Rufinamide 40mg/ml Suspension 460ml
It is used to help control certain kinds of seizures.
Drug Class
Antiepileptic drug (AED)
Pharmacologic Class
Triazole derivative, sodium channel modulator
Pregnancy Category
Category C
FDA Approved
Nov 2008
DEA Schedule
Not Controlled
Overview
What is this medicine?
Rufinamide is a medicine used to help control seizures, especially in people with a severe type of epilepsy called Lennox-Gastaut Syndrome. It works by calming overactive electrical signals in the brain that cause seizures.
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.
Always take your medication with food.
If the adapter is not already attached to the bottle, prepare it according to the instructions you received or follow the package insert guidelines.
Before using, shake the bottle well to mix the contents.
Only use the measuring device that comes with your medication to ensure accurate dosing.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start feeling better. Do not change your dose or stop taking the medication without consulting your doctor, as this may cause seizures.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it at room temperature in a dry place, avoiding bathrooms.
Discard any unused portion 90 days after opening the bottle.
Keep the bottle upright with the cap tightly closed.
What to Do If You Miss a Dose
If you miss a dose, follow these guidelines:
Take the missed dose as soon as you remember.
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 to make up for the missed one.
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.
Always take your medication with food.
If the adapter is not already attached to the bottle, prepare it according to the instructions you received or follow the package insert guidelines.
Before using, shake the bottle well to mix the contents.
Only use the measuring device that comes with your medication to ensure accurate dosing.
Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start feeling better. Do not change your dose or stop taking the medication without consulting your doctor, as this may cause seizures.
Storing and Disposing of Your Medication
To maintain the quality and safety of your medication:
Store it at room temperature in a dry place, avoiding bathrooms.
Discard any unused portion 90 days after opening the bottle.
Keep the bottle upright with the cap tightly closed.
What to Do If You Miss a Dose
If you miss a dose, follow these guidelines:
Take the missed dose as soon as you remember.
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 to make up for the missed one.
Lifestyle & Tips
- Take with food to improve absorption and reduce stomach upset.
- Do not stop taking this medication suddenly, as it can worsen seizures. Always consult your doctor before making any changes.
- Avoid alcohol and other CNS depressants, as they can increase side effects like dizziness and drowsiness.
- Use caution when driving or operating machinery until you know how this medication affects you.
- If you are using hormonal birth control, rufinamide may make it less effective. Discuss alternative or additional birth control methods with your doctor.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial: 400 mg/day in 2 divided doses. Titrate by 400 mg/day every 2 days to a target dose of 3200 mg/day in 2 divided doses.
Dose Range:
400 - 3200 mg
Condition-Specific Dosing:
Lennox-Gastaut Syndrome (LGS):
Target dose 3200 mg/day in 2 divided doses. Max 3200 mg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for infants under 1 year of age.
Child:
1 to <4 years: Initial 10 mg/kg/day in 2 divided doses. Titrate by 10 mg/kg/day every 2 days to a target dose of 45 mg/kg/day (max 1800 mg/day). Max 45 mg/kg/day or 1800 mg/day, whichever is less.
4 to <7 years: Initial 10 mg/kg/day in 2 divided doses. Titrate by 10 mg/kg/day every 2 days to a target dose of 45 mg/kg/day (max 2700 mg/day). Max 45 mg/kg/day or 2700 mg/day, whichever is less.
7 to <12 years: Initial 10 mg/kg/day in 2 divided doses. Titrate by 10 mg/kg/day every 2 days to a target dose of 45 mg/kg/day (max 3200 mg/day). Max 45 mg/kg/day or 3200 mg/day, whichever is less.
Adolescent:
12 years and older: Initial 400 mg/day in 2 divided doses. Titrate by 400 mg/day every 2 days to a target dose of 3200 mg/day in 2 divided doses. Max 3200 mg/day.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
No specific dose adjustment recommended.
Severe:
No specific dose adjustment recommended, but use with caution due to limited data.
Dialysis:
Not significantly removed by hemodialysis. No specific dose adjustment recommended, but use with caution.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended.
Moderate:
Use with caution; start at a lower dose and titrate slowly. No specific guidelines available.
Severe:
Use with caution; start at a lower dose and titrate slowly. No specific guidelines available.
Pharmacology
Mechanism of Action
Rufinamide is a triazole derivative that is thought to exert its antiepileptic effect by modulating the activity of sodium channels, specifically by prolonging the inactive state of voltage-gated sodium channels. This limits sustained repetitive firing of sodium-dependent action potentials and reduces the spread of seizure activity.
Pharmacokinetics
Absorption:
Bioavailability:
Not available (well absorbed)
Tmax:
4-6 hours
FoodEffect:
Increased Cmax and AUC by approximately 30% and 34% respectively when taken with food.
Distribution:
Vd:
0.7-1 L/kg
ProteinBinding:
Approximately 34%
CnssPenetration:
Yes
Elimination:
HalfLife:
6-10 hours
Clearance:
Not available (primarily renal excretion of metabolites)
ExcretionRoute:
Renal (approximately 85% as metabolites, <2% as unchanged drug)
Unchanged:
<2%
Pharmacodynamics
OnsetOfAction:
Not precisely defined, but therapeutic effects are observed with titration to target doses.
PeakEffect:
Correlates with Tmax (4-6 hours) for single dose; steady state achieved within 2 days with twice-daily dosing.
DurationOfAction:
Related to half-life (6-10 hours), requiring twice-daily dosing.
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
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
Shakiness or tremors
Changes in vision
Inability to control eye movements
Suicidal thoughts or actions, especially if you have a history of suicidal behavior (see below)
Like other seizure medications, this drug may increase the risk of suicidal thoughts or actions, particularly in people with a history of suicidal behavior. If you experience any new or worsening symptoms, such as:
Depression
Anxiety, restlessness, or irritability
Panic attacks
Mood or behavior changes
contact your doctor right away. If you have suicidal thoughts or actions, seek help immediately.
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 right away:
Swollen glands
Fever
Rash
Painful sores in the mouth or around the eyes
Chest pain
Signs of kidney problems, such as:
+ Inability to urinate
+ Changes in urine output
Signs of liver problems, such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
This medication may also cause a decrease in white blood cell count, increasing the risk of infection. If you experience any signs of infection, such as:
Fever
Chills
Sore throat
contact your doctor right away.
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
Nausea or vomiting
Flu-like symptoms
Nose or throat irritation
Decreased appetite
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 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
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
Shakiness or tremors
Changes in vision
Inability to control eye movements
Suicidal thoughts or actions, especially if you have a history of suicidal behavior (see below)
Like other seizure medications, this drug may increase the risk of suicidal thoughts or actions, particularly in people with a history of suicidal behavior. If you experience any new or worsening symptoms, such as:
Depression
Anxiety, restlessness, or irritability
Panic attacks
Mood or behavior changes
contact your doctor right away. If you have suicidal thoughts or actions, seek help immediately.
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 right away:
Swollen glands
Fever
Rash
Painful sores in the mouth or around the eyes
Chest pain
Signs of kidney problems, such as:
+ Inability to urinate
+ Changes in urine output
Signs of liver problems, such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
This medication may also cause a decrease in white blood cell count, increasing the risk of infection. If you experience any signs of infection, such as:
Fever
Chills
Sore throat
contact your doctor right away.
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
Nausea or vomiting
Flu-like symptoms
Nose or throat irritation
Decreased appetite
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 accompanied by fever, swollen lymph nodes, or facial swelling (signs of DRESS syndrome).
- Any changes in mood or behavior, including new or worsening depression, anxiety, agitation, or thoughts of self-harm.
- Severe dizziness, extreme tiredness, or problems with coordination.
- Vision changes, such as double vision.
- Signs of liver problems (e.g., yellowing of skin/eyes, dark urine, persistent nausea/vomiting).
- Unusual bleeding or bruising.
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 been diagnosed with Familial Short QT syndrome, a rare heart condition.
If you have liver disease, as this may affect how your body processes the medication.
This list is not exhaustive, and it is crucial to discuss all your medications, health conditions, and supplements with your doctor and pharmacist. This includes:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins
Any health problems you have or have had in the past
Your doctor needs this information to determine if it is safe for you to take this medication and to ensure that it will not interact with any other medications or worsen any health conditions you have. Do not start, stop, or change the dose of any medication without first consulting 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 been diagnosed with Familial Short QT syndrome, a rare heart condition.
If you have liver disease, as this may affect how your body processes the medication.
This list is not exhaustive, and it is crucial to discuss all your medications, health conditions, and supplements with your doctor and pharmacist. This includes:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins
Any health problems you have or have had in the past
Your doctor needs this information to determine if it is safe for you to take this medication and to ensure that it will not interact with any other medications or worsen any health conditions you have. Do not start, stop, or change the dose of any medication without first consulting your doctor.
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, ensure you understand how this drug affects you.
To minimize the risk of seizures, do not abruptly discontinue this medication without first consulting your doctor. If you need to stop taking this drug, your doctor will instruct you on how to gradually taper off the dosage. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition.
Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may cause drowsiness, consult with your doctor. If you experience any changes in the frequency or severity of seizures after starting this medication, notify your doctor promptly.
When taking this medication, it is crucial to be aware that birth control pills and other hormone-based contraceptives may be less effective in preventing pregnancy. To minimize the risk of unplanned pregnancy, consider using an additional form of birth control, such as condoms. If you are pregnant, planning to become pregnant, or are breastfeeding, discuss the potential benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
To minimize the risk of seizures, do not abruptly discontinue this medication without first consulting your doctor. If you need to stop taking this drug, your doctor will instruct you on how to gradually taper off the dosage. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition.
Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may cause drowsiness, consult with your doctor. If you experience any changes in the frequency or severity of seizures after starting this medication, notify your doctor promptly.
When taking this medication, it is crucial to be aware that birth control pills and other hormone-based contraceptives may be less effective in preventing pregnancy. To minimize the risk of unplanned pregnancy, consider using an additional form of birth control, such as condoms. If you are pregnant, planning to become pregnant, or are breastfeeding, discuss the potential benefits and risks of this medication with your doctor to ensure the best possible outcome for you and your baby.
Overdose Information
Overdose Symptoms:
- Ataxia (loss of coordination)
- Somnolence (extreme drowsiness)
- Nystagmus (involuntary eye movements)
- Headache
- Dizziness
- Nausea
- Vomiting
What to Do:
Seek immediate medical attention. Call 911 or your local poison control center (1-800-222-1222 in the US). Treatment is supportive and may include gastric lavage or activated charcoal if ingestion is recent.
Drug Interactions
Major Interactions
- Valproate (decreases rufinamide clearance, leading to increased rufinamide levels)
- Phenytoin (induces rufinamide metabolism, leading to decreased rufinamide levels)
- Carbamazepine (induces rufinamide metabolism, leading to decreased rufinamide levels)
- Phenobarbital (induces rufinamide metabolism, leading to decreased rufinamide levels)
- Oral contraceptives (rufinamide may decrease efficacy of hormonal contraceptives)
Moderate Interactions
- Topiramate (may increase rufinamide levels, monitor for adverse effects)
- Other CNS depressants (additive CNS depression)
Monitoring
Baseline Monitoring
Complete Blood Count (CBC)
Rationale: To establish baseline and monitor for potential hematologic abnormalities.
Timing: Prior to initiation
Liver Function Tests (LFTs)
Rationale: To establish baseline and monitor for potential hepatic impairment.
Timing: Prior to initiation
Renal Function Tests (RFTs)
Rationale: To establish baseline and monitor for potential renal impairment.
Timing: Prior to initiation
Electrocardiogram (ECG)
Rationale: To assess baseline QT interval, as rufinamide can cause QT shortening.
Timing: Prior to initiation
Routine Monitoring
Seizure frequency and severity
Frequency: Regularly throughout treatment
Target: Reduction in seizure frequency
Action Threshold: Lack of efficacy or worsening seizures
Adverse effects (e.g., CNS effects, skin reactions)
Frequency: Regularly, especially during titration
Target: Absence or tolerability of side effects
Action Threshold: Intolerable or severe adverse effects
Suicidal ideation/behavior
Frequency: Regularly, especially during initial therapy and dose changes
Target: Absence of suicidal thoughts or behaviors
Action Threshold: Emergence or worsening of suicidal thoughts/behaviors
QT interval on ECG
Frequency: Periodically, especially if patient has underlying cardiac conditions or is on other QT-affecting drugs
Target: Normal QT interval
Action Threshold: Significant QT shortening or cardiac symptoms
Symptom Monitoring
- Dizziness
- Somnolence
- Nausea
- Vomiting
- Headache
- Fatigue
- Diplopia
- Ataxia
- Rash (including severe cutaneous adverse reactions like DRESS syndrome)
- Changes in mood or behavior (e.g., agitation, depression, suicidal thoughts)
- Signs of hypersensitivity reaction (fever, rash, lymphadenopathy, facial swelling, organ involvement)
Special Patient Groups
Pregnancy
Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Data from pregnancy registries are limited but suggest no major increase in risk of major congenital malformations compared to general population, but higher than unexposed pregnancies. However, uncontrolled seizures pose significant risks to both mother and fetus.
Trimester-Specific Risks:
First Trimester:
Potential for increased risk of major congenital malformations, though data are limited and conflicting.
Second Trimester:
Not specifically studied, but continued exposure may affect fetal development.
Third Trimester:
Not specifically studied, but continued exposure may affect fetal development.
Lactation
Rufinamide is excreted into breast milk. The decision to breastfeed should consider the developmental and health benefits of breastfeeding, the mother’s clinical need for rufinamide, and any potential adverse effects on the breastfed infant from rufinamide or from the underlying maternal condition. Monitor breastfed infants for sedation, poor feeding, and irritability.
Infant Risk:
L3 (Moderate risk) - Monitor infant for sedation, poor feeding, and irritability.
Pediatric Use
Approved for adjunctive treatment of seizures associated with Lennox-Gastaut Syndrome (LGS) in pediatric patients 1 year of age and older. Dosing is weight-based and requires careful titration.
Geriatric Use
Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Clinical Information
Clinical Pearls
- Always take rufinamide with food to optimize absorption and minimize gastrointestinal side effects.
- Titrate the dose slowly according to the recommended schedule to minimize adverse effects, especially CNS-related ones.
- Counsel patients on the risk of suicidal thoughts and behaviors, and advise them to report any changes in mood or behavior immediately.
- Be aware of potential drug interactions, especially with other antiepileptic drugs (e.g., valproate, phenytoin, carbamazepine, phenobarbital) and hormonal contraceptives.
- Monitor for signs of severe cutaneous adverse reactions (SCARs) such as DRESS syndrome, which can be life-threatening. Discontinue rufinamide at the first sign of rash unless the rash is clearly not drug-related.
- Rufinamide can cause QT interval shortening; monitor ECG in patients with pre-existing cardiac conditions or those on other QT-affecting medications.
Alternative Therapies
- Clobazam
- Fenfluramine
- Stiripentol
- Valproate
- Lamotrigine
- Topiramate
- Cannabidiol
- Felbamate
Cost & Coverage
Average Cost:
Varies widely, typically $500-$1500+ per 460ml bottle (40mg/ml)
Generic Available:
Yes
Insurance Coverage:
Tier 3 or Tier 4 (Specialty Drug)
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.