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Local anesthetic

Active substance

Procaine

Release form, composition and packaging

Solution for injection 0.5% transparent, colorless.

Excipients: hydrochloric acid 0.1M, water for injection.

2 ml - ampoules (10) / complete with an ampoule knife or scarifier, if necessary for ampoules of this type /) - cardboard packs.
5 ml - ampoules (10) / complete with an ampoule knife or scarifier, if necessary for ampoules of this type /) - cardboard packs.
10 ml - ampoules (10) / complete with an ampoule knife or scarifier, if necessary for ampoules of this type /) - cardboard packs.

pharmachologic effect

A local anesthetic with moderate anesthetic activity and a wide range of therapeutic effects. Being a weak base, it blocks Na + channels, preventing the generation of impulses in the endings of sensory nerves and the conduction of impulses along nerve fibers. Changes the action potential in the membranes of nerve cells without a pronounced effect on the resting potential. Suppresses the conduction of not only pain, but also impulses of other modalities. When absorbed and directly vascularly introduced into the bloodstream, it reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic endings (has some ganglion-blocking effect), eliminates spasm of smooth muscles, reduces the excitability of the myocardium and motor zones of the cerebral cortex. Eliminates descending inhibitory influences of the reticular formation of the brain stem. Inhibits polysynaptic reflexes. In large doses, it can cause convulsions. It has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 hour).

Pharmacokinetics

Subject to complete systemic absorption. The extent of absorption depends on the site and route of administration (especially vascularization and blood flow rate of administration) and the final dose (amount and concentration). It is quickly hydrolyzed by esterases and the liver to form two main pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilator effect) and para-aminobenzoic acid (is a competitive antagonist of sulfonamide drugs and can weaken their effect). T 1/2 - 30-50 s, in the neonatal period - 54-114 s. It is excreted primarily by the kidneys in the form of metabolites; no more than 2% are excreted unchanged.

Indications

Infiltration (including intraosseous) anesthesia; vagosympathetic cervical, perinephric, circular and paravertebral blockades.

Contraindications

Hypersensitivity (including to para-aminobenzoic acid and other local anesthetic esters). Children's age up to 12 years.

For anesthesia using the creeping infiltrate method - pronounced fibrous changes in the tissues.

Carefully. Emergency operations accompanied by acute blood loss; conditions accompanied by a decrease in hepatic blood flow (for example, chronic 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; ; children's age from 12 to 18 years, old age (over 65 years); with caution in seriously ill and/or debilitated patients; during pregnancy and during childbirth.

Dosage

Only for procaine solution 5 mg/ml (0.5%).

For infiltration anesthesia 350-600 mg (70-120 ml) are administered. 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 the operation - no more than 2 g (400 ml) of solution.

At perinephric block(according to A.V. Vishnevsky) 50-80 ml are injected into the perinephric tissue.

At circular and paravertebral blockade 5-10 ml are injected intradermally. For vagosympathetic blockade, 30-40 ml is administered.

For reducing absorption and prolonging the action of local anesthesia, additionally inject a 0.1% solution of epinephrine hydrochloride - 1 drop per 2-5-10 ml of procaine solution.

The maximum dose for use in children over 12 years old- 15 mg/kg.

Side effects

From the central and peripheral nervous system: headache, dizziness, drowsiness, weakness, trismus.

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

From the hematopoietic organs: methemoglobinemia.

Allergic reactions: itching of the skin, skin rash, other anaphylactic reactions (including anaphylactic shock), urticaria (on the skin and mucous membranes). If, while using the drug, any of the side effects indicated in the instructions appear or they get worse, or you notice any other side effects not listed in the instructions, inform your doctor.

Overdose

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, “cold” sweat, increased breathing, tachycardia, decreased blood pressure, even collapse, apnea, methemoglobinemia. The effect on the central nervous system is manifested by a feeling of fear, hallucinations, convulsions, and motor agitation.

Treatment: maintaining adequate pulmonary ventilation, detoxification and symptomatic therapy.

Drug interactions

Strengthens the inhibitory effect on the central nervous system of drugs for general anesthesia, sleeping pills, sedatives, narcotic analgesics and tranquilizers.

Anticoagulants (ardeparin sodium, dalteparin sodium, danaparoid sodium, heparin sodium, warfarin) increase the risk of bleeding. When treating the injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.

Use with monoamine oxidase inhibitors (procarbazine, selegiline) increases the risk of developing a pronounced decrease in blood pressure. Strengthens and prolongs the effect of muscle relaxants. Vasoconstrictors (epinephrine, methoxamine, phenylephrine) prolong the local anesthetic effect.

Procaine reduces the antimyasthenic effect of drugs, especially when used in high doses, which requires additional correction of the treatment of myasthenia gravis.

Cholinesterase inhibitors (antimyasthenic drugs, cyclophosphamide, demecaria bromide, ecothiopathy iodide, thiotepa) reduce the metabolism of local anesthetic drugs.

The metabolite of procaine (para-aminobenzoic acid) is an antagonist of sulfonamides.

special instructions

Patients require monitoring of the functions of the cardiovascular system, respiratory system and central nervous system.

Monoamine oxidase inhibitors should be discontinued 10 days before local anesthetic administration.

It should be borne in mind that when performing local anesthesia using the same total dose, the toxicity of procaine is higher, the more concentrated the solution is used.

Impact on the ability to drive vehicles and machinery

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Pregnancy and lactation

If it is necessary to prescribe the drug during pregnancy, the expected benefit to the mother should be compared with the potential risk to the fetus. With caution during childbirth.

Conditions for dispensing from pharmacies

The drug is available with a prescription.

Storage conditions and periods

Store the drug in a place protected from light, at a temperature not exceeding 25°C. Keep out of the reach of children.

Shelf life - 3 years. Do not use after the expiration date stated on the packaging.

Novocaine- a synthetic drug that belongs to the group of local anesthetics.
Novocaine has a local analgesic effect, after absorption into the blood - anti-inflammatory, analgesic, antihistamine, desensitizing and antitoxic effect, reduces spasms of smooth muscles, reduces the excitability of the heart muscle.
Novocaine differs from cocaine in having less toxicity (7-10 times) and less anesthetic power. The drug does not have a local vasoconstrictor effect.
Novocaine- beta-diethylaminoethyl ester of para-aminobenzoic acid hydrochloride is a colorless, odorless, crystalline powder, bitter taste, highly soluble in water and ethyl alcohol.
Clinical studies show that novocaine, when introduced into the body, also has a resorptive effect, mainly on the functions of the nervous system.
Novocaine is capable of suppressing many interoceptive reflexes (from the circulatory, respiratory, intestinal, bladder) due to blockade of the transmission of excitation in the central links of the corresponding reflex arcs. Novocaine also has an inhibitory effect on the reticular formation of the midbrain and has a ganglion-blocking effect.
In the body, novocaine undergoes enzymatic hydrolysis, breaking down into para-aminobenzoic acid (PABA) and diethylaminoethanol, so the duration of its resorptive effect is short.
Novocaine solutions can be sterilized without decomposition.

Indications for use

Mode of application

Side effects

Contraindications

Pregnancy

Interaction with other drugs

Overdose

Storage conditions

Release form

Compound

Additionally

Main settings

Novocaine. Novocainum. Jenacain. Polocainum. Procaini Hydrochloridum.

β-Diethylaminoethyl ester of para-aminobenzoic acid hydrochloride.

Release form of the medicine. Powder and ampoules of 1, 2, 5 and 10 ml of 0.25%, 0.5%, 1% and 2% solution; 5% and 10% ointment; suppositories containing 0.1 g of novocaine.

Application and dosage of the drug. For infiltration anesthesia - 0.25-0.5% solutions, for conduction anesthesia - 1-2% solutions, for spinal anesthesia - 1-5% solutions, for terminal anesthesia (in otolaryngology and ophthalmology) - 10-20% solutions. Orally, 0.1-0.2 g of novocaine 2-3 times a day before meals. Intravenously, 10-20 ml of 0.25% solution. Intramuscularly, 2-5 ml of 2% solution. For perinephric blockade - 50-80 ml of 0.5% solution or 100-150 ml of 0.25% solution. For vagosympathetic blockade - 30-100 ml of 0.25% solution. It must be taken into account that at the same dose of the drug, its toxicity increases with increasing concentration.

Higher doses orally - single 0.25 g, daily 0.75 g; intramuscular single dose 0.1 g (5 ml of 2% solution), daily 0.1 g; intravenously - single 0.05 g (20 ml of 0.25% solution), daily 0.1 g.

For infiltration anesthesia, the highest doses: at the beginning of the operation, the first dose is 1.25 g (using a 0.25% solution, 500 ml), then 2.5 g for each hour of surgery (1000 ml of a 0.25% solution). When using a 0.5% solution, the initial dose should not exceed 0.75 g (150 ml of a 0.5% solution). To reduce the absorption of novocaine, a solution of adrenaline is added to its solution.

Action of the medicine. Novocaine inhibits the occurrence and conduction of centripetal nerve impulses by disrupting the permeability of cell membranes to sodium and potassium ions. There is evidence indicating a greater sensitivity of afferent nerve fibers compared to efferent ones. Novocaine has a local anesthetic effect during infiltration and conduction anesthesia. It has a weaker effect during terminal anesthesia, since it almost does not penetrate through the intact mucous membrane. When absorbed or administered intravenously, novocaine inhibits the synthesis of acetylcholine and reduces the reactivity of peripheral cholinoreactive systems, blocks the autonomic ganglia, gives an antispasmodic effect, reduces myocardial excitability, inhibits the motor zones of the cerebral cortex, and is a sulfonamide antagonist. Low toxicity, but some people have increased sensitivity to the drug. In the body, novocaine is quickly hydrolyzed to form physiologically active substances: para-aminobenzoic acid (vitamin H1) and diethylaminoethanol (a vasodilator).

Indications for use. Operations using infiltration, conduction, spinal anesthesia; hypertension, late toxicosis of pregnant women with hypertension, vasospasms (angina pectoris, cerebral vascular spasms), atrial fibrillation, endarteritis, phantom pain, itching, neurodermatitis, eczema, keratitis, iridocyclitis, glaucoma, sciatica, ; rheumatic and infectious origin. Treatment is carried out in a hospital setting. Novocaine is administered intravenously or intramuscularly.

Contraindications. The presence of inflammatory or purulent processes at the injection site, increased sensitivity to novocaine - esters of para-aminobenzoic acid (to detect it, novocaine is first prescribed in small doses), severe diseases of the cardiovascular system.

Possible side effects. Dizziness, general weakness, hypotension, convulsions, fainting, shock, dermatitis. During spinal anesthesia: pallor, cold sweat, weak pulse, shortness of breath, collapse. At a later date, vomiting may occur; persistent headache, symptoms of meningism.

Treatment of complications and poisonings. Gastric lavage with a suspension of activated carbon, followed by the introduction of activated carbon and a saline laxative. For agitation and convulsions - barbamyl (5-10 ml of 5% solution) intramuscularly or (0.1 mg/kg) intravenously. Intubation. Oxygen therapy. Transfusion therapy. . Analeptics are contraindicated. For severe headaches - amidopyrine. Cm. .

N.01.B.A Aminobenzoic acid esters

N.01.B.A.02 Procaine

NOVOCAINE (Novocainum). b-Diethylaminoethyl ester of para-aminobenzoic acid hydrochloride.

Synonyms: Aethocain, Allocaine, Ambocain, Aminocaine, Anesthocaine, Atoxicain, Cerocain, Chemocain, Citocain, Ethocain, Genocaine, Herocaine, ISOCain, Jenacin, Maresaine Minocain, Naucain, Neocaine, Pancain, Paracaine, Planocaine, Polocainum, Procaine, Procaini Hydrochloridum , Procaine hydrochloride, Protocaine, Sevicaine, Syncaine, Syntocain, Topocaine, etc.

Colorless crystals or odorless white crystalline powder. Very easily soluble in water (1:1), easily soluble in alcohol (1:8). Aqueous solutions are sterilized at + 100 C for 30 minutes. Solutions of novocaine are easily hydrolyzed in an alkaline environment. To stabilize, add 0.1 N. hydrochloric acid solution to pH 3.8 - 4.5.

Novocaine was synthesized in 1905. For a long time it was the main local anesthetic used in surgical practice. Compared to modern local anesthetics (lidocaine, bupivacaine, etc.), it has less strong anesthetic activity. However, due to its relatively low toxicity, large therapeutic breadth and additional valuable pharmacological properties allowing its use in various fields of medicine, it is still widely used.

Unlike cocaine, novocaine does not cause addiction.

In addition to the local anesthetic effect, novocaine, when absorbed and directly introduced into the bloodstream, has a general effect on the body: it reduces the formation of acetylcholine and reduces the excitability of peripheral cholinoreactive systems, has a blocking effect on the autonomic ganglia, reduces spasms of smooth muscles, reduces the excitability of the heart muscle and motor areas of the cerebral cortex. brain

In the body, novocaine is hydrolyzed relatively quickly, forming para-aminobenzoic acid and diethylaminoethanol.

Novocaine breakdown products are pharmacologically active substances. para-Aminobenzoic acid (vitamin H 1) is an integral part of the folic acid molecule; it is also included in a bound state in other compounds found in plant and animal tissues. For bacteria, para-aminobenzoic acid is a “growth factor”. Its chemical structure is similar to part of the sulfonamide molecule; entering into a competitive relationship with the latter, para-aminobenzoic acid weakens their antibacterial effect (see Sulfanilamide drugs). Novocaine As a derivative of para-aminobenzoic acid, it also has an antisulfonamide effect. Diethylaminoethanol has moderate vasodilatory properties.

Novocaine widely used for local anesthesia - mainly for infiltration; It is of little use for superficial anesthesia, since it slowly penetrates through intact mucous membranes. Novocaine is also widely prescribed for therapeutic blockades.

For infiltration anesthesin, 0.25 - 0.5% solutions are used; for anesthesia according to the A.V. method Vishnevsky (tight creeping infiltration) 0.125 - 0.25% solutions; for conduction anesthesia - 1 - 2% solutions; for epidural - 2% solution (20 - 25 ml).

Sometimes novocaine is also prescribed for intraosseous anesthesia.

For anesthesia of mucous membranes, novocaine is sometimes used in otorhinolaryngology. To obtain a superficial anesthetic effect, 10 - 20% solutions are required.

With local anesthesia, the concentration of novocaine solutions and their quantity depend on the nature of the surgical intervention; method of application, condition and age of the patient, etc.

It should be borne in mind that for the same total dose of the drug, the more concentrated the solution used, the higher the toxicity.

To reduce absorption and prolong the effect of novocaine solutions during local anesthesia, a solution of adrenaline hydrochloride (0.1%) is usually added to them - 1 drop per 2 - 5 - 10 ml of novocaine solution, since novocaine, unlike cocaine, does not cause vasoconstriction.

Novocaine It is also recommended for the treatment of various diseases. Novocaine blockade aims to weaken reflex reactions that occur during the development of pathological processes. For perinephric blockade (according to A.V. Vishnevsky), 50-80 ml of a 0.5% solution or 100-150 ml of a 0.25% solution of novocaine are injected into the perinephric tissue, and for vagosympathetic blockade - 30-100 ml of 0.25% solution.

Novocaine solutions are also used intravenously and orally (for hypertension, late toxicosis of pregnant women with hypertensive syndrome, spasms of blood vessels, phantom pain, gastric and duodenal ulcers, nonspecific ulcerative colitis, itching, neurodermatitis, eczema, keratitis, iridocyclitis, glaucoma, etc. .). From 1 to 10 - 15 ml of a 0.25 - 0.5% solution is injected into a vein. Introduce slowly, preferably in an isotonic sodium chloride solution. The number of injections (sometimes up to 10 - 20) depends on the severity of the disease and the effectiveness of treatment.

To relieve spasms of peripheral vessels and improve microcirculation during frostbite (in the pre-reactive period), a mixture consisting of 10 ml of 0.25% novocaine solution, 2 ml of 2% papaverine solution, 2 ml of 1% nicotinic acid solution and 10,000 units of heparin is proposed. Injected intra-arterially.

Intravenous administration of a small amount of novocaine potentiates the effect of drugs used for anesthesia, has an analgesic and anti-shock effect, and therefore it is sometimes used to prepare for anesthesia, during anesthesia (to enhance the effect of the main anesthetic) and in the postoperative period (to relieve pain and spasms).

Take 0.25 - 0.5% solution up to 30 - 50 ml orally 2 - 3 times a day.

Intradermal injections of 0.25 - 0.5% solution are recommended for circular and paravertebral blockade for eczema, neurodermatitis, sciatica, etc.

Suppositories (rectal) with novocaine are used as a local anesthetic and antispasmodic for spasms of intestinal smooth muscles.

Novocaine(5 - 10% solution) is also used using the electrophoresis method.

Due to the ability of the drug to reduce the excitability of the heart muscle, it is sometimes prescribed for atrial fibrillation - a 0.25% solution is injected into a vein, 2 - 5 ml up to 4 - 5 times. More effective and specifically acting antiarrhythmic drugs are the local anesthetics lidocaine and trimecaine and the novocaine derivative - novocainamide (see).

Novocaine used to dissolve penicillin in order to extend its duration of action (see Penicillin group drugs).

Novocaine They are also prescribed as intramuscular injections for certain diseases that are more common in old age (endarteritis, atherosclerosis, hypertension, spasms of coronary and cerebral vessels, joint diseases of rheumatic and infectious origin, etc.). Treatment is carried out in a hospital setting. A 2% solution of novocaine, 5 ml, is injected into the muscles 3 times a week; There are 12 injections per course, after which a 10-day break is taken. During the year, the course of treatment is repeated up to 4 times. The effect is observed mainly in the early stages of diseases associated with functional disorders of the central nervous system.

Novocaine It is generally well tolerated but may cause side effects and should be used with caution for all routes of administration. Some patients experience increased sensitivity to the drug (dizziness, general weakness, decreased blood pressure, collapse, shock). Allergic skin reactions (dermatitis, peeling, etc.) may develop. To identify hypersensitivity, novocaine is first prescribed in reduced doses. First, 2 ml of a 2% solution is injected intramuscularly, after 3 days in the absence of side effects - 3 ml of this solution, and only then proceed to the administration of the full dose - 5 ml per injection.

Higher doses of novocaine (for adults): single dose when taken orally 0.25 g, when administered into muscles (2% solution) - 0.1 g (5 ml), when administered into a vein (0.25% solution) - 0. 05 g (20 ml); daily intake 0.75 g; when administered into muscles (2% solution) and into a vein (0.25% solution) - 0.1 g.

For infiltration anesthesia, the following highest doses are established (for adults): the first single dose at the beginning of the operation is not more than 1.25 g of 0.25% solution (i.e. 500 ml) and 0.75 g of 0.5% solution (t i.e. 150 ml). Subsequently, during each hour of surgery - no more than 2.5 g of 0.25% solution (i.e. 1000 ml) and 2 g of 0.5% solution (i.e. 400 ml).

Release forms: powder; 0.25% and 0.5% solutions in ampoules of 1; 2; 5; 10 and 20 ml and 1% and 2% solutions, 1; 2; 5 and 10 ml; 0.25% and 0.5% sterile solutions of novocaine in bottles of 200 and 400 ml; 5% and 10% ointment; suppositories containing 0.1 g of novocaine.

Novocaine is part of the complex drug "Menovazin" (see).

Storage: List B. In well-closed orange glass jars; ampoules and suppositories - in a place protected from light.

Rp:. Sol. Novocaini 0.25% 200 ml

D.S. For infiltration anesthesia

Rp.: Sol. Novocaini 1% 10 ml

D.t.d. N. 5 in ampull.

S. For conduction anesthesia

Rp.: Novocaini 1, 25

Sodium chloride 3.0

Kalii chloridi 0.038

Calcii chloridi 0.062

Aq. pro injection. 500 ml

M. Steril.!

D.S. For anesthesia according to the method of A. V. Vishnevsky

Rp.: Novocaini 0.5

Aq. destill. 200 ml

M.D.S. 1 tablespoon inside

Rp.: Sol. Novocaini 2% 5 ml

D.t.d. N. 6 in ampull.

S. 5 ml into muscles 1 time every 2 days