Marcaine 0.25% Inj, 10ml
WARNING: Seizures, sudden loss of heart function, and death have been reported when this drug was used as an epidural during childbirth. Most of the time, this happened with a certain strength of this drug that is not meant for use during labor. If you have questions, talk with the doctor. @ COMMON USES: It is used to numb an area before a procedure.
Drug Class
Local Anesthetic
Pharmacologic Class
Amide-type Local Anesthetic
Pregnancy Category
Category C
FDA Approved
Sep 1972
DEA Schedule
Not Controlled
Overview
What is this medicine?
Bupivacaine is a medicine called a 'local anesthetic' or 'numbing medicine'. It's given by injection to numb a specific part of your body, like an arm, leg, or an area for surgery or pain relief. It works by temporarily blocking nerve signals in that area, so you don't feel pain.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to follow the instructions carefully. This medication is administered via injection.
Storing and Disposing of Your Medication
This medication will be administered in a hospital or doctor's office, so you will not need to store it at home.
Missing a Dose
Since this medication is given as needed in a healthcare setting, you will not need to worry about missing a dose. The healthcare provider will administer the medication according to your medical needs.
To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to follow the instructions carefully. This medication is administered via injection.
Storing and Disposing of Your Medication
This medication will be administered in a hospital or doctor's office, so you will not need to store it at home.
Missing a Dose
Since this medication is given as needed in a healthcare setting, you will not need to worry about missing a dose. The healthcare provider will administer the medication according to your medical needs.
Lifestyle & Tips
- Follow all post-procedure instructions from your healthcare provider regarding activity restrictions or wound care while the area is numb.
- Avoid activities that could cause injury to the numb area (e.g., hot surfaces, sharp objects) until sensation returns.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Highly variable based on procedure, site, and patient factors. For 0.25% solution, typical doses range from 5-150 mg (2-60 mL) depending on the block type. E.g., for continuous epidural, 4-12.5 mg/hr (1.6-5 mL/hr) of 0.25% solution.
Dose Range:
5 - 150 mg
Condition-Specific Dosing:
infiltration:
Up to 175 mg (70 mL of 0.25%)
peripheralNerveBlock:
5-150 mg (2-60 mL of 0.25%)
epiduralBlock:
25-100 mg (10-40 mL of 0.25%) for surgical anesthesia; 12.5-25 mg (5-10 mL of 0.25%) for obstetric analgesia
caudalBlock:
37.5-75 mg (15-30 mL of 0.25%)
Pediatric Dosing
Neonatal:
Not established for routine use; extreme caution if used. Dosing is highly individualized and weight-based.
Infant:
Dosing is highly individualized and weight-based (e.g., 0.25-0.5 mg/kg per dose, max 2.5 mg/kg/24hr). Max single dose typically 2.5 mg/kg.
Child:
Dosing is highly individualized and weight-based (e.g., 0.25-0.5 mg/kg per dose, max 2.5 mg/kg/24hr). Max single dose typically 2.5 mg/kg.
Adolescent:
Similar to adult dosing, but caution with weight-based limits.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment typically required.
Moderate:
No specific adjustment typically required, but monitor for toxicity.
Severe:
No specific adjustment typically required, but monitor for toxicity due to potential accumulation of metabolites.
Dialysis:
Not significantly removed by hemodialysis. Monitor for toxicity.
Hepatic Impairment:
Mild:
No specific adjustment.
Moderate:
Use with caution; consider reduced doses and monitor for toxicity due to impaired metabolism.
Severe:
Use with extreme caution; significant dose reduction may be necessary. Monitor closely for signs of systemic toxicity.
Pharmacology
Mechanism of Action
Bupivacaine is an amide-type local anesthetic. It reversibly blocks the initiation and conduction of nerve impulses by decreasing the permeability of the neuronal membrane to sodium ions. This action stabilizes the membrane and inhibits depolarization, thereby preventing the propagation of the action potential and resulting in local anesthesia.
Pharmacokinetics
Absorption:
Bioavailability:
Highly variable, depends on site of injection, vascularity of tissue, and presence of vasoconstrictors (e.g., epinephrine). Systemic absorption occurs from all sites of administration.
Tmax:
Varies widely depending on site of injection (e.g., intercostal block: 10-20 min; epidural: 30-45 min).
FoodEffect:
Not applicable (parenteral administration).
Distribution:
Vd:
73 L (adults)
ProteinBinding:
Approximately 95% (primarily to alpha-1-acid glycoprotein and albumin).
CnssPenetration:
Limited at therapeutic doses, but can cross the blood-brain barrier and cause CNS toxicity at higher systemic concentrations.
Elimination:
HalfLife:
1.5-5.5 hours (adults), longer in neonates and infants.
Clearance:
Approximately 0.58 L/min (adults).
ExcretionRoute:
Renal (primarily as metabolites, small amount as unchanged drug).
Unchanged:
Approximately 5% (adults).
Pharmacodynamics
OnsetOfAction:
2-10 minutes (varies by concentration, dose, and site of injection).
PeakEffect:
30-45 minutes.
DurationOfAction:
2-8 hours (varies by concentration, dose, site, and presence of vasoconstrictor).
Confidence:
Medium
Safety & Warnings
BLACK BOX WARNING
There have been reports of cardiac arrest with difficult resuscitation or death during use of bupivacaine for epidural anesthesia in obstetrical patients. In most cases, this has followed the inadvertent intravascular injection of bupivacaine. Therefore, 0.75% bupivacaine is not recommended for obstetrical anesthesia. Intravenous regional anesthesia (IVRA) should not be performed with bupivacaine due to the risk of cardiac arrest and death.
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 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 acidosis (too much acid in the blood), such as:
+ Confusion
+ Fast breathing
+ Fast heartbeat
+ Abnormal heartbeat
+ Severe stomach pain, upset stomach, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling very tired or weak
Signs of methemoglobinemia, a rare but potentially life-threatening condition, such as:
+ Blue or gray discoloration of the lips, nails, or skin
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling tired or weak
+ Shortness of breath
Other severe side effects, including:
+ Abnormal heartbeat (fast, slow, or irregular)
+ Chest pain or pressure
+ Dizziness or fainting
+ Lightheadedness, sleepiness, confusion, or blurred vision
+ Balance problems
+ Restlessness
+ Anxiety
+ Speech changes
+ Shakiness
+ Twitching
+ Ringing in the ears
+ Breathing difficulties (trouble breathing, slow breathing, or shallow breathing)
+ Seizures
+ Numbness or tingling in the mouth
+ Metallic taste
+ Severe stomach upset or vomiting
+ Feeling hot or cold
+ Feeling nervous and excitable
+ Sneezing
+ Excessive sweating
Spinal-related side effects, including:
+ Urination problems
+ Loss of bladder or bowel control
+ Erectile dysfunction
+ Long-lasting burning, numbness, tingling, or paralysis in the lower half of the body
+ Back pain
+ Fever or chills
+ Stiff neck
+ Sensitivity to bright lights
Other Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor if you have any symptoms that bother you or persist. These may include:
Mild side effects, such as headache or fatigue
* Other side effects not listed above
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, this medication can cause severe and potentially life-threatening side effects. If you experience 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 acidosis (too much acid in the blood), such as:
+ Confusion
+ Fast breathing
+ Fast heartbeat
+ Abnormal heartbeat
+ Severe stomach pain, upset stomach, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling very tired or weak
Signs of methemoglobinemia, a rare but potentially life-threatening condition, such as:
+ Blue or gray discoloration of the lips, nails, or skin
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling tired or weak
+ Shortness of breath
Other severe side effects, including:
+ Abnormal heartbeat (fast, slow, or irregular)
+ Chest pain or pressure
+ Dizziness or fainting
+ Lightheadedness, sleepiness, confusion, or blurred vision
+ Balance problems
+ Restlessness
+ Anxiety
+ Speech changes
+ Shakiness
+ Twitching
+ Ringing in the ears
+ Breathing difficulties (trouble breathing, slow breathing, or shallow breathing)
+ Seizures
+ Numbness or tingling in the mouth
+ Metallic taste
+ Severe stomach upset or vomiting
+ Feeling hot or cold
+ Feeling nervous and excitable
+ Sneezing
+ Excessive sweating
Spinal-related side effects, including:
+ Urination problems
+ Loss of bladder or bowel control
+ Erectile dysfunction
+ Long-lasting burning, numbness, tingling, or paralysis in the lower half of the body
+ Back pain
+ Fever or chills
+ Stiff neck
+ Sensitivity to bright lights
Other Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor if you have any symptoms that bother you or persist. These may include:
Mild side effects, such as headache or fatigue
* Other side effects not listed above
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:
- Lightheadedness or dizziness
- Ringing in your ears (tinnitus)
- Numbness or tingling around your mouth
- Metallic taste in your mouth
- Blurred vision or double vision
- Tremors or muscle twitching
- Feeling anxious or restless
- Feeling unusually sleepy or drowsy
- Slow or irregular heartbeat
- Difficulty breathing
- Seizures
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. Be sure to describe the allergic reaction and its symptoms.
Certain health conditions, such as:
+ Bleeding disorders
+ Abnormal heart rhythms
+ Blood infections or infections at the site where the medication will be administered
+ Low blood pressure
* If you are using or plan to use another medication similar to this one. If you are unsure, consult your doctor or pharmacist.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your existing treatments and health conditions. 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. Be sure to describe the allergic reaction and its symptoms.
Certain health conditions, such as:
+ Bleeding disorders
+ Abnormal heart rhythms
+ Blood infections or infections at the site where the medication will be administered
+ Low blood pressure
* If you are using or plan to use another medication similar to this one. If you are unsure, consult your doctor or pharmacist.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your existing treatments and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
Important Warnings and Cautions
General Precautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Until the effects of this drug have worn off and you feel fully alert, avoid driving and other activities that require your full attention.
Risk of Methemoglobinemia
This medication can cause a severe blood disorder called methemoglobinemia. Your risk may be higher if you have glucose-6-phosphate dehydrogenase (G6PD) deficiency, heart problems, or lung problems. Additionally, the risk may increase when taking certain other medications or in infants under 6 months of age. If you have a history of methemoglobinemia, inform your doctor.
Special Considerations
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Not all formulations of this medication are suitable for children, so consult with your doctor before use. If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks with your doctor to ensure the best outcome for you and your baby.
Specific Administration-Related Warnings
Mouth: Do not eat until the numbness in your mouth has resolved, as you may accidentally bite your tongue.
Spinal Administration: This medication can cause temporary loss of sensation and motor function in the lower half of your body. Wait until these effects have worn off before attempting to get out of bed or perform other activities.
* Injection (Non-Spinal): This medication can cause temporary loss of sensation and motor function at the injection site. Be cautious and avoid activities that may put you at risk until the effects have resolved.
General Precautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Until the effects of this drug have worn off and you feel fully alert, avoid driving and other activities that require your full attention.
Risk of Methemoglobinemia
This medication can cause a severe blood disorder called methemoglobinemia. Your risk may be higher if you have glucose-6-phosphate dehydrogenase (G6PD) deficiency, heart problems, or lung problems. Additionally, the risk may increase when taking certain other medications or in infants under 6 months of age. If you have a history of methemoglobinemia, inform your doctor.
Special Considerations
If you are 65 or older, use this medication with caution, as you may be more susceptible to side effects. Not all formulations of this medication are suitable for children, so consult with your doctor before use. If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks with your doctor to ensure the best outcome for you and your baby.
Specific Administration-Related Warnings
Mouth: Do not eat until the numbness in your mouth has resolved, as you may accidentally bite your tongue.
Spinal Administration: This medication can cause temporary loss of sensation and motor function in the lower half of your body. Wait until these effects have worn off before attempting to get out of bed or perform other activities.
* Injection (Non-Spinal): This medication can cause temporary loss of sensation and motor function at the injection site. Be cautious and avoid activities that may put you at risk until the effects have resolved.
Overdose Information
Overdose Symptoms:
- Severe CNS depression (drowsiness, unconsciousness, respiratory arrest)
- Seizures
- Cardiovascular collapse (severe hypotension, bradycardia, arrhythmias, cardiac arrest)
What to Do:
Immediate medical attention is required. Call 911 or your local emergency number. Treatment involves managing airway, breathing, and circulation, controlling seizures, and administering lipid emulsion therapy (Intralipid) for severe systemic toxicity. Call 1-800-222-1222 (Poison Control) for advice.
Drug Interactions
Contraindicated Interactions
- Intravenous regional anesthesia (IVRA) due to risk of cardiac arrest (especially with 0.75% concentration, but generally avoided for all concentrations).
- Obstetric paracervical block in some cases due to fetal bradycardia.
Major Interactions
- Other local anesthetics (additive systemic toxicity).
- Antiarrhythmics (e.g., Class I antiarrhythmics like lidocaine, mexiletine, tocainide) - increased risk of cardiac depression and CNS toxicity.
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin) - may increase bupivacaine plasma levels and risk of toxicity.
- Vasoconstrictors (e.g., epinephrine) - while often co-administered to prolong duration, can increase systemic absorption if inadvertently injected intravascularly, leading to higher peak plasma levels and increased risk of toxicity.
Moderate Interactions
- Opioids (additive CNS depression, respiratory depression when used intrathecally/epidurally).
- Sedatives/Hypnotics (additive CNS depression).
- Neuromuscular blockers (may prolong or enhance block).
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Patient assessment (medical history, allergies, current medications)
Rationale: To identify contraindications, potential drug interactions, and risk factors for toxicity.
Timing: Prior to administration.
Vital signs (heart rate, blood pressure, respiratory rate)
Rationale: To establish baseline and detect early signs of systemic toxicity or adverse reactions.
Timing: Prior to administration.
Neurological status (alertness, orientation)
Rationale: To establish baseline for detecting CNS toxicity.
Timing: Prior to administration.
Routine Monitoring
Vital signs (heart rate, blood pressure, respiratory rate)
Frequency: Every 5-15 minutes during and immediately after administration, then as clinically indicated.
Target: Within patient's normal range; significant deviations warrant investigation.
Action Threshold: Bradycardia (<50 bpm), hypotension (SBP <90 mmHg or >20% drop from baseline), respiratory depression (RR <10 bpm).
Neurological status (level of consciousness, presence of perioral numbness, tinnitus, dizziness, muscle twitching)
Frequency: Continuously during and immediately after administration.
Target: Alert and oriented, absence of CNS symptoms.
Action Threshold: Any new or worsening CNS symptoms (e.g., agitation, confusion, seizures).
ECG monitoring (especially with large doses or high-risk patients)
Frequency: Continuous during and immediately after administration.
Target: Normal sinus rhythm, absence of arrhythmias.
Action Threshold: Arrhythmias (e.g., ventricular tachycardia, bradycardia, asystole), QRS widening.
Pain assessment
Frequency: As needed to assess efficacy.
Target: Achieve desired level of analgesia/anesthesia.
Action Threshold: Inadequate pain control may indicate need for re-dosing or alternative approach.
Symptom Monitoring
- Lightheadedness
- Dizziness
- Tinnitus
- Perioral numbness
- Metallic taste
- Blurred vision
- Tremors
- Muscle twitching
- Seizures
- Drowsiness
- Unconsciousness
- Respiratory depression
- Bradycardia
- Hypotension
- Cardiac arrest
Special Patient Groups
Pregnancy
Category C. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Bupivacaine crosses the placenta. Fetal bradycardia and other adverse effects have been reported, particularly with paracervical block.
Trimester-Specific Risks:
First Trimester:
Limited data, but generally avoided unless clearly needed.
Second Trimester:
Use with caution, monitor fetal heart rate.
Third Trimester:
Commonly used for labor and delivery (epidural), but 0.75% concentration is contraindicated for obstetrical epidural anesthesia due to risk of cardiac arrest. Monitor maternal and fetal vital signs closely.
Lactation
Bupivacaine is excreted into breast milk in small amounts. The amount ingested by the infant is generally considered to be low and unlikely to cause adverse effects. Use with caution, monitor infant for drowsiness or feeding difficulties.
Infant Risk:
Low risk (L3).
Pediatric Use
Children, especially infants and neonates, are more susceptible to systemic toxicity due to differences in pharmacokinetics (e.g., lower protein binding, immature hepatic metabolism). Dosing must be carefully calculated on a mg/kg basis, and the lowest effective dose should be used. Close monitoring for signs of toxicity is crucial.
Geriatric Use
Elderly patients may be more susceptible to systemic toxicity due due to decreased hepatic function, renal function, and reduced lean body mass. Consider lower doses and slower administration rates. Monitor vital signs and for signs of CNS or cardiovascular toxicity more closely.
Clinical Information
Clinical Pearls
- Always aspirate prior to injection to avoid inadvertent intravascular administration, which can lead to severe systemic toxicity.
- The addition of epinephrine prolongs the duration of action and reduces systemic absorption, but should be used with caution in areas with end-arterial supply (e.g., fingers, toes, penis, nose) due to risk of ischemia.
- Bupivacaine has a higher cardiotoxicity profile compared to other local anesthetics like lidocaine, especially the 0.75% concentration. Lipid emulsion therapy (Intralipid) is the antidote for severe bupivacaine-induced systemic toxicity.
- Onset and duration of action are dose and concentration dependent; higher concentrations (e.g., 0.5%, 0.75%) provide faster onset and denser block but carry higher risk of toxicity. 0.25% is often preferred for continuous infusions or where a less dense, longer-lasting block is desired.
- Monitor for signs of local anesthetic systemic toxicity (LAST) which can manifest as CNS symptoms (lightheadedness, tinnitus, seizures) or cardiovascular symptoms (bradycardia, hypotension, arrhythmias, cardiac arrest).
Alternative Therapies
- Lidocaine (shorter acting, less cardiotoxic)
- Ropivacaine (similar to bupivacaine but with lower cardiotoxicity profile)
- Levobupivacaine (S-enantiomer of bupivacaine, potentially less cardiotoxic)
- Mepivacaine
- Chloroprocaine (ester-type, very short acting)
- General anesthesia
- Opioid analgesics (for systemic pain relief)
- NSAIDs (for systemic pain relief)
Cost & Coverage
Average Cost:
Varies widely by supplier and volume (e.g., $5 - $50 per 10mL vial of 0.25%) per 10mL vial
Generic Available:
Yes
Insurance Coverage:
Generally covered by most insurance plans as it is a commonly used generic injectable medication, typically Tier 1 or 2.
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor for further guidance. 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 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 pour them down the drain. If you are unsure about the correct disposal method, consult your pharmacist for advice. Many communities have drug take-back programs, which your pharmacist can help you locate. Some medications may come with an additional patient information leaflet; check with your pharmacist to see if this applies to your prescription. 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 emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it occurred, as this will aid in providing appropriate treatment.