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Anaesthetic FRCA Primary - eLFH Pharmacology > eLFH - Drugs used to treat Epilepsy > Flashcards

eLFH - Drugs used to treat Epilepsy Flashcards

1
Q

Cause of seizures

A

Repetitive neuronal discharges in CNS

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2
Q

Two main mechanisms of action of anticonvulsants

A

Action on CNS Na+ channels

Potentiating neurotransmitter GABA

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3
Q

Two main mechanisms for anticonvulsants acting on CNS Na+ channels

A

Inhibiting inactive fast Na+ channels - selective for abnormal neuronal discharges as these drugs have affinity for Na+ channels that are opening and closing rapidly

Stabilising presynaptic Na+ channels by inhibiting release of excitatory neurotransmitters

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4
Q

Drugs which inhibit inactive fast Na+ channels examples

A

Phenytoin

Sodium valproate

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5
Q

Drugs which stabilise presynaptic Na+ channels examples

A

Lamotrigine

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6
Q

Three main mechanisms for anticonvulsants to potentiate GABA

A

Facilitating GABA

GABA agonists

Inhibiting GABA transaminase

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7
Q

Facilitating GABA mechanism

A

Opening Cl- channels causes cell hyperpolarisation

Therefore less excitable and reduces neuronal transmission

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8
Q

Example of drugs which facilitate GABA

A

Benzodiazepines

Barbiturates

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9
Q

GABA agonist examples

A

Baclofen

Acamprosate

Used for their other effects

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10
Q

Inhibiting GABA transaminase mechanism

A

GABA transaminase is the enzyme which catalyses GABA breakdown

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11
Q

Example of drugs which inhibit GABA transaminase

A

Sodium valproate

Vigabatrin

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12
Q

Phenytoin mechanism of action

A

Binds to inactive or refractory fast Na+ channels after opening

Therefore most effective against channels opening and closing at high frequency

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13
Q

Phenytoin administration

A

PO or IV

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14
Q

Phenytoin monitoring

A

Narrow therapeutic window

Monitor plasma levels

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15
Q

Phenytoin uses

A

Generalised seizures

Partial seizures

Status epilepticus

Trigeminal neuralgia

Class 1b anti-arrhythmic - used for digoxin toxicity arrhythmias

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16
Q

Side effects of phenytoin

A

Hirsutism

Gum hyperplasia

Acne

Peripheral neuropathy

Megaloblastic anaemia

17
Q

Symptoms of phenytoin toxicity

A

Ataxia

Nystagmus

Paraesthesia

Slurred speech

18
Q

Cautions for phenytoin use

A

Teratogenic

cP450 inducer

19
Q

Phenytoin pharmacokinetics

A

90% protein bound

Liver metabolism to inactive metabolites

Renal excretion

Zero order kinetics replace First order kinetics at high drug concentrations due to enzyme saturation

20
Q

Phenytoin half life

A

~ 24 hours

21
Q

Sodium valproate administration

A

IV or PO

22
Q

Sodium valproate uses

A

Partial seizures

Generalised seizures

Myoclonic seizures

Chronic pain - trigeminal neuralgia

23
Q

Sodium valproate mechanism of action

A

Binds to inactive fast Na+ channels after opening

AND

Inhibits GABA transaminase

24
Q

Side effects of sodium valproate

A

Liver dysfunction
GI upset
Alopecia
Thrombocytopenia
Teratogenic - neural tube defects

25
Q

Sodium valproate pharmacokinetics

A

90% protein bound

Liver metabolism

Renal excretion

26
Q

Use of Lamotrigine

A

In pregnancy - less teratogenic

27
Q

Gabapentin mechanism of action

A

Increases GABA synthesis in brain

Modulates voltage gated Ca2+ channels

Inhibits excitatory glutamate

Increases 5-HT (serotonin) levels in CNS

28
Q

Gabapentin use

A

Almost exclusively used in chronic pain

29
Q

Types of GABA receptor

A

GABA A - chloride ion channel increasing intracellular Cl-

GABA B - G protein coupled receptor which increases intracellular K+

30
Q

Benzodiazepine pharmacokinetics

A

Lipid soluble

Active and inactive metabolites

Renally excreted

31
Q

Benzodiazepine effects on respiratory system

A

Depressant

Reduces TV and RR

32
Q

Benzodiazepine effect on cardiovascular system

A

Relatively cardio stable

Slight reduction in SVR but slight increase in HR

Anaesthetic FRCA Primary - eLFH Pharmacology (11 decks)

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