Novocaine bufus Renewal 0.5% solution for injection 5ml ampoules, 10pcs

Composition

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1 ml of the solution contains: Active ingredient: procaine hydrochloride-5 mg, excipients: hydrochloric acid (0.1 M hydrochloric acid solution) – up to pH 3.8-4.5, water for injection – up to 1 ml

Pharmacological action

A local anaesthetic agent with moderate anaesthetic activity and a wide range of therapeutic effects. Being a weak base, it blocks Na+channels, prevents the generation of impulses in the endings of sensitive nerves and the conduction of impulses along nerve fibers. Alters the action potential in nerve cell membranes without significantly affecting the resting potential. Suppresses not only pain, but also impulses of other modality. When absorbed and directly injected into the blood stream, it reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic endings (it has some ganglioblocking effect), eliminates smooth muscle spasm, and reduces the excitability of the myocardium and motor areas of the cerebral cortex. When administered intravenously, it has analgesic, antihypertensive and antiarrhythmic effects (increases the effective refractory period, reduces excitability, automatism and conductivity), in large doses it can disrupt neuromuscular conduction. Eliminates the descending inhibitory effects of the reticular formation of the brain stem. Depresses polysynaptic reflexes. In large doses, it can cause seizures. It has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 h). Pharmacokinetics Subject to complete systemic absorption. The degree of absorption depends on the site and route of use (especially on vascularization and blood flow rate in the area of use) and the final dose (amount and concentration). It is rapidly hydrolyzed by plasma and liver esterases to form 2 main pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilating effect) and para-aminobenzoic acid (is a competitive antagonist of sulfonamide chemotherapeutic drugs and can weaken their antimicrobial action). The half-life is 30-50 seconds, in the neonatal period-54-114 seconds. It is mainly excreted by the kidneys in the form of metabolites, and no more than 2% is excreted unchanged.

Indications

• Infiltration anesthesia;

• vagosympathetic cervical, paranephral, circular and paravertebral blockades.

Contraindications

Hypersensitivity (including to para-aminobenzoic acid and other local anesthetics), children under 12 years of age. Marked fibrotic changes in the tissues (for anesthesia by creeping infiltrate). With caution, emergency operations accompanied by acute blood loss, conditions accompanied by a decrease in hepatic blood flow (for example, with CNS, liver diseases), progression of cardiovascular insufficiency (usually due to the development of heart block and shock), inflammatory diseases or infected injection sites, pseudocholinesterase deficiency, renal failure, children (from 12 to 18 years), in elderly patients (over 65 years), weakened patients, pregnancy, delivery period.

Side effects

Headache, dizziness, drowsiness, weakness, increased or decreased blood pressure, collapse, peripheral vasodilation, bradycardia, arrhythmia, chest pain, trismus, tremor, visual and hearing impairment, nystagmus, persistent anesthesia, hypothermia, methemoglobinemia, allergic reactions (up to anaphylactic shock).

Interaction

Increases the depressing effect on the central nervous system of general anesthesia, sleeping pills and sedatives, narcotic analgesics and tranquilizers. Anticoagulants (ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin) they 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. Use with MAO inhibitors (furazolidone, procarbazine, selegiline) increases the risk of hypotension. Enhance and lengthen the effect of muscle relaxants. When prescribing procaine together with narcotic analgesics, an additive effect is noted, which is used during spinal and epidural anesthesia, while respiratory depression increases. Vasoconstrictors (epinephrine, methoxamine, phenylephrine) prolong the local anesthetic effect. Procaine reduces the antimiasthenic effect of drugs, especially when used in high doses, which requires additional correction of the treatment of myasthenia gravis. Cholinesterase inhibitors (antimiasthenic drugs, cyclophosphamide, demecarin, ecothiophate, thiotepa) reduce procaine metabolism. The procaine metabolite (para-aminobenzoic acid) is a sulfonamide antagonist.

How to take, course of use and dosage

For infiltration anesthesia, solutions of 2.5 mg/ml,5 mg/ml are used; for anesthesia by the Vishnevsky method (tight creeping infiltration) – solutions of 1.25 mg / ml,2.5 mg / ml. To reduce absorption and prolong the action under local anesthesia, an additional 0.1% solution of epinephrine hydrochloride is administered-1 drop per 2-5-10 ml of procaine solution.

Overdose

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, “cold” sweat, rapid breathing, tachycardia, decreased blood pressure up to collapse, apnea, methemoglobinemia. The effect on the central nervous system is manifested by a feeling of fear, hallucinations, convulsions, motor arousal. Treatment: maintenance of adequate pulmonary ventilation, detoxification and symptomatic therapy.

Special instructions

Regional and local anesthesia should be performed by experienced specialists in an appropriately equipped room, with the availability of ready-to-use equipment and medications necessary for monitoring cardiac activity and resuscitation measures. Anaesthetic personnel should be qualified and trained in anaesthetic techniques, and should be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications. Patients need to monitor the functions of the cardiovascular, respiratory and central nervous systems. MAO inhibitors should be discontinued 10 days before the local anesthetic is administered. During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions. Before use, it is mandatory to conduct tests for individual sensitivity to the drug. It should be borne in mind that when performing local anesthesia using the same total dose, the toxicity of novocaine is higher, the more concentrated the solution is used. It is not absorbed from the mucous membranes; it does not provide surface anesthesia when applied on the skin.

Form of production

Solution for injection

Storage conditions

In a dark place.

Shelf life

3 years

Active ingredient

Procaine

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection

Description

Nursing mothers as prescribed by a doctor, Adults as prescribed by a doctor, Pregnant women as prescribed by a doctor, Children as prescribed by a doctor, Children over 12 years of age

Indications

Anesthesia