Chloroprocaine

Chloroprocaine is a local anesthetic indicated for subarachnoid block, central nerve block, infiltration, and peripheral nerve block.

• Chloroprocaine is available under the following different brand names: Nesacaine, Clorotekal

Common side effects of Chloroprocaine include:

• restlessness
• anxiety
• dizziness or fainting
• ringing in the ears
• blurred vision
• tremors
• heart problems
• allergic reactions (such as rash, itching, redness, swelling of the throat, sneezing)
• nausea
• vomiting
• excessive sweating
• elevated temperature
• low blood pressure
• loss of bladder and bowel control
• loss of sexual function

Serious side effects of Chloroprocaine include:

• shallow, irregular breathing
• chest pain
• fast, irregular, or slow heartbeat
• pain near the injection site
• seizures
• shakiness
• shortness of breath

Rare side effects of Chloroprocaine include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Solution, injection for nerve block

• 1% (Nesacaine)
• 2% (Nesacaine, Nesacaine MPF [preservative free])
• 3% (Nesacaine MPF)

Solution, intrathecal injection

• 10 mg/mL (Clorotekal)
• Supplied as 50 mg/5 mL Chloroprocaine HCl (equivalent to 44.05 mg/5 mL [8.81 mg/mL] Chloroprocaine)

Subarachnoid block

Adult dosage

• To obtain an effective block to the T-10 level with 1 single administration in an adult of average height and weight (approximately 70 kg), the recommended dose is 50 mg
• Doses above 50 mg have not been adequately tested for efficacy and safety

Central nerve block

Adult dosage

• Nesacaine-MPF 2% and 3% injection in single-dose vials without a preservative indicated for production of local anesthesia by the central nerve block, including lumbar and caudal epidural blocks
• Caudal block, 2% to 3% solution: 15 to 25 mL initially; repeat doses may be given at 40 to 60 min intervals
• Lumbar epidural, 2% to 3% solution: 2 to 2.5 mL per segment; usual total volume is 15 to 25 mL; repeat doses of 2 to 6 mL less than the original dose may be given at 40 to 50 min intervals

Infiltration & peripheral nerve block

Adult dosage

• Nesacaine or Nesacaine-MPF 1%-2% total doses
• Mandibular (2% solution): 40 to 60 mg (2 to 3 mL)
• Infraorbital (2% solution): 10 to 20 mg (0.5 to 1 mL)
• Brachial plexus (2% solution): 600 to 800 mg (30 to 40 mL)
• Digital, without epinephrine (1% solution): 30 to 40 mg (3 to 4 mL)
• Pudendal (2% solution): 400 mg (10 mL on each side)
• Paracervical (1% solution): up to 120 mg (3 mL per each of 4 sites)
• Single doses should not exceed 800 mg; single dose with epinephrine should not exceed 1000 mg
• Cervical/thoracic region: 30-60 mg for each segment to be anesthetized

Infiltration

Pediatric dosage

• Children younger than 3 years
• Safety and efficacy not established
• Children aged 3 years and older
• 0.5%-1% concentration recommended; not to exceed 11 mg/kg

Nerve block

Pediatric dosage

• Children younger than 3 years
  • Safety and efficacy not established
• Children aged 3 years and older
  • 1%-1.5% concentration recommended; not to exceed 11 mg/kg

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Chloroprocaine has severe interactions with the following drug:
  • bupivacaine liposome
• Chloroprocaine has serious interactions with the following drug:
  • bupivacaine implant
• Chloroprocaine has moderate interactions with the following drugs:
  • hyaluronidase
  • nadolol
  • pindolol
  • propranolol
  • timolol
• Chloroprocaine has minor interactions with no other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Hypersensitivity to para-aminobenzoic acid (PABA) or parabens
• 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
• General and specific contraindications to spinal anesthesia regardless of the local anesthetic use, should be considered (eg, decompensated cardiac insufficiency, hypovolemic shock, coagulopathy)
• IV regional anesthesia (the anesthetic agent is introduced into the limb and allowed to set in while tourniquets retain the agent within the desired area)
• Serious problems with cardiac conduction
• Local infection at the site of the proposed lumbar puncture
• Septicemia

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Chloroprocaine?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Chloroprocaine?”

Cautions

• Local anesthetics should only be administered by clinicians who are well versed in diagnosis and management of dose-related toxicity and other acute emergencies that might arise from the block to be employed, and then only after ensuring 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
• Hypotension and bradycardia are well-known side effects of all local anesthetics
• Neurological damage may occur after spinal anesthesia, manifesting as paresthesia, loss of sensitivity, motor weakness, paralysis, and cauda equina syndrome; occasionally these symptoms persist and can be permanent
• Use extreme caution with lumbar and caudal epidural anesthesia in people with existing neurological disease, spinal deformities, septicemia, severe hypertension, heart block, high-grade cardiac decompensation, advanced liver or kidney impairment, elderly patients and patients in poor general condition, genetic cholinesterase deficiency, severe anemia, congenital or acquired bleeding disorder, and patients taking anticoagulants
• Use preservative-free preparations for spinal or epidural anesthesia
• Do not use solutions with epinephrine in distal areas of the body (eg, digit, nose, ear)
• The addition of vasoconstrictor, epinephrine, will promote local hemostasis, decrease systemic absorption, and increase the duration of action
• Monitor the patient's state of consciousness following the injection; anxiety, dizziness, restlessness, tremors, depression, or blurred vision may be signs of CNS toxicity
• Chondrolysis associated with intra-articular infusions following arthroscopic and other surgical procedures (off-label use)
• Hypersensitivity reactions reported; cross-reactivity among ester-type local anesthetics may occur
• Respiratory arrest reported with local anesthetics
• Methemoglobinemia
  • Use of local anesthetics may cause methemoglobinemia, a serious condition that must be treated promptly; patients with glucose-6-phosphate dehydrogenase deficiency, congenital or idiopathic methemoglobinemia, cardiac or pulmonary compromise, infants under 6 months of age, and concurrent exposure to oxidizing agents or their metabolites are more susceptible to developing clinical manifestations of the condition
  • Advise patients or caregivers to seek immediate medical attention if the patient experiences the following signs or symptoms: pale, gray, or blue-colored skin (cyanosis), headache, rapid heart rate, shortness of breath, light-headedness, or fatigue; discontinue Bicillin C-R and any other oxidizing agents; depending on the severity of signs and symptoms, patients may respond to supportive care, including oxygen therapy and hydration; a more severe clinical presentation may require treatment with methylene blue, exchange transfusion, or hyperbaric oxygen

Pregnancy and Lactation

• Data are limited regarding use in pregnant women
• Labor or delivery
  • Local anesthetics appear to cross the placenta by passive diffusion; however, the rate and degree of diffusion vary considerably among the different drugs as governed by: (1) the degree of plasma protein binding, (2) the degree of ionization, and (3) the degree of lipid solubility
  • Fetal/maternal ratios of local anesthetics appear to be inversely related to the degree of plasma protein binding as only the free, unbound drug is available for placental transfer
  • 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
  • Obstetrical anesthesia may increase the need for forceps assistance
  • Maternal hypotension has resulted from regional anesthesia; local anesthetics produce vasodilation by blocking sympathetic nerves
  • Fetal heart rate also should be monitored continuously, and electronic fetal monitoring is highly advisable
• Lactation
  • Data are not available on the presence of chloroprocaine in human milk and its effects on the breastfed infant or milk production
  • The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed child from the drug or any underlying maternal condition