Novocaine - instructions for use, dose, side effects, contraindications

Procaine is a local anesthetic with moderate anesthetic activity and a great 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 (the duration of infiltration anesthesia is 0.5-1 h).

Pharmacokinetics:

Procaine undergoes 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).Quickly hydrolyzed by esterases of plasma and liver with the formation of two major pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilator action) and para-aminobenzoic acid (a competitive antagonist of sulfonamide chemotherapeutic drugs and can weaken their antimicrobial effect).

Half-life is 30-50 seconds. It is excreted mainly by kidneys in the form of metabolites, in unchanged form not more than 2%.

Indications:

- Applied for local infiltration anesthesia, with various surgical interventions;

- for conducting novocaine blockades - paranephric and vagosympathetic;

- for circulatory and paravertebral blockades with eczema, neurodermatitis, sciatica and other painful conditions;

- to relieve spasms of peripheral vessels and improve microcirculation during frostbites (in the pre-active period).

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).

The use of monoamine oxidase inhibitors at least 10 days before the administration of a local anesthetic is contraindicated.

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);

- in elderly patients (over 65 years);

- Weakened patients;

- Pregnancy and the period of childbirth, lactation period.

Pregnancy and lactation:

During pregnancy and childbirth, the drug should be used with caution, only after evaluating the ratio of the intended benefit to the mother and the potential risk to the fetus.

Application in the period of breastfeeding is possible in cases when the expected benefit exceeds the potential risk for the child.

Dosing and Administration:

For infiltration anesthesia apply 2.5 mg / ml, 5 mg / ml solutions; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - 1.25 mg / ml, 2.5 mg / ml solutions.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.

When paranephric blockade (according to AV Vishnevsky), 50-80 ml of a 5 mg / ml solution or 100-150 ml of a 2.5 mg / ml solution is injected into the peritoneal cellulose, and with 30-100 ml of 2.5 mg of vagosympathetic blockade / ml solution.

For circulatory or paravertebral blockages intradermally injected 2.5 mg / ml, 5 mg / ml solution.

Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation - not more than 500 ml of a 2.5 mg / ml solution and 150 ml of a 5 mg / ml solution. The maximum dose for use in children older than 12 years is 15 mg / kg.

Side effects:

From the cardiovascular system: increase or decrease in blood pressure, collapse, peripheral vasodilation, bradycardia, arrhythmia.

From the nervous system: headache, dizziness, drowsiness, weakness, trismus, tremor, nystagmus, persistent anesthesia.

Allergic reactions: allergic reactions, up to anaphylactic shock.

Other: pain in the chest, methemoglobinemia, hypothermia, impaired vision and hearing.

Overdose:

When an overdose develops a coma, cramps are possible.

First aid in case of overdose is maintenance of 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.

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

Strengthen and prolong the action of muscle relaxants.

When using procaine in conjunction with narcotic analgesics, there is an additive effect, which is used in epidural anesthesia, and respiratory depression is increased. Vasoconstrictors (epinephrine, methoxamine, phenylephrine) extend the local anesthetic effect.

Procaine reduces the anti-asthma effect of drugs, especially when used in high doses, which requires an additional correction for 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.

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

Special instructions:

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

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 the procaine is the higher the more concentrated solution is used.

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

During the treatment period, it is necessary to refrain from engaging in potentially dangerous activities that require a high concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection, 5 mg / ml.

Packaging:

5 ml in ampoules of colorless neutral glass type I with a colored break ring or with a colored dot and a notch or without a kink ring, a colored dot and a notch. One, two or three color rings and / or a two-dimensional barcode, and / or alphanumeric coding or without additional color rings, a two-dimensional bar code, and alphanumeric coding can additionally be applied to the ampoules.

5 ampoules per circuit cell packaging made of polyvinylchloride film and aluminum foil foil or polymer film, or without foil and without film.

Or 5 ampoules are placed in a pre-made form (tray) with cells for laying ampoules.

1 or 2 contour squares or cardboard trays, together with the instruction for use and the scarifier or knife ampoule, or without the scarifier and the ampoule knife are placed in a cardboard package (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 30 ° C. Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000614 / 01

Date of registration:30.03.2012 / 07.08.2015

Expiration Date:Unlimited

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp24.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)