Nesacaine Mpf 2% Inj, 20ml
It is used to numb an area before a procedure.
Drug Class
Local Anesthetic
Pharmacologic Class
Ester-type Local Anesthetic; Voltage-gated Sodium Channel Blocker
Pregnancy Category
C
FDA Approved
Jun 1952
DEA Schedule
Not Controlled
Overview
What is this medicine?
Chloroprocaine is a medicine used to numb a specific part of your body to prevent pain during a medical procedure, such as surgery or childbirth. It works by temporarily blocking nerve signals in the area where it's injected.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Your doctor will administer this medication as an injection.
Storage and Disposal
This medication will be administered in a hospital or doctor's office, so you will not need to store it at home.
Missed 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. Your doctor will administer this medication as an injection.
Storage and Disposal
This medication will be administered in a hospital or doctor's office, so you will not need to store it at home.
Missed 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 given by your healthcare provider.
- Avoid activities that require full sensation or motor control in the numbed area until the effect wears off completely.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Varies by procedure and concentration. For 2% solution: Epidural: 10-20 mL (200-400 mg); Infiltration: Variable volume (e.g., 1-10 mL); Peripheral Nerve Block: Variable volume (e.g., 5-20 mL).
Condition-Specific Dosing:
epidural:
2% solution, 10-20 mL (200-400 mg); Max single dose: 11 mg/kg (not to exceed 800 mg)
caudal:
1.5% solution, 15-20 mL (225-300 mg)
infiltration:
1% or 2% solution, variable volume depending on area and desired effect
peripheral_nerve_block:
1% or 2% solution, variable volume depending on nerve and desired block
Pediatric Dosing
Neonatal:
Not established (use with extreme caution, highly individualized)
Infant:
Not established (use with extreme caution, highly individualized)
Child:
Dosing is highly individualized and weight-based (e.g., 0.5-1.5 mg/kg for specific blocks); consult pediatric anesthesia guidelines.
Adolescent:
Dosing is highly individualized and weight-based; consult pediatric anesthesia guidelines.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment typically required.
Moderate:
No specific dose adjustment typically required.
Severe:
No specific dose adjustment typically required, as metabolism is primarily by plasma pseudocholinesterase. However, monitor for signs of toxicity.
Dialysis:
Not significantly removed by dialysis. No specific dose adjustment, but monitor for signs of toxicity.
Hepatic Impairment:
Mild:
No specific dose adjustment typically required.
Moderate:
No specific dose adjustment typically required, as metabolism is primarily by plasma pseudocholinesterase. However, severe hepatic dysfunction may rarely affect pseudocholinesterase activity; monitor for signs of toxicity.
Severe:
No specific dose adjustment typically required, but monitor closely for signs of toxicity due to potential for reduced pseudocholinesterase activity in very severe cases.
Pharmacology
Mechanism of Action
Chloroprocaine is an ester-type local anesthetic that reversibly blocks the initiation and conduction of nerve impulses. It stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses, specifically by decreasing the permeability of the nerve cell membrane to sodium ions.
Pharmacokinetics
Absorption:
Bioavailability:
Not applicable (local administration)
Tmax:
Varies by site of injection; e.g., epidural: 5-10 minutes; infiltration: almost immediate.
FoodEffect:
Not applicable
Distribution:
Vd:
Not typically reported for local anesthetics in this context; rapidly distributed.
ProteinBinding:
Approximately 10-20%
CnssPenetration:
Limited (due to rapid hydrolysis in plasma)
Elimination:
HalfLife:
Approximately 0.6-1.5 minutes (in adults)
Clearance:
Very rapid due to plasma hydrolysis.
ExcretionRoute:
Renal (metabolites)
Unchanged:
< 2% (negligible)
Pharmacodynamics
OnsetOfAction:
Very rapid (e.g., 6-12 minutes for epidural, almost immediate for infiltration)
PeakEffect:
10-20 minutes
DurationOfAction:
Short (30-60 minutes)
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 immediate medical attention:
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 too much acid in the blood (acidosis), including:
+ 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, including:
+ 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, including:
+ Feeling lightheaded, sleepy, confused, or experiencing blurred vision
+ Sneezing
+ Excessive sweating
+ Fever
+ Severe stomach upset or vomiting
+ Feeling nervous and excitable
+ Restlessness
+ Headache
+ Anxiety
+ Changes in speech
+ Numbness or tingling in the mouth
+ Shakiness
+ Dizziness or fainting
+ Ringing in the ears
+ Low mood (depression)
+ Changes in balance
+ Seizures
+ Abnormal heartbeat
+ Chest pain or pressure
Spinal-related side effects, including:
+ Difficulty urinating
+ Loss of bladder or bowel control
+ Erectile dysfunction
+ Back pain
+ Long-lasting burning, numbness, tingling, or paralysis in the lower half of the body
Other Possible Side Effects
As with any medication, you may experience side effects. While many people have no side effects or only mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Irritation at the injection site
Reporting 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 immediate medical attention:
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 too much acid in the blood (acidosis), including:
+ 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, including:
+ 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, including:
+ Feeling lightheaded, sleepy, confused, or experiencing blurred vision
+ Sneezing
+ Excessive sweating
+ Fever
+ Severe stomach upset or vomiting
+ Feeling nervous and excitable
+ Restlessness
+ Headache
+ Anxiety
+ Changes in speech
+ Numbness or tingling in the mouth
+ Shakiness
+ Dizziness or fainting
+ Ringing in the ears
+ Low mood (depression)
+ Changes in balance
+ Seizures
+ Abnormal heartbeat
+ Chest pain or pressure
Spinal-related side effects, including:
+ Difficulty urinating
+ Loss of bladder or bowel control
+ Erectile dysfunction
+ Back pain
+ Long-lasting burning, numbness, tingling, or paralysis in the lower half of the body
Other Possible Side Effects
As with any medication, you may experience side effects. While many people have no side effects or only mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Irritation at the injection site
Reporting 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:
- Feeling dizzy or lightheaded
- Ringing in your ears (tinnitus)
- Numbness or tingling around your mouth
- A metallic taste in your mouth
- Muscle twitching or tremors
- Feeling confused or drowsy
- Blurred vision or other changes in eyesight
- Difficulty breathing
- Slow or irregular heartbeat
- Feeling unusually anxious or restless
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 are currently taking a sulfa (sulfonamide) drug. If you are unsure whether any of your medications contain sulfa, consult your doctor for clarification.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor. Provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your health problems, including any pre-existing conditions
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to ensure your safety. Verify that it is safe to take this medication in combination with all your other medications and health conditions.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
If you are currently taking a sulfa (sulfonamide) drug. If you are unsure whether any of your medications contain sulfa, consult your doctor for clarification.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor. Provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your health problems, including any pre-existing conditions
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to ensure your safety. Verify that it is safe to take this medication in combination with all your other medications and health conditions.
Precautions & Cautions
Important Warnings and Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Risk of Methemoglobinemia
A severe blood disorder called methemoglobinemia has been associated with drugs like this one. Your risk may be increased if you have:
- Glucose-6-phosphate dehydrogenase (G6PD) deficiency
- Heart problems
- Lung problems
- Are taking certain other medications
- Are an infant under 6 months of age
If you have a history of methemoglobinemia, notify your doctor.
Special Considerations
- Older Adults (65 and older): Use this medication with caution, as you may be more susceptible to side effects.
- Children: Use this medication with caution, as the risk of certain side effects may be higher in pediatric patients.
- Pregnancy and Breastfeeding: If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks of this medication with your doctor to make an informed decision.
Spinal Administration
After receiving this medication via spinal administration, you may experience temporary loss of sensation and motor function in the lower half of your body. To ensure your safety, do not attempt to get out of bed or perform any activities until your feeling and motor function have returned to normal.
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Risk of Methemoglobinemia
A severe blood disorder called methemoglobinemia has been associated with drugs like this one. Your risk may be increased if you have:
- Glucose-6-phosphate dehydrogenase (G6PD) deficiency
- Heart problems
- Lung problems
- Are taking certain other medications
- Are an infant under 6 months of age
If you have a history of methemoglobinemia, notify your doctor.
Special Considerations
- Older Adults (65 and older): Use this medication with caution, as you may be more susceptible to side effects.
- Children: Use this medication with caution, as the risk of certain side effects may be higher in pediatric patients.
- Pregnancy and Breastfeeding: If you are pregnant, plan to become pregnant, or are breastfeeding, discuss the benefits and risks of this medication with your doctor to make an informed decision.
Spinal Administration
After receiving this medication via spinal administration, you may experience temporary loss of sensation and motor function in the lower half of your body. To ensure your safety, do not attempt to get out of bed or perform any activities until your feeling and motor function have returned to normal.
Overdose Information
Overdose Symptoms:
- Severe dizziness or lightheadedness
- Seizures
- Unconsciousness
- Severe low blood pressure (hypotension)
- Very slow heart rate (bradycardia)
- Irregular heart rhythms (arrhythmias)
- Cardiac arrest
- Respiratory arrest
What to Do:
Overdose is a medical emergency. Immediate medical attention is required. Management includes maintaining airway and ventilation, administering oxygen, treating seizures (e.g., with benzodiazepines), managing hypotension (e.g., with vasopressors), and treating arrhythmias. Intravenous lipid emulsion therapy may be considered for severe systemic toxicity. Call 911 or your local emergency number immediately.
Drug Interactions
Contraindicated Interactions
- Hypersensitivity to chloroprocaine, ester-type local anesthetics, or para-aminobenzoic acid (PABA).
Major Interactions
- Cholinesterase inhibitors (e.g., neostigmine, pyridostigmine, donepezil, rivastigmine, galantamine): May inhibit the metabolism of chloroprocaine, leading to prolonged effects and increased risk of systemic toxicity.
- Other local anesthetics: Additive systemic toxicity if administered concurrently or sequentially in high doses.
Moderate Interactions
- Succinylcholine: Chloroprocaine may prolong the neuromuscular blockade of succinylcholine due to competition for plasma pseudocholinesterase.
- Sulfonamides: Para-aminobenzoic acid (PABA), a metabolite of chloroprocaine, can antagonize the antibacterial action of sulfonamides.
Monitoring
Baseline Monitoring
Allergy history
Rationale: To identify hypersensitivity to ester-type local anesthetics or PABA.
Timing: Prior to administration
Vital signs (BP, HR, RR)
Rationale: To establish baseline and detect early signs of systemic toxicity.
Timing: Prior to administration
Neurological status
Rationale: To establish baseline and detect early signs of CNS toxicity.
Timing: Prior to administration
Routine Monitoring
Vital signs (BP, HR, RR)
Frequency: Every 5-15 minutes during and immediately after administration, then as clinically indicated.
Target: Within patient's normal range or acceptable limits for procedure.
Action Threshold: Significant deviations (e.g., hypotension, bradycardia, tachycardia, respiratory depression) warrant immediate intervention.
Level of consciousness/CNS symptoms
Frequency: Continuously during and immediately after administration.
Target: Alert and oriented, no signs of CNS excitation or depression.
Action Threshold: Dizziness, lightheadedness, tinnitus, perioral numbness, metallic taste, muscle twitching, tremors, seizures, or somnolence require immediate assessment and intervention.
Cardiac rhythm
Frequency: Continuous ECG monitoring during and immediately after administration for high-risk procedures or large doses.
Target: Normal sinus rhythm.
Action Threshold: Arrhythmias (e.g., bradycardia, ventricular arrhythmias) require immediate intervention.
Symptom Monitoring
- Dizziness
- Lightheadedness
- Tinnitus (ringing in ears)
- Perioral numbness (numbness around the mouth)
- Metallic taste
- Muscle twitching
- Tremors
- Seizures
- Blurred vision or other visual disturbances
- Slurred speech
- Confusion
- Drowsiness or somnolence
- Bradycardia (slow heart rate)
- Hypotension (low blood pressure)
- Arrhythmias
- Respiratory depression or apnea
Special Patient Groups
Pregnancy
Chloroprocaine is classified as Pregnancy Category C. It is commonly used in obstetrics for epidural anesthesia during labor and delivery. Its rapid metabolism by plasma pseudocholinesterase limits fetal exposure, making it a relatively safe option when indicated.
Trimester-Specific Risks:
First Trimester:
Limited data, but rapid metabolism suggests low risk. Use only if clearly needed.
Second Trimester:
Considered relatively safe due to rapid metabolism and limited systemic exposure.
Third Trimester:
Commonly used for epidural anesthesia during labor and delivery. Rapid metabolism minimizes transfer to the fetus and reduces risk of fetal toxicity.
Lactation
Chloroprocaine is considered to have a low risk (L2) during lactation. Due to its very rapid metabolism in plasma, systemic exposure to the mother and transfer into breast milk are minimal. It is unlikely to cause adverse effects in a breastfed infant.
Infant Risk:
Low risk
Pediatric Use
Use with caution. Dosing must be carefully calculated based on the child's weight and the specific procedure to avoid systemic toxicity. Children, especially infants and neonates, may have lower levels of plasma pseudocholinesterase, potentially leading to slightly prolonged half-life and increased risk of toxicity, though this is generally less pronounced than with amide-type local anesthetics.
Geriatric Use
Use with caution. While metabolism is primarily by plasma pseudocholinesterase, which may be slightly reduced in some elderly patients, significant dose adjustments are usually not required. Monitor closely for signs of systemic toxicity, as elderly patients may be more sensitive to CNS and cardiovascular effects.
Clinical Information
Clinical Pearls
- Chloroprocaine is an ester-type local anesthetic, distinguished by its very rapid onset and short duration of action.
- Its rapid hydrolysis by plasma pseudocholinesterase results in a very short half-life and a lower risk of systemic toxicity compared to amide-type local anesthetics.
- The primary metabolite, para-aminobenzoic acid (PABA), can cause allergic reactions in individuals sensitive to ester-type local anesthetics or sulfonamides.
- Often chosen for procedures requiring quick onset and short duration, or as a test dose for epidural placement due to its rapid metabolism and distinct toxicity profile.
- Nesacaine-MPF is a multi-dose vial formulation, meaning it contains preservatives (e.g., methylparaben) and is not for intrathecal (spinal) use. Only preservative-free formulations are suitable for spinal anesthesia.
Alternative Therapies
- Lidocaine (amide-type local anesthetic, moderate onset/duration)
- Bupivacaine (amide-type local anesthetic, slow onset/long duration)
- Ropivacaine (amide-type local anesthetic, slow onset/long duration, less cardiotoxic than bupivacaine)
- Mepivacaine (amide-type local anesthetic, moderate onset/duration)
Cost & Coverage
Average Cost:
Varies widely per 20mL vial
Generic Available:
Yes
Insurance Coverage:
Generally covered by medical insurance for in-office or hospital procedures.
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 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 correct disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, 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 emergency medical attention. Be prepared to provide information about the medication taken, the amount, and the time it occurred.