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Pharmacology > Antiepileptic Drugs > Flashcards

Antiepileptic Drugs Flashcards

1
Q

Drugs for Partial and Generalized Tonic-Clonic Seizures

A 
Carbamazepine
Oxacarbazepine
Eslicarbazepine
Phenytoin
Fosphenytoin
Phenobarbital
Primidone
Valproate
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2
Q

Carbamazepine, Oxacarbazepine and Eslicarbazepine - MoA

A

Block voltage sensitive Na+ channels in neuronal cell membrane and inhibits the spread of abnormal electrical discharges from the seizure focus to other neurons by preventing the release of excitatory neurotransmitter from nerve terminals

Also blocks adenosine receptors in a way that leads to up-regulation of these receptors, and it blocks norepinephrine reuptake in the same way that tricyclic antidepressants block is.

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3
Q

Carbamazepine - Clinical use

A

Partial seizures
Generalized tonic-clonic seizure
Trigeminal neuralgia
Bipolar disease (alternative to lithium)

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4
Q

Carbamazepine - Adverse effects

A 
Drowziness
Ataxia
GI reactions (Nausea)
Aplastic Anemia (Rare)
Litium toxicity
Hyponatremia
Cognitive impairment
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5
Q

Carbamazepine - Interactions

A

Induce cytochrome P450 enzymes and accelerates metabolism of lamotrigine, phenytoin, topiramate and valproate.

Increase lithium toxicity

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6
Q

Oxacarbazepine - Clinical use

A

Trigeminal neuralgia

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7
Q

Eslicarbazepine - Clinical use

A

Partial-onset seizures as a sole agent (monotherapy) or as an adjunct to other AEDs

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8
Q

Phenytoin - MoA

A

Block voltage sensitive Na+ channels, by prolonging the inactivation state of the channel. Enables it to inhibit the repetitive firing of neurons in seizures.

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9
Q

Phenytoin - Clinical use

A

Partial seizure

Generalized tonic-clonic seizures

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10
Q

Phenytoin - Adverse effects

A

Interferes with folate metabolism and can lead to Megaloblastic anemia and fetal hydantoin syndrome (Cardiac defects, malformation of ears, lips, palate, mouth, and nasal bridge, mental retardation and microcephaly)

By impairing cerebellar function, phenytoin can cause ataxia, diplopia, nystagmus, and slurred speech.

By interfering with vitamin D metabolism and decreasing calcium absorption from the gut, phenytoin sometimes causes osteomalacia

Gingival hyperplasia (effects collagen metabolism)
Hirsutism
Steven-Johnsons symdrome
Toxic epidermal necrosis

Hypoprothrombinema and bleeding (give vitamin K supplements when using this drug)

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11
Q

Phenytoin - Interactions

A

Induce cytochrome P450 enzymes and accelerates the metabolism of other antiepileptic agents including felbamate, lamotrigine, topiramate, and valproate

It can also reduce levels of digoxin, steroids, vitamin K

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12
Q

Phenytoin - Contraindications

A 
Bradycardia
Hypersensitivity
Severe AV block
Sinoatrial dysfunction
Children because of adverse effects

Category D pregnancy; may reduce folate levels, two to three times increased risk of birth defects, fetal hydatoin syndrome

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13
Q

Phenobarbital - MoA

A

Enhances GABA-mediated chloride flux that causes membrane hyperpolarization.

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14
Q

Phenobarbital - Clinical use

A

Partial seizures

Generalized tonic-clonic seizures

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15
Q

Phenobarbital - Adverse effects

A 
Ataxia
Dizziness
Drowsiness
Cognitive impairment
Respiratory depression
Hypersensitivity (most frequently manifests as rash)
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16
Q

Phenobarbital - Contraindications

A

Hypersensitivity
Porphyria
Respiratory depression
Severe liver disease

Category D pregnancy; bleeding at birth, minor congenital defects

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17
Q

Primidone - MoA

A

Block sodium channels and preventing membrane depolarization. It can also potentiate GABA via formation of phenobarbital

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18
Q

Primidone - Clinical use

A

Partial seizures
Generalized tonic-clonic seizures
Essential tremor with propranolol

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19
Q

Primidone - Adverse effects

A 
Ataxia
Dizziness
Drowsiness
Cognitive impairment
Respiratory depression
Hypersensitivity (most frequently manifests as rash)
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20
Q

Primidone - Contraindications

A

Hypersensitivity

Category D Pregnancy

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21
Q

Valproate - MoA

A

Inhibit voltage sensitive sodium channels and T-type calcium channels; increase GABA synthesis and decreases GABA degradation; and it may decrease glutamate synthesis. By these actions, valproate inhibits the repetitive firing of neurons and the spread of epileptic seizures.

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22
Q

Valproate - Clinical use

A 
Broadest spectrum
Partial seizures
All forms of generalized seizures
Manic phase of bipolar (alternative to lithium)
Migraine prophylaxis
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23
Q

Valproate - Adverse effects

A 
Mild hepatotoxicity
Fetal hepatotoxicity (Rare)
Spina bifida
Weight gain
Impaired cognitive development
Nausea 
GI complaints
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24
Q

Valproate - Interactions

A

Inhibits cytochrome P450 enzymes, increases levels of lamotrigine, phenobarbital, and primidone

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25
Q

Adjunct Drugs for Partial Seizures

A 
Clorazepate 
Felbamate
Gabapentin
Lamotrigine
Topiramate 
Perampanel
Tiagabine
Levetiracetam
Brivaracetam
Zonisamide
Pregabalin
Vigabatrin
Lacosamide
Ezogabine
Rufinamide
Clobazam
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26
Q

Clorazepate - MoA

A

Prodrug, converted to diazepam

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27
Q

Clorazepate - Clinical use

A

Anxiety disorders

Partial seizures

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28
Q

Clorazepate - Adverse effects

A

Drowsiness

Lethargy

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29
Q

Clorazepate - Contraindications

A

Hypersensitivity

Category D pregnancy; increased risk of birth defects

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30
Q

Felbamate - MoA

A

Block glycine coactivation of NMDA receptors and thereby inhibit processes responsible for the initiation of seizures

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31
Q

Felbamate - Clinical use

A

Partial seizures that are refractory to other drugs

32
Q

Felbamate - Adverse effects

A

Fatal aplastic anemia

Acute hepatic failure

33
Q

Felbamate - Contraindications

A

Bone marrow depression
Hepatic disease
Hypersensitivity

Category C pregnancy

34
Q

Gabapentin and Pregabalin - MoA

A

Increase the release of GABA from central neurons

Also inhibits the L-type Calcium channel like pregabalin.

bind to the α2δ subunit of voltage-gated Ca2+ channels.

35
Q

Gabapentin - Clinical use

A

All forms of partial seizures
Postherpetic neuralgia

Restless leg syndrome

36
Q

Gabapentin - Adverse effects

A 
Ataxia
Dizziness
Drowsiness
Nystagmus
Tremor
37
Q

Lamotrigine - MoA

A

Block voltage-sensitive sodium channels and interfere with neuronal membrane conduction, and release of excitatory neurotransmitters such as glutamate.

38
Q

Lamotrigine - Clinical use

A

Partial seizure in adult and children
Generalized tonic-clonic, atonic and absence seizures
Lennox-Gastaut syndrome
Manic phase of bipolar disorder

39
Q

Lamotrigine - Adverse effects

A

Aseptic meningitis
Rash –> Stevens-Johnson syndrome
Cerebellar dysfunction
Drowsiness

40
Q

Lamotrigine - Interactions

A

Serum levels are decreased by carbamazepine and phenytoin and increased by valproate

41
Q

Lamotrigine - Contraindications

A

Hypersensitivity
Use cautiously in patient taking valproate or have hepatic or liver disease

Category C pregnancy; may reduce folate levels

42
Q

Topiramate - MoA

A

Block voltage-sensitive sodium channels, augumentation of GABA activation of GABAa receptors, and blockade of two types of excitatory glutamate receptors, kainate receptors and AMPA receptors (3-hydroxy-5-methyl-4-isoxazole proprionate acid)

43
Q

Topiramate - Clinical use

A

Partial seizures

44
Q

Topiramate - Adverse effects

A

Cleft palate

Ataxia
Dizziness
Drowsiness

45
Q

Topiramate - Contraindications

A

Hypersensitivity
Use cautiously during pregnancy, lactation, or hepatic and renal disease

Category D pregnancy; recent date showed increased incidence of cleft palate

46
Q

Perampanel - MoA

A

Noncompetitive antagonist of the ionotropic AMPA glutamate receptor on postsynaptic neurons.

47
Q

Perampanel - Clinical use

A

Partial seizure

Primary generalized tonic-clonic seizures in patients 12 years of age or older

48
Q

Tiagabine - MoA

A

Blocks GABA reuptake by binding to GABA reuptake transport protein

49
Q

Levetiracetam - MoA

A

Binds to a synaptic vesicle protein (SV2A), reducing vesicular packaging of GABA and impending neurotransmission across synapses

50
Q

Levetiracetam - Clinical use

A

Partial seizure in children

51
Q

Levetiracetam - Adverse effects

A

Somnolence
Asthenia (weakness)
Infection
Dizziness

52
Q

Brivaracetam - MoA

A

High and selective affinity for SV2A

53
Q

Brivaracetam - Clinical use

A

Partial seizures

54
Q

Zonisamide - MoA

A

Act at sodium channels and voltage-dependent transient inward currents of calcium channels. Blocks sodium channels in the inactivated state and reduces the ion flow in calcium channel proteins

55
Q

Zonisamide - Clinical use

A

Partial seizures

56
Q

Zonisamide - Adverse effects

A

Metabolic acidosis

57
Q

Pregabalin - Clinical use

A

Seizures
Neuropathic pain associated with diabetes
Posthepatic neuralgia
Fibromyalgia
Neuropathic pain after spinal cord injury

58
Q

Vigabatrin - MoA

A

Irreversible inhibition of GABA transaminase, the enzyme responsible for the breakdown of GABA in the brain. The inhibition of GABA-T enzyme leads to increase levels of the inhibitory neurotransmitter GABA

59
Q

Vigabatrin - Clinical use

A

Partial seizures

60
Q

Vigabatrin - Adverse effects

A 
Amnesia
Blurred vision
Blue-yellow color blindness
Decreased vision
Eye pains
Increase in seizures (rare)
61
Q

Lacosamide - MoA

A

Enhances inactivation of voltage-gates sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing.

62
Q

Ezogabine - MoA

A

Increase potassium ion flow, hyperpolarizes neurons and decrease their firing potential, enhance GABA mediated chloride ion currents

63
Q

Rufinamide - MoA

A

Modulate activity of sodium channels, prolong the inactive state of the channel

64
Q

Rufinamide - Clinical use

A

Seizures in children and adults with LGS

65
Q

Clobazam - MoA

A

Increases the inhibition by GABA at GABAa receptors

66
Q

Clobazam - Clinical use

A

Seizures in children and adults with LGS

67
Q

Drugs for Generalized Absence, Myoclonic, or Atonic Seizures

A

Ethosuximide

Clonazepam

68
Q

Ethosuximide - MoA

A

Inhibit T-type calcium channels in thalamic neurons

69
Q

Ethosuximide - Clinical use

A

Generalized absence seizures in children

70
Q

Ethosuximide - Adverse effects

A

Dizziness
Drowsiness
GI distress
Nausea

71
Q

Ethosuximide - Interactions

A

Valproate inhibits metabolism and increases levels

72
Q

Clonazepam - Clinical use

A

Absence, myoclonic and atonic seizures.

73
Q

Drugs for Status Epilepticus

A

Diazepam
Lorazepam
Phenytoin
Phenobarbital

74
Q

Drugs of choice for status epilepticus

A

Diazepam and Lorazepam

75
Q

Drug to use after diazepam or lorazepam has been administered for status epilepticus

A

Phenytoin

76
Q

Drug that may be effective if a benzodiazepine or phenytoin fails to control the seizures in status epilepticus

A

Phenobarbital

Pharmacology (55 decks)

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