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Pharmacology > Anti-epileptics > Flashcards

Anti-epileptics Flashcards

1
Q

How do VGSC blockers prevent epilepsy?

A

Bind to sodium channels in depolarisation, prolonging inactivation state, and reducing the likelihood of excessively high frequency action potentials.

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2
Q

Give 3 examples of 3 VGSC blocker anti-epileptics

A

Phenyotin, Carbamezapine and Lomatrigene

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3
Q

What 3 clinical advantages does lamotrigene have over other VGSC blocker anti-epileptics?

A

It is safer to use in pregnancy, has less occurrence of CNS ADRs, and can be used to treat absence seizures unlike other VGSC blockers.

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4
Q

What are some ADRs of phenytoin?

A

Dizziness, ataxia, headache, nystagmus, anxiety, ginigival hyperplasia, hepersensitity rashes, Steven-Johnson Syndrome

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5
Q

What DDIs can phenytoin cause?

A

Anything metabolised by CYP450 as it is an inducer, Cimetidine, and NSAIDs or other heavily protein bound drugs.

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6
Q

Why does phenytoin in particular need clinical monitoring?

A

It has non-linear pharmacokinetics.

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7
Q

How can phenytoin be administered?

A

Oral or IV

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8
Q

How can carbamezapine be administered?

A

Oral or rectal

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9
Q

What is a contraindication of carbamezapine use?

A

AV block

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10
Q

What are some ADRs of carbamezapine?

A

Dizziness, drowsiness, ataxia, motor disturbance, numbness, tingling, BP increases or decreases, rash, hyponatraemia and myelosupression.

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11
Q

Why is carbamezapines half-life variable and how does it change?

A

Carbamezapine is a strong CYP450 inducer, and it itself is metabolised by carbamezapine, so on giving a second dose it’s half-life decreases from 30 hours to 15 hours.

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12
Q

What DDI interferes with carbamezapine action?

A

Anti-depressants.

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13
Q

What is a contraindication for lamotrigene?

A

Liver disease

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14
Q

What are some ADRs of lamotrigene?

A

Dizziness, ataxia, somnolence and rashes.

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15
Q

What DDIs affect lamotrigene?

A

It’s levels are decreased in the presence of the OCP, but are increased in the presence of sodium valproate.

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16
Q

How do GABA mediated inhibition enhancers prevent epilepsy?

A

Raise levels or action of GABA, which itself acts to cause increased chloride post-synaptic influx, raising action potential thresholds in the central nervous system.

17
Q

How can sodium valproate and benzodiazapines be administered?

A

Orally and intravenously

18
Q

What is a contraindication of sodium valproate?

A

Liver disease.

19
Q

How does sodium valproate work?

A

It is a weak inhibitor of GABA inactivation enzymes, it is a weak agonist for GABA synthesis enzymes, and it is a weak VGSC and VGCC blocker.

20
Q

What are some ADRs of sodium valproate?

A

Ataxia, tremor, weight gain, and liver dysfunction/failure.

21
Q

What drugs antagonise sodium valproate action?

A

Antidepressants and antipsychotics.

22
Q

What drugs commonly displace or are displaced by sodium valporate from plasma proteins?

A

Sodium valproate commonly displaces phenytoin and lamotrigene, but is displaced itself by aspirin.

23
Q

What is the half-life of sodium valproate?

A

15 hours.

24
Q

What clinical monitoring is required in sodium valproate?

A

Liver function tests.

25
Q

How do benzodiazapines work?

A

Bind to receptors on GABA receptor/ Cl-channels. It also has positive allosteric effects, whereby increased benzodiazapine binding causes increased GABA binding and vice versa.

26
Q

What are 3 benzodiazapines and what are they used for?

A

Diazepam, Lorazepam and Clonazepam. All 3 can be used for treating anxiety disorders. Diazepam and Lorazepam are used in status epilepticus. Clonazepam can be used for absence seizures and short term use.

27
Q

What is a contraindication of benzodiazapine use?

A

Respiratory depression

28
Q

What are ADRs of benzodiazapines?

A

Sedation, dependance, tolerance, confusion, ataxia, aggression, CNS depression and respiratory depression.

29
Q

What can sudden withdrawal of benzodiazapines cause?

A

Seizures

30
Q

What reverses benzodiazapines, and what are risks of using it?

A

IV Flumazenil, and in some cases it can cause seizures or arrhythmias.

31
Q

What anti-epileptics can cause OCP failure?

A

Phenytoin and carbamezapine

32
Q

What are some common teratogenic effects of anti-epileptics?

A

Neural tube defects, neurological dysfunction,learning difficulties, vitamin K deficiancy (leading to cerebral haemorrhage), facial hypoplasia and digital hypoplasia. Benzodiazapines specifically can cause cleft lip and palate.

33
Q

What drugs are used in status epilepticus?

A

Intravenous phenytoin and lorzepam.

Pharmacology (19 decks)

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