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

Active substances:
Procaine hydrochloride (novocaine) -	0.25% 2.5 g
	0.5% 5.0 g
Excipients:
Water for injections	up to 1.0 liter
The hydrochloric acid 0.1 M solution	to pH 3.8 - 4.5

Description:

Transparent colorless liquid.

Pharmacotherapeutic group:Local anesthetic

ATX: & nbsp

Procain

Pharmacodynamics:

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 para-aminobenzoic acid (a competitive antagonist of sulfanilamide preparations and can weaken their antimicrobial effect). The half-life period (T1 / 2) is 30-50 sec, in the neonatal period - 54-114 sec. 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'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 (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 years); 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 the absorption and lengthening of the action with local anesthesia, an additional 0.1% solution of epinephrine is injected - 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 0.25% are administered into the peritoneal cellulose, and 30-100 ml of 0.25% solution with a vagosympathetic blockade.

For circulatory and paravertebral blockages intradermally injected 0.25% or 0.5% solution.

Higher doses for infiltration anesthesia in adults: the first single dose at the beginning of the operation - no more than 500 ml of 0.25% solution and 150 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, 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 spread of excitation in the heart, which appear on the ECG in the form of a flat T wave or a shortening of the ST segment.

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

From 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" 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 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. Strengthens and prolongs 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 performed by experienced specialists in suitably equipped room with the availability of ready-to-use equipment and drugs needed 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, care must be taken when driving vehicles and engaging in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Novocain, injection for 0.25% or 0.5%.

Packaging:

For 100, 200, 400 ml in glass bottles with the capacity of 100,250 or 450 ml.

1 bottle with instructions for medical use in a pack of cardboard. For hospitals: 36 bottles with a capacity of 100 ml, 15, 28 bottles with a capacity of 250 ml or 15 bottles with a capacity of 450 ml, along with instructions for medical use in quantities corresponding to the number of bottles, are placed in a box of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Non-wetting of the inner surface of bottles is not a contraindication to the use of the drug.

In the event of a change in the color of the preparation or the appearance of a suspension, the solution is not suitable for use.

Shelf life:

3 years. Do not use after the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003521

Date of registration:23.03.2016

Expiration Date:23.03.2021

The owner of the registration certificate:MOSFARM, LLCMOSFARM, LLC

Manufacturer: & nbsp

MOSFARM, LLC

Information update date: & nbsp25.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)