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Pharmacology > Antiepileptic Drugs > Flashcards

Antiepileptic Drugs Flashcards

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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
Adjunct Drugs for Partial Seizures
``` Clorazepate Felbamate Gabapentin Lamotrigine Topiramate Perampanel Tiagabine Levetiracetam Brivaracetam Zonisamide Pregabalin Vigabatrin Lacosamide Ezogabine Rufinamide Clobazam ```
26
Clorazepate - MoA
Prodrug, converted to diazepam
27
Clorazepate - Clinical use
Anxiety disorders | Partial seizures
28
Clorazepate - Adverse effects
Drowsiness | Lethargy
29
Clorazepate - Contraindications
Hypersensitivity | Category D pregnancy; increased risk of birth defects
30
Felbamate - MoA
Block glycine coactivation of NMDA receptors and thereby inhibit processes responsible for the initiation of seizures
31
Felbamate - Clinical use
Partial seizures that are refractory to other drugs
32
Felbamate - Adverse effects
Fatal aplastic anemia | Acute hepatic failure
33
Felbamate - Contraindications
Bone marrow depression Hepatic disease Hypersensitivity Category C pregnancy
34
Gabapentin and Pregabalin - MoA
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
Gabapentin - Clinical use
All forms of partial seizures Postherpetic neuralgia Restless leg syndrome
36
Gabapentin - Adverse effects
``` Ataxia Dizziness Drowsiness Nystagmus Tremor ```
37
Lamotrigine - MoA
Block voltage-sensitive sodium channels and interfere with neuronal membrane conduction, and release of excitatory neurotransmitters such as glutamate.
38
Lamotrigine - Clinical use
Partial seizure in adult and children Generalized tonic-clonic, atonic and absence seizures Lennox-Gastaut syndrome Manic phase of bipolar disorder
39
Lamotrigine - Adverse effects
Aseptic meningitis Rash --> Stevens-Johnson syndrome Cerebellar dysfunction Drowsiness
40
Lamotrigine - Interactions
Serum levels are decreased by carbamazepine and phenytoin and increased by valproate
41
Lamotrigine - Contraindications
Hypersensitivity Use cautiously in patient taking valproate or have hepatic or liver disease Category C pregnancy; may reduce folate levels
42
Topiramate - MoA
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
Topiramate - Clinical use
Partial seizures
44
Topiramate - Adverse effects
Cleft palate Ataxia Dizziness Drowsiness
45
Topiramate - Contraindications
Hypersensitivity Use cautiously during pregnancy, lactation, or hepatic and renal disease Category D pregnancy; recent date showed increased incidence of cleft palate
46
Perampanel - MoA
Noncompetitive antagonist of the ionotropic AMPA glutamate receptor on postsynaptic neurons.
47
Perampanel - Clinical use
Partial seizure | Primary generalized tonic-clonic seizures in patients 12 years of age or older
48
Tiagabine - MoA
Blocks GABA reuptake by binding to GABA reuptake transport protein
49
Levetiracetam - MoA
Binds to a synaptic vesicle protein (SV2A), reducing vesicular packaging of GABA and impending neurotransmission across synapses
50
Levetiracetam - Clinical use
Partial seizure in children
51
Levetiracetam - Adverse effects
Somnolence Asthenia (weakness) Infection Dizziness
52
Brivaracetam - MoA
High and selective affinity for SV2A
53
Brivaracetam - Clinical use
Partial seizures
54
Zonisamide - MoA
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
Zonisamide - Clinical use
Partial seizures
56
Zonisamide - Adverse effects
Metabolic acidosis
57
Pregabalin - Clinical use
Seizures Neuropathic pain associated with diabetes Posthepatic neuralgia Fibromyalgia Neuropathic pain after spinal cord injury
58
Vigabatrin - MoA
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
Vigabatrin - Clinical use
Partial seizures
60
Vigabatrin - Adverse effects
``` Amnesia Blurred vision Blue-yellow color blindness Decreased vision Eye pains Increase in seizures (rare) ```
61
Lacosamide - MoA
Enhances inactivation of voltage-gates sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing.
62
Ezogabine - MoA
Increase potassium ion flow, hyperpolarizes neurons and decrease their firing potential, enhance GABA mediated chloride ion currents
63
Rufinamide - MoA
Modulate activity of sodium channels, prolong the inactive state of the channel
64
Rufinamide - Clinical use
Seizures in children and adults with LGS
65
Clobazam - MoA
Increases the inhibition by GABA at GABAa receptors
66
Clobazam - Clinical use
Seizures in children and adults with LGS
67
Drugs for Generalized Absence, Myoclonic, or Atonic Seizures
Ethosuximide | Clonazepam
68
Ethosuximide - MoA
Inhibit T-type calcium channels in thalamic neurons
69
Ethosuximide - Clinical use
Generalized absence seizures in children
70
Ethosuximide - Adverse effects
Dizziness Drowsiness GI distress Nausea
71
Ethosuximide - Interactions
Valproate inhibits metabolism and increases levels
72
Clonazepam - Clinical use
Absence, myoclonic and atonic seizures.
73
Drugs for Status Epilepticus
Diazepam Lorazepam Phenytoin Phenobarbital
74
Drugs of choice for status epilepticus
Diazepam and Lorazepam
75
Drug to use after diazepam or lorazepam has been administered for status epilepticus
Phenytoin
76
Drug that may be effective if a benzodiazepine or phenytoin fails to control the seizures in status epilepticus
Phenobarbital

Pharmacology (55 decks)

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