Xcopri 50mg Tablets
It is used to help control certain kinds of seizures.
Drug Class
Anticonvulsant
Pharmacologic Class
Sodium channel blocker; GABA-A receptor positive allosteric modulator
Pregnancy Category
Not available
FDA Approved
Nov 2019
DEA Schedule
Not Controlled
Overview
What is this medicine?
Xcopri (cenobamate) is a medication used to treat partial-onset seizures in adults. It works by calming overactive nerve signals in the brain that cause seizures. It's important to start with a very low dose and slowly increase it over time to reduce the risk of a serious skin rash.
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 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 instructed 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 the 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 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 instructed 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 the 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
- Take Xcopri exactly as prescribed, usually once a day. Do not stop taking it suddenly without talking to your doctor, as this can cause seizures to worsen.
- Do not drive or operate machinery until you know how Xcopri affects you, as it can cause dizziness, drowsiness, and vision problems.
- Avoid or limit alcohol consumption, as it can increase the risk of side effects like dizziness and drowsiness.
- If you are taking hormonal birth control, be aware that Xcopri may make it less effective. Discuss alternative or additional birth control methods with your doctor.
- Report any new or worsening mood changes, thoughts of self-harm, or unusual behavior to your doctor immediately.
- Carry a medical alert card or wear medical alert jewelry stating that you have epilepsy and are taking Xcopri.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial: 12.5 mg once daily for 2 weeks; Titration: 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. Maintenance: 200 mg once daily. Max: 400 mg once daily.
Dose Range:
12.5 - 400 mg
Condition-Specific Dosing:
partial-onset seizures:
Initial: 12.5 mg once daily for 2 weeks; Titration: 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. Maintenance: 200 mg once daily. Max: 400 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment needed.
Moderate:
Initial: 12.5 mg once daily for 2 weeks; Titration: Max 300 mg once daily. Follow standard titration schedule up to 200 mg, then consider further increases cautiously.
Severe:
Initial: 12.5 mg once daily for 2 weeks; Titration: Max 300 mg once daily. Follow standard titration schedule up to 200 mg, then consider further increases cautiously.
Dialysis:
Not studied. Use with caution. Consider maximum dose of 300 mg once daily.
Hepatic Impairment:
Mild:
No dosage adjustment needed.
Moderate:
Initial: 12.5 mg once daily for 2 weeks; Titration: Max 200 mg once daily. Follow standard titration schedule up to 100 mg, then consider further increases cautiously.
Severe:
Initial: 12.5 mg once daily for 2 weeks; Titration: Max 200 mg once daily. Follow standard titration schedule up to 100 mg, then consider further increases cautiously.
Confidence:
Medium
Pharmacology
Mechanism of Action
Cenobamate is an antiepileptic drug that is thought to exert its therapeutic effect through two distinct mechanisms: 1) it reduces repetitive neuronal firing by inhibiting voltage-gated sodium currents, preferentially inactivating the persistent sodium current (INaP); and 2) it enhances gamma-aminobutyric acid (GABA) A receptor activity, acting as a positive allosteric modulator at a non-benzodiazepine binding site.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 80%
Tmax:
1 to 4 hours
FoodEffect:
Food does not significantly affect the rate or extent of absorption.
Distribution:
Vd:
Not available
ProteinBinding:
Approximately 60%
CnssPenetration:
Yes
Elimination:
HalfLife:
50 to 70 hours (mean 60 hours)
Clearance:
Not available
ExcretionRoute:
Primarily renal (89% as metabolites), minor fecal (5%)
Unchanged:
<1% (urine)
Pharmacodynamics
OnsetOfAction:
Not precisely quantified, but clinical effects are observed with titration.
PeakEffect:
Not precisely quantified, related to steady-state concentrations achieved after multiple doses.
DurationOfAction:
Due to long half-life, once-daily dosing is effective.
Confidence:
Medium
Safety & Warnings
Side Effects
Urgent 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 behaviors, especially in people with a history of suicidal tendencies. If you experience any new or worsening symptoms such as:
Depression
Anxiety, restlessness, or irritability
Panic attacks
Mood or behavior changes
contact your doctor immediately. If you have suicidal thoughts or attempts, 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 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 behaviors, especially in people with a history of suicidal tendencies. If you experience any new or worsening symptoms such as:
Depression
Anxiety, restlessness, or irritability
Panic attacks
Mood or behavior changes
contact your doctor immediately. If you have suicidal thoughts or attempts, 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 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:
- Rash (especially if it spreads, blisters, or is accompanied by fever, swollen glands, or facial swelling)
- Fever
- Swollen lymph nodes
- Swelling of the face, eyes, lips, or tongue
- Difficulty breathing or swallowing
- Yellowing of the skin or eyes (jaundice)
- Dark urine
- Unusual bruising or bleeding
- Severe fatigue or weakness
- New or worsening depression or anxiety
- Thoughts of harming yourself
- Hallucinations (seeing or hearing things that are not real)
- Confusion
- Severe dizziness or drowsiness
- Double vision or blurred vision
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.
Existing health conditions, specifically:
+ Kidney disease
+ Liver disease
+ Familial Short QT syndrome
Please note that this is not an exhaustive list of all potential interactions with this medication. Therefore, it is crucial to discuss all of your:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Health problems
with your doctor and pharmacist to ensure safe use. Before making any changes to your medication regimen, including starting, stopping, or adjusting the dose of any medication, 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.
Existing health conditions, specifically:
+ Kidney disease
+ Liver disease
+ Familial Short QT syndrome
Please note that this is not an exhaustive list of all potential interactions with this medication. Therefore, it is crucial to discuss all of your:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
Health problems
with your doctor and pharmacist to ensure safe use. Before making any changes to your medication regimen, including starting, stopping, or adjusting the dose of any medication, 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, ensure you understand how this medication affects you.
Consult 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 the frequency or severity of seizures after starting this medication, discuss these changes 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, inform your doctor.
Women taking birth control pills or using other hormone-based contraceptive methods should be aware that this medication may reduce the effectiveness of these birth control methods. Consider using an additional form of contraception, such as condoms, to prevent pregnancy.
If you are pregnant, planning to become pregnant, or are breastfeeding, consult 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, ensure you understand how this medication affects you.
Consult 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 the frequency or severity of seizures after starting this medication, discuss these changes 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, inform your doctor.
Women taking birth control pills or using other hormone-based contraceptive methods should be aware that this medication may reduce the effectiveness of these birth control methods. Consider using an additional form of contraception, such as condoms, to prevent pregnancy.
If you are pregnant, planning to become pregnant, or are breastfeeding, consult 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
- Blurred vision
- Difficulty walking or coordination problems
- Coma
What to Do:
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. There is no specific antidote for cenobamate overdose. Treatment is supportive.
Drug Interactions
Major Interactions
- Oral contraceptives (reduced efficacy)
- Phenytoin (increased phenytoin levels)
- Phenobarbital (increased phenobarbital levels)
- Clobazam (increased clobazam and N-desmethylclobazam levels)
- Lamotrigine (reduced lamotrigine levels)
Moderate Interactions
- Other CNS depressants (additive sedation)
- Drugs metabolized by CYP3A4 (e.g., midazolam, triazolam, alprazolam, simvastatin, atorvastatin, tacrolimus, cyclosporine) - cenobamate is a moderate inducer.
- Drugs metabolized by CYP2B6 (e.g., bupropion, efavirenz) - cenobamate is a moderate inducer.
- Drugs metabolized by CYP2C19 (e.g., clopidogrel, omeprazole, diazepam) - cenobamate is a weak inhibitor.
Confidence Interactions
Monitoring
Baseline Monitoring
Baseline ECG
Rationale: Although rare, cenobamate has been associated with QT shortening. Baseline ECG is recommended to rule out pre-existing cardiac abnormalities.
Timing: Prior to initiation
Routine Monitoring
Skin for rash (DRESS)
Frequency: Daily during titration and for several weeks after reaching maintenance dose
Target: Absence of rash
Action Threshold: Any new rash, especially if accompanied by fever, lymphadenopathy, or organ involvement, requires immediate discontinuation and medical evaluation.
Signs/symptoms of suicidal ideation/behavior
Frequency: Regularly, especially during initial therapy and dose changes
Target: Absence of new or worsening suicidal thoughts/behaviors
Action Threshold: Report any changes in mood, behavior, or thoughts of self-harm immediately.
CNS adverse effects (dizziness, somnolence, fatigue, diplopia)
Frequency: Regularly, especially during titration
Target: Tolerance of medication
Action Threshold: Significant or intolerable CNS effects may require dose reduction or slower titration.
Drug interactions (e.g., levels of co-administered AEDs)
Frequency: As clinically indicated, especially when initiating or adjusting cenobamate or co-administered drugs
Target: Therapeutic levels of co-administered drugs
Action Threshold: Adjust doses of co-administered drugs as needed based on therapeutic drug monitoring and clinical response.
Symptom Monitoring
- Rash (especially widespread, blistering, or accompanied by fever, swollen lymph nodes, or facial swelling)
- Fever
- Swollen lymph nodes
- Facial swelling
- Yellowing of skin or eyes (jaundice)
- Dark urine
- Unusual bruising or bleeding
- Severe fatigue
- New or worsening depression
- Anxiety
- Agitation
- Restlessness
- Panic attacks
- Insomnia
- Irritability
- Hostility
- Aggressiveness
- Impulsivity
- Akathisia (psychomotor restlessness)
- Hypomania
- Mania
- Thoughts of self-harm or suicide
- Dizziness
- Somnolence (sleepiness)
- Fatigue
- Diplopia (double vision)
- Blurred vision
- Headache
- Nausea
- Vomiting
- Constipation
Special Patient Groups
Pregnancy
Cenobamate may cause fetal harm. Data from animal studies show developmental toxicity (e.g., skeletal abnormalities, reduced fetal weight, increased fetal deaths). There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Advise pregnant patients of the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for major congenital malformations based on animal data.
Second Trimester:
Potential for developmental toxicity based on animal data.
Third Trimester:
Potential for developmental toxicity based on animal data.
Lactation
It is unknown if cenobamate is excreted in human milk. Cenobamate was excreted in the milk of lactating rats. Because of the potential for serious adverse reactions in breastfed infants, breastfeeding is not recommended during treatment with cenobamate.
Infant Risk:
Risk cannot be ruled out; potential for serious adverse reactions (e.g., sedation, poor feeding, developmental effects).
Pediatric Use
Safety and effectiveness in pediatric patients (under 18 years of age) have not been established. Not recommended for use in this population.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly subjects and younger subjects, but greater sensitivity of some older individuals cannot be ruled out. Dose adjustments may be needed for renal or hepatic impairment, which are more common in the elderly.
Clinical Information
Clinical Pearls
- **Slow Titration is Critical:** Emphasize the importance of the slow, gradual titration schedule to minimize the risk of Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS). Patients should be counseled extensively on this.
- **DRESS Awareness:** Educate patients and caregivers about the signs and symptoms of DRESS (rash, fever, swollen lymph nodes, facial swelling, organ involvement) and instruct them to seek immediate medical attention if these occur.
- **Drug Interactions:** Be mindful of significant drug interactions, particularly with oral contraceptives (reduced efficacy), phenytoin, phenobarbital, and clobazam (increased levels of these AEDs). Adjust doses of co-administered drugs as needed.
- **CNS Side Effects:** Dizziness, somnolence, and fatigue are common, especially during titration. Advise patients to avoid driving or operating heavy machinery until they know how the drug affects them.
- **Suicidal Ideation:** Like other AEDs, cenobamate carries a risk of suicidal thoughts or behavior. Monitor patients for new or worsening depression, suicidal ideation, or unusual changes in mood or behavior.
- **Once-Daily Dosing:** The long half-life allows for convenient once-daily dosing, which can improve adherence.
- **Food Independent:** Can be taken with or without food.
Alternative Therapies
- Levetiracetam (Keppra)
- Lamotrigine (Lamictal)
- Lacosamide (Vimpat)
- Carbamazepine (Tegretol)
- Oxcarbazepine (Trileptal)
- Topiramate (Topamax)
- Zonisamide (Zonegran)
- Perampanel (Fycompa)
- Brivaracetam (Briviact)
- Eslicarbazepine acetate (Aptiom)
Cost & Coverage
Average Cost:
Varies, typically $1000-$1500+ per 30 tablets (200mg)
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 consumed, and the time it occurred.