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PHARMACOLOGY > ANTIEPILEPTIC AGENTS > Flashcards

ANTIEPILEPTIC AGENTS Flashcards

1
Q

epilepsy

A

condition characterized by seizures, in unpredictable manner, not associated with stimulus

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2
Q

seizure

A

episode of disordered, synchronized, rhythmic firing of brain neurons

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3
Q

causes of epileptic seizures

A 
birth/ perinatal injuries
blood clots
head trauma
metabolic disturbances
drug/alcohol withdrawal
neoplasia
infection
genetic
hyperthermia in children
visual stimuli
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4
Q

describe partial seizures

A
  1. COMPLEX PARTIAL (most frequent)
    - partial consciousness with/without autonomic movements
  2. SIMPLE PARTIAL
    - conscious state not affected
    - localised speech/sensory/motor defects
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5
Q

describe general seizures

A
  1. GRAND MAL
    - loss of consciousness + rigid paralysis (TONIC state)
    - rhythmic jerking movement of limbs (CLONIC state)
  2. PETIT MAL (absence seizure)
    - person suddenly exhibits a blank stare + unaware of surroundings
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6
Q

describe the effects of seizures on electroencephalographs

A

tonic - disorder (+) amplitdue
clonic - strokes of high rhythmic activity

petit mal - very rhythmic (+) amplitude

partial - distinctive - only effecting certain parts of brain

best treatment = detect whilst undergoing seizure

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7
Q

what does a PET scan do

A

measure areas of high metabolism

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8
Q

Kindling model

A

repeated electrical stimulation of amygdaloid nuclei = induce state where spontaneous seizures can occur

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9
Q

Kainate model

A

KAINATE + NMDA (agonists of glutamate receptors)
= produce spontaneous seizures and PAROXYSMAL DEPOLARISING SHIFT (PDS)
- suggesting overstimulation of glutamate receptors trigger seizures

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10
Q

what can induce PDS

A

penicilin

NMDA

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11
Q

Evidence that seizures can be induced by a deficit in INHIBITORY AMINO ACID NT

A

. GAGA receptor antagonists can induce seizures in animal model system
. drugs that have anti-seizure activities
= enhance activity of GABA (benzodiazepines)
OR
= inhibit GABA degradative pathways
= GABA reuptake inhibitors

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12
Q

3 mechanisms of anti-epileptics

A
  1. enhancement of GABA binding to receptor
  2. inhibition of Na+ channel
  3. inhibition of Ca2+ channel
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13
Q

primary antiepileptic drugs

A
  • PHENYTOIN
  • CARBAMAZEPINE
  • VALPROATE
  • ETHOSUXIMIDE
  • BENZODIAZEPINES
  • BARBITUATES
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14
Q

PHENYTOIN

A

Voltage-gated Na+ channel blocker -binds to inactive channels

•Grand mal and partial; not effective in petit mal
Treats status epilepticus

  • Drug interactions: Competes for the metabolism of other drugs including oral anticoagulants
  • Side effects: dizziness, nystagmus*, ataxia^, mental confusion, gingival hyperplasia, hirsutism, birth defects
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15
Q

where does PHENYTOIN bind

A

Phenytoin preferentially binds to the inactivation gate of Na2+ channels when they are in the closed position

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16
Q

CARBAMAZEPINE

A
  • Derivative of Tricyclic Antidepressants
  • Voltage-gated Na+ channel blocker + accentuation of adenosine-based inhibition of neuron firing
  • Grand mal and partial; not effective in petit mal

• Side effects: drowsiness, dizziness, blurred vision,
ataxia, bone marrow depression (granulocytopenia
and/or aplastic anemia), birth defects

17
Q

VALPROATE

A
  • Voltage-gated Na+ channel blocker
  • Works on all types of epilepsy, including petit mal

• Side effects: Nausea, vomiting, lethargy, hair
loss, teratogenic, hepatotoxicity

18
Q

ETHOSUXIMIDE

A

• Derived from barbiturate structure

  • Inhibition of T-type (thalamic) calcium channels
  • Only useful for PETIT mal // worsen grand mal seizures

• Side effects: nausea, vomiting, anorexia, drowsiness, persistent hiccups

19
Q

BENZODIAZEPINES and BARBITUATES

A

• bind to GABAA receptors = affinity of GABA for the receptor is enhanced

  • Effective against all types (except petit mal)
  • Epilepsy is only condition, other than GE, for which barbituates have a legitimate clinical use

• Sedation, general CNS suppression are problems, along with dependence + withdrawal

20
Q

Other Antiepileptic Drugs

A

• Vigabatrin-a GABA analogue
= Irreversible inhibitor of GABA transaminase in astrocytes

  • Lamotrigine = voltage-gated Na+ channel blocker
  • Gabapentin = cyclic analogue of GABA - blocks Ca2+ channels in Dorsal Horn of SC = inhibits NMDA R and increases actions of CNS adrenergic neurons

PHARMACOLOGY (24 decks)

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