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

Active substance:
Procaine hydrochloride (novocaine)	2.5 g or 5.0 g
Excipients:
1M hydrochloric acid solution	pH from 3.8 to 4.5
Water for injections	up to 1.0 liter

Description:

Transparent colorless or slightly colored liquid.

Pharmacotherapeutic group:local anesthetic

ATX: & nbsp

N.01.B.A Ethers of aminobenzoic acid

N.01.B.A.02 Procain

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. Suppresses carrying out not only pain, but also impulses of another modality.

Has short anesthetic activity (duration infiltration anesthesia is 0.5-1 h).

Pharmacokinetics:

Procaine undergoes 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). Quickly hydrolyzed by esterases of plasma and liver with the formation of two major pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilator action) and para-aminobenzoic acid (a competitive antagonist of sulfonamide chemotherapeutic drugs and can weaken their antimicrobial effect).

Half-life is 30-50 seconds. It is excreted mainly by kidneys in the form of metabolites, in unchanged form not more than 2%.

Indications:

- Infiltration anesthesia;

- vagosympathetic cervical, paranephalic, circular and paravertebral blockades.

Contraindications:

- Hypersensitivity (including para-aminobenzoic acid and other local anesthetics);

- children's age till 12 years;

- expressed fibrotic changes in 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 (for example, in chronic heart failure, liver disease), progression of cardiovascular failure (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.

Pregnancy and lactation:

During pregnancy and lactation, the drug should be used when the benefit exceeds the risk for the pregnant and the mother, for the fetus and the newborn.

Dosing and Administration:

For infiltration anesthesia, 0.25%, 0.5% solutions are used; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - 0.25% solution.

To reduce the absorption and lengthening of the action with local anesthesia, an additional 0.1% solution of epinephrine is added, 1 drop per 2-5-10 ml of procaine solution.

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

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

For circular or paravertebral blockages 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 of a 0.25% solution or 150 ml of a 0.5% solution. In the future, during each hour of operation, not more than 1000 ml of 0.25% solution or 400 ml of 0.5% 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, motor anxiety, loss of consciousness, convulsions, trismus, tremor, visual and auditory disorders, nystagmus, cauda equina syndrome (paralysis of legs, paresthesia), paralysis of the respiratory muscles, motor and sensory block.

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

From the side of the blood: methemoglobinemia.

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

Other: return pain, persistent anesthesia, hypothermia.

Overdose:

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, "cold" sweat, quickening, breathing, 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:

Local anesthetics increase the inhibitory effect on the central nervous system for general anesthesia, hypnotics and 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 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.

Strengthen and prolong the action of muscle relaxants.

In the appointment of procaine, together with narcotic analgesics, an additive effect is noted that 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-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 cancel monoamine oxidase inhibitors 10 days before the introduction of a local anesthetic.

Before use, mandatory sampling for individual sensitivity to the drug.

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.

It is not absorbed from the mucous membranes; does not provide a superficial anesthesia for dermal application.

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:

For 100, 250 or 500 ml in polyvinyl chloride polymer containers for single-use infusion solutions of CPIR with two sterile ports.Each container is placed in a bag of polyethylene or polyethylene-polyamide films (double sterile vacuum packaging).

Containers in bags are placed in a box of corrugated cardboard with gaskets: 50, 75 pieces (100 ml), 24, 36 pieces (250 ml), 12, 18 pieces (500 ml). In the box with bags put instructions on the medical use of the drug and guidance on the use of injection solutions in polymer containers at the rate of 1 piece per 6 containers (for hospitals).

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:For hospitals

Registration number:LP-002699

Date of registration:07.11.2014

The owner of the registration certificate:MEDSINTEZ FACTORY, LTD. MEDSINTEZ FACTORY, LTD. Russia

Manufacturer: & nbsp

PLANT MEDSINTEZ, LLC Russia

Information update date: & nbsp02.09.2015

Illustrated instructions

Instructions

Novocaine (Novocaine)