Xcopri 100mg Tablets
It is used to help control certain kinds of seizures.
Drug Class
Antiepileptic Drug (AED)
Pharmacologic Class
Voltage-gated sodium channel inhibitor; Positive allosteric modulator of GABA-A receptors
Pregnancy Category
Not available
FDA Approved
Nov 2019
DEA Schedule
Not Controlled
Overview
What is this medicine?
Xcopri (cenobamate) is a prescription medicine used to treat a specific type of seizure called focal-onset seizures in adults. It works by calming overactive electrical signals in the brain that can cause seizures. It's important to take this medicine exactly as prescribed, starting with a very low dose and slowly increasing it over time to reduce the risk of serious side effects.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take the medication with or without food, as directed. If you have difficulty swallowing the tablets whole, you can mix them with water. To do this, crush the required number of tablets for your dose and add them to 25 mL of water in a cup. Stir the mixture well and drink it immediately. Do not store the mixture for later use. To ensure you take the entire dose, rinse the cup with an additional 25 mL of water and drink it. If any tablet residue remains in the cup, repeat the rinsing process.
If you have a feeding tube, you can use this medication as instructed by your healthcare provider. After administering the medication through the feeding tube, flush the tube with water.
Continue taking this medication as directed by your doctor or healthcare provider, even if you feel well.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry place, avoiding bathrooms. Keep it in a secure location where children cannot see or access it, and where others cannot reach it. Consider using a locked box or area to store the medication. Keep all medications out of reach of pets.
Missing a Dose
If you forget to take a dose, be sure to follow the instructions provided by your doctor. If you are unsure what to do in case of a missed dose, contact your doctor for guidance.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take the medication with or without food, as directed. If you have difficulty swallowing the tablets whole, you can mix them with water. To do this, crush the required number of tablets for your dose and add them to 25 mL of water in a cup. Stir the mixture well and drink it immediately. Do not store the mixture for later use. To ensure you take the entire dose, rinse the cup with an additional 25 mL of water and drink it. If any tablet residue remains in the cup, repeat the rinsing process.
If you have a feeding tube, you can use this medication as instructed by your healthcare provider. After administering the medication through the feeding tube, flush the tube with water.
Continue taking this medication as directed by your doctor or healthcare provider, even if you feel well.
Storing and Disposing of Your Medication
Store this medication at room temperature in a dry place, avoiding bathrooms. Keep it in a secure location where children cannot see or access it, and where others cannot reach it. Consider using a locked box or area to store the medication. Keep all medications out of reach of pets.
Missing a Dose
If you forget to take a dose, be sure to follow the instructions provided by your doctor. If you are unsure what to do in case of a missed dose, contact your doctor for guidance.
Lifestyle & Tips
- Do not stop taking Xcopri suddenly, as this can increase the risk of seizures. Any changes to your dose should be made under the guidance of your doctor.
- Avoid or limit alcohol consumption, as it can increase side effects like dizziness and drowsiness.
- Be cautious when driving or operating machinery until you know how Xcopri affects you, as it can cause dizziness, drowsiness, and vision problems.
- Report any new or worsening symptoms of depression, unusual changes in mood or behavior, or suicidal thoughts to your doctor immediately.
- Carry a medical alert card or wear a medical alert bracelet indicating you have epilepsy and are taking medication.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
200 mg once daily (maintenance dose)
Dose Range:
12.5 - 400 mg
Condition-Specific Dosing:
titrationSchedule:
Initiate at 12.5 mg once daily for 2 weeks, then increase to 25 mg once daily for 2 weeks, then 50 mg once daily for 2 weeks, then 100 mg once daily for 2 weeks, then 150 mg once daily for 2 weeks, then 200 mg once daily. Further increases to 400 mg once daily may be considered based on clinical response and tolerability, with increments of 50 mg every 2 weeks.
maxDose:
400 mg once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (CrCl 50-80 mL/min)
Moderate:
No adjustment needed (CrCl 30-50 mL/min)
Severe:
Maximum recommended dose is 300 mg once daily (CrCl < 30 mL/min)
Dialysis:
Maximum recommended dose is 300 mg once daily; supplemental dose after dialysis not needed due to long half-life.
Hepatic Impairment:
Mild:
Maximum recommended dose is 200 mg once daily (Child-Pugh A)
Moderate:
Maximum recommended dose is 200 mg once daily (Child-Pugh B)
Severe:
Maximum recommended dose is 150 mg once daily (Child-Pugh C)
Pharmacology
Mechanism of Action
Cenobamate is an antiepileptic drug with a dual mechanism of action. It reduces repetitive neuronal firing by inhibiting voltage-gated sodium currents, preferentially blocking the persistent (late) sodium current. It also enhances inhibitory currents by positive allosteric modulation of the GABA-A ion channel at a non-benzodiazepine binding site.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 80%
Tmax:
1-4 hours
FoodEffect:
No clinically significant effect of food on absorption.
Distribution:
Vd:
Approximately 40-50 L
ProteinBinding:
Approximately 60%
CnssPenetration:
Yes
Elimination:
HalfLife:
Approximately 50-70 hours
Clearance:
Not available (primarily metabolic clearance)
ExcretionRoute:
Primarily renal (93% as metabolites), minor fecal (5%)
Unchanged:
<1% (renal)
Pharmacodynamics
OnsetOfAction:
Gradual, due to required slow titration schedule.
PeakEffect:
Steady state concentrations are reached after approximately 14 days of stable dosing.
DurationOfAction:
Long half-life supports once-daily dosing.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe dizziness or fainting
Abnormal or rapid heartbeat
Shortness of breath, sudden weight gain, or swelling in the arms or legs
Unexplained bruising or bleeding
Severe muscle pain or weakness
Balance problems
Difficulty walking
Uncontrolled eye movements
Memory problems or loss
Confusion, difficulty focusing, or changes in behavior
Speech difficulties
Changes in vision
Like other seizure medications, this drug may increase the risk of suicidal thoughts or actions, especially in people with a history of suicidal behavior. If you experience any new or worsening symptoms, such as:
Depression
Anxiety, restlessness, or irritability
Panic attacks
Mood or behavior changes
contact your doctor right away. If you have suicidal thoughts or actions, seek medical help immediately.
A rare but potentially life-threatening condition has occurred in people taking seizure medications like this one. If you experience any of the following symptoms, contact your doctor right away:
Swollen glands
Fever
Rash
Painful sores in the mouth or around the eyes
Chest pain
Signs of kidney problems, such as:
+ Inability to urinate
+ Changes in urine output
Signs of liver problems, such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Side Effects
Most people do not experience serious side effects, and many have only minor or no side effects at all. However, if you experience any of the following side effects and they bother you or do not go away, contact your doctor:
Dizziness, drowsiness, fatigue, or weakness
Headache
Constipation, diarrhea, nausea, vomiting, or decreased appetite
Nose or throat irritation
* Back pain
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Severe dizziness or fainting
Abnormal or rapid heartbeat
Shortness of breath, sudden weight gain, or swelling in the arms or legs
Unexplained bruising or bleeding
Severe muscle pain or weakness
Balance problems
Difficulty walking
Uncontrolled eye movements
Memory problems or loss
Confusion, difficulty focusing, or changes in behavior
Speech difficulties
Changes in vision
Like other seizure medications, this drug may increase the risk of suicidal thoughts or actions, especially in people with a history of suicidal behavior. If you experience any new or worsening symptoms, such as:
Depression
Anxiety, restlessness, or irritability
Panic attacks
Mood or behavior changes
contact your doctor right away. If you have suicidal thoughts or actions, seek medical help immediately.
A rare but potentially life-threatening condition has occurred in people taking seizure medications like this one. If you experience any of the following symptoms, contact your doctor right away:
Swollen glands
Fever
Rash
Painful sores in the mouth or around the eyes
Chest pain
Signs of kidney problems, such as:
+ Inability to urinate
+ Changes in urine output
Signs of liver problems, such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Other Side Effects
Most people do not experience serious side effects, and many have only minor or no side effects at all. However, if you experience any of the following side effects and they bother you or do not go away, contact your doctor:
Dizziness, drowsiness, fatigue, or weakness
Headache
Constipation, diarrhea, nausea, vomiting, or decreased appetite
Nose or throat irritation
* Back pain
This is not a comprehensive list of all possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe skin rash, especially if accompanied by fever, swollen lymph nodes, facial swelling, or yellowing of the skin/eyes (signs of DRESS syndrome)
- Thoughts about suicide or harming yourself
- New or worsening depression, anxiety, or irritability
- Panic attacks or agitation
- Restlessness or hyperactivity
- Aggressive, angry, or violent behavior
- Extreme increase in talkativeness or activity (mania)
- Other unusual changes in behavior or mood
- Severe dizziness or feeling like you might pass out
- Double vision or blurred vision
- Problems with coordination or walking (ataxia)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have kidney disease or liver disease, as these conditions may affect how your body processes the medication.
If you have Familial Short QT syndrome, a heart condition that may be exacerbated by this medication.
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor. Please provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Any health problems you have, as they may interact with this medication
To ensure your safety, do not start, stop, or change the dose of any medication without first consulting your doctor. It is vital to verify that it is safe to take this medication with all your other medications and health conditions.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have kidney disease or liver disease, as these conditions may affect how your body processes the medication.
If you have Familial Short QT syndrome, a heart condition that may be exacerbated by this medication.
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor. Please provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
Any health problems you have, as they may interact with this medication
To ensure your safety, do not start, stop, or change the dose of any medication without first consulting your doctor. It is vital to verify that it is safe to take this medication with all your other medications and health conditions.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until you understand how this medication affects you.
Consult with your doctor before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions.
If you experience changes in your seizures or if they worsen after starting this medication, discuss this with your doctor promptly.
Do not abruptly discontinue this medication without first consulting your doctor, as this may increase your risk of seizures. If you need to stop taking this medication, your doctor will guide you on how to gradually taper off the dosage.
Be aware that this medication has the potential for abuse and dependence. Adhere strictly to your doctor's instructions for taking this medication. If you have a history of substance abuse or dependence on drugs or alcohol, inform your doctor.
Note that birth control pills and other hormone-based contraceptives may be less effective while taking this medication. To prevent pregnancy, consider using an additional form of birth control, such as condoms.
If you are pregnant, planning to become pregnant, or are breastfeeding, consult with your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
Before operating a vehicle or engaging in any activity that requires alertness and clear vision, wait until you understand how this medication affects you.
Consult with your doctor before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions.
If you experience changes in your seizures or if they worsen after starting this medication, discuss this with your doctor promptly.
Do not abruptly discontinue this medication without first consulting your doctor, as this may increase your risk of seizures. If you need to stop taking this medication, your doctor will guide you on how to gradually taper off the dosage.
Be aware that this medication has the potential for abuse and dependence. Adhere strictly to your doctor's instructions for taking this medication. If you have a history of substance abuse or dependence on drugs or alcohol, inform your doctor.
Note that birth control pills and other hormone-based contraceptives may be less effective while taking this medication. To prevent pregnancy, consider using an additional form of birth control, such as condoms.
If you are pregnant, planning to become pregnant, or are breastfeeding, consult with your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Somnolence
- Dizziness
- Ataxia
- Blurred vision
What to Do:
There is no specific antidote for cenobamate overdose. Treatment should be supportive and symptomatic. Contact a poison control center immediately (e.g., 1-800-222-1222) or seek emergency medical attention.
Drug Interactions
Major Interactions
- Oral contraceptives (reduced efficacy of hormonal contraceptives due to CYP3A4 induction)
- Phenytoin (increased phenytoin levels due to CYP2C19 inhibition)
- Phenobarbital (increased phenobarbital levels due to CYP2C19 inhibition)
- Clobazam (increased clobazam and N-desmethylclobazam levels due to CYP2C19 inhibition)
- Drugs metabolized by CYP3A4 (e.g., midazolam, alprazolam, statins, some antiarrhythmics, some antipsychotics) - reduced efficacy of these drugs
- Drugs metabolized by CYP2B6 (e.g., bupropion, efavirenz) - reduced efficacy of these drugs
- Drugs metabolized by CYP2C19 (e.g., clopidogrel, proton pump inhibitors, diazepam) - increased levels of these drugs
Moderate Interactions
- Alcohol and other CNS depressants (additive CNS depression, increased risk of somnolence and dizziness)
Monitoring
Baseline Monitoring
Liver function tests (ALT, AST, bilirubin)
Rationale: To assess baseline hepatic function, as cenobamate is extensively metabolized by the liver and can cause hepatic impairment.
Timing: Prior to initiation of therapy
Renal function (CrCl)
Rationale: To assess baseline renal function, as dose adjustments are needed in severe renal impairment.
Timing: Prior to initiation of therapy
ECG
Rationale: While not a primary concern for QTc prolongation, some AEDs can affect cardiac conduction. Baseline assessment is prudent.
Timing: Prior to initiation of therapy
Routine Monitoring
Seizure frequency and severity
Frequency: Regularly, at each follow-up visit
Target: Reduction in seizure frequency
Action Threshold: Lack of efficacy or worsening seizures may require dose adjustment or alternative therapy.
Adverse effects (e.g., dizziness, somnolence, fatigue, diplopia, rash, mood changes)
Frequency: Regularly, at each follow-up visit, especially during titration
Target: Tolerable side effect profile
Action Threshold: Intolerable side effects may require dose reduction or discontinuation.
Liver function tests (ALT, AST, bilirubin)
Frequency: Periodically, or if signs/symptoms of hepatic dysfunction develop
Target: Within normal limits
Action Threshold: Significant elevations may require dose reduction or discontinuation.
Renal function
Frequency: Periodically, or if signs/symptoms of renal dysfunction develop
Target: Stable renal function
Action Threshold: Significant decline may require dose adjustment.
Symptom Monitoring
- Severe rash (especially with fever, facial swelling, lymphadenopathy, or eosinophilia - suggestive of DRESS)
- Suicidal thoughts or behavior
- Unusual changes in mood or behavior (e.g., depression, aggression, agitation)
- Severe dizziness or somnolence
- Vision changes (e.g., diplopia, blurred vision)
- Ataxia or coordination problems
- Nausea, vomiting, abdominal pain (signs of hepatic issues)
Special Patient Groups
Pregnancy
There are no adequate and well-controlled studies of cenobamate in pregnant women. Based on animal studies, cenobamate may cause fetal harm. The FDA does not use pregnancy categories A, B, C, D, and X. A pregnancy exposure registry is available for women exposed to antiepileptic drugs during pregnancy (North American Antiepileptic Drug Pregnancy Registry: 1-888-233-2334).
Trimester-Specific Risks:
First Trimester:
Potential for increased risk of major congenital malformations, consistent with other AEDs.
Second Trimester:
Risk not well-established, but continued exposure may pose risk.
Third Trimester:
Risk not well-established, but continued exposure may pose risk.
Lactation
Cenobamate is excreted into breast milk. There are no data on the effects of cenobamate on the breastfed infant or on milk production. Due to the potential for serious adverse reactions in breastfed infants (e.g., somnolence, feeding difficulties), a decision should be made whether to discontinue breastfeeding or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Potential for somnolence, feeding difficulties, and other adverse effects due to drug excretion in milk. Risk to infant cannot be ruled out.
Pediatric Use
Safety and effectiveness in pediatric patients (under 18 years of age) have not been established.
Geriatric Use
Clinical studies did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Clinical Information
Clinical Pearls
- Strict adherence to the slow titration schedule is paramount to minimize the risk of serious adverse reactions, particularly Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) syndrome.
- Cenobamate has significant drug-drug interactions due to its effects on CYP450 enzymes (inducer of CYP3A4, CYP2B6; inhibitor of CYP2C19). Careful review of concomitant medications is essential, especially hormonal contraceptives, phenytoin, phenobarbital, and clobazam.
- The long half-life of cenobamate (50-70 hours) allows for once-daily dosing, which can improve patient adherence.
- Patients should be counseled on potential CNS depressant effects (dizziness, somnolence) and advised to avoid activities requiring mental alertness until they know how the drug affects them.
- Monitor for signs of suicidal ideation and behavior, as with all antiepileptic drugs.
Alternative Therapies
- Levetiracetam
- Lamotrigine
- Carbamazepine
- Oxcarbazepine
- Lacosamide
- Topiramate
- Zonisamide
- Perampanel
- Brivaracetam
Cost & Coverage
Average Cost:
Highly variable, typically several hundred to over a thousand USD per 30 tablets
Insurance Coverage:
Specialty Tier (requires prior authorization)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which is a patient fact sheet that provides crucial information. It is vital to read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the quantity, and the time it occurred.