Novocaine

INSTRUCTIONS for medical use of the medicinal product NOVOCAIN (NOVOCAIN)

Composition:

Active substance: procaine hydrochloride;

1 ml of solution contains procaine hydrochloride 5 mg;

Excipients: diluted hydrochloric acid, water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear, colorless liquid.

Pharmacotherapeutic group. Local anesthetic agents. Aminoethyl esters of benzoic acid. Procaine. ATC code N01B A02.

Pharmacological Properties

Pharmacodynamics. A local anesthetic agent with moderate activity and a broad therapeutic spectrum. The mechanism of anesthetic action is associated with blockade of sodium channels, inhibition of potassium current, competition with calcium, reduction of 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 blocking effects 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 rate at the injection site) as well as on the total dose (quantity and concentration). It is rapidly hydrolyzed by esterases and cholinesterases in plasma and tissues, forming two main pharmacologically active metabolites: diethylaminoethanol (which has moderate vasodilatory activity) and para-aminobenzoic acid (a competitive antagonist of sulfonamide chemotherapeutic agents, which may reduce their antimicrobial efficacy). The elimination half-life is 30–50 seconds; in neonates, it ranges from 54 to 114 seconds. The drug is excreted predominantly by the kidneys as metabolites (80%); less than 2% is excreted unchanged.

Poorly absorbed through mucous membranes.

Clinical Characteristics

Indications. For local and infiltration anesthesia, therapeutic blocks.

Contraindications

Increased individual sensitivity to the drug.

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

Interaction with other medicinal products and other types of interactions

Procaine prolongs neuromuscular blockade caused by succinylcholine (since both drugs are hydrolyzed by plasma cholinesterase).

Concomitant use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of developing arterial hypotension.

Anticholinesterase agents increase procaine toxicity (by inhibiting its hydrolysis). The drug reduces the effect of anticholinesterase agents on neuromuscular transmission. Cross-sensitization is possible.

Procaine metabolite (para-aminobenzoic acid) is a competitive antagonist of sulfonamide drugs and may reduce their antimicrobial activity.

Intravenous administration of procaine potentiates the effect of anesthetic agents. When the injection site 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 and eliminate adverse reactions, antihistamines and corticosteroids should be used. The drug is poorly suitable for topical anesthesia due to its weak ability to penetrate intact mucous membranes.

To reduce systemic effects, toxicity, and to prolong the effect during local anesthesia, procaine is used in combination with vasoconstrictors (0.1% solution of epinephrine hydrochloride, 1 drop per 2–5 ml of solution). The drug should be used with caution in case of infection at the injection site.

Skin tests with local anesthetics should be performed in individuals who have had confirmed reactions to these drugs. Particular attention is required when testing local anesthetics containing adrenaline due to an increased frequency of false-negative skin test results. Testing of patients with confirmed allergic reactions to local anesthetics should be performed only by allergologists with appropriate experience.

When using the drug, functions of the cardiovascular, respiratory, and central nervous systems should be monitored. Use with caution in severe heart diseases (heart blocks, arrhythmias, especially bradycardia), liver and kidney diseases, and in patients with a significant history of allergies.

When used for local anesthesia, the toxicity of procaine is higher with more concentrated solutions, even when the same total dose is administered. Therefore, as the solution concentration increases, the total dose should be reduced or the drug solution should be diluted to a lower concentration (with sterile isotonic sodium chloride solution).

The drug should be used with caution in conditions associated with reduced hepatic blood flow, progressive cardiovascular insufficiency (usually due to development of heart blocks and shock), inflammatory diseases, pseudocholinesterase deficiency, renal insufficiency, in elderly patients (over 65 years), critically ill, and debilitated patients.

Use during pregnancy or breastfeeding. Use during pregnancy is possible only if well tolerated.

During breastfeeding, the drug may be used only after careful assessment of the expected benefit of therapy for the mother and the potential risk to the infant.

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 necessary when driving vehicles or engaging in other potentially hazardous activities requiring increased attention and speed of 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 paravertebral block, 50–70 mL of 0.5% (5 mg/mL) procaine solution should be administered 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 — not more than 0.75 g (i.e., 150 mL of 0.5% procaine solution); thereafter, during each hour of surgery — not more than 2 g (i.e., 400 mL of 0.5% procaine solution).

Children. Do not use in children (under 18 years of age).

Overdose

Overdose is possible only when the drug is used in high doses.

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 manifest as fear, hallucinations, convulsions, and motor agitation.

Treatment. In case of overdose, administration of the drug should be immediately discontinued. Initiate general resuscitation measures, including oxygen inhalation; if necessary, perform artificial ventilation of the lungs. If seizures persist for more than 15–20 seconds, they should be controlled by intravenous administration of thiopental (100–150 mg) or diazepam (5–20 mg). In cases of arterial hypotension and/or myocardial depression, administer ephedrine intravenously (15–30 mg); in severe cases, apply detoxification and symptomatic therapy.

When performing local anesthesia, the injection site may be surrounded by adrenaline. In case of intoxication following procaine injection into the muscles of the leg or arm, a tourniquet should be urgently applied to reduce further entry of the drug into the systemic circulation.

Adverse Reactions

Novocaine is generally well tolerated; however, the following adverse effects may occasionally occur:

Sense organs: Visual and auditory disturbances, nystagmus.

Gastrointestinal tract: Nausea, vomiting, involuntary defecation.

Kidneys and urinary system: Involuntary urination.

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, return of pain, persistent anesthesia.

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

Blood and lymphatic 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, skin rashes, dermatitis, skin peeling, erythema, hyperemia.

General disorders: Hypothermia, increased sweating.

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

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after drug registration is important. It enables ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of drug efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Incompatibility. Do not use in combination with sulfonamides.

Packaging. 2 ml or 5 ml in polyethylene ampoules. 10 or 50 ampoules per cardboard pack.

Prescription status. Prescription only.

Manufacturer. LLC "FARMASEL".

Manufacturer's address and place of business.

3, Prorizna Street, Kvitneve, Brovary District, Kyiv Oblast, 07408, Ukraine.