Generic Name: procaine

Brand Names: Mericaine, Novocain

Uses

Local or Regional Anesthesia

Local or regional analgesia or anesthesia in surgical, dental, and diagnostic procedures.

Dosage and Administration

General

• Determine dosage based on anesthetic procedure, area to be anesthetized, vascularity of tissues, number of neuronal segments to be blocked, depth and duration of anesthesia, degree of muscular relaxation, individual tolerance, and physical condition of the patient. Use smallest dose and concentration required to produce the desired effect.

Administration

Injection

For solution and drug compatibility information, see Compatibility under Stability.

Administer by local infiltration, peripheral nerve block, or subarachnoid (spinal) block.

Consult specialized references for specific techniques and procedures for administering local anesthetics.

For local infiltration or peripheral nerve block, inject slowly and avoid rapid injection of large volumes; when feasible, administer in fractional (incremental) doses.

For subarachnoid (spinal) block, use 2-mL single-dose ampuls containing procaine hydrochloride 10% only. Position patient properly prior to spinal anesthesia.

For disinfection of container surface, autoclave once at 15 PSI and 121°C for 15 minutes (diluent dextrose may show some brown discoloration due to caramelization); immersion in antiseptic solution not recommended. Reautoclaving not recommended because it increases likelihood of crystal formation.

Dilution

For local infiltration, dilute appropriate dose of 1% procaine hydrochloride injection with 0.9% sodium chloride to obtain final concentration of 0.25 or 0.5%. May add 0.5–1 mL of epinephrine 0.1% to each 100 mL of anesthetic solution (to provide final epinephrine concentration of 1:200,000 to 1:100,000) for vasoconstrictive effect.

For peripheral nerve block, dilute appropriate dose of 1% procaine hydrochloride injection with 0.9% sodium chloride to obtain final concentration of 0.5%. Alternatively, may use 1% procaine hydrochloride injection without diluting. May add 0.5–1 mL of epinephrine 0.1% to each 100 mL of anesthetic solution (to provide a final epinephrine concentration of 1:200,000 to 1:100,000) for vasoconstrictive effect.

For subarachnoid (spinal) block, dilute appropriate dose of 10% procaine hydrochloride injection with sterile 0.9% sodium chloride injection, sterile water for injection, CSF, or, for hyperbaric technique, sterile dextrose injection. For anesthesia of the perineum, dilute 0.5 mL of the 10% procaine hydrochloride injection (50 mg) with an equal volume of diluent. For anesthesia of the perineum and lower extremities, dilute 1 mL of the 10% injection (100 mg) with an equal volume of diluent. For anesthesia extending up to the costal margin, dilute 2 mL of the 10% injection (200 mg) with 1 mL of diluent.

Rate of Administration

For subarachnoid (spinal) block, usual rate of injection is 1 mL/5 seconds.

Dosage

Available as procaine hydrochloride; dosage expressed in terms of the salt.

Pediatric Patients

Local or Regional Anesthesia

Local Infiltration

Up to 15 mg/kg as a 0.5% solution.

Adults

Local or Regional Anesthesia

Local Infiltration

Usually, 350–600 mg, administered as diluted solution (i.e., 140–240 mL of a 0.25% solution or 70–120 mL of a 0.5% solution).

Peripheral Nerve Block

Up to 1 g, administered undiluted (i.e., 100 mL of a 1% injection) or as diluted solution (i.e., 200 mL of a 0.5% solution).

Subarachnoid (Spinal) Block

Prescribing Limits

Pediatric Patients

Local or Regional Anesthesia

Local Infiltration

Maximum 15 mg/kg as a 0.5% solution.

Adults

Local or Regional Anesthesia

Local Infiltration, Peripheral Nerve Block

Maximum 1 g per injection.

Special Populations

Hepatic Impairment

Reduce dosage in patients with hepatic disease.

Geriatric Patients

Reduce dosage based on age, weight, and physical status.

Other Populations

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

Reduce dosage in obstetric patients and patients with increased intra-abdominal pressure.

Cautions

Contraindications

• Contraindications to spinal anesthesia: generalized septicemia, sepsis at proposed injection site, and certain diseases of the cerebrospinal system (e.g., meningitis, syphilis, spinal fluid block, cranial or spinal hemorrhage, tumors, poliomyelitis, metastatic lesions of the spinal cord).
• Known hypersensitivity to procaine, drugs of a similar chemical configuration, aminobenzoic acid or its derivatives, or any ingredient in the formulation.

Warnings/Precautions

Warnings

Experience of Supervising Clinician

Should be used only by clinicians who are sufficiently knowledgeable in the diagnosis and management of dose-related toxicity and other acute emergencies that might arise. Oxygen, resuscitative equipment, and drugs must be available for immediate use. Delay in appropriate management of dose-related toxicity, underventilation from any cause, and/or altered sensitivity may result in acidosis, cardiac arrest, and, possibly, death.

Accidental Intravascular Injection

Accidental intravascular injection of local anesthetics may result in seizures, CNS or cardiorespiratory depression, coma, and/or respiratory arrest.

Aspirate prior to and during administration to guard against intravascular injection.

Sensitivity Reactions

Hypersensitivity Reactions and Cross-sensitivity

Allergic reactions are rare.

Possible urticaria, pruritus, erythema, angioneurotic edema (including laryngeal edema), tachycardia, sneezing, nausea, vomiting, dizziness, syncope, excessive sweating, elevated temperature, and anaphylactoid reactions (including severe hypotension).

Cross-sensitivity between ester-type local anesthetics reported.

Use with caution in patients with known drug allergies and hypersensitivities.

Sulfite Sensitivity

Some procaine hydrochloride preparations contain acetone sodium bisulfite, which may cause allergic-type reactions (including anaphylaxis and life-threatening or less severe asthmatic episodes) in certain susceptible individuals.

General Precautions

CNS Effects

Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse CNS effects (e.g., anxiety, apprehension, restlessness, nervousness, disorientation, incoherent speech, confusion, dizziness, lightheadedness, blurred vision, tremors, twitching, shivering, numbness and tingling of the mouth and lips, metallic taste, tinnitus, seizures, depression, drowsiness, unconsciousness, respiratory arrest).

Carefully monitor level of consciousness after each local anesthetic administration.

Cardiovascular Effects

Toxic plasma concentrations of local anesthetics (resulting from systemic absorption) associated with adverse cardiovascular effects (e.g., myocardial depression, decreased cardiac output, heart block, hypotension, bradycardia, ventricular arrhythmias, cardiovascular collapse, cardiac arrest). Carefully monitor cardiovascular (e.g., BP) and respiratory vital signs after each local anesthetic injection.

Use with caution in patients with severe disturbances of cardiac rhythm, shock, heart block, or hypotension.

Avoid use of large doses in patients with heart block.

For solutions containing a vasoconstrictor (e.g., epinephrine), consider risk of exaggerated vasoconstrictor response in patients with peripheral or hypertensive vascular disease. Use with caution and in carefully restricted quantities in areas of the body supplied by end arteries or having otherwise compromised blood supply (e.g., digits, nose, external ear, penis).

Vasoconstrictor Administration

Concomitant use with a vasoconstrictor such as epinephrine may cause ischemic injury or necrosis.

Familial Malignant Hyperthermia

Many drugs used during the conduct of anesthesia may trigger familial malignant hyperthermia; not known whether ester-type local anesthetics trigger this reaction. However, standard protocol for management should be available. Early unexplained signs of tachycardia, tachypnea, labile BP, and metabolic acidosis may precede temperature elevation. If familial malignant hyperthermia is confirmed, discontinue triggering agent and initiate appropriate therapy (e.g., oxygen, dantrolene) and other supportive measures.

Preexisting Conditions

Employ anesthetic procedures with caution when there is inflammation and/or sepsis in the region of the proposed injection. (See Contraindications under Cautions.)

Conditions that may preclude the use of spinal anesthesia (depending on the clinician’s evaluation of the situation and ability to manage potential complications) include cardiovascular disease (e.g., shock, hypertension, hypotension, arteriosclerosis, occlusive arterial disease); pulmonary disease; renal impairment; metabolic or endocrine disorders; GI disorder (e.g., intestinal obstruction, peritonitis); complicated obstetrical deliveries; spinal deformities that make spinal puncture inadvisable or difficult; bleeding resulting from traumatic lumbar puncture; severe anemia, cachexia, or moribund condition; chronic backache; preoperative headache or history of migraine; extremes of age; and emotional instability, hysteria, or nervous tension. (See Contraindications under Cautions.)

Specific Populations

Pregnancy

Category C.

Labor and Delivery

Maternal hypotension reported. To prevent decreases in BP, elevate patient’s legs and position patient on her left side. Monitor fetal heart rate continuously; electronic fetal monitoring highly advisable.

Epidural, spinal, paracervical, or pudendal anesthesia may alter the forces of parturition through changes in uterine contractility or maternal expulsive efforts; may increase need for forceps assistance.

Possible diminished muscle strength and tone on neonate’s first or second day of life.

Lactation

Not known whether procaine is distributed into milk. Caution if used in nursing women.

Pediatric Use

Some manufacturers recommend reducing dosage of local anesthetics in proportion to age, weight, and physical condition. (See Pediatric Patients under Dosage and Administration.)

Geriatric Use

Reduce dosage based on age, weight, and physical status.

Hepatic Impairment

Use with caution; patients with severe hepatic disease are at greater risk of developing toxic plasma concentrations. Dosage reduction recommended.

Renal Impairment

Weigh benefits against risks of spinal anesthesia in patients with renal impairment.

Common Adverse Effects

Adverse CNS and cardiovascular effects, underventilation, apnea. (See CNS Effects and also Cardiovascular Effects, under Cautions.)

Spinal anesthesia: Possible postspinal headache, meningismus, arachnoiditis, palsies, spinal nerve paralysis, hypotension, respiratory impairment or paralysis, nausea, vomiting.

Interactions

When used with epinephrine, consider usual drug interactions associated with epinephrine administration.

Specific Drugs

Pharmacokinetics

Absorption

Bioavailability

Readily absorbed following parenteral administration.

Rate of systemic absorption dependent upon total dose and concentration administered, route of administration, vascularity of administration site, and presence or absence of epinephrine in solution.

Onset

2–5 minutes.

Duration

1–1.5 hours.

Distribution

Extent

Local anesthetics are distributed to some extent to all body tissues, with high concentrations found in highly perfused organs (e.g., liver, lungs, heart, brain).

Local anesthetics generally cross blood-brain and placental barriers.

Elimination

Metabolism

Rapidly and almost completely hydrolyzed by plasma cholinesterase to p-aminobenzoic acid and diethylaminoethanol.

Elimination Route

Approximately 90% of p-aminobenzoic acid and its conjugates and 33% of diethylaminoethanol are excreted in urine; <2% of administered dose is excreted in urine as unchanged drug.

Special Populations

Possible delayed metabolism in neonates, adults with liver disease, and adults with impaired renal function.

Stability

Storage

Parenteral

Injection

20–25°C. Protect from light. Discard unused portion of solutions not containing preservatives.

Do not use if crystal formation, cloudiness, or discoloration is observed.

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

Solution Compatibility

Drug Compatibility

Do not mix with other local anesthetics (insufficient clinical data).

Actions

• Local anesthetics block the generation and conduction of nerve impulses by increasing the threshold for electrical excitation, slowing the propagation of the nerve impulse, and reducing the rate of rise of the action potential.
• Produces vasodilation; may add a vasoconstrictor (e.g., epinephrine) to solutions of procaine to retard procaine’s absorption, prolong its duration of action, and maintain hemostasis.
• Has short duration of action.
• Has little topical activity.

Advice to Patients

• Prior to administration, advise patients of the possibility of temporary loss of sensation and motor activity following local or regional anesthesia.
• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., cardiovascular or liver disease).
• Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.
• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

AHFS Drug Information. © Copyright, 1959-2009, Selected Revisions December 2007. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.