Novocaine - 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 sodium channels, prevents the generation of pulses in the endings of the sensory 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.

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 (duration of infiltration anesthesia is 0.5-1 hour).

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 para-aminobenzoic acid (a competitive antagonist of sulfanilamide chemotherapeutic drugs and can weaken their antimicrobial effect). Half-life 30-50 seconds, in the neonatal period - 54-114 seconds. It is excreted mainly by kidneys in the form of metabolites, in unchanged form it is deduced no more than 2%.

Indications:

Infiltration, conductive and epidural anesthesia; vagosympathetic cervical, paranephalic, circular and paravertebral blockades.

Contraindications:

Hypersensitivity (including para-aminobenzoic acid and other local anesthetic esters).

Children under 12 years.

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

Of the Day epidural anesthesia: atrioventricular blockade, marked decrease in arterial pressure, shock, infection of the site of lumbar puncture, septicemia.

Carefully:

- Emergency operations, accompanied by acute blood loss;

- conditions accompanied by a decrease in hepatic blood flow (eg, in chronic heart failure, liver disease);

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

- inflammatory diseases or infection of the injection site;

- Pseudocholinesterase deficiency;

- kidney failure;

- Children's age (from 12 to 18 years) and in elderly patients (over 65 years);

- Weakened patients;

- pregnancy, the period of childbirth, the period of breastfeeding.

Pregnancy and lactation:

Application in pregnancy and during breastfeeding is possible in cases where the expected benefit to the mother exceeds the potential risk to the fetus or child.

Dosing and Administration:

For infiltration anesthesia, 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 the absorption and lengthening of the action with local anesthesia, an additional 0.1% solution of epinephrine hydrochloride is added - 1 drop per 2-5-10 ml of procaine solution.

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

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

For a circular or paravertebral block 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 - no 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 older than 12 years is 15 mg / kg.

For conductive anesthesia - solutions of 10 mg / ml, 20 mg / ml (up to 25 ml); for epidural anesthesia - a solution of 20 mg / ml (20-25 ml).

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, including collapse, apnea, methemoglobinemia. Action 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 sodium, dalteparin sodium, sodium danaparoid, sodium enoxaparin, heparin sodium, 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.

When using local anesthetic drugs for epidural anesthesia with guanadrel, guanethidine, mecamylamine,trimetaphan with camsylate increases the risk of a sharp drop in blood pressure and bradycardia.

Use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of a pronounced decrease in blood pressure.

Strengthens and prolongs the action of muscle relaxants.

With the appointment of procaine in conjunction with narcotic analgesics, an additive effect is noted that is used in 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, democaria bromide, eco-iodide iodide, thiotepa) reduce the metabolism of procaine.

Metabolite procaine (paraaminobenzoic acid) is a sulfonamide antagonist.

Special instructions:

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

It is necessary to cancel monoamine oxidase inhibitors 10 days before the introduction of a local anesthetic.

Before use, it is recommended that samples be taken for individual sensitivity to the drug. It should be borne in mind that when carrying out local anesthesia using the same total dose, the toxicity of the procaine is the higher the more concentrated solution is used.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection, 2.5 mg / ml, 5 mg / ml, 10 mg / ml and 20 mg / ml.

Packaging:

1 ml, 2 ml, 5 ml, 10 ml in ampoules.

For 10 ampoules of 1 ml, 2 ml, 10 ml in a box of cardboard with corrugated septa.

For 5 ampoules of 1 ml, 2 ml, 5 ml or 10 ml in a contiguous cell pack of a polyvinyl chloride film. 2 contour squares are placed in a pack of cardboard.

In each box or bundle they put instructions for use, an ampoule knife or a scarifier.

At packing of ampoules with a ring of a break, points and notches the knife ampullum or skarifikator do not put.

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 use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000353 / 03-2002

Date of registration:15.01.2009 / 05.03.2012

Expiration Date:Unlimited

The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia

Manufacturer: & nbsp

BIOSINTEZ, PAO Russia

Representation: & nbspBIOSINTEZ JSC BIOSINTEZ JSC Russia

Information update date: & nbsp25.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)