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Pharmacology > Anticonvulsants > Flashcards

Anticonvulsants Flashcards

1
Q

Name 3 mechanisms of actions of anticonvulsants

A
  • prolong inactivated state of voltage gated Na and Ca channels presynaptically: reduce likelihood repetitive action potentials, reduce necerotransmitter release, prevent seizure spread
  • enhance effects of GABA (inhibitory) via GABA - A receptor complex:open ligand gated Cl channels causing suppression of discharges
  • inhibit effects of excitatory neurotransmitter, glutamate, via NMDA receptor (and ampa R): prevent opening ligand gated Na and Ca channels
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2
Q

Name the 4 sites on the gaba-a r complex

A 
• GABA site
• Benzo
• barbiturate
• alcohol
(All neuroinhibitory) 4 bs
All very addictive.
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3
Q

Name 5 anticonvulsants that prolong the inactivated state of voltage dependent Na and Ca channels

A
  • Phenytoin
  • carbamazepine
  • valproate
  • oxcarbazepine
  • lamotrigine
  • topiramate
  • gabapentin
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4
Q

Name 3 anticonvulsants that inhibit effects of excitatory neurotransmitter glutamate by modulating NMDA (and ampa) receptors (nmda antagonists)

A 
• Topiramate
• magnesium
• felbamate
Zonisamide
(Lamotrigine)
(Ketamine)
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5
Q

Name 3 classes anticonvulsants with examples that enhance effects of inhibitory neurotransmitter GABA

A

• GABA site (inhibit GABA transaminase irreversibly): vigabatrin
• benzodiazepines (bind at GABA A r site): diazepam, clonazepam
• barbiturates: phenobarbitone
(GABA agonists: gabapentin)

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6
Q

Name an important side effect of phenytoin and carbamazepine Due to their action on CYP 450

A

Inducers

Vit D hypermetabolised causing osteopenia.

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7
Q

Name 3 indications phenytoin

A

Generalised and partial seizures, status epilepticus

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8
Q

Name 2 important pharmacokinetic components of phenytoin

A

• High protein binding 95% (increased risk toxicity if displaced)
• liver metabolism saturable: zero order kinetics (small increase dose may cause unpredictable increase in Cp with toxicity)
Old drug, so risks toxicity high

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9
Q

Name 5 important adverse effects phenytoin

A
  • CNS: cerebellar syndrome, sedation
  • allergic effects with cross sensitivity to carbamazepine: rash, hepatitis
  • skin and collagen: gum hypertrophy, coarsening of facial features, hirsutism
  • haem: megaloblastic anemia
  • teratogenic: malformations
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10
Q

Name 5 indications carbamazepine

A

• Partial seizures
• generalised seizures, excluding absence and atonic
Other
• mood stabiliser bipolar disorder prophylaxis
• trigeminal neuralgia and other chronic pain syndromes
• chronic dystonic disorders
• intractable hiccups , neurohypophyseal diabetes insipidus

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11
Q

Name 5 adverse effects carbamazepine

A 
• Ataxia
• nystagmus
• dysarthria
• vertigo
• sedation
Common but not severe, occur when levels > 8,5 mg/l
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12
Q

Name 2 drug interactions carbamazepine

A
  • Maoi: contraindicated

* CYP450 inducer: reduce efficacy warfarin, theophylline, oc, other anticonvulsants

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13
Q

Name 2 indications phenobarbitone

A

Barbiturates
• generalised and partial seizures
Second line! Too sedative in adults, behavioural disturbances in children, very addictive

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14
Q

Name 2 indications sodium valproate

A

Partial and generalised epilepsy
First line
Juvenile myoclonic epilepsy

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15
Q

Name 3 adverse effects sodium valproate

A 
• git
• liver failure and hepatic necrosis, rare.
• pancreatitis
• Hair loss -
Teratogen:ntd
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16
Q

Indication ethosuxamide?

A

Drug of choice for absence seizures children

Not others seizures, may make them worse

17
Q

Indication gabapentin?

A
  • Add on for absence seizures

* partial and generalised epilepsy monotherapy

18
Q

Gabapentin AE?

A

Somnolence

19
Q

Lamotrigine indications? (3)

A
  • Partial seizures
  • generalised
  • absence
20
Q

Contraindication lamotrigine?

A

Liver or renal failure

21
Q

Lamotrigine adverse effects (2)

A

• Hypersensitivity rashes: Steven’s Johnsons, toxic epidermal necrolysis, angioedema
• flu-like symptoms
Rare

22
Q

Name 2 indications topirimate

A

Generalised and partial seizures

Newer drug

23
Q

Name 5 adverse effects topirimate

A
  • Poor concentration and memory
  • Impaired speech
  • ataxia
  • somnolence
  • anorexia and taste perversion
  • syndrome of acute myopia associated with secondary closed angle glaucoma
24
Q

Vigabatrin indication

A

Last resort for epilepsy due to significant irreversible visual defects

25
Q

Vigabatrin contraindication?

A

History of psychosis: hallucinations as side effect

26
Q

Vigabatrin excretion?

A

Excreted unchanged by kidneys therefore not metabolised in liver

27
Q

Vigabatrin adverse effects? (3)

A
  • Drowsiness common!
  • visual hallucinations!
  • ocular potentially irreversible: retinal changes, visual field defects, photophobia
28
Q

Oxcarbazepine indications? ( 2)

A

Partial and generalised seizures
Add on in partial seizures
Carbamazepine derivative

29
Q

Clonazepam indications as antiepileptic? (5)

A 
Benzo
Long term for:
• motor seizures childhood
• absence
• infantile spasms
• complex partial seizures
• myoclonic epilepsy as add on treatment
• status epilepticus
30
Q

Name the 4 properties of actions of benzos

A

•Anxiolytic
.Hypnotic
• muscle relaxant
• anticonvulsant- not for long term use except clonazepam

31
Q

Name 4 benzos that are first line agents in status epilepticus

A
  • Diazepam
  • clobazepam
  • lorazepam
  • clonazepam
32
Q

Name the 6 steps of treatment of status epilepticus

A

1 Iv Benzo eg diazepam 10 mg over 5 minutes. Rectal in kids
2. Repeat benzos if continue
3. Iv phenytoin loading dose to prevent relapse
4 identify precipitants eg hypoglycaemia, alcohol, overdose, low plasma concentration
5.icu with Anaesthetist to administer iv thiopentone / chloromethiazole /propofol if still no response
6. Paraldehyde rectally if no facilities

33
Q

First line treatment Janz syndrome/juvenile myoclonic epilepsy?

A

Valproate

34
Q

Which anticonvulsant safest in pregnancy?

A

Lamotingine

Pharmacology (34 decks)

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