Novocaine

INSTRUCTIONS for medical use of the medicinal product NOVOCAIN (NOVOCAIN)

Composition:

Active substance: procaine hydrochloride (novocaine);

100 ml of solution contain procaine hydrochloride (novocaine) 0.5 g or 0.25 g;

Excipients: 0.1 M hydrochloric acid solution, water for injections.

Pharmaceutical form. Infusion solution.

Main physicochemical properties: clear, colorless or slightly yellowish 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 surface tension of the phospholipid layer of membranes, suppression of redox processes, and impulse generation. When absorbed into the bloodstream, it reduces acetylcholine formation, decreases excitability of peripheral cholinoreactive systems, exerts blocking action 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 blood plasma and tissues, forming two main pharmacologically active metabolites: diethylaminoethanol (which has moderate vasodilating activity) and para-aminobenzoic acid (which acts as a competitive antagonist of sulfonamide chemotherapeutic agents and may reduce their antimicrobial effect). The elimination half-life is 30–50 seconds; in neonates, it ranges from 54 to 114 seconds.

It is primarily excreted by the kidneys in the form of 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 any component of the drug.

Myasthenia gravis; 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 the creeping infiltration technique).

Interaction with other medicinal products and other types of interactions.

The drug reduces the effect of anticholinesterase agents on neuromuscular transmission. Prolongs neuromuscular blockade caused by succinylcholine (since both drugs are hydrolyzed by plasma cholinesterase). The metabolite of procaine (para-aminobenzoic acid) is a competitive antagonist of sulfonamide drugs and may weaken their antimicrobial action. Concurrent use with MAO inhibitors increases the risk of developing arterial hypotension. The toxicity of procaine is increased by anticholinesterase agents (which inhibit its hydrolysis). Cross-sensitization is possible. Intravenous administration of procaine potentiates the action of anesthetic agents.

When 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.

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

Skin tests with local anesthetics should be performed in individuals who have had confirmed reactions to these drugs. Particular caution is required when testing local anesthetics containing adrenaline due to an increased frequency of false-negative reactions. Provocation tests are recommended if skin tests yield negative results. Testing of patients with proven allergy to local anesthetics should be performed only by allergologists experienced in drug allergy.

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

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.

Monitoring of cardiovascular, respiratory, and central nervous system functions is required during drug administration. Use with caution in severe liver, kidney, or heart diseases (heart blocks, arrhythmias, especially bradycardia), and in patients with a history of allergies.

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 increases, the total dose should be reduced or the drug solution diluted to a lower concentration (with sterile 0.9% sodium chloride solution).

Use the drug cautiously in patients with a history of allergies, conditions associated with reduced hepatic blood flow, progressive cardiovascular insufficiency (usually due to development of heart blocks and shock), inflammatory conditions or infection at the injection site, pseudocholinesterase deficiency, renal insufficiency, elderly patients (aged 65 years and older), critically ill or weakened patients, and during pregnancy or breastfeeding.

Use during pregnancy or breastfeeding.

The use of the drug during pregnancy or breastfeeding is possible only after careful assessment of the expected therapeutic benefit for the mother and the potential risk to the fetus/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 vehicles or engaging in other potentially hazardous activities requiring increased attention and rapid psychomotor reactions, due to the possible development of nervous system adverse reactions (dizziness, drowsiness — see section "Adverse 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 kidney block, 50–70 mL of a 0.5% solution or 100–150 mL of a 0.25% solution of novocaine should be injected 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 of a 0.5% novocaine solution (i.e., 150 mL) or 1.25 g of a 0.25% novocaine solution (i.e., 500 mL). Thereafter, during each hour of surgery — no more than 2 g of a 0.5% novocaine solution (i.e., 400 mL) or no more than 2.5 g of a 0.25% novocaine solution (i.e., 1000 mL).

Children

Novocaine is contraindicated in children.

Overdose

In cases of overdose, administration of the drug should be immediately discontinued. When performing local anesthesia, the injection site may be infiltrated with adrenaline.

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 include feelings of fear, hallucinations, seizures, and motor agitation.

Treatment: general resuscitation measures, 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, administer ephedrine intravenously (15–30 mg); in severe cases — detoxification and symptomatic therapy.

In the event of intoxication following injection of novocaine 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; however, the following adverse reactions may occasionally occur.

Sensory organs: visual and auditory disturbances, nystagmus.

Nervous system: headache, dizziness, drowsiness, weakness, motor restlessness, loss of consciousness, seizures, trismus, tremor, cauda equina syndrome (leg paralysis, paresthesia), respiratory muscle paralysis, motor and sensory block, rebound pain, persistent anesthesia.

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

Urinary system: involuntary micturition.

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 desquamation, erythema, hyperemia.

General disorders: hypothermia, increased sweating.

Injection site reactions: when the injection site is treated with disinfectant solutions containing heavy metals, the risk of local reactions such as pain and swelling increases.

Shelf life. 3 years.

Storage conditions. Store at a temperature not exceeding 25 °C in a dark place, out of reach of children.

Incompatibility. Do not use in combination with sulfonamides.

Mixing with other infusion solutions:

Procaine solution is compatible with 0.9% sodium chloride solution (see section "Special precautions").

Packaging. 200 ml and 400 ml in bottles.

Prescription status. Prescription only.

Manufacturer. Private Joint-Stock Company "Infuziya".

Manufacturer's address and place of business activity.

84A Nemirovskе Shose St., Vinnytski Khotory, Vinnytsia District, Vinnytsia Region, Ukraine, 23219.