Chloroprocaine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

North America

Canada: Nesacaine; USA: Nesacaine.

Drug combinations

Chemistry

Chloroprocaine Hydrochloride: C~13~H~20~Cl~2~N~2~O~2~. Mw: 307.22. (1) 2-diethylaminoethyl 4-amino-2-chlorobenzoate hydrochloride; (2) Benzoic acid, 4-amino-2-chloro-2-(diethylamino) ethyl ester, monohydrochloride. CAS – 3858-89-7.

Pharmacologic Category

Local Anesthetics. (ATC-Code: N01BA04).

Mechanism of action

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. Local anesthetics, including chloroprocaine, reversibly prevent 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.

Therapeutic use

Infiltration anesthesia, peripheral nerve block, epidural anesthesia.

Pregnancy and lactiation implications

Chloroprocaine should be given to a pregnant woman only if clearly needed. This does not preclude the use of chloroprocaine at term for the production of obstetrical anesthesia. 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. 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 have also been reported. Fetal depression has occurred following unintended fetal intracranial injection while administering a paracervical and/or pudendal block. Caution should be exercised when chloroprocaine is administered to a nursing woman.

Unlabeled use

Contraindications

Hypersensitivity to chloroprocaine, other ester-type anesthetics, or any component of the formulation; myasthenia gravis; do not use for subarachnoid administration. Lumbar and caudal epidural anesthesia should be used with extreme caution in persons with the following conditions: existing neurological disease, spinal deformities, septicemia, and severe hypertension.

Warnings and precautions

Intra-articular infusions of local anesthetics following arthroscopic and other surgical procedures is an unapproved use, and there have been post-marketing reports of chondrolysis in patients receiving such infusions. CNS toxicity has been observed (constant monitoring of the patient’s state of consciousness should be performed 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). Respiratory arrest reported. Convulsions due to systemic toxicity leading to cardiac arrest have also been reported, presumably following unintentional intravascular injection. Use with caution in patients with cardiovascular disease, compromised blood supply or with hepatic impairment. Use with caution in acutely ill, debilitated patients, elderly or children (reduce dose consistent with age and physical status). Do not use solutions containing preservatives for caudal or epidural block. Intravascular injections should be avoided. A test dose is recommended prior to epidural administration (prior to initial dose) and all reinforcing doses with continuous catheter technique. 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.

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