Marcaine 0.5% Mdv Inj, 50ml
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; Voltage-gated Sodium Channel Blocker
Pregnancy Category
Category C
FDA Approved
Sep 1972
DEA Schedule
Not Controlled
Overview
What is this medicine?
Bupivacaine is a medicine used to numb a specific part of your body. It works by temporarily blocking nerve signals in that area, so you won't feel pain during a medical procedure or surgery. It's often used for local injections, nerve blocks, or epidurals.
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 specific 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 specific needs.
Lifestyle & Tips
- Avoid eating or drinking until sensation returns to the treated area, especially if the mouth or throat is affected, to prevent choking.
- Avoid activities requiring fine motor skills or full sensation (e.g., driving, operating machinery) until the effects of the anesthetic have completely worn off.
- Protect the numb area from injury (e.g., burns, cuts) as you won't feel pain.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Highly variable based on procedure, site, and patient factors. For 0.5% solution, common doses range from 5 mL (25 mg) for minor infiltration to 30 mL (150 mg) for major nerve blocks or epidural anesthesia. Max single dose: 175 mg (35 mL of 0.5% solution). Max 24-hour dose: 400 mg.
Dose Range:
5 - 175 mg
Condition-Specific Dosing:
infiltration:
Up to 60 mL of 0.25% (150 mg) or 30 mL of 0.5% (150 mg)
peripheralNerveBlock:
5-30 mL of 0.25% or 0.5% (25-150 mg) depending on nerve size and location
epiduralAnesthesia:
10-20 mL of 0.25% or 0.5% (25-100 mg) for surgical anesthesia; 5-10 mL of 0.25% (12.5-25 mg) for labor analgesia
spinalAnesthesia:
Not typically used for spinal anesthesia in 0.5% concentration; hyperbaric 0.75% or 0.5% plain is used in smaller volumes (e.g., 1-4 mL)
Pediatric Dosing
Neonatal:
Not established for routine use; extreme caution and reduced doses if used. Max 1.5-2 mg/kg.
Infant:
Max 2 mg/kg (0.4 mL/kg of 0.5% solution) as a single dose. Careful titration and monitoring.
Child:
Max 2 mg/kg (0.4 mL/kg of 0.5% solution) as a single dose. Total dose not to exceed 2.5 mg/kg/24 hours. Careful titration and monitoring.
Adolescent:
Similar to adult dosing, but consider lower end of adult range and weight-based limits.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment required.
Moderate:
No specific dose adjustment required, but monitor for signs of toxicity.
Severe:
No specific dose adjustment required, but monitor for signs of toxicity due to potential accumulation of metabolites. Use with caution.
Dialysis:
Bupivacaine is not significantly removed by hemodialysis. No specific dose adjustment, but monitor for toxicity.
Hepatic Impairment:
Mild:
No specific dose adjustment required.
Moderate:
Use with caution; consider reduced doses and extended dosing intervals due to impaired metabolism.
Severe:
Use with extreme caution; significant dose reduction may be necessary due to impaired metabolism and increased risk 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 prevents the generation and propagation of action potentials, thereby producing local anesthesia.
Pharmacokinetics
Absorption:
Bioavailability:
Highly variable depending on the site of administration (e.g., intercostal block > epidural > brachial plexus > subcutaneous infiltration). Systemic absorption is rapid from highly vascularized areas.
Tmax:
Variable, typically 10-45 minutes after epidural administration; 30-60 minutes after peripheral nerve block.
FoodEffect:
Not applicable (parenteral administration).
Distribution:
Vd:
Approximately 0.7-2.7 L/kg (adults).
ProteinBinding:
Approximately 95% (primarily to alpha-1-acid glycoprotein).
CnssPenetration:
Limited at therapeutic doses, but can cross the blood-brain barrier and placenta, leading to CNS and fetal effects at higher concentrations.
Elimination:
HalfLife:
Approximately 1.5-5.5 hours (adults), longer in neonates and pregnant women.
Clearance:
Approximately 0.58 L/min (adults).
ExcretionRoute:
Primarily renal (approximately 5-10% as unchanged drug, remainder as metabolites).
Unchanged:
Approximately 5-10%
Pharmacodynamics
OnsetOfAction:
2-10 minutes (depending on concentration, dose, and site of injection).
PeakEffect:
30-45 minutes.
DurationOfAction:
2-8 hours (longer than lidocaine, depending on concentration, dose, and presence of epinephrine).
Confidence:
Medium
Safety & Warnings
BLACK BOX WARNING
There have been reports of cardiac arrest and death during the use of bupivacaine for epidural anesthesia in obstetrical patients. In most cases, this has followed the inadvertent intravascular injection of bupivacaine. Therefore, bupivacaine 0.75% is contraindicated for obstetrical paracervical block anesthesia. Bupivacaine 0.75% is also contraindicated for intravenous regional anesthesia (Bier's block) because of the high risk of systemic toxicity.
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:
+ 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 too much acid in the blood (acidosis):
+ Confusion
+ Fast breathing
+ Fast heartbeat
+ Abnormal heartbeat
+ Severe stomach pain, upset stomach, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling extremely tired or weak
Signs of methemoglobinemia (a rare but potentially life-threatening condition):
+ Blue or gray discoloration of the lips, nails, or skin
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling extremely tired or weak
+ Shortness of breath
Other severe side effects:
+ 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 extremely hot or cold
+ Nervousness and excitability
+ Sneezing
+ Excessive sweating
Spinal-related side effects:
+ Urination difficulties
+ 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 concerns. If you experience any side effects that bother you or persist, seek medical attention.
Reporting Side Effects
If you have questions about side effects or want to report any, you can:
Contact your doctor for medical advice
Call the FDA at 1-800-332-1088
Visit the FDA's MedWatch website at https://www.fda.gov/medwatch to report side effects.
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:
+ 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 too much acid in the blood (acidosis):
+ Confusion
+ Fast breathing
+ Fast heartbeat
+ Abnormal heartbeat
+ Severe stomach pain, upset stomach, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling extremely tired or weak
Signs of methemoglobinemia (a rare but potentially life-threatening condition):
+ Blue or gray discoloration of the lips, nails, or skin
+ Abnormal heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling extremely tired or weak
+ Shortness of breath
Other severe side effects:
+ 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 extremely hot or cold
+ Nervousness and excitability
+ Sneezing
+ Excessive sweating
Spinal-related side effects:
+ Urination difficulties
+ 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 concerns. If you experience any side effects that bother you or persist, seek medical attention.
Reporting Side Effects
If you have questions about side effects or want to report any, you can:
Contact your doctor for medical advice
Call the FDA at 1-800-332-1088
Visit the FDA's MedWatch website at https://www.fda.gov/medwatch to report side effects.
Seek Immediate Medical Attention If You Experience:
- Dizziness, lightheadedness, or feeling faint
- Ringing in the ears (tinnitus)
- Numbness or tingling around the mouth (circumoral numbness)
- Unusual taste in the mouth (metallic taste)
- Restlessness, anxiety, or confusion
- Tremors or muscle twitching
- Seizures
- Slow or irregular heartbeat
- Difficulty breathing
- Excessive drowsiness or loss of consciousness
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
When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are using this drug.
To ensure your safety, avoid driving and engaging in activities that require alertness until the effects of this medication have worn off and you feel fully awake.
There is a risk of developing a severe blood disorder called methemoglobinemia associated with this type of medication. This risk may be increased in individuals with certain conditions, such as glucose-6-phosphate dehydrogenase (G6PD) deficiency, heart problems, or lung problems. Additionally, the risk may be higher when taking certain other medications or in infants under 6 months of age. If you have a history of methemoglobinemia, inform your doctor.
If you are 65 years 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 it is crucial to consult with your doctor before administering it to a child.
If you are pregnant, planning to become pregnant, or breastfeeding, discuss the potential benefits and risks of this medication with your doctor to make an informed decision.
Specific Warnings
Mouth: Do not eat or drink while your mouth is numb, as you may accidentally bite your tongue.
Spinal: This medication may cause temporary loss of sensation and motor function in the lower half of your body. Do not attempt to get out of bed or perform any activities until normal sensation and movement have returned.
* Injection (non-spinal): This medication may cause temporary loss of sensation and motor function at the injection site.
When taking this medication, it is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are using this drug.
To ensure your safety, avoid driving and engaging in activities that require alertness until the effects of this medication have worn off and you feel fully awake.
There is a risk of developing a severe blood disorder called methemoglobinemia associated with this type of medication. This risk may be increased in individuals with certain conditions, such as glucose-6-phosphate dehydrogenase (G6PD) deficiency, heart problems, or lung problems. Additionally, the risk may be higher when taking certain other medications or in infants under 6 months of age. If you have a history of methemoglobinemia, inform your doctor.
If you are 65 years 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 it is crucial to consult with your doctor before administering it to a child.
If you are pregnant, planning to become pregnant, or breastfeeding, discuss the potential benefits and risks of this medication with your doctor to make an informed decision.
Specific Warnings
Mouth: Do not eat or drink while your mouth is numb, as you may accidentally bite your tongue.
Spinal: This medication may cause temporary loss of sensation and motor function in the lower half of your body. Do not attempt to get out of bed or perform any activities until normal sensation and movement have returned.
* Injection (non-spinal): This medication may cause temporary loss of sensation and motor function at the injection site.
Overdose Information
Overdose Symptoms:
- Severe CNS toxicity (seizures, coma, respiratory arrest)
- Severe cardiovascular toxicity (bradycardia, hypotension, arrhythmias, cardiac arrest)
What to Do:
Immediate medical attention is required. Call 911 or your local emergency number. Management includes maintaining airway, breathing, and circulation, administering oxygen, managing seizures (e.g., with benzodiazepines), and treating cardiovascular collapse (e.g., with vasopressors, atropine, and lipid emulsion therapy for severe cardiotoxicity). Call 1-800-222-1222 for Poison Control.
Drug Interactions
Contraindicated Interactions
- Obstetric paracervical block (due to fetal bradycardia/death risk)
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, clarithromycin, ritonavir - may increase bupivacaine plasma levels and toxicity)
- CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin - may decrease bupivacaine plasma levels and efficacy)
Moderate Interactions
- Beta-blockers (may reduce hepatic blood flow, potentially increasing bupivacaine levels; also additive bradycardia)
- Calcium channel blockers (additive cardiac depression)
- Neuromuscular blockers (may prolong or enhance block, though not a direct interaction, consider effects on respiratory function if high block)
- Sedatives/Hypnotics (additive CNS depression)
Minor Interactions
- Not typically categorized as minor for bupivacaine due to its narrow therapeutic index and potential for severe toxicity.
Monitoring
Baseline Monitoring
Allergy history
Rationale: To identify hypersensitivity reactions to amide-type local anesthetics.
Timing: Prior to administration.
Vital signs (HR, BP, RR, SpO2)
Rationale: To establish baseline cardiovascular and respiratory status.
Timing: Prior to administration.
Neurological status
Rationale: To assess baseline mental status and identify pre-existing neurological deficits.
Timing: Prior to administration.
Coagulation status (if applicable for regional blocks)
Rationale: To assess bleeding risk for neuraxial or deep nerve blocks.
Timing: Prior to administration.
Routine Monitoring
Vital signs (HR, BP, RR, SpO2)
Frequency: Every 5-15 minutes during and immediately after administration, then as clinically indicated.
Target: Within patient's normal physiological range.
Action Threshold: Significant deviations (e.g., hypotension, bradycardia, respiratory depression) require immediate intervention.
Neurological status (e.g., level of consciousness, signs of CNS toxicity)
Frequency: Continuously during and immediately after administration, then periodically.
Target: Alert and oriented, no signs of CNS excitation or depression.
Action Threshold: Dizziness, tinnitus, circumoral numbness, metallic taste, restlessness, tremors, seizures, somnolence.
ECG monitoring
Frequency: Continuous during and immediately after administration, especially with higher doses or in patients with cardiac disease.
Target: Normal sinus rhythm, no signs of conduction abnormalities or arrhythmias.
Action Threshold: Bradycardia, QRS widening, PR prolongation, ventricular arrhythmias (e.g., VT, VF).
Symptom Monitoring
- Lightheadedness
- Dizziness
- Tinnitus
- Metallic taste
- Circumoral numbness
- Restlessness
- Anxiety
- Tremors
- Muscle twitching
- Seizures
- Drowsiness
- Unconsciousness
- Respiratory depression/arrest
- 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 essential. Risk of teratogenicity is low.
Second Trimester:
Can be used for regional anesthesia if clinically indicated, with careful monitoring.
Third Trimester:
Commonly used for labor and delivery (epidural, spinal). However, paracervical block is contraindicated due to high risk of fetal bradycardia and death. Monitor for maternal hypotension and fetal distress.
Lactation
L3 (Moderate risk). Bupivacaine is excreted into breast milk in small amounts. The relative infant dose is low, and adverse effects in breastfed infants are unlikely at typical maternal doses. However, caution is advised, especially with repeated or high doses.
Infant Risk:
Low risk of adverse effects, but monitor for drowsiness or feeding difficulties in the infant.
Pediatric Use
Use with extreme caution. Children, especially infants and neonates, are more susceptible to systemic toxicity due to immature hepatic metabolism and higher relative doses. Dosing must be carefully calculated on a mg/kg basis, and the lowest effective concentration and volume should be used. Close monitoring for signs of toxicity is essential.
Geriatric Use
Elderly patients may be more susceptible to systemic toxicity due to decreased hepatic function, reduced renal clearance of metabolites, and decreased protein binding. Consider reduced doses and slower administration rates. Monitor closely for CNS and cardiovascular effects.
Clinical Information
Clinical Pearls
- Bupivacaine has a higher potential for cardiotoxicity compared to other local anesthetics like lidocaine, especially with inadvertent intravascular injection. Always aspirate before injection to avoid intravascular administration.
- The 0.75% concentration is contraindicated for obstetric epidural anesthesia and intravenous regional anesthesia (Bier's block) due to severe cardiotoxicity risk.
- Lipid emulsion therapy (Intralipid) is the antidote for severe local anesthetic systemic toxicity (LAST) and should be readily available when administering bupivacaine.
- Onset of action is slower but duration of action is significantly longer than lidocaine.
- Adding epinephrine (if available in the formulation) can prolong the duration of action and reduce systemic absorption, but it is not present in the specified 'plain' Marcaine 0.5% Mdv Inj.
- Careful patient selection and dose titration are crucial, especially in patients with pre-existing cardiac or hepatic conditions.
Alternative Therapies
- Lidocaine (shorter acting, less cardiotoxic)
- Ropivacaine (similar to bupivacaine but with a better safety profile regarding cardiotoxicity)
- Levobupivacaine (S-enantiomer of bupivacaine, potentially less cardiotoxic)
- Mepivacaine (intermediate acting)
- Chloroprocaine (ester-type, very short acting)
Cost & Coverage
Average Cost:
Varies widely by supplier and contract, typically $10-$50 per 50 mL vial of 0.5%
Generic Available:
Yes
Insurance Coverage:
Generally covered by most medical insurance plans as it is an injectable medication administered in a clinical setting.
General Drug Facts
If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance.
To ensure safe use, do not share your medication with others, and never take someone else's medication. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion.
Proper disposal of unused or expired medications is crucial. Do not flush medications down the toilet or pour them down the drain unless specifically instructed to do so by your pharmacist or healthcare provider. If you are unsure about the best method for disposing of medications, consult your pharmacist, who can provide guidance on safe disposal practices and inform you about potential drug take-back programs in your area.
Some medications may have additional patient information leaflets available. Your pharmacist can provide more information on this. If you have any questions or concerns about your medication, it is best to 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 detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred, to ensure prompt and effective treatment.
To ensure safe use, do not share your medication with others, and never take someone else's medication. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion.
Proper disposal of unused or expired medications is crucial. Do not flush medications down the toilet or pour them down the drain unless specifically instructed to do so by your pharmacist or healthcare provider. If you are unsure about the best method for disposing of medications, consult your pharmacist, who can provide guidance on safe disposal practices and inform you about potential drug take-back programs in your area.
Some medications may have additional patient information leaflets available. Your pharmacist can provide more information on this. If you have any questions or concerns about your medication, it is best to 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 detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred, to ensure prompt and effective treatment.