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, displaces calcium from receptors located on the inner surface of the membrane and, thus, 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.

Has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 h).

When absorbed into the systemic bloodstream and by direct vascular injection, it can reduce the excitability of peripheral cholinergic systems, reduce the formation and release of acetylcholine from preganglionic endings (has some ganglion blocking effect), eliminate spasm of smooth muscles, reduce the excitability of the myocardium and motor cortex areas of the brain.

When administered intravenously, it has analgesic, anti-shock,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.

Pharmacokinetics:

When parenteral administration is well absorbed, rapidly hydrolyzed by esterases of plasma and tissues with the formation of two, the main pharmacologistsactive metabolites: diethylaminoethanol (has a moderate vasodilator effect) and paraaminobenzoic acid. The half-life is 0.7 minutes. It is excreted mainly by kidneys in the form of metabolites (80%).

Indications:

Infiltration (including intraosseous), conductive anesthesia; vagosympathetic and paranephalic blockade.

Contraindications:

Hypersensitivity (including para-aminobenzoic acid and other local anesthetics), children's age (up to 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 (for example, in chronic heart failure, liver diseases), progression of cardiovascular insufficiency (usually due to the development of heart block and shock), inflammatory diseases or infection of the injection site, pseudocholinesterase deficiency, renal insufficiency, children's age (from 12 to 18 years), in elderly patients (over 65 years), seriously ill, weakened patients, pregnancy, period childbirth.

Pregnancy and lactation:

During pregnancy and lactation, the administration of the drug is indicated if the potential benefit to the mother exceeds the possible risk to the fetus.

Dosing and Administration:

The dose and concentration of the procaine solution depend on the nature of the surgical intervention, the method of administration, the condition and age of the patient.

For infiltration anesthesia - 0.25-0.5% solutions; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - 0,125-0,25% solutions; for conductive anesthesia - 1-2% solutions.

With paranephric blockade (according to AV Vishnevsky) 50-80 ml of a 0.5% solution or 100-150 ml of a 0.25% solution are injected into the peritoneal cellulose.

With vagosympathetic blockade - 30-100 ml of 0.25% solution.

Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation, - no more than 1.0 g of a 0.25% solution and 0.75 g of a 0.5% solution (150 ml). Further, during each hour of operation - no more than 2.5 g (1000 ml for 0.25% solution) and 2 g (400 ml for 0.5% solution).

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.

Side effects:

From the central and peripheral nervous system: headache, dizziness, drowsiness, weakness, tremor, visual and auditory disorders, nystagmus.

From the cardiovascular system (SSS): increase or decrease in blood pressure, peripheral vasodilation, collapse, bradycardia, arrhythmias, chest pain.

From the side of the blood: methemoglobinemia.

Other: hypothermia; with anesthesia in dentistry: numbness and paresthesia of lips and tongue, trismus.

Allergic reactions: urticaria, itching, erythema, angioedema (including laryngeal edema), anaphylactic shock.Cases of cross-sensitivity with other local anesthetics of the ester group have been reported.

Overdose:

Symptoms

From the skin: pallor of the skin and mucous membranes, "cold" sweat.

From the central nervous system (CNS): CNS stimulation or depression; anxiety, anxiety, dizziness, noise in the ears, blurred vision, tremors, cramps. Excitation may be transient or absent, while CNS depression may be the first symptom of an overdose.

On the part of the CAS: suppression of myocardial function, reduction of cardiac output, cardiac blockade, lowering of blood pressure (BP) or sometimes increased blood pressure, bradycardia, ventricular arrhythmia, cardiac arrest.

From the side of the blood: methemoglobinemia.

Treatment: maintenance of adequate pulmonary ventilation with inhalation of oxygen, intravenous administration of short-acting drugs for general anesthesia, in severe cases - detoxification and symptomatic therapy.

Interaction:

Strengthens the inhibitory effect on the central nervous system of other drugs.

Anticoagulants (ardeparin sodium, dalteparin sodium, sodium danaparoid, sodium 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.

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

When using procaine together with narcotic analgesics, there is an additive effect that is used in conducting epidural anesthesia, and the risk of respiratory depression increases.

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

Procaine reduces the effect of the antimiasthenic action of cholinesterase inhibitors, especially when used in high doses, which requires an additional correction for the treatment of myasthenia gravis.

Cholinesterase inhibitors (including antimiasthenic drugs, cyclophosphamide, democaria bromide, eco-iodide iodide, thiotepa) reduce the metabolism of procaine.

The metabolite of procaine (paraaminobenzoic acid) is a competitive sulfonamide antagonistchemotherapeutic drugs and can weaken their antimicrobial effect.

Special instructions:

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.

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

Effect on the ability to drive transp. cf. and fur:During the period of procaine, 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, 5 mg / ml, 20 mg / ml.

Packaging:

In ampoules of 2 ml, 5 ml.

For 10 ampoules with a knife for opening ampoules and instructions for use in a cardboard box.

10 ampoules of 2 ml or 5 ampoules of 5 ml in a blister pack.

1 or 2 blister packs with a knife for opening ampoules and instructions for use are put in a pack of cardboard.

10 ampoules together with a knife for opening ampoules and instructions for use in a pack with a cardboard insert for fixing ampoules.

In case of using ampoules with a break ring or a notch and a break point, the insertion of the knife for opening ampoules is not provided.

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:П N015889 / 01

Date of registration:12.08.2009

Expiration Date:Unlimited

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Representation: & nbspBORISOVSKIY FACTORY OF MEDPREPARATES, OJSCBORISOVSKIY FACTORY OF MEDPREPARATES, OJSC

Information update date: & nbsp25.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)