Aptiom 200mg Tablets
It is used to help control certain kinds of seizures.
Drug Class
Anticonvulsant
Pharmacologic Class
Voltage-gated sodium channel blocker
Pregnancy Category
Not available
FDA Approved
Nov 2013
DEA Schedule
Not Controlled
Overview
What is this medicine?
Aptiom is a medicine used to treat seizures in people with epilepsy. It works by calming overactive nerve signals in the brain. It's taken once a day.
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 feeling better.
Storing and Disposing of Your Medication
Store this 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 your pharmacist for guidance on the best disposal method or explore local drug take-back programs.
Missing 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. Avoid taking two doses at the same time or taking 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 feeling better.
Storing and Disposing of Your Medication
Store this 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 your pharmacist for guidance on the best disposal method or explore local drug take-back programs.
Missing 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. Avoid taking two doses at the same time or taking 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 return or worsen. Always consult your doctor before making any changes.
- Avoid driving or operating machinery until you know how Aptiom affects you, as it can cause dizziness, drowsiness, and vision problems.
- Limit or avoid alcohol consumption, as it can increase side effects like dizziness and drowsiness.
- If you are a woman of childbearing potential, discuss effective birth control methods with your doctor, as Aptiom can make hormonal contraceptives less effective.
- Stay well-hydrated, especially if you are at risk for low sodium levels (hyponatremia).
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. Max: 1600 mg once daily.
Dose Range:
400 - 1600 mg
Condition-Specific Dosing:
adjunctiveTherapy:
Initial: 400 mg once daily for 1-2 weeks, then increase to 800 mg once daily. Max: 1600 mg once daily.
monotherapy:
Initial: 400 mg once daily for 1-2 weeks, then increase to 800 mg once daily. Max: 1600 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
4 to <11 years: Initial 10 mg/kg once daily for 1-2 weeks, then increase to 20 mg/kg once daily. Max 30 mg/kg once daily (not to exceed 1800 mg/day). 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.
Adolescent:
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:
CrCl 50-80 mL/min: No adjustment needed.
Moderate:
CrCl 30-50 mL/min: Initial 200 mg once daily for 1-2 weeks, then increase to 400 mg once daily. Max 600 mg once daily.
Severe:
CrCl <30 mL/min: Initial 200 mg once daily for 1-2 weeks, then increase to 200 mg every other day. Max 300 mg once daily.
Dialysis:
No supplemental dose needed after dialysis. Follow severe renal impairment dosing.
Hepatic Impairment:
Mild:
No adjustment needed.
Moderate:
No adjustment needed.
Severe:
Not studied; generally not recommended due to lack of data.
Pharmacology
Mechanism of Action
Eslicarbazepine acetate is a prodrug that is extensively metabolized to eslicarbazepine, the active moiety. Eslicarbazepine blocks voltage-gated sodium channels, stabilizing hyperexcited neuronal membranes, inhibiting repetitive neuronal firing, and decreasing synaptic impulse propagation. It preferentially binds to the inactivated state of the sodium channel.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 100% (of eslicarbazepine from the prodrug)
Tmax:
2-3 hours
FoodEffect:
No clinically significant effect of food on absorption.
Distribution:
Vd:
Approximately 100 L
ProteinBinding:
Approximately 40%
CnssPenetration:
Yes
Elimination:
HalfLife:
10-20 hours (eslicarbazepine)
Clearance:
Approximately 10 L/hour (eslicarbazepine)
ExcretionRoute:
Renal
Unchanged:
Approximately 60-70% (as eslicarbazepine and its glucuronide)
Pharmacodynamics
OnsetOfAction:
Not precisely defined for seizure control; steady-state concentrations are typically achieved within 4-5 days.
PeakEffect:
Not precisely defined for seizure control; related to steady-state concentrations.
DurationOfAction:
Once-daily dosing due to half-life.
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
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 changes in seizure patterns after starting this medication
Inability to control eye movements
Difficulty walking
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other serious reactions, which can affect body organs and be life-threatening
Signs of severe skin reactions, such as:
+ Red, swollen, blistered, or peeling skin
+ Red or irritated eyes
+ Sores in the mouth, throat, nose, eyes, genitals, or skin
+ Fever
+ Chills
+ Body aches
+ Shortness of breath
+ Swollen glands
Angioedema, a severe reaction that can be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
Other Possible Side Effects
Most people experience no side effects or only mild side effects while taking this medication. However, if you notice any of the following symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Headache
Dizziness
Drowsiness
Fatigue
Weakness
Upset stomach or vomiting
* Shakiness
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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
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 changes in seizure patterns after starting this medication
Inability to control eye movements
Difficulty walking
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other serious reactions, which can affect body organs and be life-threatening
Signs of severe skin reactions, such as:
+ Red, swollen, blistered, or peeling skin
+ Red or irritated eyes
+ Sores in the mouth, throat, nose, eyes, genitals, or skin
+ Fever
+ Chills
+ Body aches
+ Shortness of breath
+ Swollen glands
Angioedema, a severe reaction that can be life-threatening, characterized by:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
Other Possible Side Effects
Most people experience no side effects or only mild side effects while taking this medication. However, if you notice any of the following symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Headache
Dizziness
Drowsiness
Fatigue
Weakness
Upset stomach or vomiting
* Shakiness
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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 mood changes, depression, anxiety, agitation, or thoughts of self-harm (suicidal ideation)
- Severe skin rash, blistering, or peeling skin, fever, swollen glands (signs of serious skin reactions like SJS/TEN)
- Symptoms of low sodium (hyponatremia) such as nausea, tiredness, headache, confusion, or more frequent or severe seizures
- Unusual bleeding or bruising, fever, sore throat (signs of blood problems)
- Yellowing of skin or eyes, dark urine, severe stomach pain (signs of liver problems)
- Swelling of the face, lips, tongue, or throat, difficulty breathing (signs of allergic reaction)
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 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.
To guarantee your safety, do not start, stop, or modify the dose of any medication without first consulting your doctor. It is your responsibility to verify that it is safe to take this medication in conjunction 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 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.
To guarantee your safety, do not start, stop, or modify the dose of any medication without first consulting your doctor. It is your responsibility to verify that it is safe to take this medication in conjunction 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.
Caution with Daily Activities
Until you know how this medication affects you, avoid driving and other tasks that require alertness.
Stopping the Medication
Do not suddenly stop taking this medication without 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 discontinue it.
Monitoring for Rare but Serious Side Effects
Rarely, this medication can cause low blood cell counts. Immediately contact your doctor if you experience any unexplained bruising or bleeding, signs of infection such as fever, chills, or sore throat, or if you feel extremely tired or weak.
Regular Blood Tests
Follow your doctor's instructions for regular blood tests to monitor your condition.
Interactions with Other Substances
Before consuming alcohol, marijuana, or other forms of cannabis, or taking prescription or over-the-counter medications that may cause drowsiness, discuss the potential risks with your doctor.
Suicidal Thoughts or Actions
Like other medications used to treat seizures, this medication may rarely increase the risk of suicidal thoughts or actions, particularly in individuals with a history of such thoughts or actions. Immediately contact your doctor if you experience any new or worsening symptoms, such as depression, nervousness, restlessness, irritability, panic attacks, or other mood or behavioral changes. If you have suicidal thoughts or actions, seek immediate medical attention.
Special Considerations for Older Adults
If you are 60 years or older, use this medication with caution, as you may be more susceptible to side effects.
Birth Control and Pregnancy
Birth control pills and other hormone-based birth control methods may be less effective while taking this medication. Use an additional form of birth control, such as a condom, to prevent pregnancy. If you are pregnant or become pregnant while taking this medication, contact your doctor immediately, as it may harm the unborn baby.
Breastfeeding
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Children
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.
Caution with Daily Activities
Until you know how this medication affects you, avoid driving and other tasks that require alertness.
Stopping the Medication
Do not suddenly stop taking this medication without 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 discontinue it.
Monitoring for Rare but Serious Side Effects
Rarely, this medication can cause low blood cell counts. Immediately contact your doctor if you experience any unexplained bruising or bleeding, signs of infection such as fever, chills, or sore throat, or if you feel extremely tired or weak.
Regular Blood Tests
Follow your doctor's instructions for regular blood tests to monitor your condition.
Interactions with Other Substances
Before consuming alcohol, marijuana, or other forms of cannabis, or taking prescription or over-the-counter medications that may cause drowsiness, discuss the potential risks with your doctor.
Suicidal Thoughts or Actions
Like other medications used to treat seizures, this medication may rarely increase the risk of suicidal thoughts or actions, particularly in individuals with a history of such thoughts or actions. Immediately contact your doctor if you experience any new or worsening symptoms, such as depression, nervousness, restlessness, irritability, panic attacks, or other mood or behavioral changes. If you have suicidal thoughts or actions, seek immediate medical attention.
Special Considerations for Older Adults
If you are 60 years or older, use this medication with caution, as you may be more susceptible to side effects.
Birth Control and Pregnancy
Birth control pills and other hormone-based birth control methods may be less effective while taking this medication. Use an additional form of birth control, such as a condom, to prevent pregnancy. If you are pregnant or become pregnant while taking this medication, contact your doctor immediately, as it may harm the unborn baby.
Breastfeeding
If you are breastfeeding, consult your doctor to discuss any potential risks to your baby.
Children
If your child's weight changes, consult your doctor, as the dosage of this medication may need to be adjusted.
Overdose Information
Overdose Symptoms:
- Dizziness
- Double vision
- Blurred vision
- Ataxia (loss of coordination)
- Nausea
- Vomiting
- Somnolence (extreme drowsiness)
- Hyponatremia
What to Do:
Seek immediate medical attention or call Poison Control at 1-800-222-1222. Treatment is generally supportive and symptomatic. There is no specific antidote.
Drug Interactions
Major Interactions
- Oral contraceptives (decreased efficacy of hormonal contraceptives)
- Phenytoin (increased phenytoin levels, decreased eslicarbazepine levels)
- Carbamazepine (decreased eslicarbazepine levels)
- Simvastatin (decreased simvastatin levels)
Monitoring
Baseline Monitoring
Renal function (CrCl)
Rationale: To determine appropriate starting dose and dose adjustments.
Timing: Prior to initiation
Serum sodium
Rationale: To establish baseline and identify patients at higher risk for hyponatremia.
Timing: Prior to initiation
Liver function tests (ALT, AST, bilirubin)
Rationale: Although not extensively metabolized by liver, baseline is useful.
Timing: Prior to initiation
Routine Monitoring
Serum sodium
Frequency: Periodically, especially during the first 3 months of treatment 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.
Renal function (CrCl)
Frequency: Periodically, especially in elderly or those with risk factors for renal impairment.
Target: >60 mL/min (for standard dosing)
Action Threshold: CrCl <60 mL/min requires dose adjustment.
Seizure frequency and severity
Frequency: Regularly throughout treatment.
Target: Reduction or elimination of seizures
Action Threshold: Increased seizure frequency or severity may indicate need for dose adjustment or alternative therapy.
Symptom Monitoring
- Signs and symptoms of hyponatremia (e.g., nausea, malaise, headache, lethargy, confusion, seizures)
- Signs and symptoms of suicidal ideation or behavior (e.g., new or worsening depression, anxiety, agitation, panic attacks, insomnia, irritability, hostility, aggressiveness, impulsivity, akathisia, hypomania, mania)
- Dizziness, somnolence, fatigue, ataxia, blurred vision, diplopia
- Skin rash or other hypersensitivity reactions (e.g., Stevens-Johnson Syndrome, Toxic Epidermal Necrolysis)
- Signs of hepatic dysfunction (e.g., jaundice, dark urine, abdominal pain)
Special Patient Groups
Pregnancy
Aptiom may cause harm to a fetus. Use during pregnancy should only be considered if the potential benefit outweighs the potential risk to the fetus. Patients should be enrolled in a pregnancy registry.
Trimester-Specific Risks:
First Trimester:
Increased risk of major congenital malformations (e.g., neural tube defects, cardiovascular defects, oral clefts) compared to general population, though specific data for eslicarbazepine is limited. Risk may be lower than with carbamazepine.
Second Trimester:
Not specifically studied, but continued exposure may contribute to risks.
Third Trimester:
Not specifically studied, but continued exposure may contribute to risks. Potential for withdrawal symptoms in neonates if discontinued abruptly.
Lactation
Eslicarbazepine is excreted into human 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 adequate weight gain.
Infant Risk:
Low to moderate risk. Monitor for drowsiness, poor feeding, irritability.
Pediatric Use
Approved for adjunctive treatment of partial-onset seizures in patients 4 years of age and older. Dosing is weight-based for younger children. Safety and efficacy in patients younger than 4 years have not been established.
Geriatric Use
Use with caution in elderly patients due to increased risk of adverse reactions, particularly hyponatremia, dizziness, and falls. Start at the lower end of the dosing range and titrate slowly, monitoring renal function and serum sodium closely.
Clinical Information
Clinical Pearls
- Eslicarbazepine acetate is a prodrug of eslicarbazepine, which is structurally related to carbamazepine and oxcarbazepine, but has a distinct metabolic pathway.
- Once-daily dosing improves patient adherence.
- Monitor serum sodium levels, especially during the first few months of treatment, due to the risk of hyponatremia.
- Counsel patients on the risk of suicidal thoughts and behaviors, as with all AEDs.
- Be aware of significant drug interactions, particularly with oral contraceptives and other AEDs like phenytoin and carbamazepine.
Alternative Therapies
- Carbamazepine
- Oxcarbazepine
- Lamotrigine
- Levetiracetam
- Lacosamide
- Phenytoin
- Topiramate
- Zonisamide
Cost & Coverage
Average Cost:
$300-$600 per 30 tablets (200mg)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Brand), Tier 1 (Generic)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure your safety, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which is a crucial patient fact sheet. Please read it carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, we encourage you to discuss them with 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 detailed information, including the substance taken, the amount, and the time it occurred.