Chloroprocaine Hydrochloride (Monograph)

Drug class: Local Anesthetics

Medically reviewed by Drugs.com on Jun 10, 2024. Written by ASHP.

Introduction

Chloroprocaine hydrochloride is a short-acting local anesthetic of the ester type.

Uses for Chloroprocaine Hydrochloride

Chloroprocaine hydrochloride is used for infiltration anesthesia, and for peripheral, sympathetic, and epidural (including caudal) block anesthesia. Chloroprocaine hydrochloride solutions containing a preservative should not be used for caudal or epidural anesthesia. The drug is not used for spinal anesthesia. Chloroprocaine hydrochloride is not effective as a topical anesthetic.

Chloroprocaine Hydrochloride Dosage and Administration

Chloroprocaine hydrochloride may be administered by infiltration and by epidural (including caudal) block or by peripheral or sympathetic nerve block. Local anesthetics, including chloroprocaine hydrochloride, have been administered by continuous intra-articular infusion^{† [off-label]} (e.g., for control of postoperative pain); however, such use has been associated with chondrolysis. Chloroprocaine hydrochloride solutions containing preservatives should not be used for epidural or caudal block. Partially used bottles of solutions which do not contain preservatives should be discarded.

Aspiration for blood should be performed prior to injection of chloroprocaine hydrochloride to avoid intravascular administration; however, a negative aspiration does not ensure protection against inadvertent intravascular injection.

Local anesthetics should only be administered by clinicians who are experienced in the diagnosis and management of dose-related toxicities and other acute emergencies associated with these agents. Resuscitative equipment, oxygen, drugs, and personnel required for treatment of adverse reactions should be immediately available when chloroprocaine is administered. For specific procedures and techniques of administration, specialized references should be consulted.

Dosage of chloroprocaine hydrochloride varies with the anesthetic procedure, the degree of anesthesia required, and individual patient response. The usual dosages should generally be reduced in young, geriatric, or debilitated patients and in patients with cardiac and/or hepatic disease. The smallest dose and lowest concentration required to produce the desired effect should be used. Single adult doses of chloroprocaine hydrochloride (without epinephrine) should not exceed 800 mg. When administered with epinephrine (1:200,000), chloroprocaine hydrochloride doses should not exceed 1 g. The maximum dose in pediatric patients varies depending on age and weight. In children older than 3 years of age who have normal lean body mass and normal body development, a maximum dose of 11 mg/kg is recommended. Chloroprocaine hydrochloride concentrations of 0.5–1% for infiltration and 1–1.5% for nerve block are suggested in pediatric patients. It may be necessary to dilute commercially available concentrations with 0.9% sodium chloride injection to obtain the desired lower concentrations for use in infants and smaller children. A 1:200,000 epinephrine/chloroprocaine hydrochloride solution may be prepared by adding 0.1 mL of 1:1000 epinephrine hydrochloride injection to 20 mL of a 2 or 3% chloroprocaine hydrochloride solution that does not contain a preservative. Solutions containing epinephrine should not be used for interdigital block.

Solutions of 2 or 3% chloroprocaine hydrochloride with or without epinephrine and containing no preservatives are used for epidural or caudal anesthesia. To prevent intravascular or subarachnoid injection of a large epidural dose of anesthetic solution, a test dose (approximately 3 mL of a 3% solution or 5 mL of a 2% solution) should be injected prior to administering the total dose. When clinical conditions permit, use of a test dose solution that contains epinephrine should be considered to detect inadvertent intravascular injection. When a continuous block technique is used, a portion of each supplemental dose should be administered as a test dose to ensure that the catheter has not been displaced. At least 5 minutes should elapse after each test dose before proceeding further. Injection of a large, single dose through a catheter should be avoided; instead, the drug should be administered in fractional doses. If a large volume of the drug is inadvertently injected into the subarachnoid space, consideration should be given to withdrawing a moderate volume (e.g., 10 mL) of cerebrospinal fluid through the catheter after appropriate resuscitation and if the catheter is in place to attempt recovery of the drug. For epidural anesthesia in the lumbar region, 2–2.5 mL of a 2 or 3% solution (40–75 mg) may be given for each segment. The usual total volume is 15–25 mL (300–750 mg). Repeat doses which are 2–6 mL less than the initial dose may be given at 40- to 50-minute intervals. For caudal anesthesia, the initial dose is 15–25 mL of a 2 or 3% solution (300–750 mg) of chloroprocaine hydrochloride. Repeat doses may be given at 40- to 60-minute intervals.

For infiltration or nerve block anesthesia, 1 or 2% chloroprocaine hydrochloride solutions may be employed. The following doses of chloroprocaine hydrochloride have been suggested for various nerve blocks in the average adult: mandibular nerve block, 2–3 mL of a 2% solution (40–60 mg); infraorbital nerve block, 0.5–1 mL of a 2% solution (10–20 mg); brachial plexus block, 30–40 mL of a 2% solution (600–800 mg); and interdigital block, 3–4 mL of a 1% solution without epinephrine (30–40 mg). In obstetrical anesthesia, the following doses have been suggested for nerve blocks: pudendal block, 10 mL of a 2% solution (200 mg) for each side; and for paracervical block, 3 mL of a 1% solution (30 mg) per each of 4 sites.

Standardize 4 Safety

Standardized concentrations for epidural chloroprocaine have been established through Standardize 4 Safety (S4S), a national patient safety initiative to reduce medication errors, especially during transitions of care. Because recommendations from the S4S panels may differ from the manufacturer’s prescribing information, caution is advised when using concentrations that differ from labeling, particularly when using rate information from the label. For additional information on S4S (including updates that may be available), see [Web].

Cautions for Chloroprocaine Hydrochloride

Chloroprocaine hydrochloride shares the toxic potentials of local anesthetics, and the usual precautions of local anesthetic therapy should be observed.

Chloroprocaine Hydrochloride Pharmacokinetics

The onset and duration of action of chloroprocaine are somewhat shorter than those of procaine. Depending on the dose and site of injection, 1 or 2% chloroprocaine hydrochloride solutions without epinephrine produce anesthesia in 6–12 minutes and duration of action is 30–60 minutes. Addition of epinephrine 1:200,000 prolongs duration of action to 60–90 minutes.

Chloroprocaine is hydrolyzed by plasma pseudocholinesterases more rapidly than is procaine. The drug is excreted by the kidneys, chiefly as diethylaminoethanol and 2-chloro-4-aminobenzoic acid.

Chemistry and Stability

Chemistry

Chloroprocaine hydrochloride is a local anesthetic of the ester type with a short duration of action. The drug differs structurally from procaine hydrochloride only in the presence of a chlorine atom on the benzene ring. Chloroprocaine hydrochloride occurs as a white, crystalline powder and is soluble in water and slightly soluble in alcohol. Commercially available solutions of chloroprocaine hydrochloride have a pH of 2.7–4.

Stability

Chloroprocaine hydrochloride injections should be stored at 20–25°C; freezing should be avoided. If chloroprocaine hydrochloride injection is stored at low temperatures, crystallization may occur; crystals will redissolve when the solution reaches room temperature. Solutions containing undissolved material should not be used.

Solutions of chloroprocaine hydrochloride may become discolored after prolonged exposure to light and should be protected from direct sunlight. Discolored solutions should never be administered.

Chloroprocaine hydrochloride is incompatible with alkali hydroxides and their carbonates, soaps, silver salts, iodine, and iodides.

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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