Novocaine bufus, 5 mg/ml 5 ml 10 pcs

A local anesthetic with moderate anesthetic activity and a wide range of therapeutic action. Being a weak base, it blocks Na+-channels, prevents generation of impulses in the endings of sensitive nerves and conduction of impulses along the nerve fibers.

Changes the action potential in nerve cell membranes without a pronounced effect on resting potential. It suppresses not only pain impulses but also impulses of other modality.

By absorption and direct vascular injection into the blood stream it decreases the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic terminations (has some ganglion blocking effect), eliminates spasm of smooth muscles, reduces myocardial and cerebral motor areas excitability.

When administered intravenously it has analgesic, hypotensive and antiarrhythmic effect (increases the effective refractory period, decreases excitability, automaticity and conduction). Eliminates descending inhibitory effects of reticular formation of the brainstem. Inhibits polysynaptic reflexes. May cause convulsions in high doses. It has short anesthetic activity (duration of infiltration anesthesia is 0.5-1 hour).

Pharmacokinetics

Subject to complete systemic absorption. The degree of absorption depends on the place and route of administration (especially on vascularization and blood flow velocity in the area of administration) 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 moderate vasodilator effect) and para-aminobenzoic acid (is a competitive antagonist of sulfonamide chemotherapeutic agents and can weaken their antimicrobial action). The elimination half-life is 30-50 seconds, in the neonatal period – 54-114 seconds. It is excreted mainly by the kidneys in the form of metabolites, not more than 2% is excreted unchanged.

Indications

Pain, Anesthesia

• Infiltration anesthesia;

• vagosympathetic cervical, paranephral, circular and paravertebral blockades.

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Active ingredient

Procaine

Composition

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

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How to take, the dosage

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

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Interaction

Increases the suppressive effect on the central nervous system of the means for general anesthesia, sedatives and sedatives, narcotic analgesics and tranquilizers.

Anticoagulants (ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin) increase the risk of bleeding.

When treating the injection site of local anesthetic with disinfectant solutions containing heavy metals, the risk of local reaction in the form of pain and swelling increases.
Use with MAO inhibitors (furazolidone, procarbazine, selegiline) increases the risk of hypotension.
Enhance and prolong the effect of muscle relaxants.

When procaine is administered in conjunction with narcotic analgesics an additive effect is noted that is used during spinal and epidural anesthesia, with increased respiratory depression.
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 myasthenia gravis treatment.

Cholinesterase inhibitors (antimiasthenic drugs, cyclophosphamide, demecarine, ecothiopath, thiotepa) reduce the metabolism of procaine.

Metabolite of procaine (para-aminobenzoic acid) is an antagonist of sulfonamides.

Special Instructions

Regional and local anesthesia should be performed by experienced personnel in an appropriately equipped facility with equipment and medications ready for immediate use to perform cardiac monitoring and resuscitation.

The personnel performing the anesthesia must be qualified and trained in anesthesia techniques and must be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions and other complications.

Patients require monitoring of cardiovascular, respiratory and central nervous system functions. MAO inhibitors should be withdrawn 10 days before the local anesthetic is administered. During the treatment it is necessary to refrain from driving motor transport and engaging in potentially dangerous activities that require high concentration and quick psychomotor reactions.

Prior to the use it is necessary to conduct tests on individual sensitivity to the drug. It should be borne in mind that during local anesthesia when using the same total dose, the toxicity of novocaine is the higher the more concentrated solution is used. It is not absorbed from mucous membranes; it does not provide superficial anesthesia when applied topically.

Contraindications

Hypersensitivity (including to para-aminobenzoic acid and other local anesthetics), children under 12 years of age. Expressed fibrotic changes in the tissues (for anesthesia by creeping infiltration).

With caution

Emergency surgery accompanied by acute blood loss, conditions accompanied by decreased hepatic blood flow (e.g., CNS, liver disease), progression of cardiovascular insufficiency (usually due to development of heart block and shock), inflammatory diseases or infected injection sites, pseudocholinesterase deficiency, renal failure, childhood age (12 to 18 years), older patients (over 65), frail patients, pregnancy, period of labor.

Side effects

Headache, dizziness, somnolence, 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).

Overdose

Symptoms: pallor of skin and mucous membranes, dizziness, nausea, vomiting, “cold” sweat, rapid breathing, tachycardia, decreased blood pressure up to collapse, apnea, methemoglobinemia. CNS effects are manifested by feelings of fear, hallucinations, seizures, motor agitation.
Treatment: maintenance of adequate pulmonary ventilation, detoxification and symptomatic therapy.

Similarities

Novocaine, Hemorrhoid Remedies