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Pharmocolgy > P20: Anticonvulsant Therapy > Flashcards

P20: Anticonvulsant Therapy Flashcards

1
Q

What happens to neurones when someone has epilepsy?

A
  • Large groups of neurones are activated repetitively and hypersynchronously
  • The inhibitory synapses between neurones also fail
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2
Q

What are the 2 main clinically defined classes of seizures?

A

Partial and generalised

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3
Q

During a partial seizure where in the brain does the discharge occur?

A

Discharge is confined to one part of the brain (e.g. cortex)

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4
Q

What are the two types of partial seizures?

A
  • Simple (no loss in consciousness)

- Complex (loss of consciousness to some degree)

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5
Q

Partial seizures that effect the motor cortex are termed?

A

Jacksonian seizure

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6
Q

Partial seizures that effect the Temporal lobe (mood) are termed?

A

Psychomotor seizure

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7
Q

Absence seizure (aka petit mal)

A

Loss of consciousness, vacancy and unresponsiveness <30s

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8
Q

Myoclonic seizure

A

Extremely brief (< 0.1 second) muscle contraction, jerky movements

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9
Q

Clonic seizure

A

Regularly repeating myoclonic seizures, typically of 2-3 /sec

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10
Q

Tonic-clonic seizure (aka Grand mal)

A
  • Initial muscle contraction (tonic phase), which may include tongue biting, urinary incontinence and absence of breathing
  • Followed by rhythmic muscle contractions (clonic phase)
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11
Q

Atonic seizure (aka petit mal)

A

Loss of muscle tone, causing collapse

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12
Q

What are some acquired causes of epilepsy

A
  • Trauma
  • Stroke
  • Tumours
  • Infection-induced
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13
Q

Generally how does epilepsy treatment work?

A
  • Suppressing excessive synaptic activity
    OR
  • Enhancing inhibitory neurotransmitter function
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14
Q

Name some epilepsy treatment drugs that interact with sodium channels to reduce activity

A
  • Phenytoin
  • Carbamazepine
  • lamotrigine
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15
Q

Name some epilepsy treatment drugs that enhance GABA activity

A
  • Phenobarbitone
  • Diazepam/lorezepam
  • Tiagebine
  • Gabapentine
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16
Q

Name some epilepsy treatment drugs that treat absence/petit mal seizures

A
  • Ethosuximide

- Valproic acid

17
Q

What is Phenytoin? (3)

A
  • Sodium channel modifier
  • Bind to inactive sodium channels that regulate membrane excitability and keep them closed for longer
  • USE DEPENDANT so more active a neurone is the most effective it is
  • Used for all seizures except petit mal seizures
18
Q

What is Carbamazepine? (3)

A
  • Sodium channel modifiers
  • Prolongation of Na+ channel inactive state
  • For grand mal and psychomotor partial seizures
19
Q

What are the adverse effects of using Carbamazepine?

A
  • Acute intoxication: coma, convulsions, respiratory depression
  • Chronic use: ataxia, vertigo, vomiting, hypersensitivity, hyponatraemia
  • May worsen petit mal seizures
20
Q

What is Phenobarbitone? (4)

A
  • GABA modifier, Barbiturate
  • Prolonging GABAa opening (hyperpolarisng post synaptic membrane)
  • Reduction in glutamate excitation
  • affective against all but absence seizures
21
Q

What are the adverse effects of using Phenobarbitone?

A
  • Sedation
  • Megaloblastic anaemia (give folic acid)
  • Osteomalacia (bone softening; give vitamin D)
  • Overactivity in children
22
Q

What is Diazepam/lorezepam? (2)

A
  • Promote GABAA opening
  • Increases Cl- channel opening
  • used in status epilepticus, i.v. diazepam is fast but sedative
23
Q

What is Tiagabine? (4)

A
  • Selective GABA reuptake inhibitor
  • Blocks GAT-1 transporter
  • So GABA not re-uptaken
  • Partial seizures only, may induce status epilepticus
24
Q

What are the side effects of Tiagabine?

A
  • Ataxia
  • Dizziness
  • Tremor
  • Depression
25
Q

What is Ethosuximide? (2)

A
  • Inhibits neuronal T-type voltage gated Ca2+ channels, reducing Ca2+ influx
  • Petit mal
  • These currents are important in bursting behaviour of thalamic neurones – common site for initiation of epileptiform waves
26
Q

What are the side effects of Ethosuximide?

A
  • Drowsiness
  • Euphoria
  • Ataxia
  • Anxiety
  • Aggressiveness
27
Q

What is Valproic Acid?

A
  • suitable for grand and petit mal
  • Inhibits GABA transaminase, increasing synaptic GABA
  • may also increase rate of GABA synthesis
  • Hyperpolarisng post synaptic membrane
  • Use-dependently inhibits voltage-gated Na+ channel activity
28
Q

What are the side effects of Valproic Acid?

A
  • Acute: nausea, vomiting

- Chronic: weight gain, hair loss, thrombocytopaenia, tremor

29
Q

How is phenytoin administered, and eliminated

A

orally well absorbed

eliminated by hepatic metabolism

30
Q

What are the adverse effects of phenytoin

A
  • Megaloblastic anaemia(folic acid given)
  • Hirsutism (hair growth following androgen release)
  • Gum hyperplasia
31
Q

What effect does carbamazepine inducing hepatic enzymes have

A

Reduces the effect of phenytoin, oral contraceptives and warfarin

32
Q

What does excessive and insufficient inhibitory transmission cause

A

excessive - loss of consciousness

insufficient - seizures

33
Q

What effect does phenobarbitone have on children

A

Hyperactivity

34
Q

What does tiagabine act on

A

Pre-synaptically and on glia

35
Q

What effect do barbiturates and benzodiazepines have on inhibitory GABA signalling

A

enhance GABAA Cl- channel flux

Pharmocolgy (22 decks)

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