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 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:

It is subject to 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).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 sulfonamide chemotherapeutic drugs and can weaken their antimicrobial effect).

The half-life of the drug is 30 to 50 seconds, in the neonatal period 54 to 114 seconds. It is excreted mainly by kidneys in the form of metabolites, in unchanged form it is deduced no more than 2%.

Indications:

Infiltration (including intraosseous), vagosympathetic cervical and paranephalic block.

Contraindications:

Hypersensitivity (including para-aminobenzoic acid and other local anesthetics to local anesthetic esters), age to 18 years (efficacy and safety not established).

For anesthesia using the creeping infiltrate method: pronounced fibrotic changes in tissues; for subarachnoid anesthesia: AV-blockade, bleeding, arterial hypotension, 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 (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 failure, in elderly patients (over 65 years), seriously ill, weakened patients, pregnancy, childbirth.

Pregnancy and lactation:

You can use the drug during pregnancy and breastfeeding.

Dosing and Administration:

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

For infiltration anesthesia 2.5 mg / ml, 5 mg / ml; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - 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 parainal blockade (according to A.V.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 paranephalic space.

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

For circular or paravertebral blockade intradermally injected 70-100 ml of a solution of 2.5 mg / ml or 5-10 ml of a solution of 5 mg / ml.

Higher single doses at infiltration anesthesia: the first single dose at the beginning of the operation is not more than 1.0 g of a solution of 2.5 mg / ml and 0.75 g of a solution of 5 mg / ml (150 ml). Further, during each hour of operation - no more than 2.5 g (1000 ml for a solution of 2.5 mg / ml) and 2 g (400 ml for a solution of 5 mg / ml).

Side effects:

Headache, dizziness, drowsiness, weakness, increase or decrease in blood pressure, collapse, peripheral vasodilation, bradycardia, arrhythmia, chest pain, methemoglobinemia, allergic reactions (up to anaphylactic shock).

Overdose:

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, cold sweats, 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 symptomatic therapy.

Interaction:

Local anesthetics increase 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.

With the use of 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.

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

Strengthen and prolong the action of myorelaxing drugs.

With the appointment of procaine in conjunction with narcotic analgesics, there is an additive effect that is used in spinal and epidural anesthesia,with increased respiratory depression.

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 local anesthetic drugs.

Metabolite procaine (paraaminobenzoic acid) is a sulfonamide antagonist of drugs.

Special instructions:

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

It is necessary to cancel monoamine oxidase 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, 2.5 mg / ml, 5 mg / ml.

Packaging:

100, 200, 400 ml in glass bottles for blood, infusion and transfusion preparations with a capacity of 100, 250 and 450 ml respectively, sealed with rubber stoppers and crimped with aluminum caps. A label is labeled with a label or coated paper, or writing paper.

Each bottle, together with the instruction for use, is placed in a pack of cardboard for consumer containers.

56 bottles of 100 ml, 24, 28 bottles with a capacity of 250 ml and 12, 15 bottles with a capacity of 450 ml respectively are placed in boxes of cardboard corrugated with an attachment instructions for the use of the appropriate number of bottles (for hospitals).

100, 200, 250, 400, 500, 1000 ml into bags of a polyolefin film.

Directly on each package, a self-adhesive label is applied or the text of the label is applied by hot stamping, using thermal printing.

56 bags of 100 ml, 24, 28 packages of 200 or 250 ml and 12, 15 packages of 400 or 500 ml, 12 1000 ml packets are placed in boxes of cardboard corrugated together with instructions for use in an amount corresponding to the number of packages (for hospitals).

Storage conditions:

In a place protected from light and inaccessible to children at a temperature of no higher than 25 ° C.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N001206 / 01

Date of registration:04.12.2008

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

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Representation: & nbspBIOCHEMICAL JSC BIOCHEMICAL JSC Russia

Information update date: & nbsp03.09.2015

Illustrated instructions

Instructions

Novocaine (Novocaine)