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 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 the carrying out not only painful, but also impulses of other modality. With suction and direct intravascular injection reduces the excitability of peripheral cholinergic receptors, reduces the formation and release of acetylcholine from 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. With intravenous administration, 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:

It is subject to complete systemic absorption.The degree of absorption depends on the site (degree of vascularization and blood flow velocity in the area of administration), route of administration and total dosage. It is rapidly hydrolyzed by plasma and liver esterases with the formation of 2 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). The half-life is 30-50 seconds, in the neonatal period - 54-114 s. It is excreted mainly by kidneys in the form of metabolites, in the unchanged form it is deduced no more than 2%.

Indications:

- Infiltration, conductive and epidural anesthesia;

- vagosympathetic cervical, paranephalic, circular and paravertebral blockades.

Contraindications:

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

Children under 12 years.

For anesthesia using the creeping infiltrate method: pronounced fibrotic changes in tissues.

For epidural anesthesia: atrioventricular blockade, marked decrease in arterial pressure, shock, infection of the site of lumbar puncture, septicemia.

Carefully:

Emergency operations, accompanied by acute blood loss; conditions, accompanied by a decrease in hepatic blood flow (eg, in chronic heart failure, liver disease); pseudocholinesterase deficiency; kidney failure; children age from 12 to 18 years and in elderly patients (over 65 years); weakened patients; pregnancy and childbirth.

Dosing and Administration:

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

To reduce absorption and lengthening of action with local anesthesia, 0.1% solution of epinephrine hydrochloride is additionally administered - 1 drop per 2-5-10 ml of procaine solution.

Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation - no more than 500 ml for 0.25% solution or 150 ml for 0.5% solution. Further, during each hour of operation - no more than 1000 ml for 0.25% solution or 400 ml for 0.5% solution. The maximum dose for use in children older than 12 years is 15 mg / kg.

For conductive anesthesia: 1-2% solutions (up to 25 ml); for epidural - 2% solution (20-25 ml).

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, and 30-100 ml of a 0.25% solution in the case of vagosympathetic blockade.

For circular or paravertebral blockades a 0.25% -0.5% solution is injected intradermally.

Side effects:

Headache, dizziness, drowsiness, weakness, cauda equina syndrome, convulsions, increase or decrease in blood pressure, collapse, peripheral vasodilation, bradycardia, arrhythmia, chest pain, involuntary urination or defecation, impotence, methemoglobinemia, allergic reactions (up to anaphylactic shock).

From the digestive system: nausea, vomiting.

Other: return pain, persistent anesthesia, hypothermia, with anesthesia in dentistry: numbness and paresthesia of the lips and tongue, lengthening of anesthesia.

Overdose:

Symptoms: pallor of the skin and mucous membranes. Dizziness, nausea, vomiting, "cold" sweat, increased severity of side effects

Treatment: maintenance of adequate pulmonary ventilation, detoxification and sympathetic therapy.

Interaction:

Strengthens the depressing effect on the central nervous system of funds for general anesthesia, hypnotics and sedatives, narcotic analgesics and tranquilizers.

When using local anesthetic drugs for spinal and epidural anesthesia with guanadrel, guanethidine, mecamylamine, trimetaphane, the risk of a sharp decrease in blood pressure and bradycardia increases

Anticoagulants (ardeparin, dalteparin, danaparoid, 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.

Use with 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, demecarine, ecothiophate, thiotepa) reduce the metabolism of procaine.

Metabolite procaine (paraaminobenzoic acid) is a sulfonamide antagonist.

Special instructions:

Patients need control of 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 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.

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, 5 mg / ml, 20 mg / ml.

Packaging:

At 2.5 ml - 20 mg / ml, 5, 10 ml - 5 mg / ml into ampoules from neutral glass.

For 10 ampoules together with instructions for use in a pack or box of cardboard.

5 ampoules per contour cell pack. 2 contour squares in a pack of cardboard.

Each box is loaded with an ampoule knife or a scarifier or a ceramic ampoule scarifier. When you pack the ampoules with a point or ring of a fracture, the ampoule knife or scarifier does not insert.

Storage conditions:

In the dark place.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000423 / 01

Date of registration:08.12.2008

The owner of the registration certificate:Armavir Biofactory, FKPArmavir Biofactory, FKP Russia

Manufacturer: & nbsp

ARMAVIRSK BIOLOGICAL FACTORY, FSUE Russia

Information update date: & nbsp03.09.2015

Illustrated instructions

Instructions

Novocaine (Novocaine)