Novocaine-darnitsa

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

Composition:

Active substance: procaine;

1 ml of solution contains 20 mg of novocaine (procaine hydrochloride);

Excipients: hydrochloric acid, water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear colorless liquid.

Pharmacotherapeutic group. Local anesthetics. Amino-benzoic acid esters. Procaine. ATC code N01B A02.

Pharmacological properties.

Pharmacodynamics.

Novocaine is a local anesthetic agent with moderate activity and a broad therapeutic range. The mechanism of anesthetic action is associated with blockade of sodium channels, inhibition of potassium current, competition with calcium in the 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 blocking effects 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 the total dose (volume and concentration of the solution). It is rapidly hydrolyzed by plasma and tissue esterases and cholinesterases, forming two main pharmacologically active metabolites: diethylaminoethanol (which has moderate vasodilatory activity) and para-aminobenzoic acid (a competitive antagonist of sulfonamide chemotherapeutic agents, which may reduce their antimicrobial efficacy). 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%); up to 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 procaine; cardiogenic shock; marked arterial hypotension; severe forms of chronic heart failure; impaired left ventricular function; second- and third-degree atrioventricular block; severe bradycardia; Adams–Stokes syndrome; history of seizures induced by procaine; sinoatrial node weakness syndrome; severe liver function impairment; hypovolemia; hemorrhage; myasthenia; infection at the site of lumbar puncture; septicemia; 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 interactions.

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

Concomitant use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of developing arterial hypotension.

The toxicity of procaine is increased by anticholinesterase drugs (which inhibit its hydrolysis). The drug reduces the effect of anticholinesterase agents on neuromuscular transmission.

A metabolite of procaine (para-aminobenzoic acid) is a competitive antagonist of sulfonamide drugs and may reduce their antimicrobial activity.

Cross-sensitization is possible.

Intravenous administration of procaine potentiates the effect of anesthetic agents. When the injection site is treated with disinfectant solutions containing heavy metals, the risk of local reactions such as pain and swelling increases.

Potentiates the action of direct-acting anticoagulants.

Special precautions for use.

Skin tests with local anesthetics should be performed in individuals who have had confirmed reactions to these medicinal agents. Special 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 a confirmed allergic reaction to local anesthetics should be performed only by allergologists experienced in drug allergy.

Administration of novocaine may be performed only by healthcare professionals.

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

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 benefit to the mother and the potential risk to 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, patients should refrain from driving and from 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").

Administration and dosage.

The dosage of the medicinal product usually depends on the type of anesthesia, degree of tissue vascularization, required depth and duration of analgesia, as well as on individual patient characteristics. The lowest effective dose should be administered.

Recommended doses:

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

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

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

Children.

The use of this medicinal product in children is contraindicated.

Overdose.

Overdose is possible only when novocaine 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 approaching collapse, tremor, seizures, apnea, methemoglobinemia, respiratory depression, sudden cardiovascular collapse.

Effects on the central nervous system manifest as fear, hallucinations, seizures, 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 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 should be administered.

In case of intoxication following intramuscular injection into the leg or arm, a tourniquet should be urgently applied to reduce further entry of the drug into the systemic circulation.

Adverse Reactions

The medicinal product is generally well tolerated; however, the following adverse effects may occasionally occur.

Eye and ear disorders: Visual and auditory disturbances, decreased visual acuity, tinnitus, photophobia, nystagmus.

Gastrointestinal disorders: Nausea, vomiting, involuntary defecation.

Renal and urinary disorders: Involuntary urination.

Nervous system disorders: Headache, motor restlessness, increased irritability, dizziness, somnolence, weakness, loss of consciousness, seizures, trismus, tremor, cauda equina syndrome (paralysis of legs, paresthesia), numbness of the tongue and perioral area, respiratory depression, paralysis of respiratory muscles, motor and sensory block, return of pain, prolonged anesthesia, coma.

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

Blood and lymphatic system disorders: Methemoglobinemia.

Immune system disorders: Hypersensitivity reactions, including angioneurotic edema (including laryngeal edema), other anaphylactic reactions (including anaphylactic shock), urticaria (on skin and mucous membranes).

Skin and subcutaneous tissue disorders: Skin itching, skin rashes, dermatitis, skin desquamation, eczema, erythema, hyperemia.

General disorders: Hypothermia, increased sweating, back pain.

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.

Reporting of suspected adverse reactions.

Reporting of suspected adverse reactions after marketing authorization of the medicinal product is an important procedure. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reactions through the national reporting system.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze.

Keep out of reach of children.

Packaging.

2 ml in a vial; 5 vials in a blister pack; 2 blisters per carton.

Prescription category. Prescription only.

Manufacturer. JSC "Pharmaceutical Company "Darnytsia".

Manufacturer's address and location of its business activity.

13, Borispilska Street, Kyiv, 02093, Ukraine.