Novocaine - instructions for use, dose, side effects, contraindications

Pharmacodynamics: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. It suppresses not only the pain, but also the impulses of other modalities. 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:

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 two basic pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilating effect) and paraaminobenzoic acid (it is a competitive antagonist of sulfanilamide preparations and can weaken their antimicrobial effect).

Half-life 30-50 s, in the neonatal period - 54-114 s. It is excreted mainly by kidneys in the form of metabolites, in an unchanged form, no more than 2% is excreted,

Indications:

- Infiltration anesthesia;

- vagosympathetic cervical, paranephalic, circular and paravertebral blockades.

Contraindications:

- Hypersensitivity (including to paraaminobenzoic acid and other local anesthetics);

- children's age till 12 years;

- pronounced fibrotic changes and 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, in 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 from 12 to 18 years;

- elderly patients (over 65 years);

- Weakened patients;

- Pregnancy and the period of childbirth, lactation.

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 hydrochloride is injected - 1 drop per 2-5-10 ml of novocaine solution.

With parainal 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 administered to the perioral cellulose.

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

Length of circular and paravertebral block intradermally injected solution of 2.5 mg / ml or 5 mg / ml.

Higher doses for adult infiltration anesthesia: 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, increase or decrease in blood pressure, collapse, trismus, 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" 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 funds for general anesthesia, hypnotics and sedatives, narcotic analgesics and tranquilizers.

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.

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

Strengthens and prolongs the action of muscle relaxants.

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, it is recommended that samples be taken 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.

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

During the period of treatment, it is not recommended to drive vehicles or engage in potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for injection, 5 mg / ml.

Packaging:

For 5 ml of preparation and ampoule of neutral or light-protective glass with a notch marked with a dot (paint).

10 ampoules are placed in a contoured cell pack of a polyvinyl chloride film that is not covered with aluminum foil.

1 circuit cell pack together with an instruction for use, a scarifier or an ampoule knife is placed in a cardboard pack.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Do not freeze.

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:LSR-002696/10

Date of registration:31.03.2010

Expiration Date:Unlimited

The owner of the registration certificate: Mapichem AG Mapichem AG Switzerland

Manufacturer: & nbsp

WUHU KANGQI PHARMACEUTICAL, Co.Ltd. China

Representation: & nbspMapichem AGMapichem AG

Information update date: & nbsp25.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)