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 Na⁺channels prevents the generation of pulses in the endings of the sensitive 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 direct intravascular injection reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from the preganglionic endings (has some ganglion-blocking effect), eliminates spasm of smooth muscles, reduces the excitability of the myocardium and motor cortex areas of the brain. Has analgesic, 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. 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). When parenterally administered, it is rapidly hydrolyzed by plasma and liver esterases to form two major 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 is 30-50 seconds. It is excreted mainly by kidneys in the form of metabolites, in unchanged form not more than 2%.

Indications:

- Infiltration anesthesia;

- vagosympathetic cervical, paranephalic, circular and paravertebral blockades.

Contraindications:

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

- children's age till 12 years;

- pronounced fibrotic changes in the 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 failure (usually due to the development of heart block and shock);

- inflammatory diseases or infection of the injection site;

- Pseudocholinesterase deficiency;

- kidney failure;

- children from 12 to 18 years;

- elderly patients (over 65 years);

- Weakened patients;

- Pregnancy and the period of childbirth.

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

For circular or paravertebral blockades 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.

Side effects:

Headache, dizziness, drowsiness, weakness, increased or decreased blood pressure, collapse, peripheral vasodilation, bradycardia, arrhythmia, chest pain, methemoglobinemia, allergic reactions (up to anaphylactic shock), trismus, tremor, visual and hearing impairment, nystagmus , persistent anesthesia, hypothermia.

Overdose:

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, "cold" sweat, increased respiration, tachycardia, lowering blood pressure right up to 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 (MAO) inhibitors (furazolidone, procarbazine, selegiline) increases the risk of developing hypotension.

Strengthen and prolong the action of muscle relaxants.

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-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 over the functions of the cardiovascular, respiratory and central nervous systems.

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

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.

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

For 100, 200 and 400 ml (2.5 mg / ml and 5 mg / ml) of the drug in glass bottles of blood type MTO, transfusion and infusion preparations with a capacity of 100, 250, 450 and 500 ml, respectively.

One bottle with instructions for medical use of the drug is placed in a pack of boxboard.

For 28 bottles with a capacity of 100 or 250 ml or 15 bottles with a capacity of 450 or 500 ml with 10 or 5 instructions for medical use of the drug, respectively, are placed in a box of corrugated cardboard with pads and corrugated cardboard "nests" [for hospitals].

5 ml and 10 ml (5 mg / ml) of the drug into neutral glass ampoules.

For 10 ampoules, together with the instruction for medical use of the drug and the ampoule scarifier, are placed in a cardboard bundle with septa, or 5 or 10 ampoules are placed in a contiguous cell pack of a polyvinyl chloride film.

When using ampoules with a notch or a fracture ring, the scarifier is not inserted.

For 1 or 2 contour acupuncture together with the instruction for medical use of the drug is placed in a pack of cardboard.

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 N002917 / 01

Date of registration:11.09.2008

The owner of the registration certificate:ESKOM NPK, OAO ESKOM NPK, OAO Russia

Manufacturer: & nbsp

ESKOM NPK, OAO Russia

Representation: & nbspESKOM NPK, OAOESKOM NPK, OAO

Information update date: & nbsp03.09.2015

Illustrated instructions

Instructions

Novocaine (Novocaine)