NOVOCAIN-ZDOROVYA

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT NOVOCAIN-ZDOROVYE (NOVOCAIN-ZDOROVYE)

Composition:

Active substance: procaine;

1 ml of solution contains 5 mg of procaine hydrochloride;

Excipients: concentrated hydrochloric acid, water for injections.

Pharmaceutical form. Solution for injection.

Main physico-chemical properties: clear, colorless solution.

Pharmacotherapeutic group. Local anesthetics. ATC code N01BA02.

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 for 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 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 site of injection) and 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 (which acts as a competitive antagonist of sulfonamide chemotherapeutic agents and may reduce their antimicrobial efficacy). The half-life (T½) 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%); no more than 2% is excreted unchanged. It is poorly absorbed through mucous membranes.

Clinical characteristics.

Indications. Local and infiltration anesthesia, therapeutic blocks.

Contraindications.

Hypersensitivity 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 creeping infiltration technique).

Interaction with other medicinal products and other types of interactions.

Prolongs neuromuscular blockade caused by succinylcholine (because both drugs are hydrolyzed by plasma cholinesterase). Concurrent use with monoamine oxidase inhibitors (MAO inhibitors) – furazolidone, procarbazine, selegiline – increases the risk of developing arterial hypotension. Anticholinesterase agents increase procaine toxicity (by inhibiting its hydrolysis). A metabolite of procaine (para-aminobenzoic acid) is a competitive antagonist of sulfonamide drugs and may reduce their antimicrobial activity.

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

The drug reduces the effect of anticholinesterase agents on neuromuscular transmission. Cross-sensitization is possible.

Special precautions for use.

Skin tests with local anesthetics should be performed in individuals with documented hypersensitivity reactions to these drugs, according to available evidence. Particular attention is required when testing local anesthetics containing epinephrine due to an increased incidence of false-negative results. Provocation testing is recommended if skin tests yield negative results. Testing of patients with confirmed allergy to local anesthetics should be performed only by allergologists experienced in drug allergy.

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

Monitoring of cardiovascular, respiratory, and central nervous system function is required during administration of the drug. Use with caution in patients with severe heart, liver, or kidney disease.

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

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 (using sterile 0.9% sodium chloride solution).

Use the drug with caution in patients with a history of allergic disorders, conditions associated with reduced hepatic blood flow, progressive cardiovascular insufficiency (usually due to development of cardiac block and shock), inflammatory conditions or infection at the injection site, pseudocholinesterase deficiency, renal insufficiency, in elderly patients (aged 65 years and older), critically ill or debilitated patients, and during pregnancy, labor, and breastfeeding.

Use during pregnancy or breastfeeding.

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

During breastfeeding, the use of the drug is possible only after a careful assessment of the expected benefit of therapy for the mother and the potential risk for the infant.

When used during labor, bradycardia, apnea, and seizures in the newborn are possible.

Ability to affect reaction rate 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 responses.

Method of Administration and Dosage

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

For paravertebral block (by Vishnevsky), 50–70 mL of a 0.5% solution (5 mg/mL) of the drug 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 exceeding 0.75 g of a 0.5% solution of novocaine (i.e., 150 mL). Subsequently, during each hour of surgery – not exceeding 2 g of a 0.5% solution of novocaine (i.e., 400 mL).

Children. The use of the drug in children is contraindicated.

Overdose.

May occur 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, almost to 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. In cases of overdose, administration of the drug must be immediately discontinued. When performing local anesthesia, the injection site may be infiltrated with adrenaline.

Treatment: 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). In cases of arterial hypotension and/or myocardial depression, administer ephedrine intravenously (15–30 mg); in severe cases – detoxification and symptomatic therapy.

In case of intoxication developing after injection into the muscles of the leg or arm, immediate application of a tourniquet is recommended to reduce further entry of the drug into the systemic circulation.

Adverse reactions.

The drug is generally well tolerated, but sometimes the following adverse reactions may occur.

Nervous system side effects: headache, dizziness, drowsiness, weakness, motor restlessness, loss of consciousness, seizures, trismus, tremor, visual and auditory disturbances, nystagmus, cauda equina syndrome (paralysis of legs, paresthesia), respiratory muscle paralysis, motor and sensory block.

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

Urinary system side effects: involuntary urination.

Gastrointestinal side effects: nausea, vomiting, involuntary defecation.

Blood system side effects: methemoglobinemia.

Immune system side effects: skin itching, skin rashes, dermatitis, skin desquamation, other anaphylactic reactions (including angioneurotic edema, anaphylactic shock), urticaria (on skin and mucous membranes).

Other side effects: return of pain, persistent anesthesia, hypothermia, changes at the injection site.

Shelf life. 3 years.

Storage conditions. Store in original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Incompatibility. Do not use concomitantly with sulfonamides.

Packaging. 2 ml in vials, 10 in a box; 5×2, 10 in blister packs in a box. 5 ml in vials, 10 in a box; 5×2 in blisters in a box.

Prescription status. Prescription only.

Manufacturer.

LIMITED LIABILITY COMPANY "CORPORATION "ZDOROV'YA".

Manufacturer's address and place of business.

22, Shevchenko Street, Kharkiv, Kharkiv Oblast, 61013, Ukraine.