NOVOCAINE

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT NOVOCAIN (NOVOCAIN)

Composition:

Active substance: procaine hydrochloride (novocaine);

1 ml of solution contains procaine hydrochloride (novocaine) 5 mg;

Excipients: 0.1 M hydrochloric acid solution, water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear, colorless or slightly yellowish liquid.

Pharmacotherapeutic group. Local anesthetics. ATC code N01B A02.

Pharmacological Properties.

Pharmacodynamics.

A local anesthetic agent with moderate activity and a wide therapeutic index. The mechanism of anesthetic action is associated with blockade of sodium channels, inhibition of potassium current, competition with calcium, reduction of the surface tension of the phospholipid membrane layer, suppression of redox processes, and inhibition of impulse generation. When absorbed into the bloodstream, it reduces acetylcholine production, decreases excitability of peripheral cholinoreactive systems, exerts a blocking effect on autonomic ganglia, reduces smooth muscle spasms, and decreases excitability of cardiac muscle and motor areas of the cerebral cortex.

Pharmacokinetics.

After parenteral administration, it is well absorbed. The extent of absorption depends on the site and route of administration (particularly on vascularization and blood flow velocity at the injection site) and on the total dose (quantity and concentration). It is rapidly hydrolyzed by esterases and cholinesterases in blood plasma and tissues, forming two main pharmacologically active metabolites: diethylaminoethanol (which has moderate vasodilatory activity) and para-aminobenzoic acid (which acts as a competitive antagonist of sulfonamide chemotherapeutic agents and may reduce their antimicrobial effect). The elimination half-life is 30–50 seconds; in the neonatal period, it is 54–114 seconds. The drug is primarily excreted by the kidneys in the form of metabolites (80%); less than 2% is excreted unchanged. It is poorly absorbed by mucous membranes.

Clinical characteristics.

Indications. Local and infiltration anesthesia, therapeutic blocks.

Contraindications.

Hypersensitivity to any component of the drug.

Myasthenia gravis; arterial hypotension; purulent processes at the injection site; emergency surgical interventions associated with acute blood loss; pronounced fibrotic changes in tissues (for anesthesia by creeping infiltration method).

Interaction with other medicinal products and other types of interactions.

The drug reduces the effect of anticholinesterase agents on neuromuscular transmission. Prolongs neuromuscular blockade caused by suxamethonium (since both drugs are hydrolyzed by plasma cholinesterase). A metabolite of procaine (para-aminobenzoic acid) is a competitive antagonist of sulfonamide drugs and may reduce their antimicrobial activity. Concurrent use with monoamine oxidase inhibitors (MAO inhibitors) increases the risk of developing arterial hypotension. The toxicity of procaine is increased by anticholinesterase agents (which inhibit its hydrolysis). Cross-sensitization is possible. Intravenous administration of novocaine potentiates the action of anesthetic agents.

When the injection site of novocaine is treated with disinfectant solutions containing heavy metals, the risk of local reactions such as pain and swelling increases. Potentiates the effect of direct anticoagulants.

Special precautions for use.

To reduce systemic effects, toxicity, and to prolong the effect during local anesthesia, procaine should be used in combination with vasoconstrictors (0.1% solution of epinephrine hydrochloride, at a rate of 1 drop per 2–5 mL of solution).

Skin tests with local anesthetics should be performed in individuals with confirmed previous reactions to these drugs. Special caution is required when testing local anesthetics containing adrenaline due to an increased frequency of false-negative reactions. Provocation tests are recommended if skin tests yield negative results. Testing of patients with proven allergy to local anesthetics should be performed only by allergologists experienced in drug allergy.

There is no international consensus regarding procedures for performing and interpreting skin tests with medicinal products. Multicenter studies to determine the optimal drug concentration, testing protocols, and to establish specificity, sensitivity, and safety have not yet been conducted. For most drugs, there are no validated testing procedures for diagnosing drug hypersensitivity, including recommended test concentrations.

To reduce and manage adverse reactions, antihistamines and corticosteroids should be used.

The drug is poorly suitable for surface anesthesia due to its weak ability to penetrate intact mucous membranes.

Monitoring of cardiovascular, respiratory, and central nervous system functions is required during administration of the drug. Use with caution in patients with severe liver, kidney, or heart diseases (heart blocks, arrhythmias, especially bradycardia), and in patients with a significant history of allergies.

When performing local anesthesia, with the same total dose administered, the toxicity of procaine increases as the concentration of the solution increases. Therefore, with higher concentrations, the total dose should be reduced or the solution diluted to a lower concentration (with sterile 0.9% sodium chloride solution).

The drug should be used with caution in patients with a significant history of allergies, conditions associated with reduced hepatic blood flow, progressive cardiovascular insufficiency (usually due to development of cardiac blocks and shock), inflammatory conditions or infection at the injection site, pseudocholinesterase deficiency, renal insufficiency, elderly patients (aged 65 and above), critically ill or weakened patients, and during pregnancy or breastfeeding, as well as during labor.

Use during pregnancy or breastfeeding.

The use of the drug during pregnancy or breastfeeding may be considered only after careful assessment of the expected benefit of therapy for the mother and the potential risk to the fetus/child. When used during labor, bradycardia, apnea, and seizures in the newborn are possible.

Ability to affect reaction speed when driving or operating machinery.

During treatment, caution is required when driving vehicles or engaging in other potentially hazardous activities requiring increased attention and rapid psychomotor reactions.

Administration and Dosage

For local anesthesia, the dose of the drug depends on the concentration, type of surgical procedure, method of administration, and the patient's condition and age.

For perinephric blockade, inject 50–70 mL of 0.5% (5 mg/mL) procaine solution into the perirenal tissue in adults.

For infiltration anesthesia, the following maximum doses have been established (for adults): initial single dose at the beginning of surgery — 0.75 g of 0.5% procaine solution (i.e., 150 mL). Subsequently, during each hour of surgery — not more than 2 g of 0.5% procaine solution (i.e., 400 mL).

Children. Use in children is contraindicated.

Overdose.

May occur only with administration of high doses of the drug.

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, increased nervous excitability, cold sweat, tachycardia, decreased arterial pressure approaching collapse, tremor, seizures, apnea, methemoglobinemia, respiratory depression, sudden cardiovascular collapse.

Effects on the central nervous system include fear, hallucinations, seizures, and motor agitation.

Treatment: in cases of overdose, administration of the drug must be immediately discontinued. When performing local anesthesia, the injection site may be infiltrated with adrenaline. General resuscitation measures: oxygen inhalation, artificial ventilation of the lungs if necessary. If seizures last longer than 15–20 seconds, they should be controlled by intravenous administration of thiopental (100–150 mg) or diazepam (5–20 mg). For arterial hypotension and/or myocardial depression, administer ephedrine intravenously (15–30 mg); in severe cases — detoxification and symptomatic therapy.

In case of intoxication following procaine injection into the muscle of the leg or arm, immediate application of a tourniquet is recommended to reduce further drug absorption into the systemic circulation.

Adverse Reactions

The medicinal product is generally well tolerated; however, the following adverse reactions may occasionally occur.

Sense organs: Visual and auditory disturbances, nystagmus.

Nervous system: Headache, dizziness, drowsiness, weakness, motor restlessness, loss of consciousness, seizures, trismus, tremor, cauda equina syndrome (leg paralysis, paresthesia), respiratory muscle paralysis, motor and sensory block, rebound pain, persistent anesthesia.

Cardiovascular system: Increased or decreased arterial pressure, peripheral vasodilation, collapse, bradycardia, arrhythmias, chest pain.

Urinary system: Involuntary urination.

Gastrointestinal system: Nausea, vomiting, involuntary defecation.

Blood system: Methemoglobinemia.

Immune system: Hypersensitivity reactions, including angioneurotic edema (including laryngeal edema), other anaphylactic reactions (including anaphylactic shock), urticaria (on skin and mucous membranes).

Skin and subcutaneous tissue: Skin itching, rash, dermatitis, skin desquamation, erythema, hyperemia.

General disorders: Hypothermia, increased sweating.

Reactions at the site of administration: When the injection site is treated with disinfectant solutions containing heavy metals, the risk of local reactions such as pain and swelling increases.

Reporting suspected adverse reactions

Reporting of suspected adverse reactions after medicinal product registration is of great importance. It enables ongoing monitoring of the benefit-risk balance of the medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy through the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua

Shelf life. 2 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C, in a place inaccessible to children. Keep ampoules in the outer carton.

Incompatibility. Do not use in treatment with sulfonamides.

Procaine solution is compatible with 0.9% sodium chloride solution.

Packaging. 2 ml or 5 ml in polymer ampoules, 10 ampoules per pack.

Prescription status. Prescription only.

Manufacturer. Private Joint-Stock Company "Infuziya".

Manufacturer's address and location of operations.

84A Nemirovskе Highway, village Vinnitski Khutory, Vinnitsa district, Vinnitsa region, 23219, Ukraine.