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.

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:

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 esterases plasma and liver with the formation of two major pharmacologically active metabolites: diethylaminoethanol (possesses moderate vasodilating action) and para-aminobenzoic acid (a competitive antagonist of sulfonamides and can weaken their antimicrobial effect).

The half-life is 30-50 s, in the neonatal period is 54-114 s. 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) anesthesia.

Vagosympathetic cervical, paranephalic, circular and paravertebral blockades.

Contraindications:

Hypersensitivity (incl. Para-aminobenzoic acid and other local anesthetic esters).

Children under 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 (eg, 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 (12 to 18 years) and elderly patients (over 65); seriously ill patients; weakened patients; pregnancy and childbirth.

Pregnancy and lactation:

The use of the drug during pregnancy is possible if the intended benefit to the mother exceeds the potential risk to the fetus; If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

For infiltration anesthesia, 350-600 mg (70-120 ml) of a solution of 5 mg / ml is administered.

Higher doses for infiltrative anesthesia for adults: the first single dose at the beginning of the operation is not more than 0.75 g (150 ml), then no more than 2 g (400 ml) of a solution of 5 mg / ml for each hour of operation.

With paranephric blockade (according to A.V.Vishnevsky) 50-80 ml of a solution of 5 mg / ml are injected into the peritoneal cellulose.

With circulatory and paravertebral blockade, 5-10 ml of a solution of 5 mg / ml are injected intradermally.

With vagosympathetic blockade, 30-40 ml of a solution of 5 mg / ml is administered.

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 Novocain solution.

The maximum dose for use in children older than 12 years is 15 mg / kg.

Side effects:

From the central and peripheral nervous system: headache, dizziness, drowsiness, weakness, trismus.

From the cardiovascular system: increase or decrease arterial pressure, peripheral vasodilation, collapse, bradycardia, arrhythmia, chest pain.

On the part of the organs of hematopoiesis: methemoglobinemia.

Allergic reactions: urticaria (on the skin and mucous membranes), itching, rash, other anaphylactic reactions (including anaphylactic shock).

Overdose:

Symptoms: pallor of the skin and mucous membranes, "cold" sweat; dizziness, nausea, vomiting, rapid breathing, tachycardia, lowering blood pressure, including collapse, apnea, methemoglobinemia.The action on the central nervous system is manifested by a feeling of fear, a hallucinationnations, convulsions, motor excitement.

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

Interaction:

Strengthens the depressing effect on the central nervous system of medicines for general anesthesia, hypnotics, 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 injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of tenderness and swelling increases.

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

Strengthens and lengthens the action of myorelaxing drugs.

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.

The metabolite of procaine (para-aminobenzoic acid) is a sulfonamide antagonist.

Special instructions:

Before use, it is recommended that samples be tested for individual sensitivity to the drug.

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

It is necessary to cancel monoamine oxidase inhibitors 10 days before the introduction of a local anesthetic.

It should be borne in mind that when carrying out local anesthesiaand when using the same total dose, the toxicity of Novocain is higher the more concentrated solution is used.

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

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection, 5 mg / ml.

Packaging:

5 ml into neutral glass ampoules.

5 or 10 ampoules are placed in a contour mesh package made of a polyvinyl chloride film.

1 circuit cell pack of 10 ampoules or 2 contour packs of 5 ampoules with instructions for use, a scarifier or a knife ampoule placed in a pack of cardboard.

When using ampoules with a ring or break point, the scarifier or ampoule knife is not inserted.

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 expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001730

Date of registration:02.07.2012 / 03.07.2017

Expiration Date:Unlimited

The owner of the registration certificate:Company DEKO, LLC Company DEKO, LLC Russia

Manufacturer: & nbsp

Company DEKO, LLC Russia

Representation: & nbspCompany DEKO, LLCCompany DEKO, LLC

Information update date: & nbsp24.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)