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 major pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilating 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) anesthesia;

- vagosympathetic cervical and paranephalic block.

Contraindications:

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

- children's age (up to 12 years);

- expressed 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 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), seriously ill, weakened patients;

- pregnancy, lactation.

Pregnancy and lactation:

During pregnancy and during breastfeeding, the application is possible if the expected effect exceeds the potential risk for the pregnant, fetus and child.

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 are used; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - 0,125-0,25% solutions.

Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation is not 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.

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.

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.

From the CAS side: oppression 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, iv administration of short-acting drugs for general anesthesia, in severe cases - 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 warfarin) increase the risk of bleeding. When treating the injection site of a local anesthetic with antiseptic solutions containing salts, heavy metals, the risk of developing a local reaction in the form of soreness and edema increases.

With the simultaneous use of local anesthetic drugs for spinal and epidural anesthesia with guanadrel, guanethidine, mecamylamine, trimetaphan camsylate, the risk of a sharp decrease in blood pressure and bradycardia increases.

Simultaneous use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of developing a marked decrease in blood pressure, so they are canceled 10 days before the application of a local anesthetic.

Strengthen and prolong the action of myorelaxing drugs.

In the appointment of procaine, together with narcotic analgesics, an additive effect is noted that is used in spinal and 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.

Special instructions:

The main cause of development of undesirable reactions with the use of procaine is a high plasma concentration, which can be observed due to overdose, rapid systemic absorption, unintentional intravascular injection or slow metabolic degradation. In addition, a decrease in tolerance, incl. due to a deficiency of cholinesterase 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, can lead to an increase in the plasma concentration of procaine.In this regard, during anesthesia, it is necessary to monitor vital body functions (heart rate, blood pressure, respiratory rate).

Before use, mandatory sampling 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.

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

Regional and local anesthesia should be carried out by experienced specialists in an appropriately equipped room with availability of ready-to-use equipment and preparations 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.

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

During the treatment period, care must be taken when managing transport means and employment by other potentially dangerous kinds of activity demanding the raised concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection, 5 mg / ml.

Packaging:

For 5 or 10 ml in ampoules.

For 10 ampoules with instructions for use and a knife for opening ampoules or a scarifier placed in a box of cardboard.

By 5 or 10 ampoules per contour cell pack of polyvinylchloride film or polyethylene terephthalate tape and aluminum foil or paper with polyethylene coating, or without foil, or without paper.

For 1 or 2 contour packs with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a pack of cardboard.

When packaging ampoules with a break ring or break point, the ampoule opener or ampoule scarifier may not be inserted.

Storage conditions:

In the dark place at a temperature of 5 to 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N000194 / 01

Date of registration:05.03.2011

Expiration Date:Unlimited

The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia

Manufacturer: & nbsp

NOVOSIBHIMFARM, OJSC Russia

Representation: & nbspNOVOSIBHIMFARM, OJSCNOVOSIBHIMFARM, OJSC

Information update date: & nbsp25.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)