Novocaine

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

Composition:

Active substance: procaine;

1 ml of solution contains procaine hydrochloride 5 mg;

Excipients: 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 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. Upon entering the bloodstream, it reduces acetylcholine production, decreases excitability of peripheral cholinoreactive systems, blocks 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) 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 (exerts moderate vasodilatory effects) and para-aminobenzoic acid (acts as a competitive antagonist of sulfonamide chemotherapeutic agents and may reduce their antimicrobial activity). The half-life elimination is 30–50 seconds; in newborns, it ranges from 54 to 114 seconds. It is primarily excreted by the kidneys in the form of metabolites (80%); less than 2% is excreted unchanged.

Poorly absorbed by 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.

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. The toxicity of procaine is increased by anticholinesterase agents (by inhibiting its hydrolysis). A metabolite of procaine (para-aminobenzoic acid) acts as a competitive antagonist of sulfonamide drugs and may reduce their antimicrobial effect.

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 anticoagulants.

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

Special precautions for use.

To reduce and eliminate adverse reactions, antihistamines and corticosteroids should be used. Procaine 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 in case of infection at the injection site.

During use of the drug, monitoring of cardiovascular, respiratory, and central nervous system functions is required. The drug should be administered with caution in severe heart, liver, and kidney diseases.

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

Use during pregnancy or breastfeeding.

Use during pregnancy is possible if well tolerated.

During breastfeeding, the drug may be used 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 should be exercised when driving vehicles or engaging in other potentially hazardous activities requiring increased attention 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 perinephric block, 50–70 mL of 0.5% (5 mg/mL) procaine solution 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% procaine solution); thereafter, no more than 2 g per hour of surgery (i.e., 400 mL of 0.5% procaine solution).

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

Overdose.

Possible only when procaine 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 up to collapse, tremor, convulsions, apnea, methemoglobinemia, respiratory depression, sudden cardiovascular collapse.

Effects on the central nervous system manifest as fear, hallucinations, convulsions, and motor agitation. In case 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, and if necessary, artificial ventilation of the lungs. If convulsions last longer than 15–20 seconds, they should be controlled by intravenous administration of thiopental (100–150 mg) or diazepam (5–20 mg). In case of arterial hypotension and/or myocardial depression, ephedrine (15–30 mg) is administered intravenously; in severe cases – detoxification and symptomatic therapy.

In case of intoxication following procaine injection into the muscles of the leg or arm, immediate application of a tourniquet is recommended to reduce further drug entry 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 angioneurotic edema, anaphylactic shock), urticaria (on skin and mucous membranes).

Other: hypothermia.

Shelf life.

2 years.

Storage conditions.

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

Incompatibility. Do not use concomitantly with sulfonamides.

Packaging.

5 ml in ampoules. 10 ampoules per partitioned box; or 5 ampoules per blister, 2 blisters per box; or 100 ampoules per partitioned box.

Prescription category.

Prescription only.

Manufacturer.

Private Joint-Stock Company "Lekhym-Kharkiv".

Manufacturer's address.

36 Severina Pototskogo Street, Kharkiv, Kharkiv region, 61115, Ukraine.