The safety and effective use of chloroprocaine depend on proper dosage, correct
technique, adequate precautions and readiness for emergencies. Resuscitative
equipment, oxygen and other resuscitative drugs should be available for immediate
use (see WARNINGS and ADVERSE REACTIONS).
The lowest dosage that results in effective anesthesia should be used to avoid
high plasma levels and serious adverse effects. Injections should be made slowly,
with frequent aspirations before and during the injection to avoid intravascular
injection. Syringe aspirations should also be performed before and during each
supplemental injection in continuous (intermittent) catheter techniques. During
the administration of epidural anesthesia, it is recommended that a test dose
be administered (3 mL of 3% or 5 mL of 2% Nesacaine (chloroprocaine) -MPF Injection) initially
and that the patient be monitored for central nervous system toxicity and cardiovascular
toxicity, as well as for signs of unintended intrathecal administration, before
proceeding. When clinical conditions permit, consideration should be given to
employing a chloroprocaine solution that contains epinephrine for the test dose
because circulatory changes characteristic of epinephrine may also serve as
a warning sign of unintended intravascular injection. An intravascular injection
is still possible even if aspirations for blood are negative. With the use of
continuous catheter techniques, it is recommended that a fraction of each supplemental
dose be administered as a test dose in order to verify proper location of the
Injection of repeated doses of local anesthetics may cause significant increases in plasma levels with each repeated dose due to slow accumulation of the drug or its metabolites. Tolerance to elevated blood levels varies with the physical condition of the patient. Debilitated, elderly patients, acutely ill patients, and children should be given reduced doses commensurate with their age and physical status. Local anesthetics should also be used with caution in patients with hypotension or heart block.
Careful and constant monitoring of cardiovascular and respiratory (adequacy of ventilation) vital signs and the patient's state of consciousness should be accomplished after each local anesthetic injection. It should be kept in mind at such times that restlessness, anxiety, tinnitus, dizziness, blurred vision, tremors, depression or drowsiness may be early warning signs of central nervous system toxicity.
Local anesthetic injections containing a vasoconstrictor should be used cautiously and in carefully circumscribed quantities in areas of the body supplied by end arteries or having otherwise compromised blood supply. Patients with peripheral vascular disease and those with hypertensive vascular disease may exhibit exaggerated vasoconstrictor response. Ischemic injury or necrosis may result.
Since ester-type local anesthetics are hydrolyzed by plasma cholinesterase produced by the liver, chloroprocaine should be used cautiously in patients with hepatic disease. Local anesthetics should also be used with caution in patients with impaired cardiovascular function since they may be less able to compensate for functional changes associated with the prolongation of A-V conduction produced by these drugs.
Use in Ophthalmic Surgery: When local anesthetic injections are
employed for retrobulbar block, lack of corneal sensation should not be relied
upon to determine whether or not the patient is ready for surgery. This is because
complete lack of corneal sensation usually precedes clinically acceptable external
ocular muscle akinesia.
Carcinogenesis, Mutagenesis, and Impairment of Fertility
Long-term studies in animals to evaluate carcinogenic potential and reproduction
studies to evaluate mutagenesis or impairment of fertility have not been conducted
Pregnancy: Category C
Animal reproduction studies have not been conducted with chloroprocaine. It is also not known whether chloroprocaine can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. 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.
Labor and Delivery
Local anesthetics rapidly cross the placenta, and when used for epidural, paracervical,
pudendal or caudal block anesthesia, can cause varying degrees of maternal,
fetal and neonatal toxicity (see CLINICAL PHARMACOLOGY and Pharmacokinetics).
The incidence and degree of toxicity depend upon the procedure performed, the type and amount of drug used, and the technique of drug administration. Adverse reactions in the parturient, fetus and neonate involve alterations of the central nervous system, peripheral vascular tone and cardiac function.
Maternal hypotension has resulted from regional anesthesia. Local anesthetics produce vasodilation by blocking sympathetic nerves. Elevating the patient's legs and positioning her on her left side will help prevent decreases in blood pressure. The fetal heart rate also should be monitored continuously, and electronic fetal monitoring is highly advisable.
Epidural, paracervical, or pudendal anesthesia may alter the forces of parturition
through changes in uterine contractility or maternal expulsive efforts. In one
study, paracervical block anesthesia was associated with a decrease in the mean
duration of first stage labor and facilitation of cervical dilation. However,
epidural anesthesia has also been reported to prolong the second stage of labor
by removing the parturient's reflex urge to bear down or by interfering with
motor function. The use of obstetrical anesthesia may increase the need for
The use of some local anesthetic drug products during labor and delivery may be followed by diminished muscle strength and tone for the first day or two of life. The long-term significance of these observations is unknown.
Careful adherence to recommended dosage is of the utmost importance in obstetrical paracervical block. Failure to achieve adequate analgesia with recommended doses should arouse suspicion of intravascular or fetal intracranial injection. Cases compatible with unintended fetal intracranial injection of local anesthetic injection have been reported following intended paracervical or pudendal block or both. Babies so affected present with unexplained neonatal depression at birth which correlates with high local anesthetic serum levels and usually manifest seizures within six hours. Prompt use of supportivemeasures combined with forced urinary excretion of the local anesthetic has been used successfully to manage this complication.
Case reports of maternal convulsions and cardiovascular collapse following use of some local anesthetics for paracervical block in early pregnancy (as anesthesia for elective abortion) suggest that systemic absorption under these circumstances may be rapid. The recommended maximum dose of each drug should not be exceeded. Injection should be made slowly and with frequent aspiration. Allow a 5-minute interval between sides.
There are no data concerning use of chloroprocaine for obstetrical paracervical block when toxemia of pregnancy is present or when fetal distress or prematurity is anticipated in advance of the block; such use is, therefore, not recommended.
The following information should be considered by clinicians who select chloroprocaine for obstetrical paracervical block anesthesia:
- Fetal bradycardia (generally a heart rate of less than 120 per minute for
more than 2 minutes) has been noted by electronic monitoring in about 5 to
10 percent of the cases (various studies) where initial total doses of 120
mg to 400 mg of chloroprocaine were employed. The incidence of bradycardia,
within this dose range, might not be dose related.
- Fetal acidosis has not been demonstrated by blood gas monitoring around
the time of bradycardia or afterwards. These data are limited and generally
restricted to non-toxemic cases where fetal distress or prematurity was not
anticipated in advance of the block.
- No intact chloroprocaine and only trace quantities of a hydrolysis product,
2-chloro-4-aminobenzoic acid, have been demonstrated in umbilical cord arterial
or venous plasma following properly administered paracervical block with chloroprocaine.
- The role of drug factors and non-drug factors associated with fetal bradycardia
following paracervical block are unexplained at this time.
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when chloroprocaine is administered to a nursing woman.
Guidelines for the administration of Nesacaine (chloroprocaine) and Nesacaine (chloroprocaine) -MPF Injections
to children are presented in DOSAGE AND ADMINISTRATION.
Clinical studies of Nesacaine (chloroprocaine) and Nesacaine (chloroprocaine) -MPF did not include sufficient numbers of subjects 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
This drug and its metabolites are known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection and it may be useful to monitor renal function.