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Pharmacology > Epilepsy Drugs > Flashcards

Epilepsy Drugs Flashcards

1
Q

Ethosuximide mechanism of action

A

Blocks thalamic T-type Ca2+ channels

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2
Q

Side effects associated with ethosuximide

A

GI distress, fatigue, headache, urticaria, Stevens-Johnson syndrome

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3
Q

Used to treat status epilepticus

A
  1. Benzodiazepines (diazepam, lorazepam) – 1st line for acute situations
  2. Phenytoin (1st line for prophylaxis)
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4
Q

Benzodiazepine mechanism of action

A

Increased GABAA channel activity

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5
Q

Side effects of benzodiazepines

A

Sedation, tolerance, dependence, respiratory depression

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6
Q

Uses of phenytoin

A
  1. Simple partial seizures
  2. Complex partial seizures
  3. Generalized tonic-clonic seizures (1st line)
  4. Status epilepticus
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7
Q

Phenytoin mechanism of action

A

Increases Na+ channel inactivation

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8
Q

Side effects of phenytoin

A

Nystagmus, diplopia, ataxia, sedation, gingival hyperplasia, hirsutism, peripheral neuropathy, megaloblastic anemia, teratogenesis (fetal hydantoin syndrome), SLE-like syndrome, induction of cytochrome P450, lymphadenopathy, Stevens-Johnson syndrome, osteopenia

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9
Q

Version of phenytoin for parenteral use

A

Fosphenytoin

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10
Q

Uses of carbamazepine

A
  1. Simple partial seizures (1st line)
  2. Complex partial seizures (1st line)
  3. Generalized tonic-clonic seizures (1st line)
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11
Q

Carbamazepine mechanism of action

A

Increased Na+ channel inactivation

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12
Q

Side effects associated with carbamazepine

A

Diplopia, ataxia, blood dyscrasias (agranulocytosis, aplastic anemia), liver toxicity, teratogenesis, induction of cytochrome P450, SIADH, Stevens-Johnson syndrome

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13
Q

1st line drug for trigeminal neuralgia

A

Carbamazepine

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14
Q

Uses of valproic acid

A
  1. Simple partial seizures
  2. Complex partial seizures
  3. Generalized tonic-clonic seizures (1st line)
  4. Absence seizures
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15
Q

Valproic acid mechanism of action

A
  1. Increased Na+ channel inactivation

2. Increased GABA concentration via inhibition of GABA transaminase

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16
Q

Side effects associated with valproic acid

A

GI distress, rare but fatal hepatotoxicity (measure LFTs), neural tube defects (e.g., spina bifida), tremor, weight gain

Remember: valproic acid is contraindicated in pregnancy

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17
Q

Uses of gabapentin

A
  1. Simple partial seizures

2. Complex partial seizures

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18
Q

Gabapentin mechanism of action

A

Primarily inhibits high-voltage-activated Ca2+ channels

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19
Q

Side effects of gabapentin

A

Sedation, ataxia

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20
Q

In addition to being used as an anti-epileptic agent, gabapentin is also used to treat…

A

Peripheral neuropathy and postherpetic neuralgia

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21
Q

In addition to being used as an anti-epileptic agent, valproic acid is also used to treat…

A

Myoclonic seizures and bipolar disorder.

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22
Q

Uses of phenobarbital

A
  1. Simple partial seizures
  2. Complex partial seizures
  3. Generalized tonic-clonic seizures
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23
Q

Phenobarbital mechanism of action

A

Increases GABAA channel activity

24
Q

Side effects of phenobarbital

A

Sedation, tolerance, dependence, induction of cytochrome P450, cardiorespiratory depression

25
Q

1st line anti-epileptic drug in neonates

A

Phenobarbital

26
Q

Uses of topiramate

A
  1. Simple partial seizures
  2. Complex partial seizures
  3. Generalized tonic-clonic seizures
27
Q

Topiramate mechanism of action

A
  1. Blocks Na+ channels

2. Increases GABA action

28
Q

Side effects associated with topiramate

A

Sedation, mental dulling, kidney stones, weight loss

29
Q

Which anti-epileptic drug is also used to prevent migraine?

A

Topiramate

30
Q

Uses of lamotrigine

A
  1. Simple partial seizures
  2. Complex partial seizures
  3. Generalized tonic-clonic seizures
  4. Absence seizures
31
Q

Lamotrigine mechanism of action

A

Blocks voltage-gated Na+ channels

32
Q

Why must lamotrigine be titrated slowly?

A

To prevent Stevens-Johnson syndrome

33
Q

Uses of levetiracetam

A
  1. Simple partial seizures
  2. Complex partial seizures
  3. Generalized tonic-clonic seizures
34
Q

Levetiracetam mechanism of action

A

Unknown; may modulate GABA and glutamate release

35
Q

Uses of tiagabine

A
  1. Simple partial seizures

2. Complex partial seizures

36
Q

Tiagabine mechanism of action

A

Increases GABA levels by inhibiting reuptake

37
Q

Uses of vigabatrin

A
  1. Simple partial seizures

2. Complex partial seizures

38
Q

Vigabatrin mechanism of action

A

Increases GABA levels by irreversibly inhibiting GABA transaminase

39
Q

Give some examples of barbiturates

A
  1. Phenobarbital
  2. Pentobarbital
  3. Thiopental
  4. Secobarbital
40
Q

Mechanism by which barbiturates work

A

Facilitate GABAA action by increasing duration of Cl- channel opening and thus decreasing neuron firing

41
Q

In which condition are barbiturates contraindicated?

A

Porphyria

42
Q

Clinical uses of barbiturates

A

Sedative for anxiety, seizures, insomnia, induction of anesthesia (thiopental)

43
Q

Barbiturate toxicities include…

A
  1. Respiratory and cardiovascular depression
  2. CNS depression (can be exacerbated by EtOH use)
  3. Dependence
  4. Drug interactions (induces cytochrome P450)
44
Q

Give some examples of benzodiazepine drugs

A
  1. Diazepam
  2. Lorazepam
  3. Triazolam
  4. Temazepam
  5. Oxazepam
  6. Midazolam
  7. Chlordiazepoxide
  8. Alprazolam
45
Q

Mechanism by which benzodiazepines work

A

Facilitate GABAA action by increasing the frequency of Cl- channel opening; decreases REM sleep

46
Q

Most benzodiazepines have long half-lives and active metabolites. Exceptions include…

A
  1. Alprazolam
  2. Triazolam
  3. Oxazepam
  4. Midazolam

These drugs are short acting and their use is characterized by higher addictive potential.

47
Q

Clinical uses of benzodiazepines

A
  1. Anxiety
  2. Spasticity
  3. Status epilepticus (lorazepam and diazepam)
  4. Detoxification (especially alcohol withdrawal–DTs)
  5. Night terrors
  6. Sleepwalking
  7. General anesthetic (causes amnesia, muscle relaxation)
  8. Hypnotic (used to treat insomnia)
48
Q

Benzodiazepine toxicities

A
  1. Dependence
  2. Additive CNS depression effects with alcohol
  3. Less risk of respiratory depression and coma than with barbs
49
Q

Treat benzodiazepine overdose with…

A

Flumazenil (competitive antagonist at GABA receptor)

50
Q

Can be used to treat absence seizures

A
  1. Ethosuximide (first-line agent)
  2. Valproic acid
  3. Lamotrigine
51
Q

List some nonbenzodiazepine hypnotics

A
  1. Zolpidem
  2. Zaleplon
  3. Eszopiclone
52
Q

Describe the mechanism by which nonbenzodiazepine hypnotics work.

A

Act via the BZ1 subtype of the GABA receptor. Effects are reversed by flumazenil.

53
Q

Nonbenzodiazepine hypnotics are used to treat…

A

Insomnia

54
Q

Side effects of nonbenzodiazepine hypnotics

A

Ataxia, headache, confusion, decreased risk of dependence as compared to benzodiazepine use

55
Q

Unlike older sedative-hypnotics, nonbenzodiazepine hypnotics cause only modest…

A

Day-after psychomotor depression and few amnestic effects

Pharmacology (9 decks)

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