Novocaine

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

Composition:

Active substance: novocaine (procaine hydrochloride);

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

Excipient: water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear, colorless liquid.

Pharmacotherapeutic group. Local anesthetics.

ATC code: N01B A02.

Pharmacological Properties

Pharmacodynamics

A local anesthetic agent with moderate activity and a wide therapeutic range. 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 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 rate at the injection site) as well as 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 (a competitive antagonist of sulfonamide chemotherapeutic agents, potentially reducing 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.

It is 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 creeping infiltration technique).

Interaction with other medicinal products and other types of interactions

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

Intravenous administration of procaine potentiates the effect of anesthetic agents.

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

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

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

If the injection site of procaine 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

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

When using the drug, monitoring of cardiovascular, respiratory, and central nervous system functions is required. Use with caution in patients with severe liver, kidney, or heart diseases (e.g., conduction blocks, arrhythmias, especially bradycardia), and in those with a history of severe allergies.

To reduce and eliminate 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.

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

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

Skin tests with local anesthetics should be performed in individuals with documented hypersensitivity reactions to these drugs. Special attention is required when testing local anesthetics containing adrenaline (epinephrine), due to an increased frequency of false-negative results. Provocation tests are 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 no international consensus regarding the procedures for performing and interpreting skin tests with drugs. Multicenter studies have not yet been conducted to determine the appropriate drug concentration, testing protocol, specificity, sensitivity, and safety. For most drugs, there are no validated testing procedures for diagnosing hypersensitivity, particularly regarding the determination of test concentrations.

Use during pregnancy or breastfeeding

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

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

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

Ability to affect reaction speed when driving or operating machinery

During treatment, caution should be exercised when driving vehicles or engaging in other potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Method of Administration and Dosage

The dose of the drug for local anesthesia 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 – 0.75 g (150 mL of 0.5% procaine solution). Subsequently, during each hour of surgery – not more than 2 g (400 mL of 0.5% procaine solution).

Children

Use in children (under 18 years of age) is contraindicated.

Overdose

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

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

In the event of intoxication following procaine injection into the muscles of the arm or leg, immediate application of a tourniquet is recommended to reduce further drug entry 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, somnolence, 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.

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 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 suspected adverse reactions after medicinal product registration is of great importance. It enables continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare 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

3 years.

Storage conditions

Store in the original packaging at a temperature not exceeding 25 ºC. Keep out of reach of children.

Incompatibility

Do not use in combination with sulfonamides.

Packaging. 5 ml in an ampoule, 5 ampoules in a blister pack, 2 blister packs in a carton.

Prescription status. Prescription only.

Manufacturer

JSC "Halychfarm".

Manufacturer's name and address of place of business

6/8 Opryshkivska Street, Lviv, 79024, Ukraine.