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Neuropharmacology & Neuroscience > Epilepsy > Flashcards

Epilepsy Flashcards

1
Q

What percentage of the population is estimated to have epilepsy?

A

~0.5%

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2
Q

What characterises epilepsy?

A

Abnormal high-frequency discharge of neurons

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3
Q

Unconsciousness during an epileptic episode often occurs when which brain region is involved?

A

The reticular formation

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4
Q

What is often thought to be the cause of abnormal discharge at the neuronal level?

A

The homeostasis of the neuro is unstable, leading it to reach a depolarising threshold more easily- this is a hyperexcitable state.
This may apply to enhance excitable neuronal activity or to dampen inhibitory neuron activity

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5
Q

What are two theories thought to cause a hyperexcitable state in neurons?

A

1) Na+, K+, Ca2+ and Cl- ion channels having mutations causing them to not maintain an appropriate resting membrane potential
2) ATPase is not fully functional meaning that ion pumps cannot maintain a stable electrochemical gradient and resting membrane potential

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6
Q

What is a partial seizure?

A

Abnormal neuronal discharge that begins and remains locally

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7
Q

What is a general seizure?

A

Abnormal neuronal discharge that spreads to encompass significant brain areas, including both hemispheres, and often involves a loss of conciousness

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8
Q

Name other classifications of seizures.

A

Complex, simple, tonic, clonic, atonic, myoclonic and absent

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9
Q

What are conditions that are similar to epilepsy?

A

Infantile seizures and epileptic syndrome

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10
Q

What is status epilepticus?

A

Continued and uninterrupted high-frequency discharge. This is life-threatening

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11
Q

What is excitotoxicity?

A

The repeated high frequency discharge of neurons can cause complex intracellular cascades that ultimately result in the death of the neuron

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12
Q

What percentage of patients are AEDs beneficial for?

A

Between 70-80%

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13
Q

How do AEDs work to decrease seizure activity?

A

They reduce the electrical excitability of the membranes

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14
Q

How do AEDs exert their effect?

A

By enhancing GABAs properties (increased production, decreased breakdown, synthetic agonists and increase GABA potentiation)
Another mechanism is to block T-type Ca2+ channels

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15
Q

What is a common issue with AEDs?

A

They can have severely harmful effects on developing foetuses

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15
Q

What is a common issue with AEDs?

A

They can have severely harmful effects on developing foetuses

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16
Q

Name 4 common AEDs

A

Phenytoin, carbamazepine, valproate and ethosuxamide

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17
Q

Comment on the use of Phenobarbitone as an AED

A

Not commonly used as it is toxic and a sedative

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17
Q

Comment on the use of Phenobarbitone as an AED

A

Not commonly used as it is toxic and a sedative

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18
Q

What is the mechanism of action of phenytoin?

A

It stabilises the membrane and inhibits post-tetanic potentiation by blocking voltage-dependent Na+ and Ca2+ channels. It also effects Ca2+ secretory processes

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19
Q

What is an issue with the administration of phenytoin?

A

It is a weak acid and consequently its intestinal absorption is highly variable; the plasma concentration is variable.

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20
Q

How is phenytoin metabolised?

A

By the microsomal system and then excreted in bile and urine

21
Q

Which other conditions is phenytoin useful for?

A

Peripheral neuralgia

22
Q

Name some drug that phenytoin can interact with

A

Chloramphenicol, isoniazid, cimetidine and dicumarol

23
Q

Name some of the adverse effects that phenytoin has

A

Toxic to the foetus, ataxia, diplopia, hirsutism, gingival hyperplasia and blood dyscrasia

23
Q

What is carbamazepine structurally similar to?

A

Tricyclic antidepressants

23
Q

When is carbamazepine useful?

A

Useful in psychomotor seizures, trigeminal neuralgia and mania

24
Q

Does carbamazepine have adverse effects?

A

yes

25
Q

What is the mechanism of action of valproate?

A

It facilitates glutamic acid decarboxylase and inhibits GABA transaminase

26
Q

What is valproate useful for treating?

A

Absent seizures

27
Q

What are the serious adverse effects of valproate?

A

It is hepatotoxic and teratogenic

28
Q

What are other adverse effects of valproate?

A

Nausea and anorexia

29
Q

What is the mechanism of action of ethosuximide?

A

It blocks T-type Ca2+ channels

30
Q

What are some side effects of ethosuximide?

A

Nausea and anorexia

31
Q

Name three benzodiazepine AEDs

A

Diazepam, nitrazepam and clonazepam

32
Q

When is diazepam useful?

A

In status epilepticus

33
Q

When is nitrazepam useful?

A

Partial, myoclonic and infantile seizures

34
Q

When is clonazepam useful?

A

Effective at treating myoclonic seizures and can be used for partial seizures and status epilepticus

35
Q

What is a common barbiturate?

A

Phenobarbitol, also known as luminal

36
Q

When is phenobarbitol useful?

A

In treating general tonic-clonic seizures and status epilepticus

37
Q

What is the primary mechanism of action of phenobarbitol?

A

Blocking presynaptic Ca2+ currents thus reducing neurotransmitter release

38
Q

What is the secondary mechanism of action of phenobarbitol?

A

It prolongs the time the Cl- channel is open in the post synaptic membrane

39
Q

What are some adverse effects of phenobarbitol?

A

It acts as a sedative and depressant. It also has significant drug interactions

40
Q

Vigabatrin is a new AED. What is its mechanism of action?

A

Covalently binds to and blocks GABA transaminase

41
Q

Lamotrigine is a new AED. What is its mechanism of action?

A

Reduces Na+ and Ca2+ activity as well as reducing EAA release

42
Q

Tiagabine is a new AED. What is its mechanism of action?

A

Prevents the uptake of GABA

43
Q

What are two more new AEDs?

A

Gabapentin and pregabilin

44
Q

Which drugs are useful in tonic clinic (GM) seizures?

A

Carbamazepine, phenytoin and valproate

45
Q

Which drugs are useful for partial/focal seizures?

A

Carbamazepine, phenytoin, valproate and clonazepam

46
Q

Which drugs are useful in Absence seizures (PM)

A

Ethosuximide and valproate

47
Q

Which drugs are useful in myoclonic seizures

A

Valproate and clonazepam

48
Q

Which drugs are useful in status epilepticus?

A

IV diazepam

49
Q

What non-epileptic uses are there for AEDs?

A

Anxiety, mania, chronic and neuropathic pain

50
Q

List 6 antispasmodics

A

Baclofen, Benzodiazepine, Tizanedine, Botox, Dantrolene and Cannabis

Neuropharmacology & Neuroscience (10 decks)

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