NOVOCAINE-DARNITSA

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

Composition:

Active substance: procaine;

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

Excipients: hydrochloric acid, water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear colorless liquid.

Pharmacotherapeutic group. Medicinal products for local anesthesia. Amino benzoic acid esters. Procaine. ATC code N01B A02.

Pharmacological properties.

Pharmacodynamics.

A local anesthetic agent with moderate activity and a broad therapeutic range. The anesthetic mechanism of 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 impulse generation. When absorbed into the bloodstream, it reduces acetylcholine formation, 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 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 (which acts as a competitive antagonist of sulfonamide chemotherapeutic agents and may reduce their antimicrobial activity). The elimination half-life is 30–50 seconds; in the neonatal period, it ranges from 54 to 114 seconds. It is excreted predominantly by the kidneys as metabolites (80%); not more than 2% is excreted unchanged.

Poorly absorbed through mucous membranes.

Clinical characteristics.

Indications.

Local and infiltration anesthesia, therapeutic blocks.

Contraindications.

Increased individual sensitivity to the drug.

Myasthenia; arterial hypotension; purulent processes at the injection site; emergency surgical interventions accompanied by acute blood loss; pronounced 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 medicinal products and may reduce their antimicrobial activity.

Intravenous administration of novocaine 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 absorption and prolong the action of procaine solutions in local anesthesia, a 0.1% solution of adrenaline hydrochloride should be added – 1 drop per 2, 5, or 10 ml of procaine solution.

Skin tests with local anesthetics should be performed in individuals with a history of confirmed reactions to these drugs. Particular attention is required when testing local anesthetics containing adrenaline, due to an increased incidence of false-negative reactions. Provocation tests are recommended if skin tests yield negative results. Testing of patients with a confirmed allergic reaction to local anesthetics should only be performed by allergologists experienced in drug allergy.

When administering the drug, functions of the cardiovascular, respiratory, and central nervous systems must be monitored. The drug should be used with caution in patients with severe heart disease (heart blocks, arrhythmias, especially bradycardia), liver or kidney disease, and a significant history of allergic disorders.

During local anesthesia, when the same total dose is used, the toxicity of procaine increases with higher concentrations of the solution. Therefore, as the concentration increases, the total dose should be reduced or the drug solution diluted to a lower concentration with sterile isotonic sodium chloride solution.

The drug should be used cautiously 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 (aged 65 years and older), critically ill or debilitated patients, and during pregnancy or breastfeeding, as well as during labor.

Use during pregnancy or breastfeeding.

Use during pregnancy is possible if the drug is well tolerated.

During breastfeeding, the use of the drug may be considered only after a careful assessment of the expected therapeutic benefit for the mother and the potential risk for the infant.

When used during labor, bradycardia, apnea, and seizures may occur in the newborn.

Ability to affect reaction speed when driving or operating machinery.

During treatment, caution is required when driving or operating other potentially hazardous machinery requiring increased attention and rapid psychomotor reactions, due to the possibility of certain adverse reactions affecting the nervous system, sensory organs, and/or cardiovascular system (see section "Adverse reactions").

Administration and Dosage

In 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 injected into the perirenal tissue in adults. For infiltration anesthesia, the following maximum doses have been established (for adults): the initial single dose at the beginning of surgery should not exceed 0.75 g (i.e., 150 mL of 0.5% procaine solution). Thereafter, during each hour of surgery, the dose should not exceed 2 g (i.e., 400 mL of 0.5% procaine solution).

Children

The use of this medicinal product in children is contraindicated.

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 blood pressure approaching collapse, tremor, seizures, apnea, methemoglobinemia, respiratory depression, sudden cardiovascular collapse.

Effects on the central nervous system may manifest as fear, hallucinations, seizures, and motor agitation.

Treatment: In cases of overdose, administration of the drug must be immediately discontinued. General resuscitation measures should be initiated, including oxygen inhalation and, if necessary, 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, intravenous ephedrine (15–30 mg) should be administered; in severe cases, detoxification and symptomatic therapy are required.

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

Adverse reactions.

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

From the sensory organs: visual and auditory disturbances, nystagmus.

From the gastrointestinal tract: nausea, vomiting, involuntary defecation.

From the kidneys and urinary system: involuntary urination.

From the nervous system: headache, dizziness, drowsiness, weakness, motor restlessness, loss of consciousness, seizures, trismus, tremor, cauda equina syndrome (paralysis of legs, paresthesia), respiratory muscle paralysis, motor and sensory block, return of pain, persistent anesthesia.

From the cardiovascular system: increased or decreased arterial pressure, peripheral vasodilation, collapse, bradycardia, arrhythmias, chest pain.

From the blood and lymphatic system: methemoglobinemia.

From the immune system: hypersensitivity reactions, including angioneurotic edema (including laryngeal edema), other anaphylactic reactions (including anaphylactic shock), urticaria (on skin and mucous membranes).

From the skin and subcutaneous tissue: skin itching, skin rashes, dermatitis, skin peeling, erythema, hyperemia.

General disorders: hypothermia, increased sweating.

Reactions at the injection site: 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 of suspected adverse reactions after drug registration is an important procedure. It allows continuous monitoring of the benefit-risk balance for the respective medicinal product. Healthcare professionals should report any suspected adverse reactions through the national reporting system.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze.

Keep out of reach of children.

Packaging.

2 ml or 5 ml in an ampoule; 5 ampoules in a contour cellular pack; 2 contour cellular packs in a box.

Prescription category. Prescription only.

Manufacturer. JSC "Pharmaceutical Company "Darnitsya".

Manufacturer's location and address of business activity.

13, Borispilska Street, Kyiv, 02093, Ukraine.