pharamacology of anticonvulsants Flashcards

1
Q

When can someone get a seizure? What about in epilepsy?

A

Anyone can get seizure if stressed enough. Epilepsy is susceptible to seizures (threshold of stress not very high to cause seizure)

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2
Q

When do you start medication for seizures?

A

More than 1 seizure or evidence that threshold for seizure is low

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3
Q

What is the therapeutic objective for epilepsy?

A

Eliminate/reduce seizures, avoid side effects of long-term epileptic drugs, return person to normal psychological/vocational activities

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4
Q

What is important to tell people with epilepsy?

A

That they cant drive car (need to tell DVLA). If you don’t you can lose license

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5
Q

What is key to reducing frequency and severity of allergic skin reactions with lamotrigine?

A

introducing lamotrigine gradaually

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6
Q

When is sodium valproate contraindicated and why?

A

Women of child-bearing age because it has reproductive toxicity - can affect fetus (teratogenic effects) leading to neural defects, decreased IQ, autism etc

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7
Q

What is the relationship between lamotrigine and the oral contraceptive pill? What can you do to combat this?

A

Lamotrigine does not effect efficacy of OCP. OCP affects efficacy of lamotrigine because oestrogen induces metabolism of lamotrigine by upregulating enzyme that metabolises lamotrigine, so decreases lamotrigine levels. Either change contraception (best choice), change to different drug, or increase dose (hard to titrate doses)

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8
Q

What symptoms could they have if on OCP and lamotrigine at different times?

A

At 2nd/3rd weeks when oestrogen is high can get decreased dose of lamotrigine and therefore more seizures. On 4th week where there is pill break and oestrogen is low may get effects of too much lamotrigine giving depressed side effects.

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9
Q

When hospitalized for seizure what is first line treatment? What if this is unavailable?

A

First line treatment is lorazepam 4mg IV as single dose initially and repeat dose after 10-20 minutes if required (if seizure not terminated after first dose). If lorazepam unavailable give IV diazepam or buccal midazolam

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10
Q

What is difference in seizure in hospital treatment and seizure in community treatment?

A

In hospital benzodiazepines used. IV lorazepam works best. In community give buccal midazolam (quick administration)

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11
Q

What is mechanism of lamotrigine?

A

Blocks voltage gated sodium channels preventing sodium ion influx, preventing depolarisation of glutaminergic neurones & reducing glutamate excitotoxicity.

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12
Q

What is target of lamotrigine?

A

Voltage gated sodium channels

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13
Q

What are side effects of lamotrigine?

A

Drowsiness, rash. Less common/serious: steven johnsons syndrome, suicidal thoughts.

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14
Q

Why drowsiness with lamotrigine?

A

Block all excitatory channels so slows down other parts of brain giving generalised depressive effect (lethargy, sleepy)

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15
Q

Mechanism of sodium valproate?

A

Inhibition of GABA transaminase so prevents breakdown of GABA, increasing concentrations of GABA in synapse and indirectly prolonging GABA in synapse by inhibiting its metabolism

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16
Q

Target of sodium valproate?

A

GABA transaminase

17
Q

Side effects of sodium valproate?

A

Stomach pain, diarrhoea, drowsiness, weight gain, hair loss. Serious: hepatotoxicity, teratogenic effects, pancreatitis.

18
Q

What effects does sodium valproate have on other drugs and why?

A

Is a broad CYP enzyme inhibitor so increases serum concentrations of many co-administered drugs

19
Q

Mechanism of diazepam?

A

Increases chloride ion influx in response to GABA binding at GABA-A receptor, leading to hyperpolarisation of excitatory neurones

20
Q

Target of diazepam?

A

Benzodiazepine site on GABA-A receptor (alosteric site)

21
Q

Side effects of diazepam?

A

Drowsiness, respiratory depression high dose or IV, uncommon -> haemolytic anaemia, jaundice

22
Q

Why isnt diazepam used for long term treatment of seizures?

A

Addiction prone people can become dependent on it

23
Q

Mechanism of levetiracetam?

A

Inhibition of synaptic vesicle protein SV2A, preventing vesicle exocytosis so reducing glutamate secretion and excitotoxicity

24
Q

What is site of levetiracetam?

A

Synaptic vesicle protein SV2A

25
Q

Side effects of levetiracetam?

A

Dizziness, somnolence, fatigue, headache

26
Q

Why is levetiracetam a good drug to use?

A

No effect on cytochrome P450 enzyme system so no drug-drug interactions (Favourable)