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, 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 location and the route of administration (particularly by the introduction and vascularization flow rate) and total dose (the 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 (including para-aminobenzoic acid and other local anesthetic esters);

- children's age till 12 years;

- for anesthesia using the creeping infiltrate method: pronounced fibrous changes in the tissues.

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 failure (usually due to the development of blockade of intracardiac conduction 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 and the period of childbirth.

Pregnancy and lactation:

If it is necessary to prescribe the drug during pregnancy, one should compare the expected benefit to the mother and the potential risk to the fetus.

If it is necessary to prescribe the drug during the period of feeding, the question of stopping breastfeeding should be resolved.

Dosing and Administration:

Only for the solution of procaine 5 mg / ml (0.5%).

For infiltration anesthesia inject 350-600 mg (70-120 ml).

Higher single doses for infiltration anesthesia for adults: One dose at the beginning of the operation - not exceeding 0.75 g (150 ml), subsequently for each hour of operation - no more than 2 g (400 ml) solution.

With parainal blockade (according to AV Vishnevsky) 50-80 ml is administered to the peritoneal cellulose.

With circular and paravertebral blockade intradermally injected 5-10 ml.

With vagosympathetic blockade injected with 30-40 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.

Maximum dose for application in children over 12 years of age - 15 mg / kg.

Side effects:

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

From the cardiovascular system: increase or decrease in blood pressure, peripheral vasodilation, collapse, bradycardia, arrhythmias, chest pain.

On the part of the organs of hematopoiesis: methemoglobinemia.

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

If any of the side effects indicated in the instruction appear or become worse, or if you notice any other side effects not listed in the instructions, inform your doctor about it.

Overdose:

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, "cold" sweat, quickening of the breath, tachycardia, lowering of blood pressure, including 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 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.

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 local anesthetic drugs.

Metabolite procaine (paraaminobenzoic 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 anesthesia using the same total dose, the toxicity of the procaine is the 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 other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection, 5 mg / ml.

Packaging:

2, 5 or 10 ml into neutral glass ampoules.

10 ampoules are placed in a box of cardboard.

By 5 or 10 ampoules are placed in a contour mesh box made of a polyvinylchloride film and aluminum foil printed lacquered or foil-free.

1 circuit cell package with 10 ampoules or 1,2 contour packs with 5 ampoules are placed in a pack of cardboard.

In each pack, the box is enclosed with instructions for use and the ampoule scaler. When using ampoules with a kink ring or with a notch and a dot the ampoule scaper 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:P N000758 / 01

Date of registration:30.03.2011

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products SYNTHESIS, JSC Joint-stock Kurgan Society of Medical Preparations and Products Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp24.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)