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 sodium 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). It is 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 (a competitive antagonist of sulfanilamide chemotherapeutic drugs and can weaken their antimicrobial effect).

The half-life of the drug is 30-50 s, in the neonatal period - 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 anesthetics);

- children under 12 years of age:

- pronounced fibrotic changes in the 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's age (from 12 to 18 beds);

- elderly patients (over 65 years);

- Weakened patients.

Pregnancy and lactation:

During pregnancy and during breastfeeding, the safety and efficacy of the drug is not established.

The use of the drug during pregnancy and during breastfeeding is possible only if prescribed by the doctor, if the intended benefit to the mother exceeds the potential risk to the fetus or the baby.

Dosing and Administration:

For infiltration anesthesia apply 0,25% and 0,5% solutions; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - 0,125% and 0,25% solutions. To reduce absorption and lengthening, local anesthesia is additionally administered 0,1% solution of epinephrine - by 1 drop on 2-5-10 ml of the rolling solution.

With parainal blockade (according to LV Vishnevsky), 50-80 ml of a 0.5% solution or 100-150 ml of 0.25% are administered into the peritoneal cellulose, and 30-100 ml of 0.25% solution with a vagosympathetic blockade.

For circulatory or paravertebral blockade intradermally injected 0,25% or 0,5% solution.

Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation - no more than 500 ml 0,25% solution and 150 ml 0,5% solution. Maximum dose for use in children older than 12 years - 15 mg / kg.

The procedure for working with a polymer ampoule:

1. Take an ampoule and shake it, holding it by the neck.

2. Press the ampoule with your hand, while the drug should not be isolated, and rotate and separate the valve with rotating movements.

3. Connect the syringe to the ampoule immediately through the opening.

4. Turn over the ampoule and slowly fill the syringe with its contents.

5. Put the needle on the syringe.

Side effects:

From the central and peripheral system: headache, dizziness, drowsiness, weakness, trismus, tremor, nystagmus, persistent anesthesia, motor anxiety, loss of consciousness, convulsions, visual and auditory disorders.

From the side of the cardiovascular system: increase or decrease in blood pressure, collapse, peripheral vasodilation, bradycardia, arrhythmia, chest pain, changes in the distribution of excitation in the heart, which appear on the ECG in the form of a flat T wave or segment shortening ST.

Co of the respiratory system: spasms of the respiratory tract or difficulty breathing.

Co the side of the urinary system: involuntary urination.

From the digestive system: nausea, vomiting.

From the side of the blood: methemoglobinemia.

Allergic reactions: allergic reactions, up to anaphylactic shock.

Other: return pain, persistent anesthesia, hypothermia, tremor, swelling of the lips, face, mouth, tongue and throat.

Overdose:

When used in high doses, excessive absorption is possible.

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:

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.

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

Strengthen and prolong the action of muscle relaxants.

When using procaine in conjunction with narcotic analgesics, there is an additive effect, which is used for spinal and epidural anesthesia, and respiratory depression is increased.

Vasoconstrictors (epinephrine, methoxamine, phenylephrine) extend the local anesthetic effect.

Procaine reduces the anti-asthma effect of drugs, especially when used in high doses, which requires an additional correction for 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.

When using local anesthetics for epidural anesthesia with guanadrel, with guanethidine, mecamylamine, trimetaphan camsylate, the risk of a sharp decrease in blood pressure and bradycardia increases.

Special instructions:

Anesthesia should be carried out by experienced specialists in an appropriately equipped room with availability of ready-to-use equipment and preparations necessary for cardiac monitoring and resuscitation. To prevent accidental intravascular injection, it is recommended to perform an aspirate test (in two stages).

Patients need control over the functions of the cardiovascular, respiratory and central nervous systems.The use of monoamine oxidase inhibitors at least 10 days before the administration of a local anesthetic is contraindicated. 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 the procaine is the higher the more concentrated solution is used.

The drug should be stored in a secondary package.

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, 0.25% and 0.5%.

Packaging:

Ampoules (0.5% solution)

By 5 or 10 ml into ampoules of low-density polyethylene or polypropylene.

For 5 or 10 ampoules together with instructions for use in a pack of cardboard.

Vials (0.25% and 0.5% solutions)

100, 200, 250, 400 or 500 ml in polypropylene bottles, sealed with welded polypropylene caps.

One bottle together with instructions for use in a pack of cardboard.

For hospitals

From 1 to 40 vials of 100, 200, 250, 400 or 500 ml together with instructions for use in an amount equal to the number of vials in a corrugated box of cardboard.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiration date

Terms of leave from pharmacies:On prescription

Registration number:LP-003091

Date of registration:14.07.2015

The owner of the registration certificate:GROTEKS, LLC GROTEKS, LLC Russia

Manufacturer: & nbsp

GROTEKS, LLC Russia

Representation: & nbspGROTEKS, LLCGROTEKS, LLC

Information update date: & nbsp02.09.2015

Illustrated instructions

Instructions

Novocaine (Novocaine)