Novocaine

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

Composition:

Active substance: procaine;

1 ml of solution contains 5 mg of procaine hydrochloride;

Excipients: concentrated hydrochloric acid, water for injections.

Pharmaceutical form. Injection solution.

Main physico-chemical properties: clear, colorless solution, practically free from particles.

Pharmacotherapeutic group.
Preparations for local anesthesia. ATC code N01B A02.

Pharmacological properties.

Pharmacodynamics.

A local anesthetic agent with moderate activity and a wide therapeutic range. The anesthetic mechanism of 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 a blocking effect on autonomic ganglia, reduces smooth muscle spasms, and decreases excitability of myocardial tissue 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 (amount and concentration). It is rapidly hydrolyzed by esterases and cholinesterases in plasma and tissues, forming two main pharmacologically active metabolites: diethylaminoethanol (exerts moderate vasodilatory effect) and para-aminobenzoic acid (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%); no 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 site of injection, 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 (since 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). The metabolite of procaine (para-aminobenzoic acid) acts as a competitive antagonist of sulfonamide drugs and may reduce their antimicrobial activity.

When disinfectant solutions containing heavy metals are used to treat the injection site of a local anesthetic, the risk of local reactions such as pain and swelling increases. Potentiates the effect of direct anticoagulants.

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

Intravenous administration of novocaine potentiates the action of anesthetic agents.

Special precautions for use.

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 (epinephrine) in their formulation, due to the increased frequency of false-negative reactions. Provocation tests are recommended if skin tests yield negative results. Testing of patients with confirmed allergic reactions to local anesthetics should be performed only by allergologists with appropriate experience.

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.

To reduce systemic effects, toxicity, and to prolong the anesthetic effect, procaine is used in combination with vasoconstrictors (0.1% epinephrine hydrochloride solution, at a rate of 1 drop per 2–5 mL of solution). The drug should be used with caution if the injection site is infected.

When using the drug, monitoring of cardiovascular, respiratory, and central nervous system functions is required. Use with caution in patients with severe heart, liver, or kidney diseases and a significant history of allergies.

When used for local anesthesia, the higher the concentration of the solution, the greater the toxicity of procaine for the same total dose. Therefore, with increasing concentration, the total dose should be reduced or the solution diluted to a lower concentration (using 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 cardiac block and shock), inflammatory diseases, pseudocholinesterase deficiency, renal insufficiency, in elderly patients (over 65 years), and in severely ill or weakened patients.

Use during pregnancy or breastfeeding.

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

During breastfeeding, the drug may be used only after 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 in the newborn are possible.

Ability to affect reaction speed when driving or operating machinery.

During treatment, caution is required when driving or performing other potentially hazardous activities requiring high concentration 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 paravertebral block, 50–70 mL of 0.5% (5 mg/mL) solution of Novocaine is 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 (i.e., 150 mL of 0.5% Novocaine solution); thereafter, no more than 2 g (i.e., 400 mL of 0.5% Novocaine solution) per each hour of surgery.

Children

Novocaine is not administered to children under 18 years of age.

Overdose

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 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, including oxygen inhalation; 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, ephedrine (15–30 mg) should be administered intravenously; in severe cases – detoxification and symptomatic therapy.

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

Adverse Reactions.

Central and peripheral nervous system: 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, rebound pain, persistent anesthesia.

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

Urinary system: involuntary urination.

Gastrointestinal system: nausea, vomiting, involuntary defecation.

Blood system: methemoglobinemia.

Allergic reactions: skin itching, rash, dermatitis, skin desquamation, other anaphylactic reactions (including angioedema, anaphylactic shock), urticaria (on skin and mucous membranes).

Other: hypothermia.

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.

5 ml in a vial; 5 vials in a blister pack made of film, 1 or 2 blisters per carton.

5 ml in a vial; 10 vials in a cardboard carton with cardboard dividers.

Prescription status. Prescription only.

Manufacturer.

JSC "Lubnifarm".

Manufacturer's address and location of business activity.

16, Barvinkova Street, Lubny, Poltava region, 37500, Ukraine.