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Chloroprocaine

Pronunciation

(klor oh PROE kane)

Index Terms

  • Chloroprocaine Hydrochloride

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Solution, Injection, as hydrochloride:

Nesacaine: 1% (30 mL); 2% (30 mL) [contains disodium edta, methylparaben]

Generic: 2% (30 mL [DSC]); 3% (30 mL [DSC])

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 8-diethylaminoethanol (80% conjugated before elimination)

Excretion

Urine (minimal as unchanged drug in urine; metabolites: Cloro-aminobenzoic acid and 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)

Use: Labeled Indications

Local anesthesia: Production of local anesthesia by infiltration and peripheral nerve block (chloroprocaine with preservatives); production of local anesthesia by infiltration and peripheral and central nerve block, including lumbar and caudal epidural blocks (chloroprocaine without preservatives).

Limitations of use: Do not use chloroprocaine with or without preservatives for subarachnoid administration. Do not use chloroprocaine with preservatives for lumbar or caudal epidural anesthesia.

Contraindications

Hypersensitivity to chloroprocaine, other para aminobenzoic acid (PABA) ester type anesthetics, or any component of the formulation

Dosing: Adult

Injectable local anesthetic: 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 cardiac disease.

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 block: 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

Injectable local anesthetic: 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 cardiac 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.

Reconstitution

Dilute with NS. To prepare 1:200,000 epinephrine-chloroprocaine injection, add 0.1 mL of a 1 mg/mL epinephrine injection to 20 mL of preservative free chloroprocaine.

Administration

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.

Storage

Store at 20°C to 25°C (68°F to 77°F) in original container; protect from freezing. Protect from light. Discard 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.

Drug Interactions

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

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

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

Frequency not defined.

Cardiovascular: Bradycardia, hypotension, ventricular arrhythmia

Central nervous system: Anxiety, dizziness, loss of consciousness, restlessness

Dermatologic: Erythema, pruritus, urticaria

Hypersensitivity: Anaphylactoid reaction, angioedema, hypersensitivity reaction

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

Ophthalmic: Blurred vision

Otic: Tinnitus

<1% (Limited to important or life-threatening): Seizure (0.1%)

Warnings/Precautions

Concerns related to adverse effects:

• 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. Treatment is primarily symptomatic and supportive. Use extreme caution in patients with existing neurological disease.

• 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 arrest: Local anesthetics have been associated with rare occurrences of sudden respiratory arrest.

• Seizures: Convulsions due to systemic toxicity leading to cardiac arrest have also been reported, presumably following unintentional intravascular injection.

Disease-related concerns:

• Cardiovascular disease: Use extreme caution in patients with severe hypertension; use with caution in patients with impaired cardiovascular function, including hypotension or heart block.

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• Myasthenia gravis: Use with extreme caution in patients with myasthenia gravis; may cause significant weakness (Haroutiunian 2009).

• Septicemia: Use extreme caution in patients with septicemia.

• Spinal deformities: Use extreme caution in patients with spinal deformities.

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.

Dosage form specific issues:

• Preservative-containing solutions: Do not use solutions containing preservatives for lumbar or caudal epidural anesthesia.

Other warnings/precautions:

• Administration: 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.

• Test dose: A test dose is recommended prior to epidural administration (prior to initial dose) and all reinforcing doses with continuous catheter technique.

• 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?)

• Patient may experience injection site irritation. Have patient report immediately to prescriber severe nausea, severe vomiting, sneezing, sweating a lot, severe anxiety, fatigue, agitation, tremors, severe dizziness, passing out, tinnitus, change in balance, seizures, bradycardia, arrhythmia, angina, vision changes, eye pain, eye irritation, weakness, numbness or tingling, severe skin irritation, mood changes, confusion, or blue-black skin coloration (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 healthcare 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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