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Chloroprocaine

Pronunciation

(klor oh PROE kane)

Index Terms

  • Chloroprocaine Hydrochloride
  • Clorotekal

Dosage Forms

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)

Brand Names: U.S.

  • Nesacaine
  • Nesacaine-MPF

Pharmacologic Category

  • Local Anesthetic

Pharmacology

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.

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)

Excretion

Urine (minimal as unchanged drug in urine; metabolites: Chloro-aminobenzoic acid and beta-diethylaminoethanol primarily excreted unchanged)

Onset of Action

6 to 12 minutes

Duration of Action

Up to 60 minutes (patient, type of block, concentration, and method of anesthesia dependent)

Half-Life Elimination

In vitro, plasma: Neonates: 43 ± 2 seconds; Adults: 21 ± 2 seconds (males), 25 ± 1 second (females)

Special Populations: Renal Function Impairment

Pharmacokinetic parameters can be significantly altered.

Special Populations: Hepatic Function Impairment

Pharmacokinetic parameters can be significantly altered.

Special Populations: Elderly

Pharmacokinetic parameters can be significantly altered.

Use: Labeled Indications

Local anesthesia:

Chloroprocaine (with preservatives):

Production of local anesthesia by infiltration and peripheral nerve block.

Chloroprocaine (without preservatives):

Production of local anesthesia by infiltration and peripheral nerve block, as well as epidural and caudal administration; production of local anesthesia by subarachnoid block (spinal anesthesia) in adults (Clorotekal only).

Note: Due to chloroprocaine’s fast onset and short duration of action, it is most often used to establish adequate epidural anesthesia (eg, in a parturient prior to delivery) or possibly, for peripheral nerve block in a patient undergoing short (<60 minutes) ambulatory surgery that is not anticipated to produce significant postoperative pain (Alley 2014; Miller 2010).

Limitations of use: Nesacaine, Nesacaine-MPF: The manufacturer recommends against using either formulation (ie, with or without preservatives) for subarachnoid administration (ie, spinal anesthesia); however, the use of chloroprocaine without preservatives (Nesacaine-MPF) has been safely used off-label for spinal anesthesia (Goldblum 2013; Miller 2010; Yoos 2005). Do not use chloroprocaine with preservatives (Nesacaine) for epidural or spinal anesthesia.

Contraindications

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; septicemia.

Dosing: Adult

Local anesthesia: 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; Yoos 2005).

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:

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 for Cesarean delivery: Preservative free: 3%: 15 to 25 mL total dose (includes test dose of 2 or 3 mL) (Abboud 1983; Bjornestad 2006; Chestnut 2014; Feng 2012)

Lumbar epidural anesthesia, non-parturient: 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 every 40 to 50 minutes.

Dosing: Geriatric

Dosage should be reduced; refer to adult dosing.

Dosing: Pediatric

Local anesthesia: 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.

Children >3 years (normally developed) 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

Dosing: Renal Impairment

There are no dosage adjustments provided in the manufacturer’s labeling. Use with caution due to increased risk of adverse effects.

Dosing: Hepatic Impairment

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.

Administration

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. 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. 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).

Storage

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.

Drug Interactions

Alpha-/Beta-Agonists: Chloroprocaine may enhance the hypertensive effect of Alpha-/Beta-Agonists. 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. Liposomal bupivacaine may be administered 20 minutes or more after the administration of lidocaine, but the optimal duration of dose separation for other local anesthetics is unknown Avoid combination

Ergot Derivatives: Chloroprocaine may enhance the hypertensive effect of Ergot Derivatives. Monitor therapy

Hyaluronidase: May enhance the adverse/toxic effect of Local Anesthetics. Monitor therapy

Neuromuscular-Blocking Agents: Local Anesthetics may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents. Monitor therapy

Phenylephrine (Systemic): Chloroprocaine may enhance the hypertensive effect of Phenylephrine (Systemic). Monitor therapy

Sulfonamide Antibiotics: Chloroprocaine may diminish the therapeutic effect of Sulfonamide Antibiotics. Management: Avoid concurrent use of chloroprocaine and systemic sulfonamide-based antimicrobials whenever possible. 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. Monitor therapy

Adverse Reactions

>10%: Central nervous system: Procedural pain (16%)

1% to 10%:

Cardiovascular: Hypotension (5%)

Central nervous system: Headache (<2%)

Endocrine & metabolic: Hyperglycemia (<2%)

Gastrointestinal: Nausea (<2%)

Local: Injection site pain (4%)

Frequency not defined.

Cardiovascular: Bradycardia, syncope, ventricular arrhythmia

Central nervous system: Anxiety, dizziness, increased body temperature, loss of consciousness, restlessness

Dermatologic: Diaphoresis, erythema, pruritus, urticaria

Hypersensitivity: Anaphylactoid reaction, angioedema, hypersensitivity reaction

Neuromuscular & skeletal: Chondrolysis (continuous intra-articular administration)

Ophthalmic: Blurred vision

Otic: Tinnitus

Respiratory: Laryngeal edema, respiratory arrest, sneezing

<1% (Limited to important or life-threatening): Akathisia, anaphylaxis, arachnoiditis, auditory impairment, back pain, burning sensation, cardiac arrhythmia, cardiac insufficiency, cardiac arrest, cauda equine syndrome, diplopia, drowsiness, dysesthesia, dyspnea, erythema multiforme, fecal incontinence, feeling hot, groin pain, hypertension, hypoesthesia, limb pain, localized numbness (perineal; causing sexual dysfunction), malaise, motor dysfunction, myocardial depression, myoclonus, oral hypoesthesia, oral paresthesia, paresthesia, peripheral neuropathy, photophobia, presyncope, prolonged emergency from anesthesia, respiratory arrest, respiratory depression, seizure, sexual disorder, speech disturbance, spinal cord injury, tachycardia, tremor, urinary incontinence, urinary retention, visual disturbance, vomiting

Warnings/Precautions

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 2012]).

• 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 2012]).

• 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.

• 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.

• Renal impairment: Use with caution in patients with severe renal impairment.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

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.

• Elderly: 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 septicemia; 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.

Monitoring Parameters

Cardiovascular and respiratory status; mental status; vital signs; signs of CNS toxicity

Pregnancy Risk Factor

C

Pregnancy Considerations

Animal reproduction studies have not been conducted. Local anesthetics rapidly cross the placenta and may cause varying degrees of maternal, fetal, and neonatal toxicity. Close maternal and fetal monitoring (heart rate and electronic fetal monitoring advised) are required during obstetrical use. Maternal hypotension has resulted from regional anesthesia. Positioning the patient on her left side and elevating the legs may help. Epidural, paracervical, or pudendal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts. The use of some local anesthetic drugs during labor and delivery may diminish muscle strength and tone for the first day or two of life. Administration as a paracervical block is not recommended with toxemia of pregnancy, fetal distress, or prematurity. Administration of a paracervical block early in pregnancy has resulted in maternal seizures and cardiovascular collapse. Fetal bradycardia and acidosis also have been reported. Fetal depression has occurred following unintended fetal intracranial injection while administering a paracervical and/or pudendal block.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Have patient report immediately to prescriber severe nausea, vomiting, sneezing, sweating a lot, severe anxiety, fatigue, agitation, headache, change in speech, numbness or tingling in the mouth, tremors, severe dizziness, passing out, hearing impairment, tinnitus, depression, blurred vision, change in balance, seizures, bradycardia, tachycardia, abnormal heartbeat, angina, sexual dysfunction, urinary incontinence, fecal incontinence, back pain, severe injection site irritation, or blue-black skin discoloration (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

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