Novocaine-Vial (Solution) Instructions for Use

ATC Code

N01BA02 (Procaine)

Active Substance

Procaine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Local anesthetic

Pharmacotherapeutic Group

Anesthetics; local anesthetics; aminobenzoic acid esters

Pharmacological Action

A local anesthetic agent with moderate anesthetic activity and a wide therapeutic range. Being a weak base, it blocks sodium channels, prevents the generation of impulses in the endings of sensory nerves and the conduction of impulses along nerve fibers.

It alters the action potential in the membranes of nerve cells without a pronounced effect on the resting potential. It suppresses the conduction of not only pain impulses but also impulses of other modalities.

Upon absorption and direct vascular administration into the bloodstream, it reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic endings (has some ganglion-blocking action), relieves spasm of smooth muscles, reduces the excitability of the myocardium and the motor areas of the cerebral cortex.

It eliminates the descending inhibitory influences of the brainstem reticular formation. It depresses polysynaptic reflexes. It has short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 hour).

Pharmacokinetics

It undergoes complete systemic absorption. The degree of absorption depends on the site and route of administration (especially on vascularization and blood flow rate at the injection site) and the final dose (amount and concentration).

Procaine is rapidly hydrolyzed by plasma and liver esterases to form two main pharmacologically active metabolites: diethylaminoethanol (which has a moderate vasodilating effect) and p-aminobenzoic acid (which is a competitive antagonist of sulfonamide drugs and may weaken their antimicrobial effect).

T_1/2 is 30-50 sec, in the neonatal period it is 54-114 sec. It is excreted mainly by the kidneys in the form of metabolites; no more than 2% is excreted unchanged.

Indications

Infiltration (including intraosseous), conduction, retrobulbar (regional), epidural anesthesia; vagosympathetic cervical, paranephric, circular and paravertebral blockades.

ICD codes

Dosage Regimen

Determine the dosage individually based on the type of anesthesia, procedure, patient condition, and age.

For infiltration anesthesia, use a 0.25% or 0.5% solution. The maximum single dose is 500 ml of a 0.25% solution or 200 ml of a 0.5% solution.

For conduction anesthesia, use a 1% or 2% solution. Do not exceed 100 ml of a 1% solution or 50 ml of a 2% solution as a single dose.

For epidural anesthesia, administer 15-25 ml of a 0.5% solution or 10-15 ml of a 1% solution.

For retrobulbar anesthesia, inject 2-4 ml of a 1%, 2%, or 4% solution.

For therapeutic blockades (e.g., cervical, paranephric), use 5-100 ml of a 0.25% or 0.5% solution depending on the blockade type and anatomical region.

Always perform an aspiration test in two stages prior to injection to prevent accidental intravascular administration.

Reduce the total dose for debilitated, elderly, or pediatric patients. The maximum single dose for a healthy adult is 1 gram of procaine.

Use the lowest effective dose and concentration to achieve the desired anesthetic effect and minimize toxicity risk.

Adverse Reactions

From the nervous system headache, dizziness, drowsiness, persistent anesthesia, weakness, motor restlessness, nervousness, loss of consciousness, convulsions, trismus, tremor, visual and auditory disturbances, nystagmus, cauda equina syndrome (paralysis of the legs, paresthesia), paralysis of the respiratory muscles, motor and sensory block.

From the cardiovascular system increase or decrease in blood pressure, collapse, peripheral vasodilation, bradycardia, arrhythmia, chest pain, changes in the process of excitation propagation in the heart, which are manifested on the ECG as a flat T wave or shortening of the ST segment.

From the respiratory system respiratory tract spasms or difficulty breathing.

From the digestive system nausea, vomiting.

Allergic reactions skin itching, skin rash, angioedema, anaphylactic reactions (including anaphylactic shock), urticaria.

Other involuntary urination, methemoglobinemia, hypothermia, shivering, swelling of the lips, face, mouth, tongue and throat.

Contraindications

Hypersensitivity to procaine; children under 12 years of age; pronounced fibrotic changes in tissues (for anesthesia by the creeping infiltrate method).

With caution emergency operations accompanied by acute blood loss; conditions accompanied by reduced hepatic blood flow (e.g., in chronic heart failure, liver diseases); progression of cardiovascular failure (usually due to the development of heart block and shock); inflammatory diseases or infection of the injection site; pseudocholinesterase deficiency; renal failure; children (from 12 to 18 years); elderly patients (over 65 years); debilitated patients.

Use in Pregnancy and Lactation

During pregnancy and breastfeeding, it should be used only after consultation with a doctor, in cases where the intended benefit to the mother outweighs the potential risk to the fetus or infant.

Use in Hepatic Impairment

It should be used with caution in patients with conditions accompanied by reduced hepatic blood flow (e.g., with liver diseases).

Use in Renal Impairment

It should be used with caution in patients with renal failure.

Pediatric Use

Contraindicated in children under 12 years of age. It should be used with caution in children and adolescents aged 12-18 years.

Geriatric Use

It should be used with caution in elderly patients (over 65 years).

Special Precautions

Anesthesia should be performed by experienced specialists in an appropriately equipped room with readily available equipment and drugs necessary for cardiomonitoring and resuscitation.

To prevent accidental intravascular injection, it is recommended to perform an aspiration test (in 2 stages).

When using the product, monitoring of the function of the cardiovascular and respiratory systems, and the CNS is required.

The use of MAO inhibitors is contraindicated for at least 10 days before the use of procaine.

Before using procaine, it is necessary to perform tests for individual sensitivity.

It should be taken into account that during local anesthesia when using the same total dose, the toxicity of procaine is higher the more concentrated the solution used.

It is not absorbed from the mucous membranes; it does not provide superficial anesthesia when applied to the skin.

Effect on the ability to drive vehicles and mechanisms

During the use of procaine, patients should exercise caution when driving vehicles and mechanisms, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use, Procaine enhances the inhibitory effect on the CNS of general anesthetics, hypnotics and sedatives, narcotic analgesics and tranquilizers.

With simultaneous use, anticoagulants (ardeparin sodium, dalteparin sodium, danaparoid sodium, enoxaparin sodium, heparin sodium, warfarin) increase the risk of bleeding.

When treating the injection site of a local anesthetic with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of soreness and swelling increases.

With simultaneous use of procaine with MAO inhibitors (furazolidone, procarbazine, selegiline) increases the risk of hypotension.

With simultaneous use, Procaine enhances and prolongs the action of muscle relaxants.

When procaine is used together with narcotic analgesics, an additive effect is noted, which is used during spinal and epidural anesthesia, while respiratory depression is enhanced.

With simultaneous use, vasoconstrictors (epinephrine, methoxamine, phenylephrine) prolong the local anesthetic action of procaine.

With simultaneous use, Procaine reduces the antimyasthenic effect of drugs, especially when used in high doses, which requires additional correction of myasthenia gravis treatment.

With simultaneous use, cholinesterase inhibitors (antimyasthenic drugs, cyclophosphamide, demecarium bromide, ecothiopate iodide, thiotepa) reduce the metabolism of procaine.

The metabolite of procaine (p-aminobenzoic acid) is an antagonist of sulfonamides.

When using local anesthetics for epidural anesthesia with guanadrel, with guanethidine, mecamylamine, trimethaphan camsilate, the risk of a sharp decrease in blood pressure and bradycardia increases.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.