Included as part of the "PRECAUTIONS" Section
Risks With Neuraxial Administration
Local anesthetics should only be administered by clinicians who are well versed in diagnosis and
management of dose-related toxicity and other acute emergencies which might arise from the
block to be employed, and then only after insuring the immediate availability of oxygen, other
resuscitative drugs, cardiopulmonary resuscitative equipment, and the personnel resources
needed for proper management of toxic reactions and related emergencies [see ADVERSE REACTIONS and OVERDOSE]. Delay in proper management of dose-related toxicity,
underventilation from any cause and/or altered sensitivity may lead to the development of
acidosis, cardiac arrest, and, possibly, death.
The clinician should take the appropriate measures to avoid an intravascular injection [see
DOSAGE AND ADMINISTRATION]. In addition, it is essential for the clinician to know how to recognize and
treat undesirable effects, systemic toxicity and other complications. If signs of acute systemic
toxicity or total spinal block are observed, the injection of the local anesthetic must be stopped
immediately [see OVERDOSE].
Cardiovascular System Reactions
Hypotension and bradycardia are well known side effects of all local anesthetics [see ADVERSE REACTIONS and OVERDOSE].
A serious, undesirable effect of spinal anesthesia is high or total spinal block, with consequent
cardiovascular and respiratory depression. Cardiovascular depression is induced by an extended
block of the sympathetic nervous system, which may induce severe hypotension and bradycardia
to the point of cardiac arrest. Respiratory depression is induced by the block of the respiratory
musculature and the diaphragm. Careful and constant monitoring of cardiovascular and
respiratory (adequacy of ventilation) vital signs and the patient’s state of consciousness should
be accomplished after CLOROTEKAL injection.
Patients over 65 years, particularly those with hypertension, may be at increased risk for
experiencing the hypotensive effects of CLOROTEKAL. Blood pressure should, therefore, be
carefully monitored after CLOROTEKAL injection. Hypotension may be controlled by
vasoconstrictors in dosages depending on the severity of hypotension and response of treatment.
Central Nervous System Reactions
Neurological damage may occur after spinal anesthesia, manifesting as paresthesia, loss of
sensitivity, motor weakness, paralysis, cauda equina syndrome. Occasionally these symptoms
persist and can be permanent. Carefully evaluate patients with underlying neuromuscular
disorders and consider the risk-benefit ratio prior to treatment.
Carefully and constantly monitor cardiovascular and respiratory (adequacy of ventilation) vital
signs and the patient’s state of consciousness after local anesthetic injection. Restlessness,
headache, anxiety, incoherent speech problems, lightheadedness, paresthesia, numbness and
tingling of the mouth and lips, hearing problems, tinnitus, dizziness, blurred vision, convulsions,
loss of consciousness tremors, depression, or drowsiness may be early warning signs of central
nervous system toxicity [see ADVERSE REACTIONS and OVERDOSE].
Risk Of Hypersensitivity Reactions
CLOROTEKAL is contraindicated in patients hypersensitive to drugs of the PABA ester group.
Allergic type reactions may occur as a result of sensitivity to the local anesthetic or to other
formulation ingredients. These reactions are characterized by signs such as urticaria, pruritus,
erythema, angioneurotic edema (including laryngeal edema), tachycardia, sneezing, nausea,
vomiting, dizziness, syncope, excessive sweating, elevated temperature, and possibly,
anaphylaxis type symptomatology (including severe hypotension). Cross sensitivity among
members of the ester-type local anesthetic group has been reported. The usefulness of screening
for sensitivity has not been definitely established [see ADVERSE REACTIONS].
Risk Of Chondrolysis In Patients Receiving Intraarticular Injections
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. The majority of reported cases of chondrolysis have involved the
shoulder joint; cases of gleno-humeral chondrolysis have been described in pediatric and adult
patients following intra-articular infusions of local anesthetics with and without epinephrine for
periods of 48 to 72 hours. There is insufficient information to determine whether shorter infusion
periods are not associated with these findings. The time of onset of symptoms, such as joint pain,
stiffness, and loss of motion, can be variable, but may begin as early as the 2nd month after
surgery. Currently, there is no effective treatment for chondrolysis. Patients who experienced
chondrolysis have required additional diagnostic and therapeutic procedures and some required
arthroplasty or shoulder replacement.
Conditions Requiring Special Attention
Some patients require special attention in order to reduce the risk of serious undesirable effects,
even when locoregional anesthesia constitutes the optimum choice for the surgical intervention:
- Patients with total or partial heart block, since local anesthetics can suppress myocardial
- Patients with high grade cardiac decompensation
- Patients with advanced liver or kidney damage [see Use In Specific Populations]
- Elderly patients and patients in poor general condition [see Use In Specific Populations
and CLINICAL PHARMACOLOGY]
- Patients with genetic deficiency of plasma cholinesterase [see ADVERSE REACTIONS and CLINICAL PHARMACOLOGY]
- Patients taking anticoagulants or with congenital or acquired bleeding disorder
- Patients with severe anemia
Because ester-type local anesthetics are hydrolyzed by plasma cholinesterase produced by the
liver, use CLOROTEKAL cautiously in patients with advanced hepatic disease [see Use In Specific Populations].
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.
Carcinogenesis, Mutagenesis, Impairment Of Fertility
Long-term studies in animals to evaluate carcinogenic potential of chloroprocaine have not been
2-chloroprocaine and the main metabolite, ACBA, were negative in the in vitro bacterial reverse
mutation test (Ames assay) and the in vitro chromosome aberrations assay.
Impairment Of Fertility
Studies in animals to evaluate the impairment of fertility have not been conducted with
Use In Specific Populations
The limited available data with chloroprocaine use in pregnant women are insufficient to inform
a drug associated risk of adverse developmental outcomes. There are no animal reproduction
studies for chloroprocaine. There are risks to the mother and the fetus associated with use of
chloroprocaine during labor and delivery (see Clinical Considerations).
The estimated background risk of major birth defects and miscarriage for the indicated
population is unknown. All pregnancies have a background risk of birth defect, loss, or other
adverse outcomes. In the U.S. general population, the estimated background risk of major birth
defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%,
Labor or 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]. 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.
Spinal anesthesia may alter the forces of parturition through changes in uterine contractility or
maternal expulsive efforts. Spinal 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 forceps assistance.
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.
Maternal hypotension has resulted from regional anesthesia. Local anesthetics produce
vasodilation by blocking sympathetic nerves. The fetal heart rate also should be monitored
continuously, and electronic fetal monitoring is highly advisable.
There are no data on the presence of chloroprocaine in human milk, the effects on the breastfed
infant, or the effects on milk production.
The developmental and health benefits of breastfeeding should be considered along with the
mother’s clinical need for CLOROTEKAL and any potential adverse effects on the breastfed
infant from CLOROTEKAL or from the underlying maternal condition.
Safety and effectiveness in pediatric patient have not been established.
Patients over 65 years, particularly those with hypertension, may be at increased risk of
developing hypotension while undergoing spinal anesthesia with CLOROTEKAL.
Clinical studies of CLOROTEKAL 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 an elderly patient will have greater frequency of decreased hepatic, renal, or cardiac
function, and of concomitant disease or other drug therapy [see WARNINGS AND PRECAUTIONS
and CLINICAL PHARMACOLOGY].
Hepatic And Renal Impairment
Since ester-type local anesthetics are hydrolyzed by plasma cholinesterase produced by the liver,
the risk of toxic reactions might be greater in patients with advanced hepatic disease [see CLINICAL PHARMACOLOGY].
This drug and its metabolites are known to be substantially excreted by the kidney, and the risk
of toxic reactions might be greater in patients with impaired renal function [see CLINICAL PHARMACOLOGY].