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.

With intravenous administration, analgesic, anti-shock, 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 (volume 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 (T_1/2) - 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), conductive, epidural, spinal anesthesia; vagosympathetic cervical and paranephalic blockade, retrobulbar (regional) anesthesia.

Contraindications:

Children under 12 years.

Hypersensitivity to the components of the drug (including para-aminobenzoic acid and other local anesthetic esters).

For anesthesia using the creeping infiltrate method: pronounced fibrotic changes in tissues, 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 (eg, in chronic heart failure, liver disease), progression of cardiovascular insufficiency (usually due to the development of heart block and shock), inflammatory diseases or injection site infection, pseudocholinesterase deficiency, kidney failure, childhood (12 -18 years), in elderly patients (over 65 years), seriously ill, weakened patients, pregnancy, childbirth.

Pregnancy and lactation:

The use of the drug is permissible, if the expected benefit for the mother exceeds the potential risk to the fetus and the baby.

Dosing and Administration:

The dose and concentration of novocaine solution depend on the nature of the operative interference, application, condition and age of the patient.

For infiltration anesthesia 2.5-5 mg / ml solutions are used; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - 1,25-2,5 mg / ml solutions; for conductive anesthesia - 10-20 mg / ml solutions (up to 25 ml); for epidural anesthesia - 20 mg / ml solution (20-25 ml).

Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation is not more than 0.75 g (150 ml), then during each hour of operation - not more than 2 g (400 ml) of the solution.

With parainal blockade (according to AV Vishnevsky), 50-80 ml of a 5 mg / ml solution or 100-150 ml of a 2.5 mg / ml solution are injected into the perioral cellulose.

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

With vagosympathetic blockade injected with 30-40 ml.

With vagosympathetic blockade - 15-50 ml of a 5 mg / ml solution.

With retrobulbar (regional) anesthesia - 5-8 ml of a 20 mg / ml solution.

To reduce the absorption and lengthening of the action with local anesthesia, an additional 0.1% solution of epinephrine is added, 1 capillary per 2-5-10 ml of novocaine 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, tremor, visual and auditory disorders, nystagmus.

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

From the side of the blood: methemoglobinemia.

Other: hypothermia.

With anesthesia in dentistry: numbness and paresthesia of lips and tongue, trism.

Allergic reactions: urticaria, itching, erythema, angioedema (including laryngeal edema), anaphylactic shock. Cases of cross-sensitivity with other local anesthetics of the ester group have been reported.

Overdose:

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, cold sweats, increased respiration, tachycardia, lowering 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 with inhalation of oxygen,intravenous administration of short-acting drugs for general anesthesia, in severe cases - detoxification and symptomatic therapy.

Interaction:

Strengthens the inhibitory effect on the central nervous system of others medicines.

Anticoagulants (ardeparin sodium, dalteparin sodium, sodium danaparoid, enoxaparin sodium, heparin, warfarin) increase the risk of bleeding.

When treating the site of injection of a local anesthetic with antiseptic solutions containing salts of heavy metals, the risk of local reaction in the form of soreness and edema increases.

With the simultaneous use of local anesthetic drugs for spinal and epidural anesthesia with guanadrel, guanethidine, mecamylamine, trimetaphan camsylate, the risk of a sharp decrease in blood pressure and bradycardia increases.

Simultaneous use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of developing a marked decrease in blood pressure, so they are canceled 10 days before the application of a local anesthetic.

Strengthen and prolong the action of myorelaxing drugs.

With the simultaneous use of procaine with narcotic analgesics, there is an additive effect, which is used in 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 local anesthetic drugs.

Metabolite procaine (paraaminobenzoic acid (PABA)) is a sulfonamide antagonist.

Special instructions:

The main cause of development of undesirable reactions with the use of procaine is a high plasma concentration, which can be observed due to overdose, rapid systemic absorption, unintentional intravascular injection or slow metabolic degradation.

In addition, a decrease in tolerance, incl. due to a deficiency of cholinesterase in the plasma, the presence of factors affecting the association with plasma proteins such as acidosis, concomitant diseases leading to hypoalbuminemia, competition with other drugs for communication with plasma proteins, can lead to an increase in the plasma concentration of procaine. In this regard, during anesthesia, it is necessary to monitor vital body functions (heart rate, blood pressure, respiratory rate).

Regional and local 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. Personnel performing anesthesia should be qualified and trained in the technique of performing anesthesia, should be familiar with the diagnosis and treatment of systemic toxic reactions, adverse events and reactions, and other complications.

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

During the treatment period, care must be taken when administering vehicles and employment by other potentially dangerous kinds of activity demanding the raised concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for injection, 5 mg / ml and 20 mg / ml.

Packaging:

2 ml or 5 ml into neutral glass ampoules.

5 ampoules are placed in a contour mesh package made of a polyvinyl chloride film. 1 or 2 contour squares are placed in a pack of cardboard.

5.10 ampoules are placed in a pack of cardboard with baffles or lattices, or a separator made of cardboard or sack paper.

10 ampoules are placed in a box of cardboard.

In each pack or box, put the instructions for use and the ampoule scaler.

In the case of using ampoules with incisions, rupture rings or break points, the ampoule scapegrator 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 expiry date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-001406

Date of registration:02.08.2011 / 19.08.2015

Expiration Date:Unlimited

The owner of the registration certificate:Promomed Rus, Open CompanyPromomed Rus, Open Company Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Representation: & nbspBIOCHEMICAL JSC BIOCHEMICAL JSC Russia

Information update date: & nbsp24.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)