Procaine

Procaine
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

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Overview

Procaine is a local anesthetic that is FDA approved for the {{{indicationType}}} of local Anesthetic for local infiltration and peripheral nerve block. Common adverse reactions include myocardial depression, hypotension and sometimes hypertension, bradycardia, ventricular arrhythmias, and cardiac arrest,nausea/vomiting, cutaneous lesions of delayed onset, urticaria, and edema related to allergic reactions , nervousness, dizziness, blurred vision, and tremors may occur due to systemic toxicity; however, drowsiness or convulsions with subsequent unconsciousness and respiratory arrest..

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Parenteral route

Infiltration Anesthesia

• Procaine 0.25% to 0.5% solutions in doses of 350 to 600 milligrams may be used for Infiltration Anesthesia. Epinephrine may be added for vasoconstrictive effect to give a final concentration of 1:200,000.

Peripheral Nerve Block

• For, Procaine 0.5% solution (up to 200 milliliters), 1% solution (up to 100 milliliters), or 2% solution (up to 50 milliliters) is recommended. The 2% solution is generally limited to procedures requiring a small volume of anesthetic, ie, 10 to 25 milliliters (mL). An anesthetic solution of 0.5 mL to 1 mL of Epinephrine 1:1,000 per 100 mL may be used to promote vasoconstriction (1:200,000 or 1:100,000).
• To prepare 60 milliliters (mL) of a 0.5% solution (5 milligrams/mL), dilute 30 mL of the 1% solution with 30 mL sodium chloride 0.9% injection. To prepare 60 mL of a 0.25% solution (2.5 milligrams/mL), dilute 15 mL of the 1% solution with 45 mL sodium chloride 0.9% injection .

Anesthesia of the perineum

• A dose of procaine 50 milligrams of a 10% solution mixed with an equal amount of diluent may be used for Anesthesia of the perineum; 100 milligrams (1 milliliter) diluted with an equal amount of diluent for the perineum and lower extremities; and up to 200 milligrams (2 milliliters) with 1 milliliter of diluent for anesthesia of the costal margin.

Maximum Dose

• Usual total dose of Procaine during one treatment should not exceed 1000 milligrams.

Dosage in Renal Failure

• The serum half-life of Procaine has been prolonged in some uremic patients.

Dosage in Hepatic Insufficiency

• The serum half-life of Procaine has been prolonged in patients with liver disease; dosage reductions are recommended.

Dosage in Geriatric Patients

• Patient response to Procaine varies, and reduced doses should be given to elderly or acutely ill patients (Prod Info Novocain(R), 1990a).

Dosage in Other Disease States

• Procaine doses should be reduced in patients with cardiac disease.
• Reduced doses of procaine may be necessary for obstetric delivery and in patients with increased intra-abdominal pressure.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Procaine in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Procaine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Parenteral route

• For Infiltration Anesthesia, the maximum recommended Procaine dose is 15 milligrams/kilogram of a 0.5% solution in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Procaine in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Procaine in pediatric patients.

Contraindications

NOVOCAIN is contraindicated in patients with a known hypersensitivity to procaine, drugs of a similar chemical configuration, or para-aminobenzoic acid or its derivatives.

It is also contraindicated in patients with a known hypersensitivity to other components of solutions of NOVOCAIN.

Warnings

Contains acetone sodium bisulfite, a sulfite that may cause allergic-type reactions including anaphylactic symptoms and life-threatening or less severe asthmatic episodes in certain susceptible people. The overall prevalence of sulfite sensitivity in the general population is unknown and probably low. Sulfite sensitivity is seen more frequently in asthmatic than in nonasthmatic people.

LOCAL ANESTHETICS SHOULD ONLY BE EMPLOYED 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 also ADVERSE REACTIONS and PRECAUTIONS.) 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.

It is essential that aspiration for blood or cerebrospinal fluid, where applicable, be done prior to injecting any local anesthetic, both the original dose and all subsequent doses, to avoid intravascular or subarachnoid injection. However, a negative aspiration does not ensure against an intravascular or subarachnoid injection.

Reactions resulting in fatality have occurred on rare occasions with the use of local anesthetics, even in the absence of a history of hypersensitivity. Large doses of local anesthetics should not be used in patients with heartblock.

NOVOCAIN with epinephrine or other vasopressors should not be used concomitantly with ergot-type oxytocic drugs, because a severe persistent hypertension may occur. Likewise, solutions of NOVOCAIN containing a vasoconstrictor, such as epinephrine, should be used with extreme caution in patients receiving monoamine oxidase inhibitors (MAOI) or antidepressants of the triptyline or imipramine types, because severe prolonged hypertension or disturbances of cardiac rhythm may occur.

Local anesthetic procedures should be used with caution when there is inflammation and/or sepsis in the region of the proposed injection.

Mixing or the prior or intercurrent use of any local anesthetic with NOVOCAIN cannot be recommended because of insufficient data on the clinical use of such mixtures.

Adverse Reactions

Clinical Trials Experience

Reactions to procaine are characteristic of those associated with other ester-type local anesthetics. A major cause of adverse reactions to this group of drugs is excessive plasma levels which may be due to overdosage, rapid absorption, inadvertent intravascular injection, or slow metabolic degradation.

A small number of reactions may result from hypersensitivity, idiosyncrasy, or diminished tolerance to normal dosage.

Systemic:

The most commonly encountered acute adverse experiences which demand immediate countermeasures are related to the central nervous system and the cardiovascular system. These adverse experiences are generally dose related and due to high plasma levels which may result from overdosage, rapid absorption from the injection site, diminished tolerance, or from unintentional intravascular injection of the local anesthetic solution. In addition to systemic dose-related toxicity, unintentional subarachnoid injection of drug during the intended performance of nerve blocks near the vertebral column (especially in the head and neck region), may result in underventilation or apnea (“Total or High Spinal”). Factors influencing plasma protein binding, such as acidosis, systemic diseases which alter protein production, or competition of other drugs for protein binding sites may diminish individual tolerance.

Plasma cholinesterase deficiency may also account for diminished tolerance to ester-type local anesthetics.

Central Nervous System Reactions:

These are characterized by excitation and/or depression. Restlessness, anxiety, dizziness, tinnitus, blurred vision, or tremors may occur, possibly proceeding to convulsions. However, excitement may be transient or absent, with depression being the first manifestation of an adverse reaction. This may quickly be followed by drowsiness merging into unconsciousness and respiratory arrest.

The incidence of convulsions associated with the use of local anesthetics varies with the procedure used and the total dose administered.

Cardiovascular Reactions:

High doses or inadvertent intravascular injection may lead to high plasma levels and related depression of the myocardium, decreased cardiac output, heartblock, hypotension (or sometimes hypertension), bradycardia, ventricular arrhythmias, and cardiac arrest. (See WARNINGS, PRECAUTIONS, and OVERDOSAGE sections.)

Allergic:

Allergic-type reactions are rare and may occur as a result of sensitivity to the local anesthetic or to other formulation ingredients, such as the antimicrobial preservative chlorobutanol contained in multiple-dose vials. 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, anaphylactoid-like 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.

Neurologic:

The incidences of adverse neurologic reactions associated with the use of local anesthetics may be related to the total dose of local anesthetic administered, and are also dependent upon the particular drug used, the route of administration, and the physical status of the patient. Many of these effects may be related to local anesthetic techniques, with or without a contribution from the drug.

Postmarketing Experience

There is limited information regarding Procaine Postmarketing Experience in the drug label.

Drug Interactions

The administration of local anesthetic solutions containing epinephrine or norepinephrine to patients receiving monoamine oxidase inhibitors or tricyclic antidepressants may produce severe, prolonged hypertension. Concurrent use of these agents should generally be avoided. In situations when concurrent therapy is necessary, careful patient monitoring is essential.

Concurrent administration of vasopressor drugs and of ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents.

Phenothiazines and butyrophenones may reduce or reverse the pressor effect of epinephrine.

The clinical observation has been made that despite adequate sulfonamide therapy, local infections have occurred in areas infiltrated with procaine hydrochloride prior to diagnostic punctures and drainage procedures. Therefore, NOVOCAIN should not be used in any condition in which a sulfonamide drug is being employed since para-aminobenzoic acid inhibits the action of the sulfonamide.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Procaine in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Procaine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Procaine during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Procaine in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Procaine in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Procaine in geriatric settings.

Gender

There is no FDA guidance on the use of Procaine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Procaine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Procaine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Procaine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Procaine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Procaine in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Procaine Administration in the drug label.

Monitoring

There is limited information regarding Procaine Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Procaine and IV administrations.

Overdosage

Acute emergencies from local anesthetics are generally related to high plasma levels encountered during therapeutic use of local anesthetics or to unintended subarachnoid injection of local anesthetic solution. (See ADVERSE REACTIONS, WARNINGS, and PRECAUTIONS.)

Management of Local Anesthetic Emergencies:

The first consideration is prevention, best accomplished by careful and constant monitoring of cardiovascular and respiratory vital signs, and the patient’s state of consciousness after each local anesthetic injection. At the first sign of change, oxygen should be administered.

The first step in the management of systemic toxic reactions, as well as underventilation or apnea due to unintentional subarachnoid injection of drug solution, consists of immediate attention to the establishment and maintenance of a patent airway, and effective assisted or controlled ventilation with 100% oxygen with a delivery system capable of permitting immediate positive airway pressure by mask. This may prevent convulsions if they have not already occurred.

If necessary, use drugs to control the convulsions. A 50 mg to 100 mg bolus IV injection of succinylcholine will paralyze the patient without depressing the central nervous or cardiovascular systems and facilitate ventilation. A bolus IV dose of 5 mg to 10 mg of diazepam or 50 mg to 100 mg of thiopental will permit ventilation and counteract central nervous system stimulation, but these drugs also depress central nervous system, respiratory and cardiac function, add to postictal depression, and may result in apnea. Intravenous barbiturates, anticonvulsant agents, or muscle relaxants should only be administered by those familiar with their use. Immediately after the institution of these ventilatory measures, the adequacy of the circulation should he evaluated. Supportive treatment of circulatory depression may require administration of intravenous fluids and, when appropriate, a vasopressor dictated by the clinical situation (such as ephedrine or epinephrine to enhance myocardial contractile force).

Endotracheal intubation, employing drugs and techniques familiar to the clinician, may be indicated, after initial administration of oxygen by mask, if difficulty is encountered in the maintenance of a patent airway or if prolonged ventilatory support (assisted or controlled) is indicated.

Recent clinical data from patients experiencing local anesthetic-induced convulsions demonstrated rapid development of hypoxia, hypercarbia, and acidosis within a minute of the onset of convulsions. These observations suggest that oxygen consumption and carbon dioxide production are greatly increased during local anesthetic convulsions, and emphasize the importance of immediate and effective ventilation with oxygen which may avoid cardiac arrest.

If not treated immediately, convulsions with simultaneous hypoxia, hypercarbia, and acidosis plus myocardial depression from the direct effects of the local anesthetic may result in cardiac arrhythmias, bradycardia, asystole, ventricular fibrillation, or cardiac arrest. Respiratory abnormalities, including apnea, may occur. Underventilation or apnea due to unintentional subarachnoid injection of local anesthetic solution may produce these same signs and also lead to cardiac arrest if ventilatory support is not instituted. If cardiac arrest should occur, standard cardiopulmonary resuscitative measures should be instituted and maintained for a prolonged period if necessary. Recovery has been reported after prolonged resuscitative efforts.

The supine position is dangerous in pregnant women at term because of aortocaval compression by the gravid uterus. Therefore, during treatment of systemic toxicity, maternal hypotension, or fetal bradycardia following regional block, the parturient should be maintained in the left lateral decubitus position if possible, or manual displacement of the uterus off the great vessels be accomplished.

The intravenous and subcutaneous and intraperitoneal LD50 of procaine hydrochloride in mice is 46 mg/kg to 80 mg/kg and 400 mg/kg and 200 mg/kg respectively.

Pharmacology

There is limited information regarding Procaine Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Procaine Mechanism of Action in the drug label.

Structure

There is limited information regarding Procaine Structure in the drug label.

Pharmacodynamics

There is limited information regarding Procaine Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Procaine Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Procaine Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Procaine Clinical Studies in the drug label.

How Supplied

Single-dose containers and multiple-dose containers of NOVOCAIN may be sterilized by autoclaving at 15-pound pressure, 121°C (250°F) for 15 minutes. Do not use solutions if crystals, cloudiness, or discoloration is observed. Examine solution carefully before use. Reautoclaving increases likelihood of crystal formation. Do not administer solutions which are discolored or which contain particulate matter. Protect solutions from light.

Unused portions of solutions not containing preservatives, i.e., those supplied in ampuls, should be discarded following initial use.

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Storage

There is limited information regarding Procaine Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Procaine Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Procaine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Procaine Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Procaine Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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