Procaine Hydrochloride

Class: Local Anesthetics
ATC Class: N01BA52
VA Class: CN204
Chemical Name: 4-amino-, 2-(diethylamino) ethyl ester monohydrochloride
CAS Number: 51-05-8

Introduction

Short-acting local anesthetic (ester type).a

Uses for Procaine Hydrochloride

Local or Regional Anesthesia

Local or regional analgesia or anesthesiac d in surgical, dental, and diagnostic procedures.a b

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Procaine Hydrochloride 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.c d Use smallest dose and concentration required to produce the desired effect.a c d

Administration

Injection

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

Administer by local infiltration, peripheral nerve block, or subarachnoid (spinal) block.a c d Has been administered by continuous intra-articular infusion (e.g., for control of postoperative pain); however, such use associated with chondrolysis.200 201 202 203 204 205 206 207 208 209 (See Risk of Chondrolysis Associated with Intra-articular Infusions of Local Anesthetics under Cautions.)

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

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

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

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

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%.a d 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.a

For peripheral nerve block, dilute appropriate dose of 1% procaine hydrochloride injection with 0.9% sodium chloride to obtain final concentration of 0.5%.a d Alternatively, may use 1% procaine hydrochloride injection without diluting.d 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.a

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.a c For anesthesia of the perineum, dilute 0.5 mL of the 10% procaine hydrochloride injection (50 mg) with an equal volume of diluent.a For anesthesia of the perineum and lower extremities, dilute 1 mL of the 10% injection (100 mg) with an equal volume of diluent.a For anesthesia extending up to the costal margin, dilute 2 mL of the 10% injection (200 mg) with 1 mL of diluent.a

Rate of Administration

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

Dosage

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

Pediatric Patients

Local or Regional Anesthesia
Local Infiltration

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

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).a d

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).a d

Subarachnoid (Spinal) Block
Recommended Dosage for Spinal Anesthesia in Adultsac

Extent of Anesthesia

Total Dose of Procaine Hydrochloride (mg) (as 10% Injection)

Site of Injection (Lumbar Interspace)

Perineum

50

4th

Perineum and lower extremities

100

3rd or 4th

Up to costal margin

200

2nd, 3rd, or 4th

Prescribing Limits

Pediatric Patients

Local or Regional Anesthesia
Local Infiltration

Maximum 15 mg/kg as a 0.5% solution.d

Adults

Local or Regional Anesthesia
Local Infiltration, Peripheral Nerve Block

Maximum 1 g per injection.a

Special Populations

Hepatic Impairment

Reduce dosage in patients with hepatic disease.a

Geriatric Patients

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

Other Populations

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

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

Cautions for Procaine Hydrochloride

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).b c

  • Known hypersensitivity to procaine, drugs of a similar chemical configuration, aminobenzoic acid or its derivatives, or any ingredient in the formulation.c d

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.b c d Oxygen, resuscitative equipment, and drugs must be available for immediate use.a b 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.b d

Risk of Chondrolysis Associated with Intra-articular Infusions of Local Anesthetics

Chondrolysis (necrosis and destruction of articular cartilage) reported in patients receiving continuous intra-articular infusions of local anesthetics, administered for 48–72 hours via elastomeric infusion devices, for treatment of postoperative pain.200 201 202 203 204 205 206 207 208 209 Primarily observed in the shoulder joint following arthroscopic or other shoulder surgery.200 May result in long-term disability; often requires intervention (e.g., debridement, arthroplasty).200 202 203 204 205 206 209 Not known whether the drug, infusion device, and/or other factors contributed to the development of chondrolysis.200 201 Neither local anesthetics nor elastomeric infusion devices are approved for use for continuous intra-articular infusion therapy.200 201

Accidental Intravascular Injection

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

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

Sensitivity Reactions

Hypersensitivity Reactions and Cross-sensitivity

Allergic reactions are rare.b d

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).c d

Cross-sensitivity between ester-type local anesthetics reported.b d

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

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.a b

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).b c d

Carefully monitor level of consciousness after each local anesthetic administration.c d

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).b c d Carefully monitor cardiovascular (e.g., BP) and respiratory vital signs after each local anesthetic injection.a c d

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

Avoid use of large doses in patients with heart block.c d

For solutions containing a vasoconstrictor (e.g., epinephrine), consider risk of exaggerated vasoconstrictor response in patients with peripheral or hypertensive vascular disease.d 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).d

Vasoconstrictor Administration

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

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.d However, standard protocol for management should be available.d Early unexplained signs of tachycardia, tachypnea, labile BP, and metabolic acidosis may precede temperature elevation.d If familial malignant hyperthermia is confirmed, discontinue triggering agent and initiate appropriate therapy (e.g., oxygen, dantrolene) and other supportive measures.d

Preexisting Conditions

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

Specific Populations

Pregnancy

Category C.d

Labor and Delivery

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

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.b

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

Lactation

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

Pediatric Use

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

Geriatric Use

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

Hepatic Impairment

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

Renal Impairment

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

Common Adverse Effects

Adverse CNS and cardiovascular effects, underventilation, apnea.d (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.c

Interactions for Procaine Hydrochloride

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

Specific Drugs

Drug

Interaction

Comments

Aminosalicylic acid

Possible antagonism of aminosalicylic acid activitya

Consider avoiding concomitant usea b

Antidepressants, tricyclics

Possible severe, prolonged hypertension or disturbances of cardiac rhythm due to epinephrine componentd

Avoid concomitant use with epinephrine; if must be used concomitantly, careful monitoring is requiredd

Butyrophenones

Possible reduction or reversal of pressor effect of epinephrined

Ergot alkaloid oxytocics (ergonovine, methylergonovine)

Possible severe, persistent hypertension or cerebrovascular accidents (e.g., rupture of cerebral blood vessel) due to epinephrine componentc d

Avoid concomitant use with epinephrined

MAO inhibitors

Possible severe, prolonged hypertension or disturbances of cardiac rhythm due to epinephrine componentd

Avoid concomitant use with epinephrine; if must be used concomitantly, careful monitoring is requiredd

Phenothiazines

Possible reduction or reversal of pressor effect of epinephrine;d severe sustained hypertension or hypotension also may occurc

Use concomitantly with epinephrine with extreme cautionc

Succinylcholine

Possible increase in neuromuscular blocking effect with high IV doses of procaineb

Sulfonamides

Possible antagonism of sulfonamide activityb

Avoid concomitant usea b

Procaine Hydrochloride Pharmacokinetics

Absorption

Bioavailability

Readily absorbed following parenteral administration.c

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.d

Onset

2–5 minutes.a

Duration

1–1.5 hours.a c d

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).d

Local anesthetics generally cross blood-brain and placental barriers.b d

Elimination

Metabolism

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

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.d

Special Populations

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

Stability

Storage

Parenteral

Injection

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

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

Compatibility

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

Parenteral

Solution CompatibilityHID

Compatible

Dextran 6% in dextrose 5%

Dextran 6% in sodium chloride 0.9%

Dextrose-Ringer's injection combinations

Dextrose-Ringer’s injection, lactated, combinations

Dextrose-saline combinations

Dextrose 2½, 5, or 10% in water

Fructose 10% in sodium chloride 0.9%

Fructose 10% in water

Invert sugar 5 and 10% in sodium chloride 0.9%

Invert sugar 5 and 10% in water

Ionosol products

Ringer's injection

Ringer's injection, lactated

Sodium chloride 0.45 or 0.9%

Sodium lactate (1/6) M

Drug Compatibility

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

Admixture CompatibilityHID

Compatible

Ascorbic acid injection

Hydrocortisone sodium succinate

Penicillin G potassium

Penicillin G sodium

Vitamin B complex with C

Incompatible

Amobarbital sodium

Chlorothiazide sodium

Magnesium sulfate

Phenobarbital sodium

Phenytoin sodium

Sodium bicarbonate

Variable

Aminophylline

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.b c d

  • 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.a d

  • Has short duration of action.a

  • Has little topical activity.a

Advice to Patients

  • Prior to administration, advise patients of the possibility of temporary loss of sensation and motor activity following local or regional anesthesia.d

  • 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).c d

  • Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.c d

  • Importance of informing patients of other important precautionary information.c d (See Cautions.)

Preparations

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

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Procaine Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Bulk

Powder*

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions February 1, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

200. Food and Drug Administration. Information for healthcare professionals: Chondrolysis reported with continuously infused local anesthetics (marketed as bupivacaine, chloroprocaine, lidocaine, mepivacaine, procaine, and ropivacaine). Rockville, MD; Updated 2010 Feb 16. From FDA website ().

201. Todd JF. Chondrolysis linked to intra-articular infusions. Medical Devices Alerts and Notices. Silver Spring, MD: Food and Drug Administration; 2010 June. From FDA website ().

202. Hansen BP, Beck CL, Beck EP et al. Postarthroscopic glenohumeral chondrolysis. Am J Sports Med. 2007; 35:1628-34. [PubMed 17609526]

203. Bailie DS, Ellenbecker TS. Severe chondrolysis after shoulder arthroscopy: a case series. J Shoulder Elbow Surg. 2009 Sep-Oct; 18:742-7.

204. Anakwenze OA, Hosalkar H, Huffman GR. Case Reports: Two Cases of Glenohumeral Chondrolysis after Intraarticular Pain Pumps. Clin Orthop Relat Res. 2010; :.

205. Anderson SL, Buchko JZ, Taillon MR et al. Chondrolysis of the glenohumeral joint after infusion of bupivacaine through an intra-articular pain pump catheter: a report of 18 cases. Arthroscopy. 2010; 26:451-61. [PubMed 20362823]

206. Rapley JH, Beavis RC, Barber FA. Glenohumeral chondrolysis after shoulder arthroscopy associated with continuous bupivacaine infusion. Arthroscopy. 2009; 25:1367-73. [PubMed 19962061]

207. Scheffel PT, Clinton J, Lynch JR et al. Glenohumeral chondrolysis: A systematic review of 100 cases from the English language literature. J Shoulder Elbow Surg. 2010; :. [PubMed 20421168]

208. Ballieul RJ, Jacobs TF, Herregods S et al. The peri-operative use of intra-articular local anesthetics: a review. Acta Anaesthesiol Belg. 2009; 60:101-8. [PubMed 19594092]

209. Busfield BT, Romero DM. Pain pump use after shoulder arthroscopy as a cause of glenohumeral chondrolysis. Arthroscopy. 2009; 25:647-52. [PubMed 19501296]

a. AHFS drug information 2011. McEvoy GK, ed. Procaine Hydrochloride. Bethesda, MD: American Society of Health-System Pharmacists; e-pub ahead of print.

b. AHFS drug information 2011. McEvoy GK, ed. Local Anesthetics, Parenteral, General Statement. Bethesda, MD: American Society of Health-Systems Pharmacists; e-pub ahead of print.

c. Hospira, Inc. Novocain (procaine hydrochloride) injection 10% solution for spinal anesthesia prescribing information. Lake Forest, IL; 2005 Jul.

d. Hospira, Inc. Novocain (procaine hydrochloride) injection prescribing information. Lake Forest, IL; 2005 Jun.

HID. Trissel LA. Handbook on injectable drugs. 14th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2007:1395-7.

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