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Questions and Answers
What kind of effect does Xcorpi® have on the GABA-A chloride channel?
What kind of effect does Xcorpi® have on the GABA-A chloride channel?
- Acts as an inhibitor of the chloride channel
- Acts as a negative allosteric modulator
- Has no significant effect on the chloride channel
- Acts as a positive allosteric modulator (correct)
What is a common adverse drug reaction (ADR) associated with Xcorpi®?
What is a common adverse drug reaction (ADR) associated with Xcorpi®?
- Nausea and vomiting
- Chest pain
- Severe allergic reaction
- Dose-related somnolence (correct)
Which statement best describes the medication's categorization regarding substance control?
Which statement best describes the medication's categorization regarding substance control?
- Schedule II controlled substance
- Schedule V controlled substance (correct)
- Schedule IV controlled substance
- Not a controlled substance
Which role does Xcorpi® play concerning CYP450 enzymes?
Which role does Xcorpi® play concerning CYP450 enzymes?
What was the role of phenobarbital in treating seizures compared to its current status?
What was the role of phenobarbital in treating seizures compared to its current status?
What is the primary mechanism of action of Stiripentol?
What is the primary mechanism of action of Stiripentol?
What is one of the indications for the use of Stiripentol?
What is one of the indications for the use of Stiripentol?
Which enzyme's inhibition is associated with reduced neuron excitability due to Stiripentol?
Which enzyme's inhibition is associated with reduced neuron excitability due to Stiripentol?
How is Stiripentol primarily metabolized in the body?
How is Stiripentol primarily metabolized in the body?
What percentage of Stiripentol is eliminated via urine?
What percentage of Stiripentol is eliminated via urine?
What percentage of adults treated with vigabatrin experience visual field impairment?
What percentage of adults treated with vigabatrin experience visual field impairment?
Which side effect is NOT classified as a common adverse drug reaction (ADR) of tiagabine?
Which side effect is NOT classified as a common adverse drug reaction (ADR) of tiagabine?
How does tiagabine primarily reduce seizures?
How does tiagabine primarily reduce seizures?
What is a significant metabolic pathway for levetiracetam?
What is a significant metabolic pathway for levetiracetam?
What unique mechanism of action does levetiracetam exhibit?
What unique mechanism of action does levetiracetam exhibit?
Which serious adverse reaction is associated with vigabatrin?
Which serious adverse reaction is associated with vigabatrin?
In children under 3 years old, what percentage may experience intramyelinic edema?
In children under 3 years old, what percentage may experience intramyelinic edema?
Which physiological effect does tiagabine NOT induce?
Which physiological effect does tiagabine NOT induce?
What type of channels does brivaracetam block to exert its effects?
What type of channels does brivaracetam block to exert its effects?
Which serious side effect is associated with Zonisamide that affects the body's ability to regulate temperature?
Which serious side effect is associated with Zonisamide that affects the body's ability to regulate temperature?
Which of the following is an indication for the use of brivaracetam?
Which of the following is an indication for the use of brivaracetam?
Which medication is associated with cognitive and psychiatric side effects such as depression and psychosis?
Which medication is associated with cognitive and psychiatric side effects such as depression and psychosis?
What is a common side effect associated with both Zonisamide and other carbonic anhydrase inhibitors?
What is a common side effect associated with both Zonisamide and other carbonic anhydrase inhibitors?
What warning must all anti-seizure medications include in their prescribing information?
What warning must all anti-seizure medications include in their prescribing information?
Which of the following medications is FDA approved in combination with clobazam for treating Dravet syndrome?
Which of the following medications is FDA approved in combination with clobazam for treating Dravet syndrome?
Which enzyme does carbamazepine induce?
Which enzyme does carbamazepine induce?
Which of the following medications does NOT have any CYP inhibition or induction effect?
Which of the following medications does NOT have any CYP inhibition or induction effect?
What primary route of elimination does pregabalin primarily utilize?
What primary route of elimination does pregabalin primarily utilize?
Which antiepileptic drug is known for its oxidations and renal excretion mechanisms?
Which antiepileptic drug is known for its oxidations and renal excretion mechanisms?
Which of the following medications is indicated for increased risk of suicidal thoughts according to its prescribing information?
Which of the following medications is indicated for increased risk of suicidal thoughts according to its prescribing information?
Which CYP pathway is inhibited by felbamate?
Which CYP pathway is inhibited by felbamate?
What type of metabolic pathway does ethosuximide primarily follow?
What type of metabolic pathway does ethosuximide primarily follow?
What is the main route of degradation for stiripentol?
What is the main route of degradation for stiripentol?
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Study Notes
Xcorpi®
- Positive allosteric modulator of the GABA-A chloride channel
- Oral treatment for focal onset seizures
- Common ADRs: somnolence, dizziness, headache, fatigue, diplopia.
- Psychiatric ADRs: increased risk of suicidal thoughts or behavior
- Can cause euphoria and feelings of drunkenness
- Physical dependence may develop
- Schedule V controlled substance
- Inducer of CYP2B6, 2C8, and 3A4
- Moderate inhibitor of CYP2C19
Phenobarbital
- Schedule III controlled substance
- Metabolized by CYP3A4 followed by glucuronidation
- Elimination 48% feces; 22% urine
- Adjunct therapy for seizures associated with Dravet syndrome in patients two years of age and older who are taking clobazam
Stiripentol
- Allosteric modulator of the GABA-A receptor with direct activating effects
- Increases duration of the opening of the chloride channel
- Inhibits the reuptake of GABA
- Inhibits GABA metabolism
- Inhibits lactate dehydrogenase
- Moderate inhibitor of both CYP1A2 and CYP2C19
- ADRs: somnolence, decreased appetite, agitation, ataxia, weight loss, hypotonia, nausea, tremor, dysarthria, and insomnia
- Metabolism: CYP2C19 & CYP3A4 (major) ; CYPA12 (minor)
Vigabatrin
- Patients must undergo visual field testing
- Visual field impairment occurs in 52% of adults and 34% of children
- Intramyelinic edema in 20% of children < 3 years old
- Can lower serum concentrations of phenytoin
- REMS requirement for dispensing
Tiagabine
- Inhibits neuronal and glial reuptake of GABA
- ADRs: dizziness, somnolence, and tremor
- Adjunct for focal onset seizures
Levetiracetam
- 1st line treatment of focal and tonic-clonic seizures
- Effective as add-on therapy for refractory myoclonic seizures
- May be useful in children with Lennox-Gastaut
- Major metabolic pathway is hydrolysis
- Binds specifically to the SV2A protein on synaptic vesicles
- Inhibits rectifying K+ channels
Zonisamide
- Blocks voltage gated Na+ channels and T-Type Ca2+ channels
- FDA- approved as adjunct for focal onset seizures in adults
- ADRs: dizziness, somnolence, ataxia, anorexia, confusion, abnormal thinking, nervousness, fatigue, cognitive and psychiatric side effects, nephrolithiasis, weight loss, fatigue, somnolence, oligohidrosis, hyperthermia/heat stroke
- Contraindicated in patients with sulfonamide hypersensitivity
AED CYP Induction Table
- Many anti-epileptic drugs (AEDs) are metabolized via the cytochrome P450 (CYP) system
- Table shows: Main route of elimination, CYP degradation, CYP inhibition, UGT degradation, UGT, induction, and UGT inhibition
- AEDs presented include: carbamazepine, clobazam, clonazepam, eslicarbazepine acetate, ethosuximide, felbamate, phenobarbital, phenytoin, pregabalin, rufinamide, stiripentol
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