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, displaces calcium from receptors located on the inner surface of the membrane and, thus, 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. Has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 h).

When absorbed into the systemic bloodstream and by direct vascular injection, it can reduce the excitability of peripheral cholinergic systems, reduce the formation and release of acetylcholine from preganglionic endings (has some ganglion blocking effect), eliminate spasm of smooth muscles, reduce 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.

Pharmacokinetics:

When parenteral administration is well absorbed, rapidly hydrolyzed by esterases of plasma and tissues with the formation of two major pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilating effect) and paraaminobenzoic acid. The half-life is 0.7 minutes. It is excreted mainly by kidneys in the form of metabolites (80%).

Indications:

Infiltration, conductive, epidural anesthesia; vagosympathetic cervical and paranephalic block.

Contraindications:

Hypersensitivity (including para-aminobenzoic acid and other local anesthetic esters), children under 12 years.

For anesthesia using the creeping infiltrate method: pronounced fibrotic changes in tissues.

Carefully:

With caution, procaine solutions are used for emergency operations accompanied by acute blood loss; at conditions accompanied by a decrease in hepatic blood flow (with chronic heart failure, liver disease); with the progression of cardiovascular insufficiency (usually due to the development of heart block and shock); with inflammatory diseases or infection of the injection site; with pseudocholinesterase deficiency; with renal insufficiency; in children aged 12 to 18 years, in elderly patients (over 65 years); in seriously ill patients, weakened patients; in pregnancy and childbirth.

Pregnancy and lactation:

Apply with caution in the event that the need for the expected anesthetic effect exceeds the potential risk to the fetus or child.

Dosing and Administration:

The dose and concentration of the procaine solution depend on the nature of the surgical intervention, the method of administration, the condition and age of the patient.

For infiltration anesthesia apply 0.25-0.5% solutions; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - 0,125-0,25% solutions; for conductive anesthesia - 1-2% solutions (up to 25 ml); for epidural - 2% solution (20-25 ml).

With paranephric blockade (according to AV Vishnevsky) 50-80 ml of a 0.5% solution or 100-150 ml of a 0.25% solution are injected into the peritoneal cellulose.

With vagosympathetic blockade - 30-100 ml of 0.25% solution.

To reduce the absorption and lengthening of the action of procaine under local anesthesia, 0.1% solution of epinephrine hydrochloride is injected additionally - 1 drop per 2-10 ml of procaine solution.

Higher doses of procaine for infiltration anesthesia for adults: the first single dose at the beginning of the operation - not more than 0.75 g 0.5% solution (150 ml), then to 400 ml 0.5% solution for each hour. The maximum dose of procaine for use in children older than 12 years - up to 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, trismus.

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, "cold" sweat, excitation or depression of the central nervous system (excitation may be transitory or absent, while oppression may be the first symptom of an overdose), anxiety, anxiety, dizziness, tinnitus, blurred vision perception, tremor, cramps; oppression of myocardial function, reduction of cardiac output, blockade of intracardiac conduction, decrease or increase in arterial pressure, bradycardia, ventricular tachycardia, cardiac arrest; methemoglobinemia.

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:

Procaine intensifies the inhibitory effect on the central nervous system of other drugs.

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

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

With the simultaneous use of procaine in epidural anesthesia with guanadrel, guanethidine, mecamylamine, trimetaphan camsylate, the risk of a sharp decrease in blood pressure increases, so they are canceled 10 days before the use of procaine. Simultaneous use of procaine with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of lowering blood pressure, so they should be canceled 10 days before the use of procaine. Procain strengthens and lengthens the action of myorelaxing drugs. With the simultaneous use of procaine with narcotic analgesics, there is an additive effect that is used in conducting epidural anesthesia, while increasing the risk of respiratory depression.

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

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 novocaine.

Metabolite procaine (paraaminobenzoic acid) is a sulfonamide antagonist.

Special instructions:

The main cause of development of undesirable reactions with the use of procaine is its high plasma concentration, which can be observed due to overdose, rapid systemic absorption, unintentional intravascular injection or slow metabolic degradation. An increase in the plasma concentration of procaine may be caused by a decrease in tolerance (including due to a deficiency of cholinesterase in the plasma, the presence of factors affecting the association with plasma proteins such as acidosis), hypoalbuminemia as a result of concomitant diseases, competition with other drugs for binding to plasma proteins .

Before using procaine it is necessary to carefully collect allergological anamnesis, make skin tests for compatibility, and during anesthesia it is necessary to monitor vital body functions (heart rate, blood pressure, respiratory rate).

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

Procaine can cause side effects that affect the ability to drive vehicles and engage in potentially hazardous activities requiring increased concentration and speed of psychomotor reactions, so care must be taken when dealing with such activities in the first hours after anesthesia.

Form release / dosage:Solution for injection, 0.5% and 2%.

Packaging:

Solution for injection 0.5% 2 ml and 5 ml; 2% of 2 ml in ampoules.

For 5 ampoules of 2 ml or 5 ml of 0.5% solution, or 2 ml of a 2% solution in a contour mesh package made of PVC film.

2 contour packs of 5 ampoules of 2 ml or 5 ml of a 0.5% solution or 2 ml of a 2% solution or 10 ampoules of 2 ml or 5 ml of a 0.5% solution or 2 ml of a 2% solution together with instructions for medical use and a disc with a ceramic or knife ampoule ceramic in a pack of cardboard.

It is allowed when packing the drug in ampoules with a ring of fracture or a point and a notch disc cutting ceramic or an ampoule ceramic knife not to invest.

Storage conditions:

In the dark place at a temperature of 15 ° C to 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:П N015216 / 01

Date of registration:15.12.2008

The owner of the registration certificate:HEALTH PHARMACEUTICAL COMPANY, LTD. HEALTH PHARMACEUTICAL COMPANY, LTD. Ukraine

Manufacturer: & nbsp

HEALTH PHARMACEUTICAL COMPANY, LTD. Ukraine

Information update date: & nbsp03.09.2015

Illustrated instructions

Instructions

Novocaine (Novocaine)