Chloroprocaine 2%-400mg Inj 20ml
It is used to numb an area before a procedure.
Drug Class
Local Anesthetic
Pharmacologic Class
Ester Local Anesthetic; Sodium Channel Blocker
Pregnancy Category
Category C
FDA Approved
Jan 1952
DEA Schedule
Not Controlled
Overview
What is this medicine?
Chloroprocaine is a medication used to numb a specific part of your body. It's a 'local anesthetic' that works by temporarily blocking nerve signals, so you don't feel pain during a medical procedure like surgery or childbirth. It works 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. 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. 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
- Inform your healthcare provider about all medications you are taking, including over-the-counter drugs, supplements, and herbal products.
- Report any history of allergies, especially to local anesthetics or sulfa drugs.
- Follow all post-procedure instructions given by your healthcare provider, especially regarding activity restrictions or monitoring for numbness/weakness.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Varies significantly by procedure and concentration. For epidural anesthesia: 15-25 mL of 2% or 3% solution (300-750 mg). For caudal block: 15-25 mL of 2% or 3% solution (300-750 mg). For peripheral nerve block: 5-20 mL of 1% or 2% solution (50-400 mg). Max single dose: 800 mg (without epinephrine) or 1000 mg (with epinephrine).
Dose Range:
50 - 1000 mg
Condition-Specific Dosing:
epidural:
2% or 3% solution, 15-25 mL (300-750 mg)
caudal:
2% or 3% solution, 15-25 mL (300-750 mg)
peripheral_nerve_block:
1% or 2% solution, 5-20 mL (50-400 mg)
infiltration:
0.5% or 1% solution, up to 400 mg
Pediatric Dosing
Neonatal:
Not established for routine use; use with extreme caution due to immature pseudocholinesterase activity.
Infant:
Not established for routine use; use with extreme caution due to immature pseudocholinesterase activity.
Child:
Dosing is highly individualized based on weight, age, and procedure. For caudal block: 2-3 mg/kg of 2% solution. Max dose: 11 mg/kg (without epinephrine) or 14 mg/kg (with epinephrine).
Adolescent:
Similar to adult dosing, but adjusted for weight and body surface area. Max dose: 11 mg/kg (without epinephrine) or 14 mg/kg (with epinephrine).
Dose Adjustments
Renal Impairment:
Mild:
No specific adjustment recommended, as metabolism is primarily via plasma pseudocholinesterase.
Moderate:
No specific adjustment recommended.
Severe:
No specific adjustment recommended, but monitor for signs of systemic toxicity if prolonged exposure is anticipated.
Dialysis:
Not significantly removed by dialysis due to rapid metabolism. No specific adjustment.
Hepatic Impairment:
Mild:
No specific adjustment recommended, as metabolism is primarily via plasma pseudocholinesterase.
Moderate:
No specific adjustment recommended.
Severe:
No specific adjustment recommended, but monitor for signs of systemic toxicity, especially if pseudocholinesterase levels are significantly reduced (rare).
Confidence:
Medium
Pharmacology
Mechanism of Action
Chloroprocaine is an ester-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 stabilizes the membrane and inhibits depolarization, thereby preventing the propagation of the action potential.
Pharmacokinetics
Absorption:
Bioavailability:
Dependent on site of administration and presence of vasoconstrictors; systemic absorption occurs from injection site.
Tmax:
Variable, typically within minutes of injection, depending on vascularity of injection site.
FoodEffect:
Not applicable (parenteral administration).
Distribution:
Vd:
Not readily available, but generally distributes rapidly to highly perfused tissues.
ProteinBinding:
Approximately 15-20%
CnssPenetration:
Yes, crosses blood-brain barrier, leading to CNS effects at toxic concentrations.
Elimination:
HalfLife:
Very short; approximately 21 seconds (adults) due to rapid hydrolysis.
Clearance:
High, due to rapid enzymatic hydrolysis.
ExcretionRoute:
Metabolites (PABA and diethylaminoethanol) are primarily excreted by the kidneys.
Unchanged:
< 2% (due to rapid metabolism)
Pharmacodynamics
OnsetOfAction:
Rapid; 6-12 minutes (epidural), 2-5 minutes (infiltration/nerve block).
PeakEffect:
5-15 minutes.
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 too much acid in the blood (acidosis), including:
+ 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, including:
+ 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, including:
+ Feeling lightheaded, sleepy, confused, or experiencing 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, 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
Like all medications, this drug can cause side effects, although not everyone will experience them. If you have any of the following side effects or any other concerns, contact your doctor:
Irritation at the injection site
* Other side effects not listed here
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, 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 too much acid in the blood (acidosis), including:
+ 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, including:
+ 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, including:
+ Feeling lightheaded, sleepy, confused, or experiencing 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, 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
Like all medications, this drug can cause side effects, although not everyone will experience them. If you have any of the following side effects or any other concerns, contact your doctor:
Irritation at the injection site
* Other side effects not listed here
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:
- Dizziness or lightheadedness
- Ringing in the ears (tinnitus)
- Numbness or tingling around the mouth
- Unusual taste in the mouth (metallic taste)
- Blurred vision or double vision
- Tremors or muscle twitching
- Feeling anxious or restless
- Difficulty breathing
- Feeling unusually sleepy or confused
- Slow or irregular heartbeat
- Severe headache
- Any signs of an allergic reaction (e.g., rash, itching, swelling, severe dizziness, trouble breathing)
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 and its symptoms.
If you are currently taking a sulfa (sulfonamide) drug. If you are unsure whether any of your medications contain sulfa, consult your doctor.
This is not an exhaustive list of all potential interactions with this medication. Therefore, it is crucial to discuss the following with your doctor and pharmacist:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your existing health problems
To ensure your safety, verify that it is acceptable to take this medication with all your other medications 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, such as foods or drugs. Be sure to describe the allergic reaction and its symptoms.
If you are currently taking a sulfa (sulfonamide) drug. If you are unsure whether any of your medications contain sulfa, consult your doctor.
This is not an exhaustive list of all potential interactions with this medication. Therefore, it is crucial to discuss the following with your doctor and pharmacist:
All prescription and over-the-counter (OTC) medications you are taking
Any natural products or vitamins you are using
* Your existing health problems
To ensure your safety, verify that it is acceptable to take this medication with all your other medications 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.
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
- Elderly Patients (65 and older): Use this medication with caution, as you may be more susceptible to side effects.
- Pediatric Patients: Use this medication with caution in children, as the risk of certain side effects may be higher.
- 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 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.
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
- Elderly Patients (65 and older): Use this medication with caution, as you may be more susceptible to side effects.
- Pediatric Patients: Use this medication with caution in children, as the risk of certain side effects may be higher.
- 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 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 CNS effects (seizures, unconsciousness, respiratory arrest)
- Cardiovascular depression (severe hypotension, bradycardia, arrhythmias, cardiac arrest)
What to Do:
Immediate medical attention is required. Call 911 or your local emergency number. In the US, you can also call Poison Control at 1-800-222-1222.
Drug Interactions
Major Interactions
- Sulfonamides (due to PABA metabolite, which can antagonize sulfonamide antibacterial activity)
- Cholinesterase inhibitors (e.g., neostigmine, pyridostigmine, donepezil, rivastigmine, galantamine, echothiophate): May decrease the metabolism of chloroprocaine, increasing risk of systemic toxicity.
Moderate Interactions
- Other local anesthetics: Additive systemic toxicity if combined.
- Opioids, sedatives: May enhance CNS depression when used concurrently with epidural/spinal anesthesia.
Monitoring
Baseline Monitoring
Patient history (allergies, pseudocholinesterase deficiency, cardiovascular disease, CNS disorders)
Rationale: To identify contraindications or risk factors for adverse reactions.
Timing: Prior to administration
Vital signs (BP, HR, RR, O2 saturation)
Rationale: To establish baseline and detect early signs of systemic toxicity or cardiovascular effects.
Timing: Prior to administration
Routine Monitoring
Vital signs (BP, HR, RR, O2 saturation)
Frequency: Every 5-15 minutes during and immediately after administration, then as clinically indicated.
Target: Within patient's normal limits; monitor for significant deviations.
Action Threshold: Hypotension, bradycardia, respiratory depression, or desaturation requiring intervention.
Level of consciousness/CNS status
Frequency: Continuously during and immediately after administration.
Target: Alert and oriented, or appropriate sedation level.
Action Threshold: Dizziness, tinnitus, perioral numbness, seizures, somnolence.
Sensory and motor block assessment
Frequency: As needed to confirm efficacy and monitor spread of block.
Target: Desired level of anesthesia/analgesia.
Action Threshold: Inadequate block or signs of high spinal/epidural block.
Symptom Monitoring
- Lightheadedness
- Dizziness
- Tinnitus
- Perioral numbness
- Metallic taste
- Blurred vision
- Tremors
- Muscle twitching
- Seizures
- Drowsiness
- Unconsciousness
- Respiratory depression
- Hypotension
- Bradycardia
- Cardiac arrest
- Urticaria
- Pruritus
- Erythema
- Angioedema
- Bronchospasm
- Anaphylaxis
Special Patient Groups
Pregnancy
Category C. Use only if the potential benefit justifies the potential risk to the fetus. While rapidly metabolized, systemic absorption can occur. It has been used for epidural anesthesia during labor and delivery.
Trimester-Specific Risks:
First Trimester:
Limited data; theoretical risk of teratogenicity, but rapid metabolism minimizes systemic exposure.
Second Trimester:
Generally considered safer than first trimester, but still Category C.
Third Trimester:
Commonly used for epidural anesthesia during labor. Rapid metabolism limits fetal exposure, but fetal bradycardia has been reported with paracervical block.
Lactation
L3 (Moderately Safe). Due to its very rapid metabolism by plasma pseudocholinesterase, chloroprocaine is unlikely to be excreted in significant amounts into breast milk. Any amount that does enter breast milk would likely be rapidly hydrolyzed in the infant's gastrointestinal tract. Considered compatible with breastfeeding by many sources.
Infant Risk:
Low risk of adverse effects to the infant.
Pediatric Use
Use with caution, especially in neonates and infants, due to potentially lower levels of plasma pseudocholinesterase, which could lead to prolonged half-life and increased risk of systemic toxicity. Dosing must be carefully calculated based on weight and age. Not recommended for routine use in very young children.
Geriatric Use
No specific dose adjustment is typically required based on age alone, as metabolism is primarily via plasma pseudocholinesterase. However, elderly patients may have reduced pseudocholinesterase activity or be more sensitive to the systemic effects of local anesthetics, requiring careful titration and monitoring. Consider reduced lean body mass and potential comorbidities.
Clinical Information
Clinical Pearls
- Chloroprocaine is an ester-type local anesthetic, known for its very rapid onset and short duration of action, making it suitable for procedures requiring quick onset and limited duration.
- Its rapid hydrolysis by plasma pseudocholinesterase minimizes systemic toxicity and accumulation, even with repeated doses, compared to amide-type local anesthetics.
- The PABA metabolite can cause allergic reactions in susceptible individuals, particularly those with a history of allergy to ester-type local anesthetics or sulfonamides.
- Avoid use in patients with known pseudocholinesterase deficiency, as this can lead to prolonged half-life and increased risk of systemic toxicity.
- Epinephrine is often added to prolong the duration of action and reduce systemic absorption, but it should be used with caution in patients with cardiovascular disease or in areas with end-arterial blood supply (e.g., fingers, toes, nose, penis, ears).
- Monitor for signs of systemic toxicity (CNS and cardiovascular) even with appropriate dosing, as accidental intravascular injection can occur.
Alternative Therapies
- Lidocaine (amide-type local anesthetic, intermediate duration)
- Bupivacaine (amide-type local anesthetic, long duration)
- Ropivacaine (amide-type local anesthetic, long duration, less cardiotoxic than bupivacaine)
- Mepivacaine (amide-type local anesthetic, intermediate duration)
- Procaine (ester-type local anesthetic, similar to chloroprocaine but less potent)
Cost & Coverage
Average Cost:
Varies widely by concentration, volume, and supplier. Typically ranges from $10-$50 per 20mL vial. per 20mL vial
Generic Available:
Yes
Insurance Coverage:
Generally covered by most medical insurance plans when administered in a clinical setting for approved indications.
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, never share your prescription medications with others, and do not take medications prescribed to someone else. 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 dispose of them by flushing down the toilet or pouring down the drain unless specifically instructed to do so by a healthcare professional or pharmacist. If you are unsure about the correct disposal method, consult with your pharmacist, who can provide guidance on safe disposal practices. Many communities offer drug take-back programs, which your pharmacist can help you locate.
Some medications may come with an additional patient information leaflet. If you have questions or concerns about your medication, it is important 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.
Proper disposal of unused or expired medications is crucial. Do not dispose of them by flushing down the toilet or pouring down the drain unless specifically instructed to do so by a healthcare professional or pharmacist. If you are unsure about the correct disposal method, consult with your pharmacist, who can provide guidance on safe disposal practices. Many communities offer drug take-back programs, which your pharmacist can help you locate.
Some medications may come with an additional patient information leaflet. If you have questions or concerns about your medication, it is important 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.