Novocain Bufus - instructions for use, dose, side effects, contraindications

A local anesthetic with moderate anesthetic activity and a large breadth of therapeutic effect. Being a weak base, it blocks Na⁺channels prevents the generation of pulses in the endings of the sensitive nerves and impulses along nerve fibers. Changes the action potential in the membranes of nerve cells without a pronounced effect on the resting potential. Suppresses carrying out not only pain, but also impulses of another modality.

With absorption and direct vascular injection into the blood flow reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic endings (possesses some ganglion-blocking action), eliminates spasm of smooth muscles, reduces the excitability of the myocardium and motor cortex areas of the brain.

With intravenous administration, analgesic, hypotensive and antiarrhythmic action (increases the effective refractory period, reduces excitability, automatism and conductivity), in large doses can disrupt neuromuscular conduction. Eliminates the descending inhibitory effects of the reticular formation of the brain stem.Oppresses polysynaptic reflexes. In large doses can cause seizures. Has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 h).

Pharmacokinetics:

It is subject to complete systemic absorption. The degree of absorption depends on the site 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 with the formation of two basic pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilating effect) and paraaminobenzoic acid (a competitive antagonist of sulfanilamide chemotherapeutic drugs and can weaken their antimicrobial effect). The half-life is 30-50 seconds, in the neonatal period - 54-114 s. It is excreted mainly by the kidneys in the form of metabolites, in the unchanged form, no more than 2%.

Indications:

- Infiltration anesthesia;

- vagosympathetic cervical, paranephalic, circular and paravertebral blockades.

Contraindications:

- Hypersensitivity (including to paraaminobenzoic acid and other local anesthetics);

- children's age till 12 years;

- pronounced fibrotic changes in the tissues (for anesthesia using the creeping infiltrate method).

Carefully:

- Emergency operations, accompanied by acute blood loss;

- conditions accompanied by a decrease in hepatic blood flow (for example, in CHS, liver diseases);

- progression of cardiovascular insufficiency (usually due to the development of heart block and shock);

- inflammatory diseases or infected injection sites;

- Pseudocholinesterase deficiency;

- kidney failure;

- Children's age (from 12 to 18 years);

- in elderly patients (over 65 years);

- Weakened patients;

- Pregnancy, childbirth.

Dosing and Administration:

For infiltration anesthesia use solutions of 2.5 mg / ml, 5 mg / ml; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - solutions of 1.25 mg / ml, 2.5 mg / ml. To reduce absorption and lengthen action with local anesthesia, 0.1% solution of epinephrine hydrochloride - 1 drop per 2-5-10 ml of procaine solution.

With paranephric blockade (according to AV Vishnevsky) 50-80 ml of 5 mg / ml or 100-150 ml of a solution of 2.5 mg / ml are administered to the peritoneal cellulose.

With vagosympathetic blockade injected 30-100 ml of a solution of 2.5 mg / ml.

For circular and paravertebral blockades intradermally injected solution of 2.5 mg / ml or 5 mg / ml.

Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation is not more than 500 ml of a solution of 2.5 mg / ml or 150 ml of a solution of 5 mg / ml.

The maximum dose for use in children is up to 15 mg / kg.

Side effects:

Headache, dizziness, drowsiness, weakness, increase or decrease in 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 the skin and mucous membranes, dizziness, nausea, vomiting, cold sweats, increased respiration, tachycardia, lowering blood pressure right up to collapse, apnea, methemoglobinemia. The effect on the central nervous system is manifested by a feeling of fear, hallucinations, convulsions, motor excitement.

Treatment: maintenance of adequate pulmonary ventilation, detoxification and symptomatic therapy.

Interaction:

Strengthens the depressing effect on the central nervous system of funds for general anesthesia, hypnotics and sedatives, narcotic analgesics and tranquilizers.

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

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

Use with MAO inhibitors (furazolidone, procarbazine, selegiline) increases the risk of developing hypotension.

Strengthen and prolong the action of muscle relaxants.

When appointing procaine and together with narcotic analgesics there is an additive effect that is used for spinal and epidural anesthesia, and respiratory depression is increased.

Vasoconstrictors (epinephrine, methoxamine, phenylephrine) extend the local anesthetic effect.

Procaine reduces the anti-myasthenic action of drugs, especially when used in high doses, which requires an additional correction of the treatment of myasthenia gravis.

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

Metabolite procaine (paraaminobenzoic acid) is a sulfonamide antagonist.

Special instructions:

Regional and local anesthesia should be carried out by experienced specialists in an appropriately equipped room with availability of ready-to-use equipment and drugs necessary for cardiac monitoring and resuscitation. Personnel performing anesthesia should be qualified and trained in the technique of performing anesthesia, should be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.

Patients need control over the functions of the cardiovascular, respiratory and central nervous systems.

It is necessary to abolish MAO inhibitors 10 days before the introduction of a local anesthetic.

Before use, mandatory sampling for individual sensitivity to the drug. It should be borne in mind that when carrying out local anesthesia with the same total dose, the toxicity of novocaine is higher the more concentrated solution is used.

It is not absorbed from the mucous membranes; does not provide a superficial anesthesia for dermal application.

Effect on the ability to drive transp. cf. and fur:During the treatment period, it is necessary to refrain from driving motor vehicles and engage in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection, 5 mg / ml.

Packaging:

By 2 ml, 5 ml, 10 ml into polymer ampoules, from polyethylene.

For 10, 100 ampoules of polymer with instructions for use are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:3 years.

Do not apply but the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-009446/08

Date of registration:26.11.2008 / 07.08.2015

Expiration Date:Unlimited

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Representation: & nbspUPDATE OF PFC, CJSCUPDATE OF PFC, CJSC

Information update date: & nbsp25.06.2018

Illustrated instructions

Instructions

Novocain Bufus (Novocaine bufus)