Chloroprocaine

Pronunciation: klor-oh-PROE-kane
Class: Local anesthetic

Trade Names

Chloroprocaine
- Injection 2%
- Injection 3%

Nesacaine
- Injection 1%
- Injection 2%

Nesacaine-MPF
- Injection 2%
- Injection 3%

Pharmacology

Stabilizes neuronal membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses, thereby effecting local anesthetic action.

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Pharmacokinetics

Distribution

Crosses the placenta by passive diffusion; distributed to some extent to all body systems, with high concentrations found in highly perfused organs, such as the liver, lungs, heart, and brain.

Metabolism

Rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase.

Elimination

Excreted by the kidney. The plasma half-life in adults is approximately 21 sec for men and 25 sec for women.

Onset

6 to 12 min.

Duration

Up to 60 min.

Special Populations

Pharmacokinetic parameters can be significantly altered.

Pharmacokinetic parameters can be significantly altered.

Pharmacokinetic parameters can be significantly altered.

The plasma half-life in neonates is approximately 43 sec.

Indications and Usage

Production of local anesthesia by infiltration and peripheral nerve block.

Contraindications

Hypersensitivity to drugs of the PABA ester group.

Dosage and Administration

IV 15 to 25 mL of chloroprocaine 2% or 3% solution without preservatives. Repeated doses may be given at 40- to 60-min intervals.

IV 30 to 40 mL (600 to 800 mg) as chloroprocaine 2% solution with or without preservatives.

IV 3 to 4 mL (30 to 40 mg) as chloroprocaine 1% solution with or without preservatives (without epinephrine).

IV 0.5 to 1 mL (10 to 20 mg) as chloroprocaine 2% solution with or without preservative.

IV 2 to 3 mL (40 to 60 mg) as chloroprocaine 2% solution with or without preservatives.

IV 3 mL per each of 4 sites as chloroprocaine 1% solution without preservatives; total dose, up to 120 mg.

IV 10 mL, 1 each side as chloroprocaine 2% solution with or without preservative; total dose, 400 mg.

IV Use concentrations of 0.5% to 1%.

IV Use concentrations of 1% to 1.5%.

IV 2 to 2.5 mL per segment of chloroprocaine 2% or 3% solution without preservatives. The usual total volume is from 15 to 25 mL. Repeated doses 2 to 6 mL less than the original dose may be given at 40- to 50-min intervals.

Reduce dosage for elderly.

Reduce dosage for patients with liver disease.

Reduce dosage in cardiac, debilitated, and acutely ill patients.

General Advice

• Administer as a single injection or continuously through an indwelling catheter. Do not use for subarachnoid administration.
• Avoid rapid injection; use fractional doses when feasible.
• In adults, max single dose without epinephrine is 11 mg/kg, not to exceed a max total dose of 800 mg. Max single dose with epinephrine is 14 mg/kg, not to exceed a max total dose of 1,000 mg.
• In children, max dose is 11 mg/kg (without epinephrine) determined by the child's age and body weight. This max dose is for children who have a healthy lean body mass and healthy body weight.
• Use an adequate test dose (3 mL of chloroprocaine 3% without preservatives or 5 mL of chloroprocaine 2% without preservatives) prior to induction of complete block. Repeat this test dose if the patient is moved in such a fashion as to have displaced the epidural catheter. Allow adequate time for onset of anesthesia following administration of each test dose.
• To prepare a 1:200,000 epinephrine-chloroprocaine injection, add 0.1 mL of 1:1,000 epinephrine to 20 mL of chloroprocaine without preservatives.
• Chloroprocaine is incompatible with caustic alkalis and their carbonates, soaps, silver salts, and iodides.
• Do not administer if particulate matter, cloudiness, or discoloration noted.
• To avoid intravascular administration, aspirate injection site before anesthetic solution is injected.
• Do not use anesthetic solutions containing preservatives for lumbar or caudal anesthesia.

Storage/Stability

Store at 68° to 77°F. Keep from freezing and protect from light. Discard unused chloroprocaine without preservatives remaining in vial.

Drug Interactions

Do not use vasopressors in the presence of ergot-type oxytocic drugs because severe, persistent hypertension or cerebrovascular accidents may occur.

The PABA metabolite of chloroprocaine inhibits the action of sulfonamides; do not coadminister.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Bradycardia, cardiac arrest, hypotension, myocardium depression, ventricular arrhythmias.

CNS

Anxiety, CNS excitement or depression, convulsions, dizziness, drowsiness, headache, restlessness, tremors, unconsciousness.

EENT

Blurred vision, tinnitus.

Miscellaneous

Allergic reactions (characterized by urticaria, pruritus, erythema, angioneurotic edema, tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, and possibly, anaphylactoid-type symptomatology), backache, respiratory arrest.

Precautions

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and effectiveness not established in children younger than 3 yr of age.

Elderly

Exercise caution in dose selection, 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.

Special Risk Patients

Use with caution in areas of the body supplied by end arteries or having compromised blood supply, and in patients with neurological disease, spinal deformities, septicemia, severe hypertension, impaired CV function, hypotension, heart block, or hepatic disease.

Mixing local anesthetics

Exercise caution regarding toxic equivalence when mixtures of local anesthetics are employed.

Ophthalmic surgery

When using for retrobulbar block, do not rely upon lack of corneal sensation to determine wether or not the patient is ready for surgery.

Peripheral or hypertensive vascular disease

May exhibit exaggerated vasoconstrictor response, and ischemic injury or necrosis may result.

Overdosage

Symptoms

None well documented.

Patient Information

• Advise patient that medication will be prepared and administered by a health care provider in a medical setting.
• Caution patient that temporary loss of sensation and motor activity may be experienced.
• Instruct patient to inform health care provider if any of the following are experienced during or after the anesthetic injection: anxiety, blurred vision, dizziness, drowsiness or change in mental status, hot or cold sensations, rapid breathing or feeling of shortness of breath, rapid heart rate, restlessness, ringing in the ears.

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