Xcopri 100-150mg Maintenance Pak 56
It is used to help control certain kinds of seizures.
Drug Class
Anticonvulsant
Pharmacologic Class
Voltage-gated sodium channel inhibitor; GABA-A receptor positive allosteric modulator
Pregnancy Category
Not available
FDA Approved
Nov 2019
DEA Schedule
Schedule V
Overview
What is this medicine?
Xcopri (cenobamate) is a medication 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 cause seizures. It's very important to start this medication at a very low dose and slowly increase it over many weeks to reduce the risk of a serious skin reaction.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
You can take your medication with or without food.
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 make sure 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 directed by your healthcare provider. After administering the medication, flush the feeding tube.
Continuing Your Medication
Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom.
Keep your medication in a safe and secure location, out of sight and reach of children and pets. Consider using a locked box or area to store your medication.
* Keep all medications away from pets.
Missing a Dose
If you forget to take a dose, make sure you know what to do. If you are unsure, contact your doctor for guidance.
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
You can take your medication with or without food.
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 make sure 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 directed by your healthcare provider. After administering the medication, flush the feeding tube.
Continuing Your Medication
Continue taking your medication as directed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, away from the bathroom.
Keep your medication in a safe and secure location, out of sight and reach of children and pets. Consider using a locked box or area to store your medication.
* Keep all medications away from pets.
Missing a Dose
If you forget to take a dose, make sure you know what to do. If you are unsure, contact your doctor for guidance.
Lifestyle & Tips
- Do not stop taking Xcopri suddenly, as this can increase your risk of seizures.
- Avoid alcohol and other medications that cause drowsiness, as Xcopri can increase these effects.
- Be cautious when driving or operating machinery until you know how Xcopri affects you, as it can cause dizziness and sleepiness.
- Use effective non-hormonal birth control methods if you are taking hormonal contraceptives, as Xcopri can make them less effective.
- Maintain regular follow-up appointments with your doctor to monitor your condition and adjust your dose as needed.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Maintenance dose typically 200 mg once daily, can be increased to 400 mg once daily based on response and tolerability. Titration is critical: Start 12.5 mg once daily for 2 weeks, then 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 300 mg and 400 mg can occur at 2-week intervals.
Dose Range:
12.5 - 400 mg
Condition-Specific Dosing:
Maintenance Pak 100-150mg:
This specific pak is for the maintenance phase, providing 100mg and 150mg tablets for continued titration or stable dosing after initial lower dose titration.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment needed (CrCl 50-80 mL/min).
Moderate:
No dosage 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. Administer after dialysis on dialysis days.
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 anticonvulsant with a dual mechanism of action. It reduces repetitive neuronal firing by inhibiting voltage-gated sodium currents, preferentially inactivating the persistent 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:
80%
Tmax:
1-4 hours
FoodEffect:
No clinically significant effect of food on absorption.
Distribution:
Vd:
Approximately 40 L
ProteinBinding:
Approximately 60%
CnssPenetration:
Yes
Elimination:
HalfLife:
50-60 hours
Clearance:
Not available (primarily metabolic clearance)
ExcretionRoute:
Primarily renal (88% as metabolites), 12% in feces.
Unchanged:
<1%
Pharmacodynamics
OnsetOfAction:
Gradual, due to required slow titration (weeks to months to reach therapeutic levels).
PeakEffect:
Not directly quantifiable for seizure control, but plasma concentrations peak 1-4 hours post-dose.
DurationOfAction:
Prolonged, due to long half-life, allowing once-daily dosing.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
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 help right away:
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, significant weight gain, or swelling in the arms or legs
Unexplained bruising or bleeding
Severe muscle pain or weakness
Changes in balance or coordination
Difficulty walking
Inability to control 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, particularly in people with a history of suicidal ideation. If you experience any new or worsening symptoms, such as:
Depression
Anxiety, restlessness, or irritability
Panic attacks
Mood or behavioral changes
contact your doctor immediately. If you have suicidal thoughts or actions, seek help right away.
A rare but potentially life-threatening condition has been reported in people taking seizure medications like this one. If you experience any of the following symptoms, contact your doctor immediately:
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 Possible Side Effects
Most people taking this medication do not experience significant side effects, but some may occur. If you experience any of the following side effects, contact your doctor if they bother you or do not go away:
Dizziness, drowsiness, fatigue, or weakness
Headache
Constipation, diarrhea, nausea, vomiting, or decreased appetite
Nose or throat irritation
* Back pain
This is not an exhaustive list of 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 help right away:
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, significant weight gain, or swelling in the arms or legs
Unexplained bruising or bleeding
Severe muscle pain or weakness
Changes in balance or coordination
Difficulty walking
Inability to control 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, particularly in people with a history of suicidal ideation. If you experience any new or worsening symptoms, such as:
Depression
Anxiety, restlessness, or irritability
Panic attacks
Mood or behavioral changes
contact your doctor immediately. If you have suicidal thoughts or actions, seek help right away.
A rare but potentially life-threatening condition has been reported in people taking seizure medications like this one. If you experience any of the following symptoms, contact your doctor immediately:
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 Possible Side Effects
Most people taking this medication do not experience significant side effects, but some may occur. If you experience any of the following side effects, contact your doctor if they bother you or do not go away:
Dizziness, drowsiness, fatigue, or weakness
Headache
Constipation, diarrhea, nausea, vomiting, or decreased appetite
Nose or throat irritation
* Back pain
This is not an exhaustive list of 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:
- New or worsening rash (especially if severe, widespread, or accompanied by fever)
- Fever
- Swollen glands (lymph nodes)
- Swelling of the face, eyes, lips, or tongue
- Yellowing of the skin or eyes (jaundice)
- Dark urine
- Unusual bruising or bleeding
- Severe fatigue or weakness
- Muscle aches
- New or worsening depression, anxiety, or irritability
- Thoughts of harming yourself (suicidal ideation)
- Unusual changes in behavior or mood
- Severe dizziness or extreme sleepiness
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 allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Kidney disease
+ Liver disease
+ Familial Short QT syndrome
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure your safety, please disclose all of the following to your doctor and pharmacist:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* All your health problems
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to confirm it is safe to do so.
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 allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Kidney disease
+ Liver disease
+ Familial Short QT syndrome
This list is not exhaustive, and it is crucial to discuss all your health problems and medications with your doctor.
To ensure your safety, please disclose all of the following to your doctor and pharmacist:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* All your health problems
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to confirm it is safe to do so.
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 seizure patterns 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 instruct 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, and inform your doctor if you have a history of substance abuse or dependence on any drugs or alcohol.
If you are using birth control pills or other hormone-based contraception, note that this medication may reduce their effectiveness. Consider using an additional form of birth control, such as condoms, to prevent pregnancy.
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 seizure patterns 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 instruct 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, and inform your doctor if you have a history of substance abuse or dependence on any drugs or alcohol.
If you are using birth control pills or other hormone-based contraception, note that this medication may reduce their effectiveness. Consider using an additional form of birth control, such as condoms, to prevent pregnancy.
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:
- Severe drowsiness
- Dizziness
- Confusion
- Difficulty breathing
- Coma
What to Do:
Seek immediate medical attention or call 911. For poison control, call 1-800-222-1222. Management is supportive, including airway management and monitoring of vital signs.
Drug Interactions
Major Interactions
- Phenytoin (cenobamate can decrease phenytoin levels)
- Phenobarbital (cenobamate can decrease phenobarbital levels)
- Clobazam (cenobamate can decrease clobazam and N-desmethylclobazam levels)
- Oral Contraceptives (cenobamate can decrease efficacy of hormonal contraceptives)
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin, phenobarbital - may decrease cenobamate levels)
Moderate Interactions
- Lamotrigine (cenobamate can decrease lamotrigine levels)
- Valproate (cenobamate can decrease valproate levels)
- Drugs metabolized by CYP2C19 (e.g., diazepam, omeprazole - cenobamate is a CYP2C19 inhibitor)
- Drugs metabolized by CYP2B6 (e.g., bupropion, efavirenz - cenobamate is a CYP2B6 inducer)
- CNS depressants (e.g., alcohol, benzodiazepines, opioids - additive CNS depression)
Monitoring
Baseline Monitoring
Liver function tests (ALT, AST, bilirubin)
Rationale: To establish baseline and monitor for potential drug-induced liver injury, especially given DRESS risk.
Timing: Prior to initiation
Renal function (CrCl)
Rationale: To guide dose adjustments in patients with severe renal impairment.
Timing: Prior to initiation
Baseline seizure frequency and characteristics
Rationale: To assess efficacy of treatment.
Timing: Prior to initiation
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., somnolence, dizziness, fatigue, diplopia, headache)
Frequency: Regularly, especially during titration and dose increases
Target: Minimization of side effects
Action Threshold: Intolerable side effects may require dose reduction or slower titration.
Signs/symptoms of DRESS (Drug Reaction with Eosinophilia and Systemic Symptoms)
Frequency: Daily patient self-monitoring, and at each visit, especially during the first 3 months
Target: Absence of symptoms
Action Threshold: Any suspicion of DRESS (rash, fever, lymphadenopathy, eosinophilia, organ involvement) requires immediate discontinuation and medical evaluation.
Mental status and mood changes (including suicidal ideation)
Frequency: Regularly, at each follow-up visit
Target: Stable mood and cognitive function
Action Threshold: New or worsening depression, suicidal thoughts, or unusual behavior changes require immediate evaluation.
ECG (QTc interval)
Frequency: Not routinely recommended unless patient has pre-existing cardiac conditions or is on other QTc-prolonging drugs.
Target: Normal QTc interval
Action Threshold: Significant QTc prolongation may require dose adjustment or discontinuation.
Symptom Monitoring
- Rash (especially widespread, blistering, or accompanied by fever)
- Fever
- Swollen lymph nodes
- Swelling of face, eyes, lips, or tongue
- Difficulty breathing or swallowing
- Yellowing of skin or eyes (jaundice)
- Dark urine
- Unusual bruising or bleeding
- Severe fatigue
- Muscle aches or weakness
- New or worsening depression
- Suicidal thoughts or behavior
- Unusual changes in mood or behavior
- Dizziness
- Somnolence (excessive sleepiness)
- Fatigue
- Headache
- Diplopia (double vision)
- Nausea
- Vomiting
Special Patient Groups
Pregnancy
Cenobamate may cause fetal harm. Data from animal studies show developmental toxicity. There is a pregnancy exposure registry for women taking antiepileptic drugs during pregnancy. Discuss risks and benefits with a healthcare provider. Use effective contraception during treatment and for 4 weeks after the last dose.
Trimester-Specific Risks:
First Trimester:
Potential for major congenital malformations, consistent with other antiepileptic drugs. Data are limited.
Second Trimester:
Potential for adverse pregnancy outcomes, including reduced fetal growth. Data are limited.
Third Trimester:
Potential for adverse pregnancy outcomes, including reduced fetal growth. Data are limited.
Lactation
Cenobamate is excreted into human milk. Due to the potential for serious adverse reactions in breastfed infants (e.g., somnolence, poor feeding), breastfeeding is not recommended during treatment and for 4 days after the last dose. A risk-benefit assessment should be made.
Infant Risk:
L3 (Moderately Safe - limited human data, potential for adverse effects; monitor infant for sedation, poor feeding, developmental milestones).
Pediatric Use
Safety and effectiveness in pediatric patients (under 18 years of age) have not been established.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly patients and younger adults, but greater sensitivity of some older individuals cannot be ruled out. Start at the lower end of the dosing range and monitor for adverse effects due to potential for decreased renal/hepatic function and concomitant diseases/medications.
Clinical Information
Clinical Pearls
- The slow titration schedule is paramount to minimize the risk of Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS), a potentially life-threatening hypersensitivity reaction. Patients must be educated on DRESS symptoms.
- Cenobamate has a long half-life, allowing for once-daily dosing, which can improve adherence.
- Significant drug-drug interaction potential due to its effects on CYP450 enzymes (inducer of CYP3A4, CYP2B6; inhibitor of CYP2C19). Careful review of concomitant medications is essential, especially hormonal contraceptives, other AEDs, and drugs with narrow therapeutic indices.
- Patients should be advised about potential CNS depressant effects (dizziness, somnolence) and cautioned against activities requiring mental alertness, especially during titration.
- Consider baseline and periodic monitoring of liver function tests, especially if DRESS is suspected.
Alternative Therapies
- Levetiracetam (Keppra)
- Lacosamide (Vimpat)
- Lamotrigine (Lamictal)
- Carbamazepine (Tegretol)
- Oxcarbazepine (Trileptal)
- Topiramate (Topamax)
- Zonisamide (Zonegran)
- Perampanel (Fycompa)
- Brivaracetam (Briviact)
Cost & Coverage
Average Cost:
Varies widely, typically several hundred to over a thousand USD per 30 tablets
Insurance Coverage:
Tier 3 or 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 provides crucial information for patients. Please 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 amount, and the time it occurred.