and epilepsy
- phenytoin and carbamazepine are enzyme inducing - potential drug interactions - in HIV-infected women of child bearing age, lamotrigine is preferred to valproate

Pharmacology (5th year) (15 decks)

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