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. 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).Rapidly hydrolyzed by esterases plasma and liver with the formation of two major pharmacologically active metabolites: diethylaminoethanol (possesses moderate vasodilating action) and para-aminobenzoic acid (a competitive antagonist of sulfonamides 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 anesthesia; vagosympathetic cervical, paranephalic, circular and paravertebral blockades.

Contraindications:

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

Children under 12 years.

Pronounced fibrotic changes in 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 (eg, in chronic heart failure, liver disease); progression of cardiovascular failure (usually due to the development of blockadesheart 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 and the period of childbirth, the period of breastfeeding.

Pregnancy and lactation:

Application in pregnancy and during lactation 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 is injected - 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 cervical blockade injected 30-100 ml of a solution of 2.5 mg / ml.

For a circular or paravertebral block with eczema, atopic dermatitis and sciatica, a solution of 2.5 mg / ml or 5 mg / ml is intradermally administered.

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.

Dosage regimens for children (12 to 18 years), depending on age and body weight, are not developed; the maximum dose is 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" sweat, quickening of the breath, tachycardia, lowering of 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 means 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.

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.

When using procaine together with narcotic analgesics, an additive effect is noted, while 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:

Procaine has a high allergenic potential. The main reason for the development of unwanted reactions in the use of procaine is a high plasma concentration, which can be observed due to overdose, rapid systemic absorption, unintentional vascular injection or slow metabolic degradation. In addition, a decrease in tolerance, including due to a deficiency of cholesterase in the plasma, the presence of factors affecting the association with plasma proteins, such as acidosis, concomitant diseases leading to hypoalbuminemia, competition with other drugs for communication with plasma proteins may lead to an increase plasma concentration of procaine. In connection with this, during anesthesia, it is required to monitor 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 and 5 mg / ml.

Packaging:

On 200 ml and 400 ml in bottles glass, ukuporennye stoppers from rubber and crimped by aluminum caps. Each bottle, together with instructions for use, is placed in a pack of cardboard.

24, 28 bottles of 200 ml or 12, 15 bottles of 400 ml with an equal number of instructions for use are placed in a group box - boxes of cardboard corrugated with gaskets and gratings.

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 / 02-2001

Date of registration:16.10.2008 / 27.01.2012

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)