Version May 2024
Dose varies with procedure, desired depth, and duration of anesthesia, desired muscle relaxation, vascularity of tissues, physical condition, and age of patient. The smallest dose and concentration required to produce the desired effect should be used. Decrease dose in debilitated patients and patients with cardiac disease.
Anesthesia, local injectable and peripheral nerve block: Children >3 years and Adolescents: Maximum dose without epinephrine: 11 mg/kg; for infiltration, concentrations of 0.5% to 1% are recommended; for nerve block, concentrations of 1% to 1.5% are recommended
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling. Use with caution due to increased risk of adverse effects.
There are no specific dosage adjustments provided in the manufacturer's labeling; however, dosage should be reduced. Use with caution due to increased risk of adverse effects.
(For additional information see "Chloroprocaine (systemic): Drug information")
Local anesthesia: Note: Use the smallest dose and concentration required to produce the desired result. Dosage varies with anesthetic procedure, the vascularity of the tissues, depth of anesthesia required, degree of muscle relaxation required, duration of anesthesia, and physical condition of the patient. Use reduced doses in debilitated patients and patients with cardiovascular disease. During epidural administration, a test dose (3 mL of 3% or 5 mL of 2%) is recommended prior to induction of complete block and all reinforcing doses with continuous catheter technique.
Clorotekal: Subarachnoid block (spinal anesthesia): Intrathecal: 1%: 50 mg single dose (effective block to the T 10 level). Note: Other preservative- and antioxidant-free formulations (eg, Nesacaine-MPF) have also been used off-label (dosage range: 20 to 60 mg) for spinal anesthesia for short-duration ambulatory procedures; ensure that preservative-free products do not contain the antioxidant sodium bisulfite prior to administration (Gebhardt 2017; Hejtmanek 2011; Wesselink 2022).
Nesacaine, Nesacaine-MPF:
Maximum single dose (without epinephrine): 11 mg/kg; maximum total dose: 800 mg.
Maximum single dose (with epinephrine 1:200,000): 14 mg/kg; maximum total dose: 1,000 mg.
Caudal block (preservative free): 2% or 3%: 15 to 25 mL; may repeat at 40- to 60-minute intervals.
Infiltration and peripheral nerve block:
Brachial plexus: 2%: 30 to 40 mL; total dose 600 to 800 mg.
Digital (without epinephrine): 1%: 3 to 4 mL; total dose: 30 to 40 mg.
Infraorbital: 2%: 0.5 to 1 mL; total dose 10 to 20 mg.
Mandibular: 2%: 2 to 3 mL; total dose 40 to 60 mg.
Paracervical: 1%: 3 mL per each of four sites; total dose: up to 120 mg.
Pudendal: 2%: 10 mL each side; total dose: 400 mg.
Lumbar epidural anesthesia, Cesarean delivery (preservative free): 3%: 15 to 20 mL total dose (includes test dose of 2 or 3 mL) (Bjornestad 2006; Feng 2012; Reschke 2020).
Lumbar epidural anesthesia, nonpregnant (preservative free): 2% or 3%: 2 to 2.5 mL per segment; usual total volume: 15 to 25 mL; may repeat with doses that are 2 to 6 mL less than initial dose at 40- to 50-minute intervals.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer’s labeling. Use with caution due to increased risk of adverse effects.
There are no specific dosage adjustments provided in the manufacturer’s labeling; however, dosage should be reduced. Use with caution due to increased risk of adverse effects.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%:
Cardiovascular: Hypotension (5%)
Endocrine & metabolic: Hyperglycemia (<2%)
Gastrointestinal: Nausea (<2%)
Local: Pain at injection site (4%)
Nervous system: Headache (<2%)
Postmarketing:
Cardiovascular: Bradycardia, cardiac arrhythmia, cardiac insufficiency, hypertension, presyncope, tachycardia
Dermatologic: Erythema multiforme
Gastrointestinal: Fecal incontinence, oral hypoesthesia, oral paresthesia, vomiting
Genitourinary: Groin pain, sexual disorder, urinary incontinence
Hypersensitivity: Hypersensitivity reaction (including anaphylaxis, angioedema, nonimmune anaphylaxis)
Nervous system: Akathisia, anxiety, arachnoiditis, burning sensation, cauda equina syndrome, dizziness, drowsiness, dysesthesia, feeling hot, hypoesthesia, loss of consciousness, malaise, motor dysfunction, myoclonus, paresthesia, peripheral neuropathy, restlessness, seizure, speech disturbance, tremor
Neuromuscular & skeletal: Back pain, limb pain
Ophthalmic: Blurred vision, diplopia, photophobia, visual disturbance
Otic: Auditory impairment, tinnitus
Respiratory: Apnea, dyspnea, respiratory depression
Hypersensitivity to chloroprocaine, other para aminobenzoic acid (PABA) ester type anesthetics, or any component of the formulation.
Additional contraindications described in the Clorotekal labeling (clinically, some may be applicable to other products): Contraindications specific to spinal anesthesia (eg, decompensated cardiac insufficiency, hypovolemic, shock, coagulopathy); IV regional anesthesia; serious cardiac conduction problems; local infection at the site of proposed lumbar puncture; sepsis.
Concerns related to adverse effects:
• Cardiovascular effects: Local anesthetics, at high systemic concentrations, are commonly associated with hypotension and bradycardia especially with inadvertent intravascular administration. Perform preventive measures (eg, limiting cumulative dose, use ultrasound or direct visualization for catheter placement). Careful and constant monitoring of the patient's cardiovascular vital signs should be done during and following each local anesthetic injection (Cox 2003; Dickerson 2014). In the event of cardiovascular collapse and/or severe CNS toxicity, treatment in accordance with the American Society of Regional Anesthesia and Pain Medicine’s Checklist for Treatment of Local Anesthetic Toxicity is recommended (Neal [ASRA 2021]).
• CNS toxicity: Careful and constant monitoring of the patient's state of consciousness should be done following each local anesthetic injection; at such times, restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression, or drowsiness may be early warning signs of CNS toxicity. Use extreme caution in patients with existing neurological disease. Seizures due to systemic toxicity leading to cardiac arrest have also been reported, presumably following unintentional intravascular injection. In the event of cardiovascular collapse and/or severe CNS toxicity, treatment in accordance with the American Society of Regional Anesthesia and Pain Medicine’s Checklist for Treatment of Local Anesthetic Toxicity is recommended (Neal [ASRA 2021]).
• Intra-articular infusion related chondrolysis: Continuous intra-articular infusion of local anesthetics after arthroscopic or other surgical procedures is not an approved use; chondrolysis (primarily in the shoulder joint) has occurred following infusion, with some cases requiring arthroplasty or shoulder replacement.
• Methemoglobinemia: Has been reported with local anesthetics; clinically significant methemoglobinemia requires immediate treatment along with discontinuation of the anesthetic and other oxidizing agents. Onset may be immediate or delayed (hours) after anesthetic exposure. Patients with G6PD deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, exposure to oxidizing agents or their metabolites, or infants <6 months of age are more susceptible and should be closely monitored for signs and symptoms of methemoglobinemia (eg, cyanosis, headache, rapid pulse, shortness of breath, lightheadedness, fatigue).
• Respiratory effects: Local anesthetics have been associated with rare occurrences of sudden respiratory arrest. Careful and constant monitoring of the patient's respiratory (adequacy of ventilation) vital signs should be done following each local anesthetic injection.
Disease-related concerns:
• Cardiovascular disease: Use extreme caution in patients with cardiovascular disease, including severe hypertension, hypotension, heart block, and severe cardiac decompensation.
• Hepatic impairment: Use with caution in patients with severe hepatic impairment.
• Myasthenia gravis: Use with extreme caution in patients with myasthenia gravis; may cause significant weakness (Haroutiunian 2009).
• Plasma cholinesterase disorders: Use with caution in patients with genetic deficiency of plasma cholinesterase.
• Kidney impairment: Use with caution in patients with severe kidney impairment.
Special populations:
• Acutely ill patients: Use with caution in acutely ill; reduce dose consistent with age and physical status.
• Debilitated patients: Use with caution in debilitated patients; reduce dose consistent with age and physical status.
• Older adult: Use with caution in the elderly; reduce dose consistent with age and physical status.
• Pediatric: Use with caution in children; reduce dose consistent with age and physical status.
Other warnings/precautions:
• Administration: Intravascular injections should be avoided; aspiration should be performed prior to administration; the needle must be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided.
• Epidural (thoracic, lumbar, or caudal) and intrathecal/spinal administration: Do not use solutions containing preservatives. Use extreme caution in patients with spinal deformities, neurologic disease, septicemia, and severe hypertension when used for thoracic, lumbar, and caudal epidural administration. With intrathecal/spinal administration, neurologic damage may occur after anesthesia (eg, paresthesia, loss of sensitivity, motor weakness, paralysis, cauda equina syndrome); symptoms may persist and may be permanent; carefully evaluate patients with underlying neuromuscular disorders while considering risk vs. benefit prior to treatment. Use with caution or avoid epidural or intrathecal/spinal administration in patients with bleeding disorders (congenital or acquired) and severe anemia (Horlocker 2010). Clorotekal (a product with specific FDA approval for intrathecal/spinal administration) is contraindicated in patients with serious cardiac conduction abnormalities, local infection at proposed lumbar puncture site, or sepsis; contraindications to intrathecal/spinal anesthesia should be taken into consideration.
• Trained personnel: Clinicians using local anesthetic agents should be well trained in diagnosis and management of emergencies that may arise from the use of these agents. Resuscitative equipment, oxygen, and other resuscitative drugs should be available for immediate use.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Injection, as hydrochloride:
Nesacaine: 1% (30 mL); 2% (30 mL) [contains disodium edta, methylparaben]
Solution, Injection, as hydrochloride [preservative free]:
Nesacaine-MPF: 2% (20 mL); 3% (20 mL) [methylparaben free]
Generic: 2% (20 mL); 3% (20 mL)
Solution, Intrathecal, as hydrochloride [preservative free]:
Clorotekal: 1% (5 mL)
Yes
Solution (Chloroprocaine HCl (PF) Injection)
2% (per mL): $1.28
3% (per mL): $1.34
Solution (Clorotekal Intrathecal)
50 mg/5 mL (per mL): $3.69
Solution (Nesacaine Injection)
1% (per mL): $0.72
2% (per mL): $0.74
Solution (Nesacaine-MPF Injection)
2% (per mL): $1.28
3% (per mL): $1.34
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Parenteral: Administer locally as a single injection or continuously through an indwelling catheter. Avoid rapid injection. Do not use for subarachnoid administration. Intravascular injections should be avoided; aspiration should be performed prior to administration; the needle must be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided.
Infiltration or peripheral nerve block: Administer locally as a single injection or continuously through an indwelling catheter (peripheral nerve block). Avoid rapid injection. Intravascular injections should be avoided; aspiration should be performed prior to administration; the needle must be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided.
Epidural (thoracic, lumbar, or caudal) and subarachnoid block (spinal anesthesia): Do not use solutions containing preservatives. Use a filter needle to draw up solution from ampule when using Clorotekal. Clorotekal is intended for intrathecal administration only; the manufacturer recommends against using for epidural administration. Use of Clorotekal via continuous spinal catheters is not recommended (safety has not been established). Do not puncture areas of the skin with signs of infection/inflammation. Intravascular injections should be avoided; aspiration should be performed prior to administration; the needle must be repositioned until no return of blood can be elicited by aspiration; however, absence of blood in the syringe does not guarantee that intravascular injection has been avoided.
Store at 20°C to 25°C (68°F to 77°F) in original container; protect from freezing. Protect from light. Discard Clorotekal and Nesacaine-MPF following single use. Solution in vials may become discolored with prolonged exposure to light; do not administer discolored solutions. Crystals of chloroprocaine may develop when exposed to low temperatures; when the vial is returned to room temperature, the crystals will redissolve with shaking; do not use solutions that contain undissolved matter. Do not heat before use; do not autoclave. Use immediately after initial puncture of vial or after ampule opening.
Production of local anesthesia by local infiltration and peripheral nerve block techniques (Nesacaine, Nesacaine-MPF: FDA approved in children and adults); production of central nerve blocks including lumbar and caudal epidural blocks (Nesacaine-MPF: FDA approved in adults); production of local anesthesia by subarachnoid block (spinal anesthesia) (Clorotekal: FDA approved in adults).
Limitations of use: Nesacaine, Nesacaine-MPF: The manufacturer recommends against using either formulation (ie, with or without preservatives) for subarachnoid administration (ie, spinal anesthesia). Do not use chloroprocaine with preservatives (Nesacaine) for epidural or spinal anesthesia.
Nesacaine may be confused with Neptazane
The Institute for Safe Medication Practices (ISMP) includes this medication (epidural administration) among its list of drug classes which have a heightened risk of causing significant patient harm when used in error.
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Alpha-/Beta-Agonists: Chloroprocaine (Systemic) may enhance the hypertensive effect of Alpha-/Beta-Agonists. Risk C: Monitor therapy
BUPivacaine: Local Anesthetics may enhance the adverse/toxic effect of BUPivacaine. Management: Avoid using any additional local anesthetics within 96 hours after insertion of the bupivacaine implant (Xaracoll) or bupivacaine and meloxicam periarticular solution (Zynrelef) or within 168 hours after subacromial infiltration (Posimir brand). Risk C: Monitor therapy
BUPivacaine (Liposomal): Local Anesthetics may enhance the adverse/toxic effect of BUPivacaine (Liposomal). Management: Liposomal bupivacaine should not be administered with local anesthetics, but may be administered 20 minutes or more after lidocaine. Avoid all local anesthetics within 96 hours after administration of liposomal bupivacaine. Risk X: Avoid combination
Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Chloroprocaine (Systemic) may enhance the hypertensive effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy
Hyaluronidase: May enhance the adverse/toxic effect of Local Anesthetics. Risk C: Monitor therapy
Methemoglobinemia Associated Agents: May enhance the adverse/toxic effect of Local Anesthetics. Specifically, the risk for methemoglobinemia may be increased. Risk C: Monitor therapy
Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Risk C: Monitor therapy
Phenylephrine (Systemic): Chloroprocaine (Systemic) may enhance the hypotensive effect of Phenylephrine (Systemic). Risk C: Monitor therapy
Sulfonamide Antibiotics: Chloroprocaine (Systemic) may diminish the therapeutic effect of Sulfonamide Antibiotics. Management: Avoid concurrent use of chloroprocaine and systemic sulfonamide-based antimicrobials whenever possible. Risk D: Consider therapy modification
Technetium Tc 99m Tilmanocept: Local Anesthetics may diminish the diagnostic effect of Technetium Tc 99m Tilmanocept. Management: Avoid mixing and simultaneously co-injecting technetium Tc 99m tilmanocept with local anesthetics. This interaction does not appear to apply to other uses of these agents in combination. Risk C: Monitor therapy
Chloroprocaine crosses the placenta (Kuhnert 1980).
Exposure to the fetus is expected to be limited due to the short maternal half-life but varies by route of administration (Nau 1985; Togioka 2022). Chloroprocaine may potentially cause varying degrees of maternal, fetal, and neonatal toxicity involving the CNS, peripheral vascular tone, and cardiac function depending on dose and administration technique.
Chloroprocaine is used in obstetric anesthesia (ACOG 2019; Novikova 2012; Reschke 2020). Use may be beneficial when a short onset of action is needed (Reschke 2020).
Blood pressure, heart rate, respiration, signs of CNS toxicity (lightheadedness, dizziness, tinnitus, restlessness, tremors, twitching, drowsiness, circumoral paresthesia, mental status).
Chloroprocaine is an ester-type local anesthetic, which stabilizes the neuronal membranes and prevents initiation and transmission of nerve impulses thereby affecting local anesthetic actions. Chloroprocaine reversibly prevents generation and conduction of electrical impulses in neurons by decreasing the transient increase in permeability to sodium. The differential sensitivity generally depends on the size of the fiber; small fibers are more sensitive than larger fibers and require a longer period for recovery. Sensory pain fibers are usually blocked first, followed by fibers that transmit sensations of temperature, touch, and deep pressure. High concentrations block sympathetic somatic sensory and somatic motor fibers. The spread of anesthesia depends upon the distribution of the solution. This is primarily dependent on the volume of drug injected.
Onset of action: 6 to 12 minutes
Duration (patient, type of block, concentration, and method of anesthesia dependent): Up to 60 minutes
Distribution: Vd: Depends upon route of administration; high concentrations found in highly perfused organs such as liver, lungs, heart, and brain
Metabolism: Rapidly hydrolyzed by plasma enzymes to 2-chloro-4-aminobenzoic acid and beta-diethylaminoethanol (80% conjugated before elimination)
Half-life elimination: In vitro, plasma: Neonates: 43 ± 2 seconds; Adults: 21 ± 2 seconds (males), 25 ± 1 second (females)
Excretion: Urine (minimal as unchanged drug in urine; metabolites: Chloro-aminobenzoic acid and beta-diethylaminoethanol primarily excreted unchanged)
Hepatic function impairment: Pharmacokinetic parameters can be significantly altered.
Older adult: Pharmacokinetic parameters can be significantly altered.
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