Novocain-zdorovya

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

Composition:

Active substance: procaine;

1 ml of solution contains procaine hydrochloride 20 mg;

Excipients: hydrochloric acid concentrated, water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear, colorless solution.

Pharmacotherapeutic group. Local anesthetics. ATC code N01B A02.

Pharmacological properties.

Pharmacodynamics.

A local anesthetic agent with moderate activity and a broad therapeutic range. The anesthetic mechanism of action is associated with blockade of sodium channels, inhibition of potassium current, competition with calcium in the surface tension of the phospholipid layer of membranes, suppression of redox processes, and impulse generation. Upon entering the bloodstream, it reduces acetylcholine production, decreases excitability of peripheral cholinoreactive systems, exerts blocking action on autonomic ganglia, reduces smooth muscle spasms, and lowers 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 on the total dose (volume and concentration of the solution). It is rapidly hydrolyzed by esterases and cholinesterases in 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 half-life (T½) is 30–50 seconds; in the neonatal period, it ranges from 54 to 114 seconds. It is primarily excreted by the kidneys as metabolites (80%); less than 2% is excreted unchanged. It is poorly absorbed through mucous membranes.

Clinical characteristics.

Indications.

Conduction, epidural, and spinal anesthesia in surgery, urology, ophthalmology, dentistry, otolaryngology; blockade of peripheral nerves and nerve plexuses.

Contraindications.

Hypersensitivity to the drug, cardiogenic shock, pronounced arterial hypotension, severe forms of chronic heart failure, reduced left ventricular function, second- to third-degree atrioventricular block, severe bradycardia, Adams-Stokes syndrome; history of seizures induced by procaine administration; sinoatrial node weakness syndrome, severe hepatic dysfunction, hypovolemia, hemorrhage, myasthenia gravis, infection at the site of lumbar puncture, sepsis, purulent processes at the site of drug administration, emergency surgical interventions associated with acute blood loss.

In glaucoma, retrobulbar administration of the drug is contraindicated.

Interaction with other medicinal products and other forms of interaction.

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

Concomitant use with monoamine oxidase inhibitors (MAOIs) – 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 the injection site of the local anesthetic is disinfected with antiseptic 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.

Skin tests with local anesthetics should be performed in individuals with documented reactions to these drugs. Special attention is required when testing local anesthetics containing epinephrine (adrenaline) 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 procedures for performing and interpreting skin tests with drugs. Multicenter studies to determine the appropriate drug concentration, testing protocol, and to establish specificity, sensitivity, and safety have not yet been conducted. For most drugs, there are no validated testing procedures for diagnosing drug hypersensitivity, including test concentrations.

Administration of procaine must be performed only by healthcare professionals.

• Extreme caution should be exercised during local anesthesia of tissues with rich vascularization (e.g., neck during thyroid surgery) to avoid intravascular injection.
• Lower doses of the drug should be used in the head and neck area, including retrobulbar and dental injections, as well as for stellate ganglion block, due to the risk of systemic toxic effects from retrograde penetration of the drug into cerebral circulation.
• The safety of using amide-type anesthetics in patients predisposed to malignant hyperthermia is questionable; therefore, their use should be avoided in such cases.
• Care must be taken to avoid accidental subdural or intravascular injection. Close monitoring for systemic toxic effects on the cardiovascular and central nervous systems is required (since doses intended for epidural anesthesia are always higher than those for subdural administration).
• Extreme caution is necessary when performing spinal anesthesia in patients with neurological disorders, spinal deformities, sepsis, or severe arterial hypertension.
• Before administering procaine in patients with heart disease (hypokalemia reduces lidocaine effectiveness), serum potassium levels should be normalized.
• Particular caution is required when using procaine in patients with circulatory insufficiency, arterial hypotension, hepatic or renal impairment. Caution is also advised when prescribing procaine to elderly patients (aged 65 years and older), patients with epilepsy, cardiac conduction disorders, respiratory insufficiency, pseudocholinesterase deficiency, critically ill or debilitated patients, and during pregnancy, childbirth, and breastfeeding.
• To reduce systemic effects, toxicity, and to prolong the anesthetic effect, procaine should be used in combination with vasoconstrictors during local anesthesia.

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 careful assessment of the expected benefit of therapy for the mother and the potential risk for the infant.

When used during childbirth, bradycardia, apnea, and seizures in the newborn are possible.

Ability to affect reaction speed when driving or operating machinery.

During treatment, patients should refrain from driving vehicles or engaging in other potentially hazardous activities requiring high concentration and rapid psychomotor responses, due to the possible occurrence of certain adverse reactions affecting the nervous system, sensory organs, and/or cardiovascular system (see section "Adverse reactions").

Method of administration and dosage.

The dose of the drug usually depends on the type of anesthesia, degree of tissue vascularization, required depth and duration of analgesia, as well as individual patient characteristics. It is recommended to administer the lowest effective dose.

Recommended doses:

*To obtain a 1% solution of novocaine, sterile 0.9% sodium chloride solution should be used.

For caudal and lumbar epidural blockade, administer 15–25 mL of a 2% solution. The maximum single dose volume should not exceed 25 mL. Repeat doses, usually 2–6 mL lower than the initial dose, should be administered at 40–50 minute intervals.

The maximum single dose for adults is 11 mg/kg body weight, but not exceeding the maximum total dose of 800 mg. Dosage should be reduced in elderly patients, debilitated patients, and patients with cardiovascular and/or hepatic diseases (see also section "Special precautions").

Children. Contraindicated in children.

Overdose.

May occur only with administration of high doses of the drug.

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, increased nervous excitability, cold sweat, tachycardia, decreased arterial pressure, almost 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.

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

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

In case of intoxication developing after intramuscular injection into the leg or arm, immediate application of a tourniquet is recommended to reduce further drug entry into systemic circulation.

Adverse Reactions

The drug is generally well tolerated; however, the following adverse reactions may occasionally occur.

Nervous system side effects: headache, motor restlessness, increased irritability, dizziness, drowsiness, weakness, loss of consciousness, seizures, trismus, tremor, cauda equina syndrome (leg paralysis, paresthesia), numbness of the tongue and perioral area, respiratory depression, paralysis of respiratory muscles, motor and sensory block, coma.

Sensory organs: visual and auditory disturbances, decreased visual acuity, tinnitus, photophobia, nystagmus.

Gastrointestinal system: nausea, vomiting, involuntary defecation.

Cardiovascular system: chest pain, increased or decreased arterial pressure, collapse, peripheral vasodilation, reduced cardiac output, bradycardia, arrhythmias, heart block, cardiac arrest.

Urinary system: involuntary urination.

Blood system: methemoglobinemia.

Immune system: skin itching, skin rashes, dermatitis, skin desquamation, eczema, erythema, angioneurotic edema (including laryngeal edema), other anaphylactic reactions (including anaphylactic shock), urticaria (on skin and mucous membranes).

Other: return of pain, prolonged anesthesia, hypothermia, increased sweating, back pain, local site reactions.

Shelf life. 3 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach of children.

Incompatibility. Do not use concomitantly with sulfonamides. Use only the recommended solvent.

Packaging. 2 ml in ampoules, pack of 10 in a box; 5x2, 10 in blister packs in a box.

Prescription category. Prescription only.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVIYA".

Manufacturer's address and place of business.

22 Shevchenko Street, Kharkiv, Kharkiv Oblast, 61013, Ukraine.