Levetiracetam 500mg/5ml Inj, 5ml
It is used to treat seizures.
Drug Class
Anticonvulsant
Pharmacologic Class
Pyrrolidine derivative, Synaptic Vesicle Protein 2A (SV2A) ligand
Pregnancy Category
C
FDA Approved
Nov 1999
DEA Schedule
Not Controlled
Overview
What is this medicine?
Levetiracetam is a medication used to treat certain types of seizures (epilepsy). It works by affecting certain substances in the brain to help calm overactive nerve signals that cause seizures. The injection form is used when you cannot take the medicine by mouth, for example, in a hospital setting.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and adhere to all guidelines provided. This medication is administered as an intravenous infusion, which means it is given through a vein over a specified period of time.
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
If you need to store this medication at home, consult with your doctor, nurse, or pharmacist to determine the proper storage procedure.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
Lifestyle & Tips
- Do not stop taking this medication suddenly, as it can worsen seizures. Always consult your doctor before making any changes.
- Avoid driving or operating heavy machinery until you know how this medication affects you, as it can cause dizziness and drowsiness.
- Avoid alcohol consumption, as it can increase drowsiness and dizziness.
- Report any new or worsening mood changes, depression, or suicidal thoughts to your doctor immediately.
- Maintain regular follow-up appointments with your doctor to monitor your condition and medication effectiveness.
Available Forms & Alternatives
Available Strengths:
- Levetiracetam 100mg/ml Solution
- Levetiracetam 1000mg Tablets
- Levetiracetam 250mg Tablets
- Levetiracetam 750mg Tablets
- Levetiracetam 500mg Tablets
- Levetiracetam ER 500mg Tablets
- Levetiracetam ER 750mg Tablets
- Levetiracetam 500mg/5ml Inj, 5ml
- Levetiracetam ER 500mg Tablets
- Levetiracetam ER 750mg Tablets
Dosing & Administration
Adult Dosing
Standard Dose:
Initial 500 mg IV twice daily (BID), infused over 15 minutes. May increase by 500 mg BID every 2 weeks to a maximum of 1500 mg BID.
Dose Range:
500 - 1500 mg
Condition-Specific Dosing:
partialOnsetSeizures:
Initial 500 mg IV BID, max 1500 mg IV BID.
myoclonicSeizures:
Initial 500 mg IV BID, max 1500 mg IV BID.
generalizedTonicClonicSeizures:
Initial 500 mg IV BID, max 1500 mg IV BID.
Pediatric Dosing
Neonatal:
Not established (often used off-label, dose typically 10-20 mg/kg/dose every 12 hours, adjusted based on response and tolerability).
Infant:
1 month to <4 years: Initial 10 mg/kg IV BID, increase by 10 mg/kg BID every 2 weeks to a maximum of 25 mg/kg IV BID.
Child:
4 years to <16 years: Initial 10 mg/kg IV BID, increase by 10 mg/kg BID every 2 weeks to a maximum of 30 mg/kg IV BID.
Adolescent:
16 years and older: Same as adult dosing (Initial 500 mg IV BID, max 1500 mg IV BID).
Dose Adjustments
Renal Impairment:
Mild:
CrCl 50-80 mL/min: 500-1000 mg IV BID.
Moderate:
CrCl 30-50 mL/min: 250-750 mg IV BID.
Severe:
CrCl <30 mL/min: 250-500 mg IV BID.
Dialysis:
ESRD patients on dialysis: 500-1000 mg IV once daily, with an additional 250-500 mg IV post-dialysis.
Hepatic Impairment:
Mild:
No dose adjustment necessary.
Moderate:
No dose adjustment necessary.
Severe:
No dose adjustment necessary for hepatic impairment alone. If severe hepatic impairment is accompanied by significant renal impairment, dose adjustment for renal impairment should be applied.
Pharmacology
Mechanism of Action
The precise mechanism of action of levetiracetam is unknown. It differs from other antiepileptic drugs. It binds to the synaptic vesicle protein 2A (SV2A), a ubiquitous integral membrane protein of synaptic vesicles, which is thought to be involved in the modulation of neurotransmitter release. This binding may contribute to its anticonvulsant effects by preventing hypersynchronization of burst firing and propagation of seizure activity.
Pharmacokinetics
Absorption:
Bioavailability:
100%
Tmax:
Not applicable (IV administration, immediate systemic availability)
FoodEffect:
Not applicable (IV administration)
Distribution:
Vd:
0.5-0.7 L/kg
ProteinBinding:
<10%
CnssPenetration:
Yes
Elimination:
HalfLife:
Adults: 7 Âą 1 hours; Children: 5-7 hours; Renal impairment: Prolonged (up to 25 hours in ESRD)
Clearance:
Approximately 0.96 mL/min/kg in adults
ExcretionRoute:
Renal (primarily unchanged drug and inactive metabolite)
Unchanged:
Approximately 66%
Pharmacodynamics
OnsetOfAction:
Rapid (within minutes of IV administration)
PeakEffect:
Rapid (within minutes of IV administration)
DurationOfAction:
Approximately 12 hours (consistent with BID 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
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Hallucinations (seeing or hearing things that are not there)
Severe dizziness or fainting
Changes in balance
Difficulty walking
Suicidal thoughts or actions (especially if you have a history of suicidal thoughts or actions)
New or worsening symptoms of depression, nervousness, restlessness, or mood changes
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 may include:
- 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
Low blood cell counts, which can increase the risk of:
+ Infections
+ Bleeding problems
+ Anemia
+ Signs may include:
- Fever
- Chills
- Sore throat
- Unexplained bruising or bleeding
- Feeling very tired or weak
Angioedema, a severe reaction that can be life-threatening, with signs including:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
Other Possible Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Diarrhea
Stomach pain
Upset stomach
Vomiting
Decreased appetite
Dizziness
Drowsiness
Fatigue
Weakness
Nose or throat irritation
Trouble sleeping
Headache
Flu-like symptoms
This is not an exhaustive list of possible side effects. If you have questions or concerns, 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
Signs of liver problems, including:
+ Dark urine
+ Tiredness
+ Decreased appetite
+ Upset stomach or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or eyes
Hallucinations (seeing or hearing things that are not there)
Severe dizziness or fainting
Changes in balance
Difficulty walking
Suicidal thoughts or actions (especially if you have a history of suicidal thoughts or actions)
New or worsening symptoms of depression, nervousness, restlessness, or mood changes
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 may include:
- 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
Low blood cell counts, which can increase the risk of:
+ Infections
+ Bleeding problems
+ Anemia
+ Signs may include:
- Fever
- Chills
- Sore throat
- Unexplained bruising or bleeding
- Feeling very tired or weak
Angioedema, a severe reaction that can be life-threatening, with signs including:
+ Swelling of the hands, face, lips, eyes, tongue, or throat
+ Trouble breathing
+ Trouble swallowing
+ Unusual hoarseness
Other Possible Side Effects
Most people do not experience severe side effects, but some may occur. If you notice any of the following symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Diarrhea
Stomach pain
Upset stomach
Vomiting
Decreased appetite
Dizziness
Drowsiness
Fatigue
Weakness
Nose or throat irritation
Trouble sleeping
Headache
Flu-like symptoms
This is not an exhaustive list of possible side effects. If you have questions or concerns, 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:
- Severe dizziness or drowsiness
- Unusual mood or behavior changes (e.g., agitation, aggression, depression, anxiety)
- Thoughts of self-harm or suicide
- New or worsening seizures
- Fever, sore throat, or other signs of infection (rare, but possible blood dyscrasias)
- Unusual bruising or bleeding
- Severe skin rash (rare, but possible Stevens-Johnson syndrome or toxic epidermal necrolysis)
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 kidney disease or are undergoing dialysis.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication in conjunction with your other medications and health issues. Never start, stop, or adjust the dosage 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 symptoms you experienced.
If you have kidney disease or are undergoing dialysis.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health conditions with your doctor and pharmacist. They will help determine if it is safe to take this medication in conjunction with your other medications and health issues. Never start, stop, or adjust the dosage 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.
Until you understand how this drug affects you, avoid operating a vehicle or engaging in any activities that require your full attention. Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions, consult with your doctor.
As directed by your doctor, regularly undergo blood tests and other laboratory examinations to monitor your condition. If you experience any changes in the frequency or severity of seizures after starting this medication, discuss these changes with your doctor.
Do not abruptly discontinue this medication without first consulting your doctor, as this may increase your risk of experiencing seizures. If it is necessary to stop taking this drug, your doctor will instruct you on how to gradually taper off the medication to minimize potential risks.
If you are 65 years or older, exercise caution when using this medication, as you may be more susceptible to side effects. Similarly, when administering this drug to children, use it with caution, as they may have a higher risk of experiencing certain side effects. Not all formulations of this medication are suitable for all children, so it is crucial to consult with your doctor before giving it to a child.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor, as you will need to discuss the potential benefits and risks of this medication to both you and your baby. Be aware that this drug may be less effective in controlling seizures during pregnancy, and if you have any concerns, consult with your doctor.
Until you understand how this drug affects you, avoid operating a vehicle or engaging in any activities that require your full attention. Before consuming alcohol, using marijuana or other cannabis products, or taking prescription or over-the-counter medications that may impair your reactions, consult with your doctor.
As directed by your doctor, regularly undergo blood tests and other laboratory examinations to monitor your condition. If you experience any changes in the frequency or severity of seizures after starting this medication, discuss these changes with your doctor.
Do not abruptly discontinue this medication without first consulting your doctor, as this may increase your risk of experiencing seizures. If it is necessary to stop taking this drug, your doctor will instruct you on how to gradually taper off the medication to minimize potential risks.
If you are 65 years or older, exercise caution when using this medication, as you may be more susceptible to side effects. Similarly, when administering this drug to children, use it with caution, as they may have a higher risk of experiencing certain side effects. Not all formulations of this medication are suitable for all children, so it is crucial to consult with your doctor before giving it to a child.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor, as you will need to discuss the potential benefits and risks of this medication to both you and your baby. Be aware that this drug may be less effective in controlling seizures during pregnancy, and if you have any concerns, consult with your doctor.
Overdose Information
Overdose Symptoms:
- Somnolence
- Agitation
- Aggression
- Depressed level of consciousness
- Respiratory depression
- Coma
What to Do:
In case of overdose, seek immediate medical attention or call a Poison Control Center (1-800-222-1222). There is no specific antidote. Treatment is supportive and may include gastric lavage or emesis if oral overdose, and hemodialysis can remove levetiracetam.
Drug Interactions
Major Interactions
- Methotrexate (Levetiracetam may decrease the renal clearance of methotrexate, potentially leading to methotrexate toxicity. Monitor methotrexate levels and adjust dose as needed.)
Moderate Interactions
Monitoring
Baseline Monitoring
Renal function (CrCl)
Rationale: Levetiracetam is primarily renally eliminated, and dose adjustments are necessary in patients with impaired renal function.
Timing: Prior to initiation of therapy.
Routine Monitoring
Clinical response (seizure frequency and severity)
Frequency: Ongoing, at each follow-up visit.
Target: Reduction or cessation of seizures.
Action Threshold: Inadequate seizure control may warrant dose increase or addition of another AED.
Adverse effects (e.g., somnolence, dizziness, behavioral changes, psychiatric symptoms)
Frequency: Ongoing, at each follow-up visit.
Target: Absence or tolerability of side effects.
Action Threshold: Significant or intolerable side effects may require dose reduction or discontinuation.
Renal function (CrCl)
Frequency: Periodically, especially in elderly patients or those with pre-existing renal impairment, or if clinical status changes.
Target: Stable renal function.
Action Threshold: Decline in renal function necessitates dose adjustment.
Symptom Monitoring
- Drowsiness
- Dizziness
- Fatigue
- Weakness
- Coordination difficulties
- Irritability
- Aggression
- Anxiety
- Depression
- Mood changes
- Psychotic symptoms
- Suicidal thoughts or behavior
- New or worsening seizures
Special Patient Groups
Pregnancy
Levetiracetam is classified as Pregnancy Category C. Studies in animals have shown adverse effects on the fetus, but there are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Women of childbearing potential should be counseled on the risks and benefits.
Trimester-Specific Risks:
First Trimester:
Potential for increased risk of major congenital malformations, though data are somewhat conflicting and overall risk appears lower than some other AEDs. Discuss with physician.
Second Trimester:
Continued monitoring of maternal and fetal health.
Third Trimester:
Continued monitoring. Consider monitoring levetiracetam levels as clearance may increase during pregnancy, potentially requiring dose adjustments.
Lactation
Levetiracetam is excreted into human breast milk. The decision to breastfeed should consider the potential for infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. Monitor breastfed infants for drowsiness, irritability, and poor feeding.
Infant Risk:
Low to moderate risk. Monitor for sedation, poor feeding, or developmental milestones.
Pediatric Use
Approved for use in children as young as 1 month for certain seizure types. Dosing is weight-based and adjusted according to age and response. Younger children may have faster clearance, requiring higher mg/kg doses.
Geriatric Use
No specific dose adjustment is required based on age alone. However, elderly patients are more likely to have decreased renal function, which necessitates dose adjustment based on creatinine clearance. Start with lower doses and titrate slowly, monitoring for adverse effects.
Clinical Information
Clinical Pearls
- Levetiracetam has a broad spectrum of activity against various seizure types and is generally well-tolerated.
- It has a favorable pharmacokinetic profile with minimal protein binding and no significant CYP450 interactions, making it a good choice for polytherapy.
- The IV formulation is useful for patients who are NPO (nothing by mouth), in status epilepticus, or when rapid attainment of therapeutic levels is needed.
- Behavioral and psychiatric side effects (e.g., irritability, aggression, depression, anxiety) are common, especially early in treatment or with rapid dose escalation. Patients and caregivers should be counseled on these potential effects.
- Renal dose adjustment is crucial to prevent accumulation and toxicity.
Alternative Therapies
- Phenytoin (IV)
- Fosphenytoin (IV)
- Valproate (IV)
- Lacosamide (IV)
- Benzodiazepines (e.g., lorazepam, diazepam - for acute seizure termination)
- Phenobarbital (IV)
Cost & Coverage
Average Cost:
Check current market pricing per 5ml vial
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (for generic), Tier 3 (for brand)
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, do not flush medications down the toilet or drain. If you are unsure about the proper disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may have additional patient information leaflets, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek medical attention. Be prepared to provide information about the medication taken, the amount, and the time it occurred.