Chloroprocaine Hcl 3% Inj, 20ml

Manufacturer HIKMA PHARMACEUTICALS USA Active Ingredient Chloroprocaine(klor oh PROE kane) Pronunciation klor oh PROE kane
It is used to numb an area before a procedure.
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Drug Class
Local Anesthetic
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Pharmacologic Class
Ester-type Local Anesthetic; Sodium Channel Blocker
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Pregnancy Category
C
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FDA Approved
Jan 1970
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Chloroprocaine is a medication used to numb a specific part of your body, preventing you from feeling pain during medical procedures like surgery or childbirth. It works by temporarily blocking nerve signals in the area where it's injected.
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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.

Missed Doses

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.
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Lifestyle & Tips

  • Inform your healthcare provider about all medications you are taking, including over-the-counter drugs, supplements, and herbal products.
  • Report any unusual symptoms or discomfort during or after the procedure, such as dizziness, ringing in the ears, numbness, or tingling.
  • Follow all post-procedure instructions from your healthcare provider, especially regarding activity restrictions while the numbing effect wears off.
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Available Forms & Alternatives

Dosing & Administration

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Adult Dosing

Standard Dose: Varies significantly by procedure and site of injection. Typically 40-80 mg for spinal anesthesia (3% solution), up to 800 mg for epidural (2% or 3% solution) or nerve blocks.

Condition-Specific Dosing:

spinal_anesthesia: 30-60 mg (1-2 mL of 3% solution)
epidural_anesthesia_lumbar: Up to 800 mg (e.g., 20-30 mL of 2% or 3% solution) for surgical anesthesia; lower doses for labor analgesia.
peripheral_nerve_block: Varies by nerve, typically 50-400 mg (e.g., 5-20 mL of 1% or 2% solution). Max single dose 800 mg (1000 mg with epinephrine).
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Pediatric Dosing

Neonatal: Not established for routine use; use with extreme caution if at all.
Infant: Not established for routine use; use with extreme caution if at all.
Child: Dosing is highly individualized based on weight, age, and procedure. Max dose typically 11 mg/kg (without epinephrine) or 14 mg/kg (with epinephrine), not to exceed adult maximums. Spinal anesthesia: 0.5-1 mg/kg.
Adolescent: Similar to adult dosing, adjusted for weight and body surface area.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment recommended.
Moderate: No specific adjustment recommended.
Severe: No specific adjustment recommended, as it is primarily metabolized by plasma pseudocholinesterase. However, caution is advised due to potential accumulation of metabolites.
Dialysis: Not significantly removed by dialysis. No specific adjustment, but monitor for signs of toxicity.

Hepatic Impairment:

Mild: No specific adjustment recommended.
Moderate: No specific adjustment recommended.
Severe: No specific adjustment recommended, as it is primarily metabolized by plasma pseudocholinesterase. However, caution is advised in severe hepatic dysfunction due to potential altered protein binding or overall patient fragility.

Pharmacology

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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, leading to a lack of propagation of the action potential and thus local anesthesia.
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Pharmacokinetics

Absorption:

Bioavailability: Dependent on site of injection and presence of vasoconstrictor; systemic absorption occurs from the site of administration.
Tmax: Rapid, typically within minutes of injection, depending on site.
FoodEffect: Not applicable (parenteral administration).

Distribution:

Vd: Not extensively studied, but generally distributes rapidly to highly perfused tissues.
ProteinBinding: Low (approximately 10-20%)
CnssPenetration: Limited, but can cross blood-brain barrier if systemic levels are high enough to cause CNS toxicity.

Elimination:

HalfLife: Very short; approximately 20-50 seconds in adults due to rapid hydrolysis.
Clearance: Very rapid due to plasma pseudocholinesterase activity.
ExcretionRoute: Metabolites (PABA) are primarily excreted by the kidneys.
Unchanged: < 2% (due to rapid metabolism)
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Pharmacodynamics

OnsetOfAction: Very rapid; 6-12 minutes for epidural, 2-5 minutes for spinal.
PeakEffect: Within minutes of onset.
DurationOfAction: Very short; 30-60 minutes for epidural, 30-60 minutes for spinal (without epinephrine). Epinephrine prolongs duration.

Safety & Warnings

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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 concerned about any of the following:

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.
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Seek Immediate Medical Attention If You Experience:

  • Feeling lightheaded or dizzy
  • Ringing in your ears (tinnitus)
  • Numbness or tingling around your mouth
  • Unusual taste in your mouth (metallic taste)
  • Blurred or double vision
  • Tremors or muscle twitching
  • Feeling unusually sleepy or confused
  • Difficulty breathing
  • Slow or irregular heartbeat
  • Skin rash, itching, or hives
  • Swelling of the face, lips, or tongue
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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 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

Carefully review your medications and health conditions with your doctor to ensure it is safe to take this medication. Never start, stop, or change the dose of any medication without first consulting your doctor.
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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 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: Use this medication with caution, as the risk of certain side effects may be higher in children.
- 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.
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Overdose Information

Overdose Symptoms:

  • Severe dizziness or lightheadedness
  • Seizures
  • Unconsciousness
  • Respiratory arrest (stopping breathing)
  • Cardiac arrest (heart stopping)

What to Do:

If you experience any severe symptoms, or if someone else has received too much of this medication, seek immediate emergency medical attention. Call 911 or your local emergency number. For general poison control, call 1-800-222-1222.

Drug Interactions

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Major Interactions

  • Sulfonamides (due to PABA metabolite antagonism)
  • Cholinesterase inhibitors (e.g., neostigmine, pyridostigmine, donepezil): May decrease metabolism of chloroprocaine, increasing risk of toxicity.
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Moderate Interactions

  • Other local anesthetics: Additive systemic toxicity.
  • Opioids: May enhance analgesic effect but also increase risk of respiratory depression if systemic absorption is significant.

Monitoring

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Baseline Monitoring

Patient history (allergies, medical conditions, current medications)

Rationale: To identify contraindications, risk factors for adverse reactions, and potential drug interactions.

Timing: Pre-procedure

Vital signs (heart rate, blood pressure, respiratory rate, oxygen saturation)

Rationale: To establish baseline and detect early signs of systemic toxicity or adverse reactions.

Timing: Pre-procedure

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Routine Monitoring

Vital signs (heart rate, blood pressure, respiratory rate, oxygen saturation)

Frequency: Continuously during and immediately after administration, then as clinically indicated.

Target: Within patient's normal physiological range.

Action Threshold: Significant deviations (e.g., bradycardia, hypotension, hypoxemia) require immediate intervention.

Level of consciousness/Neurological status

Frequency: Continuously during and immediately after administration.

Target: Alert and oriented, no signs of CNS excitation or depression.

Action Threshold: Drowsiness, dizziness, tinnitus, perioral numbness, seizures, or loss of consciousness indicate systemic toxicity.

Motor and sensory block assessment

Frequency: As needed to confirm efficacy and monitor spread of block.

Target: Desired level of anesthesia/analgesia.

Action Threshold: Inadequate block requires re-dosing or alternative strategy; excessive block may indicate unintended spread.

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Symptom Monitoring

  • Lightheadedness
  • Dizziness
  • Tinnitus
  • Perioral numbness
  • Metallic taste
  • Blurred vision
  • Tremors
  • Muscle twitching
  • Seizures
  • Drowsiness
  • Unconsciousness
  • Bradycardia
  • Hypotension
  • Cardiac arrest
  • Respiratory depression/arrest
  • Urticaria
  • Pruritus
  • Erythema
  • Angioedema
  • Bronchospasm
  • Anaphylaxis

Special Patient Groups

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Pregnancy

Chloroprocaine is classified as Pregnancy Category C. While animal studies have shown adverse effects at high doses, its rapid metabolism by plasma pseudocholinesterase limits fetal exposure. It is often considered a preferred local anesthetic for epidural anesthesia in obstetrics due to its rapid onset, short duration, and low potential for systemic toxicity in both mother and fetus.

Trimester-Specific Risks:

First Trimester: Limited data, but rapid metabolism suggests low risk.
Second Trimester: Often used for procedures during this trimester.
Third Trimester: Commonly used for labor and delivery (epidural/spinal anesthesia) due to favorable safety profile.
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Lactation

Lactation Risk Category L3 (Moderately Safe). Due to its very short half-life and rapid metabolism in plasma, systemic exposure to the infant via breast milk is expected to be minimal. It is generally considered compatible with breastfeeding.

Infant Risk: Low risk of adverse effects to the breastfed infant.
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Pediatric Use

Use with caution and reduced doses. Children, especially infants and neonates, may have lower levels of plasma pseudocholinesterase, potentially leading to slower metabolism and increased risk of systemic toxicity. Dosing must be carefully calculated based on weight and age, and close monitoring for signs of toxicity is essential.

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Geriatric Use

No specific dose adjustment is typically required based solely on age. However, elderly patients may be more susceptible to the systemic effects of local anesthetics due to decreased physiological reserve, co-morbidities, and polypharmacy. Use with caution and consider lower initial doses, monitoring closely for adverse effects.

Clinical Information

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Clinical Pearls

  • Chloroprocaine is an ester-type local anesthetic known for its very rapid onset and very short duration of action, making it suitable for procedures requiring quick onset and limited post-procedure numbness.
  • Its rapid hydrolysis by plasma pseudocholinesterase minimizes systemic toxicity and makes it a favorable choice for obstetric anesthesia, as fetal exposure is very low.
  • The PABA metabolite can antagonize the antibacterial action of sulfonamides; avoid concurrent use if possible.
  • Patients with atypical pseudocholinesterase deficiency are at significantly increased risk of prolonged systemic toxicity and should generally avoid chloroprocaine.
  • Always aspirate prior to injection to avoid inadvertent intravascular administration, which can lead to rapid systemic toxicity.
  • The 3% solution is typically used for spinal anesthesia or when a denser, more rapid block is required (e.g., surgical epidural).
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Alternative Therapies

  • Lidocaine (Amide-type local anesthetic, moderate duration)
  • Bupivacaine (Amide-type local anesthetic, long duration)
  • Ropivacaine (Amide-type local anesthetic, long duration, less cardiotoxic than bupivacaine)
  • Mepivacaine (Amide-type local anesthetic, moderate duration)
  • Tetracaine (Ester-type local anesthetic, long duration, primarily for spinal anesthesia)
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Cost & Coverage

Average Cost: Varies, typically $50-$150 per 20mL vial of 3% solution
Generic Available: Yes
Insurance Coverage: Generally covered by most insurance plans when administered in a clinical setting for a covered procedure.
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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 guidance. To ensure your safety and the safety of others, never share your medication with anyone, and do not take medication prescribed to someone else.

Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion. Properly dispose of any unused or expired medication. Unless instructed to do so by a healthcare professional or pharmacist, avoid flushing medications down the toilet or pouring them down the drain. If you are unsure about the best method for disposing of your medication, consult with your pharmacist, as they can provide guidance on safe disposal methods or inform you about potential drug take-back programs in your area.

Some medications may come with an additional patient information leaflet; check with your pharmacist to see if this applies to your prescription. If you have any questions or concerns about your medication, do not hesitate 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 information about the medication taken, the quantity, and the time it was taken, as this will aid healthcare professionals in providing appropriate care.