Aptiom 400mg Tablets
It is used to help control certain kinds of seizures.
Drug Class
Antiepileptic drug (AED)
Pharmacologic Class
Voltage-gated sodium channel blocker
Pregnancy Category
D
FDA Approved
Nov 2013
DEA Schedule
Not Controlled
Overview
What is this medicine?
Aptiom (eslicarbazepine) is a medication used to treat seizures in people with epilepsy. It works by calming overactive nerves in the brain that cause seizures. It can be used alone or with other seizure medications.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food, and it can be swallowed whole or crushed. Continue taking the 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 location, avoiding the bathroom. Keep all medications in a safe place, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to check if there are any drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you're unsure about what to do if you miss a dose, contact your doctor for advice.
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food, and it can be swallowed whole or crushed. Continue taking the 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 location, avoiding the bathroom. Keep all medications in a safe place, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, consult with your pharmacist for guidance on the best disposal method. You may also want to check if there are any drug take-back programs available in your area.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses. If you're unsure about what to do if you miss a dose, contact your doctor for advice.
Lifestyle & Tips
- Do not stop taking Aptiom suddenly, as this can cause seizures to worsen or occur more frequently. Always consult your doctor before making any changes to your dose.
- Avoid alcohol and other CNS depressants while taking Aptiom, as they can increase side effects like dizziness and drowsiness.
- Aptiom can cause dizziness, drowsiness, and vision problems. Avoid driving or operating machinery until you know how this medication affects you.
- If you are a woman of childbearing potential, discuss effective birth control methods with your doctor, as Aptiom can reduce the effectiveness of hormonal contraceptives. Consider non-hormonal methods.
- Carry a medical alert card or wear a medical alert bracelet indicating you have epilepsy and are taking this medication.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial 400 mg once daily for 1-2 weeks, then increase to 800 mg once daily. May increase to 1200 mg once daily based on clinical response and tolerability.
Dose Range:
400 - 1200 mg
Condition-Specific Dosing:
adjunctive_therapy_focal_onset_seizures:
Initial 400 mg once daily for 1-2 weeks, then 800 mg once daily. Max 1200 mg once daily.
monotherapy_focal_onset_seizures:
Initial 400 mg once daily for 1-2 weeks, then 800 mg once daily. Max 1200 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Adjunctive therapy for focal-onset seizures (4 to <11 years): Initial 10 mg/kg once daily (max 400 mg/day) for 1-2 weeks, then increase to 20-30 mg/kg/day (max 1200 mg/day).
Adolescent:
Adjunctive therapy for focal-onset seizures (11 to <18 years): Initial 400 mg once daily for 1-2 weeks, then increase to 800 mg once daily. Max 1200 mg once daily.
Dose Adjustments
Renal Impairment:
Mild:
No adjustment (CrCl 50-79 mL/min).
Moderate:
Initial 200 mg once daily for 1-2 weeks, then 400 mg once daily (CrCl 30-49 mL/min). Max 600 mg once daily.
Severe:
Not recommended (CrCl <30 mL/min).
Dialysis:
Not recommended. Eslicarbazepine is dialyzable, but specific dosing recommendations for patients on dialysis are not available.
Hepatic Impairment:
Mild:
No adjustment.
Moderate:
No adjustment.
Severe:
Not studied; not recommended.
Pharmacology
Mechanism of Action
Eslicarbazepine acetate is a prodrug that is rapidly and extensively metabolized to eslicarbazepine, the active moiety. Eslicarbazepine stabilizes the inactive state of voltage-gated sodium channels, preventing their return to the active state and thereby reducing repetitive neuronal firing. This action is thought to be the primary mechanism by which it exerts its antiepileptic effects.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100%
Tmax:
2-3 hours (for eslicarbazepine)
FoodEffect:
Food has no significant effect on the rate or extent of absorption.
Distribution:
Vd:
Approximately 100 L
ProteinBinding:
Approximately 40%
CnssPenetration:
Yes
Elimination:
HalfLife:
10-20 hours (for eslicarbazepine)
Clearance:
Approximately 3 L/hour (renal clearance)
ExcretionRoute:
Primarily renal (urine)
Unchanged:
Approximately 66% (as eslicarbazepine in urine)
Pharmacodynamics
OnsetOfAction:
Not precisely defined for antiepileptic effect; therapeutic effects are observed after titration to target doses.
PeakEffect:
Steady-state concentrations are typically reached within 4-5 days of once-daily dosing.
DurationOfAction:
Sustained effect with once-daily dosing due to half-life.
Confidence:
High
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek immediate medical attention:
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
Signs of low sodium levels, including:
+ Headache
+ Trouble focusing
+ Memory problems
+ Feeling confused
+ Weakness
+ Seizures
+ Change in balance
Signs of liver problems, such as:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Urination problems, including inability to pass urine or changes in urine output
Shortness of breath, significant weight gain, or swelling in the arms or legs
Chest pain or pressure
Severe muscle pain or weakness
Changes in eyesight
Worsening or altered seizures
Inability to control eye movements
Difficulty walking
Severe Skin Reactions
This medication can cause severe skin reactions, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and other serious reactions. These reactions can be life-threatening and may affect other body organs. Seek immediate medical help if you experience:
Red, swollen, blistered, or peeling skin
Red or irritated eyes
Sores in your mouth, throat, nose, eyes, genitals, or skin
Fever
Chills
Body aches
Shortness of breath
Swollen glands
Angioedema
A severe reaction called angioedema has been reported with this medication. This reaction can be life-threatening. Seek immediate medical help if you experience:
Swelling of the hands, face, lips, eyes, tongue, or throat
Trouble breathing
Trouble swallowing
Unusual hoarseness
Other Side Effects
Most people taking this medication do not experience severe side effects. However, some may occur. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you or do not go away:
Headache
Dizziness
Drowsiness
Fatigue
Weakness
Upset stomach or vomiting
Shakiness
Reporting Side Effects
If you have questions about side effects or experience any side effects not listed here, 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, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek immediate medical attention:
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
Signs of low sodium levels, including:
+ Headache
+ Trouble focusing
+ Memory problems
+ Feeling confused
+ Weakness
+ Seizures
+ Change in balance
Signs of liver problems, such as:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Urination problems, including inability to pass urine or changes in urine output
Shortness of breath, significant weight gain, or swelling in the arms or legs
Chest pain or pressure
Severe muscle pain or weakness
Changes in eyesight
Worsening or altered seizures
Inability to control eye movements
Difficulty walking
Severe Skin Reactions
This medication can cause severe skin reactions, including Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and other serious reactions. These reactions can be life-threatening and may affect other body organs. Seek immediate medical help if you experience:
Red, swollen, blistered, or peeling skin
Red or irritated eyes
Sores in your mouth, throat, nose, eyes, genitals, or skin
Fever
Chills
Body aches
Shortness of breath
Swollen glands
Angioedema
A severe reaction called angioedema has been reported with this medication. This reaction can be life-threatening. Seek immediate medical help if you experience:
Swelling of the hands, face, lips, eyes, tongue, or throat
Trouble breathing
Trouble swallowing
Unusual hoarseness
Other Side Effects
Most people taking this medication do not experience severe side effects. However, some may occur. If you experience any of the following side effects, contact your doctor or seek medical help if they bother you or do not go away:
Headache
Dizziness
Drowsiness
Fatigue
Weakness
Upset stomach or vomiting
Shakiness
Reporting Side Effects
If you have questions about side effects or experience any side effects not listed here, 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 skin rash, especially if severe, widespread, or blistering (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis)
- Fever, swollen glands, or other signs of a severe allergic reaction (e.g., DRESS syndrome)
- Unusual tiredness, confusion, severe headache, nausea, or muscle weakness (signs of low sodium levels)
- New or worsening depression, anxiety, or panic attacks
- Thoughts about self-harm or suicide
- Unusual changes in mood or behavior (e.g., agitation, irritability, aggression, restlessness)
- Vision changes (e.g., double vision, blurred vision)
- Difficulty with coordination or balance
- Any signs of liver problems (e.g., yellowing of skin/eyes, dark urine, persistent nausea/vomiting, abdominal pain)
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.
If you have liver disease, as this may affect the safety and efficacy of the medication.
* If you are currently taking oxcarbazepine, as this may interact with the medication.
This list is not exhaustive, and it is crucial to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you may have. Your doctor and pharmacist need this information to ensure safe treatment and minimize potential interactions.
To guarantee your safety, do not start, stop, or change the dose of any medication without first consulting your doctor. It is your responsibility 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 allergic reaction you experienced, including any symptoms that occurred.
If you have liver disease, as this may affect the safety and efficacy of the medication.
* If you are currently taking oxcarbazepine, as this may interact with the medication.
This list is not exhaustive, and it is crucial to disclose all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you may have. Your doctor and pharmacist need this information to ensure safe treatment and minimize potential interactions.
To guarantee your safety, do not start, stop, or change the dose of any medication without first consulting your doctor. It is your responsibility to verify that it is safe to take this medication with all your other medications and health conditions.
Precautions & Cautions
Important Warnings and Cautions for Patients Taking This Medication
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Precautions and Safety Measures
Avoid driving and engaging in activities that require alertness until you understand how this medication affects you.
Do not abruptly stop taking this medication without consulting your doctor, as this may increase the risk of seizures. If you need to discontinue this medication, your doctor will guide you on how to gradually taper off the dosage.
Be aware of the rare risk of low blood cell counts associated with this medication. Immediately contact your doctor if you experience unexplained bruising or bleeding, signs of infection such as fever, chills, or sore throat, or feel extremely tired or weak.
Regular blood tests will be necessary, as directed by your doctor, to monitor your condition.
Interactions and Contraindications
Before consuming alcohol, marijuana, or other forms of cannabis, or taking prescription or over-the-counter medications that may cause drowsiness, consult your doctor.
As with other seizure medications, this drug may rarely increase the risk of suicidal thoughts or actions, particularly in individuals with a history of suicidal ideation or attempts. Immediately notify your doctor if you experience new or worsening symptoms such as depression, anxiety, restlessness, irritability, panic attacks, or mood changes. If suicidal thoughts or actions occur, seek medical attention right away.
Special Considerations
If you are 60 years or older, use this medication with caution, as you may be more susceptible to side effects.
Birth control pills and other hormone-based contraceptives may be less effective while taking this medication. Consider using an additional form of birth control, such as a condom.
If you are pregnant or become pregnant while taking this medication, contact your doctor immediately, as it may harm the unborn baby.
If you are breastfeeding, consult your doctor to discuss potential risks to your baby.
Pediatric Considerations
* If your child's weight changes, consult your doctor, as the dosage of this medication may need to be adjusted.
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Precautions and Safety Measures
Avoid driving and engaging in activities that require alertness until you understand how this medication affects you.
Do not abruptly stop taking this medication without consulting your doctor, as this may increase the risk of seizures. If you need to discontinue this medication, your doctor will guide you on how to gradually taper off the dosage.
Be aware of the rare risk of low blood cell counts associated with this medication. Immediately contact your doctor if you experience unexplained bruising or bleeding, signs of infection such as fever, chills, or sore throat, or feel extremely tired or weak.
Regular blood tests will be necessary, as directed by your doctor, to monitor your condition.
Interactions and Contraindications
Before consuming alcohol, marijuana, or other forms of cannabis, or taking prescription or over-the-counter medications that may cause drowsiness, consult your doctor.
As with other seizure medications, this drug may rarely increase the risk of suicidal thoughts or actions, particularly in individuals with a history of suicidal ideation or attempts. Immediately notify your doctor if you experience new or worsening symptoms such as depression, anxiety, restlessness, irritability, panic attacks, or mood changes. If suicidal thoughts or actions occur, seek medical attention right away.
Special Considerations
If you are 60 years or older, use this medication with caution, as you may be more susceptible to side effects.
Birth control pills and other hormone-based contraceptives may be less effective while taking this medication. Consider using an additional form of birth control, such as a condom.
If you are pregnant or become pregnant while taking this medication, contact your doctor immediately, as it may harm the unborn baby.
If you are breastfeeding, consult your doctor to discuss potential risks to your baby.
Pediatric Considerations
* If your child's weight changes, consult your doctor, as the dosage of this medication may need to be adjusted.
Overdose Information
Overdose Symptoms:
- Severe dizziness or drowsiness
- Nausea and vomiting
- Double vision
- Uncontrolled eye movements (nystagmus)
- Ataxia (lack of coordination)
- Confusion
- Coma
- Hyponatremia
What to Do:
Seek immediate medical attention or call 911. Contact a poison control center at 1-800-222-1222. Treatment is generally supportive, including gastric lavage, activated charcoal, and monitoring of vital signs and serum electrolytes.
Drug Interactions
Major Interactions
- Oral contraceptives (estrogen and progestin-containing): Eslicarbazepine can decrease the efficacy of hormonal contraceptives due to CYP3A4 induction. Patients should use alternative or additional non-hormonal birth control methods.
- Carbamazepine: Co-administration can decrease eslicarbazepine exposure and increase carbamazepine epoxide levels, potentially leading to increased adverse effects from carbamazepine.
Moderate Interactions
- Phenytoin: Decreased eslicarbazepine levels and increased phenytoin levels.
- Phenobarbital: Decreased eslicarbazepine levels.
- Primidone: Decreased eslicarbazepine levels.
- Rosuvastatin, Simvastatin: Increased statin exposure due to inhibition of OATP1B1 by eslicarbazepine.
- Topiramate: Increased topiramate levels.
- Oxcarbazepine: Not recommended due to potential for additive adverse effects and similar mechanism of action.
Monitoring
Baseline Monitoring
Renal function (serum creatinine, eGFR)
Rationale: To determine appropriate dosing, especially in patients with impaired renal function.
Timing: Prior to initiation of therapy.
Hepatic function (ALT, AST, bilirubin)
Rationale: To assess baseline liver health, though severe hepatic impairment is not recommended for use.
Timing: Prior to initiation of therapy.
Serum sodium
Rationale: Eslicarbazepine can cause hyponatremia.
Timing: Prior to initiation of therapy.
Complete Blood Count (CBC)
Rationale: To assess baseline hematologic parameters, as some AEDs can cause blood dyscrasias.
Timing: Prior to initiation of therapy.
Suicidal ideation/behavior screening
Rationale: All AEDs carry a risk of suicidal thoughts or behavior.
Timing: Prior to initiation of therapy.
Routine Monitoring
Serum sodium
Frequency: Periodically, especially during the first few months of therapy or after dose increases, and if symptoms of hyponatremia develop.
Target: 135-145 mEq/L
Action Threshold: <130 mEq/L or symptomatic hyponatremia requires dose reduction or discontinuation.
Seizure frequency and severity
Frequency: Ongoing clinical assessment.
Target: Reduction or elimination of seizures.
Action Threshold: Increased seizure frequency or lack of efficacy may warrant dose adjustment or alternative therapy.
Adverse effects (e.g., dizziness, somnolence, nausea, rash)
Frequency: Ongoing clinical assessment, particularly during titration.
Target: Tolerable level of side effects.
Action Threshold: Intolerable side effects may require dose reduction or discontinuation.
Suicidal ideation/behavior
Frequency: Regularly, especially during the initial weeks of therapy and with dose changes.
Target: Absence of suicidal thoughts or behaviors.
Action Threshold: Any new or worsening suicidal thoughts or behaviors require immediate clinical evaluation and intervention.
Symptom Monitoring
- Skin rash (especially severe, widespread, or blistering)
- Fever, swollen glands, or other signs of hypersensitivity reaction
- Symptoms of hyponatremia (e.g., nausea, malaise, headache, confusion, lethargy, muscle weakness, seizures)
- New or worsening depression, anxiety, or agitation
- Panic attacks
- Insomnia
- Irritability
- Hostility or aggression
- Impulsivity
- Restlessness
- Extreme increase in activity and talking (mania)
- Unusual changes in mood or behavior
- Dizziness
- Somnolence/drowsiness
- Vision changes (e.g., diplopia, blurred vision)
- Coordination problems (ataxia)
Special Patient Groups
Pregnancy
Pregnancy Category D. Eslicarbazepine may cause fetal harm when administered to a pregnant woman. Data from animal studies show developmental toxicity. Human data are limited but suggest a potential for increased risk of major congenital malformations (e.g., cardiac, neural tube defects) and adverse developmental outcomes. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Women of childbearing potential should be advised about the risks and the need for effective contraception.
Trimester-Specific Risks:
First Trimester:
Potential for increased risk of major congenital malformations.
Second Trimester:
Continued risk of developmental effects.
Third Trimester:
Continued risk of developmental effects; potential for withdrawal symptoms in neonate if exposed late in pregnancy.
Lactation
Eslicarbazepine and its active metabolite are excreted into human breast milk. The decision to breastfeed should consider the developmental and health benefits of breastfeeding, the mother’s clinical need for Aptiom, and any potential adverse effects on the breastfed infant from Aptiom or from the underlying maternal condition. Monitor breastfed infants for sedation, poor feeding, and rash.
Infant Risk:
L3 (Moderately Safe - some data, possible risk). Potential for infant drowsiness, poor feeding, rash, or other adverse effects.
Pediatric Use
Approved for adjunctive therapy of focal-onset seizures in children 4 years of age and older. Safety and efficacy in children younger than 4 years have not been established. Dosing is weight-based for children 4 to <11 years. Monitor for adverse effects similar to adults, including hyponatremia and suicidal ideation.
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. Eslicarbazepine is primarily renally eliminated, and elderly patients are more likely to have decreased renal function. Therefore, 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 concomitant disease or other drug therapy. Monitor renal function and serum sodium closely.
Clinical Information
Clinical Pearls
- Eslicarbazepine is a prodrug of eslicarbazepine, which is the active moiety. It is structurally related to carbamazepine and oxcarbazepine but has a different metabolic pathway, which may lead to fewer drug interactions compared to carbamazepine.
- Once-daily dosing improves patient adherence.
- Titration is necessary to minimize CNS side effects like dizziness and somnolence.
- Hyponatremia is a known side effect, especially in the first few months of treatment. Monitor serum sodium, particularly in patients at risk (e.g., elderly, those on diuretics).
- Patients should be counseled on the risk of serious dermatologic reactions (e.g., SJS/TEN, DRESS) and instructed to seek immediate medical attention if a rash develops.
- Advise women of childbearing potential about the reduced efficacy of hormonal contraceptives and the need for alternative birth control methods.
Alternative Therapies
- Carbamazepine
- Oxcarbazepine
- Lamotrigine
- Levetiracetam
- Phenytoin
- Valproic acid
- Topiramate
- Lacosamide
- Zonisamide
- Gabapentin
- Pregabalin
Cost & Coverage
Average Cost:
Varies widely, typically $300-$1000+ per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Brand), Tier 1 (Generic)
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety and the effectiveness of your treatment, never share your medication with others or take someone else's medication.
This medication is accompanied by a Medication Guide, which is a valuable resource that provides important information about your treatment. Please read this guide carefully and review it again whenever you receive a refill of your medication. If you have any questions or concerns about your medication, do not hesitate to consult with your doctor, pharmacist, or other healthcare provider.
In the event of a suspected overdose, it is crucial to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide detailed information about the overdose, including the name of the medication taken, the amount, and the time it occurred. This information will help healthcare professionals provide you with the most effective treatment.
This medication is accompanied by a Medication Guide, which is a valuable resource that provides important information about your treatment. Please read this guide carefully and review it again whenever you receive a refill of your medication. If you have any questions or concerns about your medication, do not hesitate to consult with your doctor, pharmacist, or other healthcare provider.
In the event of a suspected overdose, it is crucial to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide detailed information about the overdose, including the name of the medication taken, the amount, and the time it occurred. This information will help healthcare professionals provide you with the most effective treatment.