Nesacaine 1% Inj, 30ml
It is used to numb an area before a procedure.
Drug Class
Local Anesthetic
Pharmacologic Class
Ester-type Local Anesthetic
Pregnancy Category
Category C
FDA Approved
Jun 1952
DEA Schedule
Not Controlled
Overview
What is this medicine?
Chloroprocaine is a medication used to numb a specific area of your body before a medical procedure or surgery. It works by temporarily blocking nerve signals in that area, so you won't feel pain. It starts working very quickly and its effects wear off relatively fast.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided to you. It is essential to follow the instructions carefully. This medication is administered via 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 specific needs.
To use this medication correctly, follow your doctor's instructions and read all the information provided to you. It is essential to follow the instructions carefully. This medication is administered via 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 specific needs.
Lifestyle & Tips
- Avoid eating or drinking until the numbness completely wears off if the injection affects areas involved in swallowing.
- Avoid activities that require fine motor skills or full sensation until the anesthetic effect has worn off, especially if the injection was in an extremity.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Varies by procedure and concentration. For Nesacaine 1% (Chloroprocaine HCl 10 mg/mL): Infiltration and Nerve Block. Max single dose without epinephrine: 600 mg (60 mL of 1%). Max single dose with epinephrine: 800 mg (80 mL of 1%).
Condition-Specific Dosing:
infiltration:
Up to 60 mL of 1% solution (600 mg) without epinephrine; up to 80 mL of 1% solution (800 mg) with epinephrine.
peripheralNerveBlock:
Up to 60 mL of 1% solution (600 mg) without epinephrine; up to 80 mL of 1% solution (800 mg) with epinephrine.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Dosing should be calculated on a mg/kg basis, generally not exceeding 11 mg/kg (1.1 mL/kg of 1% solution) for single injection. Lower concentrations and total doses are typically used.
Adolescent:
Similar to adult dosing, but caution advised, especially in younger adolescents.
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment needed due to rapid plasma metabolism.
Moderate:
No specific adjustment needed due to rapid plasma metabolism.
Severe:
No specific adjustment needed due to rapid plasma metabolism.
Dialysis:
Not significantly affected by dialysis due to rapid metabolism.
Hepatic Impairment:
Mild:
No specific adjustment needed due to primary metabolism by plasma pseudocholinesterase.
Moderate:
No specific adjustment needed due to primary metabolism by plasma pseudocholinesterase.
Severe:
No specific adjustment needed due to primary metabolism by plasma pseudocholinesterase.
Pharmacology
Mechanism of Action
Chloroprocaine, an ester-type local anesthetic, stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of nerve impulses. This action is primarily achieved by blocking voltage-gated sodium channels, thereby preventing the propagation of action potentials along nerve fibers.
Pharmacokinetics
Absorption:
Bioavailability:
High, but systemic absorption rate depends on the site of injection, vascularity of the tissue, and presence of vasoconstrictors (e.g., epinephrine).
Tmax:
Rapid, typically within minutes of injection.
FoodEffect:
Not applicable (parenteral administration).
Distribution:
Vd:
Not well-defined, but rapidly distributed to highly perfused tissues.
ProteinBinding:
Low (approximately 10-20%)
CnssPenetration:
Limited, but can cross the blood-brain barrier if systemic levels are high enough to cause toxicity.
Elimination:
HalfLife:
Very short; approximately 20-50 seconds in adults, slightly longer in neonates due to lower pseudocholinesterase activity.
Clearance:
Very rapid due to enzymatic hydrolysis.
ExcretionRoute:
Metabolites (PABA and diethylaminoethanol) are primarily excreted by the kidneys.
Unchanged:
< 2% (due to rapid metabolism)
Pharmacodynamics
OnsetOfAction:
Very rapid; 6-12 minutes for infiltration, 3-9 minutes for nerve block.
PeakEffect:
Within minutes of onset.
DurationOfAction:
Short; 30-60 minutes (without epinephrine), 60-90 minutes (with epinephrine).
Confidence:
Medium
Safety & Warnings
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
+ Irregular heartbeat
+ Severe stomach pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling extremely 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
+ Irregular heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling extremely tired or weak
+ Shortness of breath
Other severe side effects, such as:
+ Feeling lightheaded, sleepy, confused, or having blurred vision
+ Sneezing
+ Excessive sweating
+ Fever
+ Severe nausea or vomiting
+ Feeling nervous or agitated
+ Restlessness
+ Headache
+ Anxiety
+ Changes in speech
+ Numbness or tingling in the mouth
+ Shakiness
+ Dizziness or fainting
+ Ringing in the ears
+ Depression
+ Changes in balance
+ Seizures
+ Abnormal heartbeat
+ Chest pain or pressure
Spinal-related side effects, such as:
+ 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
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're bothered by any of the following:
Irritation at the injection site
If you have questions or concerns about side effects, don't hesitate to reach out to 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
+ Irregular heartbeat
+ Severe stomach pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling extremely 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
+ Irregular heartbeat
+ Seizures
+ Severe dizziness or fainting
+ Severe headache
+ Excessive sleepiness
+ Feeling extremely tired or weak
+ Shortness of breath
Other severe side effects, such as:
+ Feeling lightheaded, sleepy, confused, or having blurred vision
+ Sneezing
+ Excessive sweating
+ Fever
+ Severe nausea or vomiting
+ Feeling nervous or agitated
+ Restlessness
+ Headache
+ Anxiety
+ Changes in speech
+ Numbness or tingling in the mouth
+ Shakiness
+ Dizziness or fainting
+ Ringing in the ears
+ Depression
+ Changes in balance
+ Seizures
+ Abnormal heartbeat
+ Chest pain or pressure
Spinal-related side effects, such as:
+ 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
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're bothered by any of the following:
Irritation at the injection site
If you have questions or concerns about side effects, don't hesitate to reach out to 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:
- Dizziness or lightheadedness
- Ringing in the ears (tinnitus)
- Numbness or tingling around the mouth
- Blurred vision or double vision
- Muscle twitching or tremors
- Feeling unusually sleepy or confused
- Difficulty breathing
- Slow or irregular heartbeat
- Feeling faint or dizzy when standing up
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 are currently taking a sulfa (sulfonamide) drug. If you are unsure whether any of your medications contain sulfa, consult your doctor.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor. Provide a comprehensive list of your:
Prescription medications
Over-the-counter (OTC) medications
Natural products
Vitamins
Your doctor and pharmacist need this information to ensure safe use of this medication. Do not initiate, discontinue, or modify the dosage of any medication without first consulting your doctor to confirm it is safe to do so.
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 are currently taking a sulfa (sulfonamide) drug. If you are unsure whether any of your medications contain sulfa, consult your doctor.
This list is not exhaustive, and it is crucial to discuss all your medications and health conditions with your doctor. Provide a comprehensive list of your:
Prescription medications
Over-the-counter (OTC) medications
Natural products
Vitamins
Your doctor and pharmacist need this information to ensure safe use of this medication. Do not initiate, discontinue, or modify the dosage of any medication without first consulting your doctor to confirm it is safe to do so.
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.
Risk of Methemoglobinemia
A severe blood disorder called methemoglobinemia has been associated with medications 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 younger than 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: This medication should be used with caution in children, as they may have a higher risk of experiencing certain side effects.
- Pregnancy and Breastfeeding: If you are pregnant, plan to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.
Spinal Administration
After receiving this medication via spinal administration, you may experience temporary loss of feeling 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.
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.
Risk of Methemoglobinemia
A severe blood disorder called methemoglobinemia has been associated with medications 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 younger than 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: This medication should be used with caution in children, as they may have a higher risk of experiencing certain side effects.
- Pregnancy and Breastfeeding: If you are pregnant, plan to become pregnant, or are breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.
Spinal Administration
After receiving this medication via spinal administration, you may experience temporary loss of feeling 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 (convulsions)
- Unconsciousness
- Respiratory arrest (stopping breathing)
- Severe low blood pressure
- Slow heart rate (bradycardia)
- Cardiac arrest
What to Do:
If you experience any severe symptoms after receiving this medication, seek immediate medical attention. In case of suspected overdose, call emergency services (e.g., 911 in the US) or Poison Control (1-800-222-1222) immediately. Management involves supportive care, maintaining airway, breathing, and circulation, and treating seizures or arrhythmias.
Drug Interactions
Major Interactions
- Cholinesterase inhibitors (e.g., neostigmine, pyridostigmine, donepezil): May inhibit the metabolism of chloroprocaine, leading to prolonged effects and increased risk of systemic toxicity.
- Sulfonamides: The metabolite PABA can antagonize the antibacterial action of sulfonamides.
Monitoring
Baseline Monitoring
Allergy history
Rationale: To identify prior hypersensitivity reactions, especially to ester-type local anesthetics or PABA.
Timing: Prior to administration
Vital signs (heart rate, blood pressure, respiratory rate)
Rationale: To establish baseline and identify pre-existing cardiovascular or respiratory compromise.
Timing: Prior to administration
Routine Monitoring
Vital signs (heart rate, blood pressure, respiratory rate)
Frequency: During and immediately after administration, then as clinically indicated.
Target: Within patient's normal limits.
Action Threshold: Significant deviations (e.g., bradycardia, hypotension, respiratory depression) warrant immediate intervention.
Signs and symptoms of systemic toxicity (CNS and cardiovascular)
Frequency: Continuously during and for at least 30 minutes after administration.
Target: Absence of symptoms.
Action Threshold: Any signs of CNS toxicity (e.g., circumoral numbness, dizziness, tinnitus, visual disturbances, muscle twitching, seizures) or cardiovascular toxicity (e.g., bradycardia, hypotension, arrhythmias) require immediate cessation of administration and supportive care.
Symptom Monitoring
- Lightheadedness
- Dizziness
- Tinnitus
- Visual disturbances (blurred vision, diplopia)
- Numbness or tingling around the mouth (circumoral paresthesia)
- Muscle twitching
- Tremors
- Shivering
- Convulsions (seizures)
- Drowsiness
- Unconsciousness
- Respiratory depression or arrest
- Bradycardia
- Hypotension
- Cardiac arrhythmias
- Cardiac arrest
Special Patient Groups
Pregnancy
Chloroprocaine is classified as Pregnancy Category C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks. It is rapidly metabolized, which may limit fetal exposure.
Trimester-Specific Risks:
First Trimester:
Risk not ruled out. Use only if potential benefit justifies potential risk to the fetus.
Second Trimester:
Risk not ruled out. Use only if potential benefit justifies potential risk to the fetus.
Third Trimester:
Risk not ruled out. Can be used for obstetric anesthesia, but careful monitoring of maternal and fetal status is essential. Rapid metabolism may be advantageous in this setting.
Lactation
Chloroprocaine is considered L3 (Moderately safe) according to the Hale's Lactation Risk Category. Due to its very rapid metabolism by plasma pseudocholinesterase, systemic exposure to the infant via breast milk is expected to be minimal. It is unlikely to cause adverse effects in a breastfed infant.
Infant Risk:
Low risk of adverse effects to the infant.
Pediatric Use
Use with caution. Dosing must be carefully calculated based on weight and age to avoid systemic toxicity. Lower concentrations and total doses are generally recommended. Neonates and infants may have lower pseudocholinesterase activity, potentially leading to slightly prolonged half-life, though still very short.
Geriatric Use
Elderly patients may be more susceptible to the systemic effects of local anesthetics due to decreased physiological reserve and potential for altered pharmacokinetics (e.g., reduced plasma pseudocholinesterase activity, though less significant for chloroprocaine). Lower doses and careful titration are recommended.
Clinical Information
Clinical Pearls
- Chloroprocaine is the shortest-acting local anesthetic available, making it ideal for procedures requiring rapid onset and brief duration of action.
- Its rapid hydrolysis by plasma pseudocholinesterase results in very low systemic toxicity compared to amide-type local anesthetics, as it is quickly inactivated before reaching the liver or kidneys in significant concentrations.
- Patients with pseudocholinesterase deficiency (genetic or acquired) may experience prolonged effects and increased risk of toxicity, though this is rare.
- The metabolite PABA can cause allergic reactions in susceptible individuals, particularly those with a history of allergy to ester-type local anesthetics or sulfonamides.
- Nesacaine-MPF (methylparaben-free) formulations are available to avoid allergic reactions to methylparaben, a preservative found in some multi-dose vials.
Alternative Therapies
- Lidocaine (amide-type, intermediate duration)
- Bupivacaine (amide-type, long duration)
- Mepivacaine (amide-type, intermediate duration)
- Ropivacaine (amide-type, intermediate to long duration)
- Procaine (ester-type, short duration, less commonly used)
Cost & Coverage
Average Cost:
Varies significantly by supplier and contract. Typically in the range of $50-$150 per 30mL vial of 1% solution
Generic Available:
Yes
Insurance Coverage:
Generally covered by most insurance plans as a medical supply/drug when administered in a clinical setting.
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 pour them down the 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 of ingestion.