Chloroprocaine is an anesthetic drug that inhibits the initiation and transmission of neuronal impulses primarily in the sensory nerves. It has the following uses:

• As a local anesthetic (with preservatives) by infiltration locally and for peripheral nerve block.

• Chloroprocaine (without preservatives) is used for nerve block, local infiltration, for epidural & caudal administration, and spinal anesthesia when administered into the subarachnoid space in adults.

Note:

• Because of its fast onset of action and a very short duration of action, it is used only in short (prior to delivery) and ambulatory procedures.
• Chloroprocaine with preservatives should not be used for epidural or spinal anesthesia.

Chloroprocaine Dose in Adults

Use of Chloroprocaine in the treatment of Local anesthesia:

• The smallest dose and concentration should be used, depending on the vascularity of the tissues, the depth, and degree of pain relief, the duration of anesthesia required, and the clinical condition of the patient.
• Emaciated Patients and those with preexisting cardiovascular diseases should be injected with the lowest possible dose.
• A test dose of 3 mL of 3% or 5 mL of 2%  is recommended during epidural administration, prior to the induction of complete block.

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• Clorotekal use (intrathecal) for spinal anesthesia (Subarachnoid block):

  • 50 mg of 1% solution as a single dose.

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• Nesacaine and Nesacaine-MPF:

  • A maximum single dose ( without epinephrine) of 11 mg/kg (to a maximum total dose of 800 mg)
  • A Maximum single dose (with epinephrine 1:200,000) of 14 mg/kg ( to a maximum total dose of 1,000 mg).

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• Caudal block:

  • 2% or 3%: 15 - 25 mL.
  • The dose may be repeated at 40 - 60-minute intervals.

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• Infiltration and peripheral nerve block:

  • Digital without epinephrine:
    • 3 to 4 mL of 1% injection
    • A total dose of 30 - 40 mg may be used.
  • Infraorbital injection:
    • 0.5 - 1 mL of 2% injection
    • A total dose of 10 to 20 mg
  • Mandibular:
    • 2 - 3 mL of 2% injection
    • Total dose 40 - 60 mg
  • Paracervical:
    • 3 mL of 1% per each of four sites
    • A total dose of up to 120 mg
  • Pudendal:
    • 10 mL of 2% on each side
    • A total dose of 400 mg

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  • Lumbar epidural anesthesia for Cesarean delivery:
    • 15 - 25 mL of 3% solution.
    • A total dose of 2 or 3 mL including the test dose

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  • Lumbar epidural anesthesia:
    •  2 - 2.5 mL per segment of 2% or 3% injection
    • The usual total volume is 15 - 25 mL
    • The dose may be repeated with doses that are 2 to 6 mL less than the initial dose every 40 - 50 minutes.

Chloroprocaine Dose in Childrens

• The smallest dose and concentration should be used, depending on the vascularity of the tissues, the depth, and degree of pain relief, the duration of anesthesia required, and the clinical condition of the patient.
• Emaciated Patients and those with preexisting cardiovascular diseases should be injected with the lowest possible dose.

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As Anesthetic agent for local and peripheral nerve block:

• Children older than 3 years and Adolescents:
  • The Maximum dose without epinephrine is 11 mg/kg;
  • For local infiltration, 0.5% to 1% should be used.
  • For nerve block, 1% - 1.5% should be used.

Pregnancy Risk Factor C

• It can cross the placental barrier, and cause maternal or fetal toxicities.
• It is important to monitor the mother, the neonate, and the fetus closely.
• Hypotension can also be experienced in mothers. This could happen if the mother elevates her legs or lateral positions.
• A reduced maternal expulsive effort may be possible with paracervical, epidural, and pudendal anesthesia.
• Patients with prematurity, toxemia of pregnancy, or fetal distress should not use the paracervical blocking. These may include maternal seizures or fetal bradycardia and acidosis.
• Fetal depression may be caused by an accidental intracranial injection.

Chloroaprocaine use during breastfeeding:

• It is unknown whether breastmilk contains chloroprocaine.
• It should be used sparingly by lactating mothers.

Chloroprocaine Dose in Renal Disease:

Dose adjustment in patients with renal disease is not required, but caution must be exercised.

Chloroprocaine Dose in Liver Disease:

• The manufacturer has not recommended any dose adjustment in patients with liver disease.
• Adverse effects may be increased in patients with liver disease, therefore caution must be exercised. 

Common Side Effects of Chloroprocaine include:

• Central nervous system:
  • Procedural pain

Less Common Side Effects Of Chloroprocaine include:

• Cardiovascular:
  • Hypotension
• Central nervous system:
  • Headache
• Endocrine & metabolic:
  • Hyperglycemia
• Gastrointestinal:
  • Nausea
• Local:
  • Injection site pain

Frequency not defined.

• Cardiovascular:
  • Syncope
  • Ventricular arrhythmia
• Central nervous system:
  • Central nervous system depression
  • Central nervous system stimulation
  • Increased body temperature
• Dermatologic:
  • Diaphoresis
  • Erythema
• Gastrointestinal:
  • Loss of anal sphincter control
• Hypersensitivity:
  • Anaphylactoid reaction
  • Angioedema
• Respiratory:
  • Laryngeal edema
  • Respiratory arrest
  • Sneezing

Contraindication to Chloroprocaine include:

• Allergies to chloroprocaine or other ester-type anesthetics or any component of this formulation
• There are certain contraindications to spinal anesthesia, such as hypovolemia, shock and decompensated cardiac disease.
• Intravenous administration
• Serious problems with cardiac conduction
• Local infection at the proposed site for lumbar puncture
• Septicemia.

Warnings and Precautions

• Cardiovascular effects
  • Bradycardia and hypotension can occur when higher doses of IV are administered.
  • During administration, patients should be closely monitored for vital signs.
• CNS toxicity:
  • It may result in restlessness, anxiety, tinnitus, dizziness, tremors, blurred vision, depression, or drowsiness.
  • Patients suffering from a neurological condition should be cautious.
• Infusion-related intra-articular chondrolysis
  • Infusions of chloroprocaine intra-articular are continuousNotAn approved condition known as chondrolysis (mainly the shoulder joint) can occur and may require arthroplasty.
• Methemoglobinemia:
  • It is possible to develop severe methemoglobinemia, which requires immediate treatment and discontinuation of the drug.
  • Patients with G6PD deficiency or methemoglobinemia, cardiac and pulmonary compromise, or exposure to oxidizing agent should be closely monitored for signs and symptoms of methemoglobinemia.
• Respiratory effects
  • It has been reported that patients have suffered sudden respiratory arrest. Each injection should be closely monitored.
• Cardiovascular disease
  • Injections of chloroprocaine can cause severe hypertension/hypotension, heart block and severe cardiac decompensation.
• Hepatic impairment
  • Patients with severe liver disease should be cautious.
• Myasthenia gravis:
  • It can cause weakness or worsen myasthenic symptoms.
• Renal impairment
  • Patients with severe renal impairments should be cautious when using it.

Chloroprocaine: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use    

Monitor:​​​​​​​

• Cardiovascular and respiratory status.
• mental status.
• vital signs including the pulse and Blood pressure.
• Signs of CNS toxicity.

How to Administer Chloroprocaine?

• When used for Infiltration or peripheral nerve block:

  • Administer as a single injection locally or through an indwelling catheter for peripheral nerve block continuously.
  • Intravascular injections and rapid bolus injections should be avoided
  • Before injecting, aspirate and reposition the needle until the blood cannot be drawn by aspiration.

• Epidural (thoracic, lumbar, or caudal) and for spinal anesthesia (subarachnoid block):

  • Preparations containing preservatives should not be used.
  • Injections into an infected or inflamed overlying skin should be avoided.
  • Avoid intravascular injections.

Mechanism of action of chloroprocaine:​​​​​​​

• It is an ester-type local pain reliever.
• It stabilizes neuronal membranes, and prevents transmission and initiation nerve impulses.
• It reduces the nerve membrane permeability for sodium and reversibly prevents the transmission and generation of electrical impulses.
• It first blocks the sensory pain fibers, then the sensory fibers temperature, touch and pressure.
• It blocks the sympathetic motor and sensory nerve fibers in high doses. This is dependent on how much of the drug is injected.

It has beenStartAction of 6-12 minutes and itseffect lastsIt can last up to an hour, depending on the patient and method of administration. The concentration of the drug used, as well as the type of block, will also affect the time.

Depending on the route takenAdministrationThe drug is most concentrated in the most perfused organs like the liver, brains and lungs. It is growing rapidlyMetabolized by enzymes in the plasma to 2-chloro-4-aminobenzoic acid and beta-di-ethyl-amino-ethanol. It has been a half-life eliminationOf 43 seconds for neonates, and 21-25 seconds for adults It is primarily excretedIn the urine.   

International brands of Chloroprocaine:

• Ampres
• Clorotekal
• Ivracain
• Nesacaine

Chloroprocaine Brands in Pakistan:

 No brands available in Pakistan