Novocain maximum single dose. Medicinal reference book geotar. Terms and conditions of storage

As part of Novocaine solution includes the active ingredient, as well as additional components: hydrochloric acid, water.

Part suppositories included active ingredient procaine hydrochloride and solid fat as an additional component.

Release form

Produced Novocain solution 0.5% for injection. It is a colorless transparent liquid. Contains in ampoules of 2 ml, 5 ml, 10 ml. The cardboard package contains 10 ampoules, as well as a knife or scarifier.

Also produced Novocain 0.25%, Novocain 2%- a clear solution without color or slightly yellowish.

Novocaine is produced in the form rectal suppositories. In a cardboard box - 10 pcs.

pharmachologic effect

Wikipedia indicates that Novocaine (INN: Procaine) is a local anesthetic that exhibits moderate anesthetic activity. Name in Latin Novocainum. The formula of the active substance is C13H20N2O2. Qualitative reactions to novocaine are described in pharmaceutical textbooks. It has a wide range of therapeutic effects. The active substance blocks Na + - channels, preventing the generation of impulses and their conduction along the nerve fibers.

Under the influence of procaine, the action potential in the membranes changes nerve cells, while there is no pronounced effect on the resting potential. The agent suppresses the conduction of pain impulses in the body, and impulses of another modality.

When administered directly into the bloodstream and during absorption, it lowers the level of excitability of peripheral cholinergic systems, reduces the production and release of acetylcholine from preganglionic endings.

As evidenced by the pharmacopoeia, Novocain relieves spasm of smooth muscles, reduces the level of excitability of the myocardium and motor areas of the cerebral cortex. Under its influence, polysynaptic reflexes are suppressed, the descending inhibitory effects of the reticular formation of the brain stem are eliminated. When taking large doses of the drug, the patient may develop convulsions.

There is a short anesthetic activity of the drug. The duration of infiltration anesthesia is from 0.5 to 1 hour.

Pharmacokinetics and pharmacodynamics

In the body, complete systemic absorption of the active substance is noted.

The level of absorption depends on the route of administration, the site of administration, as well as the dose of the drug. The substance in the body is rapidly hydrolyzed, resulting in the formation of two main metabolites, pharmacologically active. This diethylaminoethanol , which produces a moderate vasodilating effect, and para-aminobenzoic acid (competitive antagonist of sulfanilamide drugs, weakening their antimicrobial effect). The half-life is 30-50 s, the half-life in the neonatal period is 54-114 s. It is mainly excreted from the body through the kidneys, about 2% is excreted unchanged. It is poorly absorbed through the mucous membranes.

Indications for use

The use of Novocain is practiced for infiltration, intraosseous, epidural, conduction, spinal . It is also used for anesthesia of the mucous membranes in the treatment of ENT diseases. Also, this tool is used for pararenal, vagosympathetic cervical, paravertebral and circular blockade.

Novocaine is administered intravenously in order to potentiate the effect of the main drugs used to conduct ; also administered intravenously for the purpose of stopping pain syndrome different origin.

Used intramuscularly to dissolve penicillin to prolong its duration. It is also noted that such a remedy as an auxiliary drug for the following diseases:

  • endarteritis ;
  • spasms of cerebral vessels and coronary vessels;
  • arterial hypertension ;
  • joint diseases of infectious and rheumatic origin.

Candles with Novocaine are used rectally for and, in case of spasms of the smooth muscles of the intestine.

Contraindications

There are some contraindications to the use of the drug. Novocain should not be used intramuscularly and intramuscularly with high sensitivity to the agent, as well as to other local anesthetic esters and para-aminobenzoic acid. Do not prescribe the drug to children under 12 years of age.

For local anesthesia, the agent is not used in the presence of pronounced fibrotic changes in the tissues.

Caution Novocaine is used for:

  • emergency surgical interventions that accompanies acute blood loss ;
  • conditions that are characterized by a decrease in hepatic blood flow;
  • cardiovascular insufficiency progressive;
  • lack pseudocholinesterase ;
  • inflammatory diseases or infection of the injection site;
  • renal failure;
  • under the age of 18 and over 65.

Side effects

During the application, the following side effects may occur:

  • central and peripheral NS: headaches , , manifestations drowsiness , lockjaw , weakness;
  • hematopoiesis: methemoglobinemia ;
  • the cardiovascular system: increase or decrease in blood pressure, bradycardia , peripheral vasodilation , arrhythmias , collapse , pain in chest;
  • allergy symptoms: rash on the skin , itching , other anaphylactic manifestations, .

In the event of the development of the negative manifestations described above or other side effects you need to immediately report this to the treating specialist.

Application instruction of Novocaine (Way and dosage)

Novocaine 0.5% is used for infiltration anesthesia at a dose of 350-600 mg. Adults at the beginning of surgery are given a dose of not more than 0.75 g (150 ml), then, every hour surgical operation- no more than 2 g (400 ml) of solution.

Holding pararenal blockade provides for the introduction of 50-80 ml of solution into the perirenal tissue.

Holding circular And paravertebral blockade involves the introduction of intradermal 5-10 ml of solution. In case of vagosympathetic blockade, 30-40 ml should be administered.

In order to reduce absorption and prolong the effect during local anesthesia, an additional solution is administered at the rate of 1 drop per 2-5-10 ml of solution procaine .

When used in adolescents after 12 years of age, the highest dose is 15 mg per 1 kg of body weight.

Candles Novocain, instructions for use

The use of suppositories is carried out according to individual scheme, depending on the disease. The candle should be inserted into anus by 3-4 cm. The introduction is carried out after a bowel movement or after an enema. As a rule, a candle is administered 1-2 times a day. The treatment period is up to 1 month.

Overdose

With an overdose of the drug, the patient may experience pallor of the mucous membranes and skin, nausea , dizziness , vomit , the appearance of "cold" sweat, , increased respiration, lowering blood pressure up to collapse, methemoglobinemia , . LS affects nervous system which manifests itself as a feeling of fear, convulsions , hallucinations , motor excitation.

In case of overdose, it is necessary to maintain adequate pulmonary ventilation, carry out symptomatic and detoxification treatment.

Interaction

Novocaine potentiates the effect on the central nervous system of drugs used for general anesthesia, sedatives and hypnotics, tranquilizers and narcotic analgesics.

When taken concurrently anticoagulants increases the likelihood of bleeding.

If the injection site has been treated with disinfectant solutions containing heavy metals, the risk of swelling and tenderness as a local reaction increases.

The use of Novocain simultaneously with inhibitors monoamine oxidase increases the likelihood of a sharp decline .

Novocaine prolongs and increases the effect of muscle relaxant drugs.

The local anesthetic effect is lengthened by vasoconstrictors ( phenylephrine , epinephrine , methoxamine ).

Under the influence of procaine, the antimyasthenic effect of the drugs decreases. Therefore, further adjustment of therapy may be required. .

Para-aminobenzoic acid (procaine metabolite) is a sulfonamide antagonist.

With the simultaneous use of cholinesterase inhibitors, the metabolism of local anesthetic drugs decreases.

Terms of sale

You can buy Novocaine 0.5% 5.0 by prescription, the doctor writes out a prescription in Latin.

Storage conditions

Novocain should be stored at room temperature, in a dry and dark place, keep away from children.

Best before date

Can be stored for 3 years, after the expiration date can not be used.

special instructions

Before using the product, you need to conduct an individual test for sensitivity to the drug.

In the process of treatment, it is necessary to control the functions of blood vessels, the heart, the central nervous system, and the respiratory system.

10 days prior to the administration of local anesthetic, monoamine oxidase inhibitors should be discontinued locally.

It is important to consider that when using the same dose of novocaine, the toxicity of procaine is higher if the solution is more concentrated.

Since procaine penetrates poorly through intact mucous membranes, it is not effective for superficial anesthesia.

During treatment, caution is needed when driving vehicles, as well as in other activities that require concentration.

Electrophoresis with Novocain at carried out after diagnosis and under the supervision of the attending physician.

You can not drip a solution of Novocain into the eyes without the consent of such actions with the doctor.

Analogues

Coincidence in the ATX code of the 4th level:

A number of drugs are produced that are analogues of this drug. These are the means Novocaine Bufus , Novocain-Vial , , Procaine Hydrochloride and others. The most optimal remedy is selected by the doctor, taking into account the patient's diagnosis.

children

The medicine is not used for children under 12 years of age. Adolescents from 12 to 18 years of age are used with caution.

Novocain during pregnancy and lactation

If there is a need to use Novocain during pregnancy, experts determine the expected benefits and possible risks. During childbirth, use with caution. If you need to use Novocain during breastfeeding, lactation should be stopped.

Reviews

Novocaine is spoken of as popular remedy for anesthesia. As a rule, it provides effective anesthesia and is well tolerated by patients. Users write about the successful use of Novocain in surgical interventions, in dental practice, etc.

The effectiveness of other means with procaine – patients use solutions, drops, spray, etc. As a positive point, the low cost of the medicine is noted.

Novocaine price, where to buy

The price of Novocain in ampoules is from 30 rubles. for 10 pcs. You can buy the drug at any pharmacy.

  • Internet pharmacies in Russia Russia
  • Internet pharmacies of Ukraine Ukraine
  • Internet pharmacies of Kazakhstan Kazakhstan

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Tradename: Novocaine

International non-proprietary name:

procaine

Dosage form:

injection.

Composition:

1 ml of the solution contains 5 mg or 20 mg of procaine hydrochloride as an active substance and excipients - a solution of hydrochloric acid 0.1 m, water for injection.
Description: clear colorless or slightly colored liquid.

Pharmacotherapeutic group:

local anesthetic.
ATX code:[ N01BA02 ]

Pharmacodynamics
A local anesthetic with moderate anesthetic activity and a wide range of therapeutic effects. Being a weak base, it blocks Na + channels, prevents the generation of impulses in the endings sensory nerves and 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. With absorption and direct intravascular administration, it reduces the excitability of peripheral cholinergic receptors, reduces the formation and release of acetylcholine from preganglionic endings (it has some ganglion-blocking effect), eliminates spasm of smooth muscles, and reduces the excitability of the myocardium and motor areas of the cerebral cortex. At intravenous administration has an analgesic, hypotensive and antiarrhythmic effect (increases the effective refractory period, reduces excitability, automatism and conductivity), in large doses it can disrupt neuromuscular conduction. Eliminates the descending inhibitory influences of the reticular formation of the brain stem. Inhibits polysynaptic reflexes. In high doses, it can cause convulsions. It has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 hour).

Pharmacokinetics
Undergoes complete systemic absorption. The degree of absorption depends on the site (the degree of vascularization and the rate of blood flow in the injection site), the route of administration and the total dosage. It is rapidly hydrolyzed by plasma and liver esterases with the formation of 2 main pharmacologically active metabolites: diethylaminoethonol (has a moderate vasodilating effect) and para-aminobenzoic acid (it is a competitive antagonist of sulfanilamide chemotherapy drugs and can weaken their antimicrobial effect). The half-life is 30-50 seconds, in neonotal period -54-114 s. It is excreted mainly by the kidneys in the form of metabolites, no more than 2% is excreted unchanged.

Indications for use

  • infiltration, conduction and epidural anesthesia;
  • vagosympathetic cervical, pararenal, circular and paravertebral blockades.

Contraindications
Hypersensitivity (including to para-aminobenzoic acid and other local anesthetics), childhood up to 12 years old.
For anesthesia by the method of creeping infiltrate: pronounced fibrotic changes in tissues. For epidural anesthesia: atrioventricular block, pronounced decrease blood pressure, shock, infection of the lumbar puncture site, septicemia.

Carefully
emergency operations accompanied by acute blood loss; conditions accompanied by a decrease in hepatic blood flow (for example, in chronic heart failure, liver diseases); pseudocholinesterase deficiency; kidney failure; children's age from 12 to 18 years and in elderly patients (over 65 years); weakened patients; pregnancy and childbirth.

Dosage and administration
For infiltration anesthesia: use 0.25-0.5% solutions; for anesthesia according to the Vishnevsky method (tight creeping infiltration) - 0.125-0.25% solutions. To reduce absorption and prolong the action during local anesthesia, an additional 0.1% solution of epinephrine hydrochloride is administered - 1 drop per 2-5-10 ml of procaine solution. Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation - no more than 500 ml for a 0.25% solution or 150 ml for a 0.5% solution. In the future, during each hour of the operation - no more than 1000 ml for a 0.25% solution or 400 ml for a 0.5% solution.
Maximum dose for use in children over 12 years of age -15 mg / kg.
For conduction anesthesia: 1-2% solutions (up to 25 ml); for epidural - 2% solution (20-25 ml). With pararenal blockade (according to A.V. Vishnevsky), 50-80 ml of a 0.5% solution or 100-150 ml of a 0.25% solution are injected into the perirenal tissue, and with vagosympathetic blockade - 30-100 ml of a 0.25% solution.
For circular or paravertebral blockades, a 0.25% - 0.5% solution is injected intradermally.

Side effect
Headache, dizziness, drowsiness, weakness, cauda equina syndrome, convulsions, increased or decreased blood pressure, collapse, peripheral vasodilation, bradycardia, arrhythmia, chest pain, involuntary urination or defecation, impotence, methemoglobinemia, allergic reactions(up to anaphylactic shock).
From the side digestive system: nausea, vomiting.
Other: return of pain, persistent anesthesia, hypothermia, with anesthesia in dentistry: numbness and paresthesia of the lips and tongue, prolongation of anesthesia.

Overdose
Symptoms: pale skin and mucous membranes. Dizziness, nausea, vomiting, "cold" sweat, increased severity of side effects. Treatment: maintenance of adequate pulmonary ventilation, detoxification and sympathetic therapy.

Interaction
Enhances the inhibitory effect on the central nervous system of general anesthesia, hypnotics and sedatives, narcotic analgesics and tranquilizers.
When using local anesthetic drugs for spinal and epidural anesthesia with guanadrel, guanethidine, mecamylamine, trimetaphan, the risk sharp decline blood pressure and bradycardia.
Anticoagulants (ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin) increase the risk of bleeding. When treating the injection site of local anesthetic disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.
Use with MAO inhibitors (furazolidone, procarbazine, selegeline) increases the risk of hypotension.
Strengthen and lengthen the action of muscle relaxants.
When prescribing procaine together with narcotic analgesics, an additive effect is noted, which is used during spinal and epidural anesthesia, while respiratory depression is enhanced.
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 in the treatment of myasthenia gravis.
Cholinesterase inhibitors (anti-myasthenic JIC, cyclophosphamide, demecarine, ecothiophate, thiotepa) reduce the metabolism of procaine.
The procaine metabolite (para-aminobenzoic acid) is a sulfonamide antagonist.

special instructions
Patients require control of the functions of the cardiovascular, respiratory and central nervous systems. It is necessary to cancel MAO inhibitors 10 days before the introduction of a local anesthetic. During the period of treatment, it is necessary to refrain from driving vehicles and engaging in potentially dangerous species activities that require increased concentration of attention and speed of psychomotor reactions. Before use, mandatory testing for individual sensitivity to the drug. It should be borne in mind that when conducting local anesthesia using the same total dose, the toxicity of novocaine is the higher, the more concentrated the solution is used. Not absorbed from mucous membranes; does not provide superficial anesthesia when applied to the skin.

Release form:

solution for injections 5 mg/ml, 20 mg/ml. 2.5ml-20mg/ml, 5.10ml - 5mg/ml in neutral glass ampoules. 10 ampoules with instructions for use in a pack or cardboard box. 5 ampoules in a blister pack. 2 blister packs in a cardboard box. An ampoule knife or a scarifier or an ampoule ceramic scarifier is put into each box. When packing ampoules with a break point or ring, an ampoule knife or a scarifier is not included.

Storage conditions
List B. In a dark place.

Best before date
3 years. Do not use after the expiry date stated on the packaging.

Terms of dispensing from pharmacies
Released by prescription.

Manufacturer / Organization accepting claims:
FSUE "Armavir Biological Factory"
352212. Russia, Krasnodar Territory, Novokubansky district, Progress settlement, st. Mechnikova, 11


Novocaine- a synthetic drug, 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 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 - a colorless crystalline powder, odorless, 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 able to suppress many interoceptive reflexes (from the circulatory, respiratory, intestinal, Bladder) due to the blockade of the transfer 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 ganglioblocking effect.
In the body, novocaine undergoes enzymatic hydrolysis, breaking down into para-aminobenzoic acid (PABA) and diethylaminoethanol, so the duration of its resorptive action is short.
Solutions of novocaine can be sterilized without decomposition.

Indications for use

Novocaine it is applied for local anesthesia, for infiltration anesthesia, novocaine vagosympathetic and pararenal blockade, anesthesia of Zakharyin-Ged zones, for pain relief during childbirth, for anesthesia in dental practice, for conduction and sacral anesthesia, for anesthesia by the method of tissue infiltration, for epidural and spinal anesthesia, for potentiation of action major drugs with general anesthesia.

Mode of application

For infiltration anesthesia, higher doses novocaine at the beginning of the operation, no more than 500 ml of a 0.25% solution or 150 ml of a 0.5% solution, then every hour up to 1000 ml of a 0.25% solution or 400 ml of a 0.5% solution for every hour. For conduction anesthesia, 1-2% solutions are used, with epidural (the introduction of a local anesthetic into the epidural space of the spinal canal to anesthetize areas innervated by the spinal nerves) - 20-25 ml of a 2% solution, for spinal - 2-3 ml of a 5% solution, with pararenal blockade - 50-80 ml of a 0.5% solution, with vagosympathetic blockade - 30-100 ml of a 0.25% solution, as a local anesthetic and antispasmodic (relieving spasms), the drug is used in suppositories of 0.1 g.

Side effects

Side effects from the use of the drug Novocaine may occur from the central and peripheral nervous system: headache, dizziness, drowsiness, weakness, lockjaw.
From the side of cardio-vascular system: increase or decrease in blood pressure, peripheral vasodilation, collapse, bradycardia, arrhythmias, chest pain.
On the part of the hematopoietic organs: methemoglobinemia.
Allergic reactions: skin itching, skin rash, other anaphylactic reactions (including anaphylactic shock), urticaria (on the skin and mucous membranes). If during the use of the drug any of the side effects indicated in the instructions appear or they are aggravated, or you notice any other side effects not indicated in the instructions, tell your doctor about it.

Contraindications

:
Contraindications to the use of the drug Novocaine are: hypersensitivity (including to para-aminobenzoic acid and other local anesthetic esters). Children's age up to 12 years.
For anesthesia by the method of creeping infiltrate - 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 heart failure, liver disease); progression of cardiovascular insufficiency (usually due to the development of heart blocks and shock); inflammatory diseases or infection at the injection site; pseudocholinesterase deficiency; kidney failure; children's age from 12 to 18 years, elderly age(over 65 years old); with caution in seriously ill and / or debilitated patients; during pregnancy and during childbirth.

Pregnancy

:
If necessary, the prescription of the drug Novocaine during pregnancy, the expected benefit to the mother and the potential risk to the fetus should be compared. With caution during childbirth. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.

Interaction with other drugs

Novocaine enhances the inhibitory effect on the central nervous system of drugs for general anesthesia, hypnotics, sedatives, narcotic analgesics and tranquilizers.
Anticoagulants (sodium ardeparin, sodium dalteparin, sodium danaparoid, sodium enoxaparin, sodium heparin, 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 (furazolidone, procarbazine, selegiline) increases the risk of developing a pronounced decrease in blood pressure. Enhances and prolongs the action of muscle relaxant drugs. 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 in the treatment of myasthenia gravis. Cholinesterase inhibitors (antimyasthenic medicines, cyclophosphamide, demecarium bromide, ecothiopa iodide, thiotepa) reduce the metabolism of local anesthetic drugs. The metabolite of procaine (para-aminobenzoic acid) is a sulfonamide antagonist.

Overdose

:
Symptoms of drug overdose Novocaine: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, "cold" sweat, increased respiration, tachycardia, lowering blood pressure, up to collapse, apnea, methemoglobinemia. The action on the central nervous system is manifested by a feeling of fear, hallucinations, convulsions, motor excitation.
Treatment: maintaining adequate pulmonary ventilation, detoxification and symptomatic therapy.

Storage conditions

List B. Powder - in a well-corked dark container, ampoules and suppositories - in a cool, dark place.

Release form

Powder; 0.25% and 0.5% solutions in ampoules of 1; 2; five; 10 and 20 ml and 1% and 2% solutions 1 each; 2; 5 and 10 ml; 0.25% and 0.5% sterile solutions of novocaine in vials of 200 and 400 ml; 5% and 10% ointment; candles containing 0.1 g of novocaine.

Composition

:
Procaine hydrochloride (novocaine) - 2.5 g or 5 g
Hydrochloric acid solution 0.1 M - up to pH 3.8 - 4.5
Water for injection - up to 1 l

Additionally

:
Novocaine is part of combined drugs menovazin, novocindol, synthomycin (1%) liniment with novocaine, solutan and efatin.

main parameters

Name: NOVOCAINE
ATX code: N01BA02 -

Novocaine is a local anesthetic a wide range therapeutic action with moderate anesthetic activity.

Release form and composition

Dosage forms of Novocain:

  • Solution for injection 0.5%: colorless, clear liquid (2, 5 or 10 ml per ampoule; in a carton box 10 ampoules complete with a scarifier or ampoule knife);
  • Solution for injection 2%: colorless, transparent or slightly colored liquid (2 or 5 ml per ampoule, in a carton box 10 ampoules complete with a scarifier or ampoule knife; 5 ampoules in a blister pack, in a carton box 2 packs complete with scarifier or ampoule knife.In packs with ampoules with a ring or a break point, do not put a scarifier or ampoule knife);
  • Solution for injection 0.25% (1, 2, 5 or 10 ml per ampoule, 10 ampoules in a carton box);
  • Solution for injection 1% (1, 2 or 5 ml per ampoule, 10 ampoules in a carton box);
  • Rectal suppositories (5 pcs. in a contour pack, 2 packs in a carton box; 5 pcs. in a contour pack, 2 packs in a carton box).

Active ingredient: procaine hydrochloride (in 1 ml of solution - 2.5; 5; 10 or 20 mg; in 1 suppository - 100 mg).

Additional components:

  • Solution for injection: water for injection, hydrochloric acid;
  • Rectal suppositories: solid fat.

Indications for use

Injection

  • Infiltration, epidural and conduction anesthesia;
  • Vagosympathetic cervical, circular, pararenal and paravertebral blockades.

Suppositories rectal

Contraindications

Injection

Absolute

  • With epidural anesthesia: a pronounced decrease in blood pressure, atrioventricular blockade, shock, septicemia, infection of the lumbar puncture site;
  • During anesthesia by the method of creeping infiltrate: pronounced fibrous changes in the tissues;
  • Age up to 12 years;
  • Hypersensitivity to the components of the drug (including para-aminobenzoic acid and other local anesthetics-ethers).

Relative (should be used with extreme caution, as there is a risk of complications):

  • Emergency operations occurring with acute blood loss;
  • Conditions accompanied by a decrease in hepatic blood flow (liver damage, chronic heart failure);
  • Progression of cardiovascular insufficiency (usually due to shock and the development of blockades);
  • Inflammatory diseases or infection of the injection site;
  • kidney failure;
  • Pseudocholinesterase deficiency;
  • Age from 12 to 18 years;
  • Old age (over 65 years).

With extreme caution, the drug should be used in seriously ill and / or debilitated patients, as well as during childbirth.

During pregnancy, the use of Novocain is possible only after a careful balance of the possible benefits of taking the drug and the risk of side effects. When prescribing the drug during lactation, it is required to stop breastfeeding.

Suppositories rectal

  • Hypersensitivity to the components of the drug (including para-aminobenzoic acid and other local anesthetic esters);
  • Age up to 18 years.

Method of application and dosage

Injection

For infiltration anesthesia, 0.25-0.5% solutions of the drug are prescribed, when anesthesia is carried out by the creeping infiltrate method (according to the Vishnevsky method) - 0.125-0.25% solutions. To prolong the action of the drug and reduce absorption during local anesthesia, an additional 0.1% solution of epinephrine hydrochloride is additionally used, administering 1 drop per 2-5-10 ml of procaine solution.

For adults, when performing infiltration anesthesia at the beginning of the operation, the first single dose should not exceed 150 ml for a 0.5% solution or 500 ml for a 0.25% solution. During the operation, during each hour it is recommended to inject no more than 400 ml for a 0.5% solution and 1000 ml for a 0.25% solution.

In children over 12 years of age, the maximum single dose is 15 mg / kg.

For conduction anesthesia, 1-2% solutions are used (not higher than 25 ml), for epidural - 2% solution (20-25 ml). During the pararenal blockade (according to A.V. Vishnevsky), a 0.5% solution at a dose of 50-80 ml or a 0.25% solution at a dose of 100-150 ml is injected into the perirenal tissue. With vagosympathetic blockade, the recommended dose of a 0.25% solution is 30-100 ml. For paravertebral or circular blockade, injections of 0.25-0.5% solution are carried out intradermally.

Suppositories rectal

The drug is injected deep into the anus, 1 suppository 1-2 times a day after a bowel movement or cleansing enema. As a local anesthetic, it is recommended to use no more than 5 days. When saving pain after the course of treatment, you should consult your doctor.

Side effects

  • Cardiovascular system: chest pain, arrhythmias, bradycardia, collapse, peripheral vasodilation, decrease or increase in blood pressure;
  • Nervous system: trismus, weakness, drowsiness, dizziness, headache, convulsions, cauda equina syndrome;
  • Urinary system: involuntary urination;
  • Organs of hematopoiesis: methemoglobinemia;
  • Digestive system: vomiting, nausea, involuntary defecation;
  • Allergic reactions: skin rash, skin itching, urticaria (on mucous membranes and skin), anaphylactic reactions (including anaphylactic shock);
  • Others: hypothermia, persistent anesthesia, return of pain; with anesthesia in dentistry - lengthening of anesthesia, paresthesia and numbness of the lips and tongue;
  • Local reactions: a feeling of discomfort and the urge to defecate (observed in the first days of the use of suppositories and pass on their own, without requiring discontinuation of therapy); rarely - itching and hyperemia in the anus (when used in high doses).

Symptoms of an overdose of Novocain are: vomiting, nausea, dizziness, pallor of the mucous membranes and skin, increased respiration, "cold" sweat, lowering blood pressure (up to collapse), tachycardia, methemoglobinemia, apnea, fear, hallucinations, motor agitation, convulsions . In this condition, measures are taken to maintain adequate ventilation of the lungs, detoxification and symptomatic therapy is carried out.

special instructions

Before using the drug, it is mandatory to conduct tests for individual sensitivity to its components.

In the case of therapy with monoamine oxidase inhibitors, the use of the latter must be canceled 10 days before the use of a local anesthetic.

It should be borne in mind that with the introduction of the same total dose of the drug, the toxicity of procaine is directly proportional to the concentration of the solution used.

During the introduction of the drug, it is required to monitor the activity of the central nervous, respiratory and cardiovascular systems.

When applied on the skin, Novocaine does not provide surface anesthesia.

drug interaction

It should be borne in mind that when combined with Novocaine:

  • Warfarin, sodium heparin, sodium enoxaparin, sodium danaparoid, sodium dalteparin, sodium ardeparin (anticoagulants) - increase the risk of bleeding;
  • Trimethaphan, mecamylamine, guanethidine, guanadrel - increase the risk of a sharp decrease in blood pressure and bradycardia;
  • Disinfectant solutions containing heavy metals (when treating the injection site) - increase the risk of swelling and pain at the injection site;
  • Selegiline, procarbazine, furazolidone (monoamine oxidase inhibitors) - exacerbate the threat of severe hypotension;
  • Phenylephrine, methoxamine, epinephrine (vasoconstrictors) - prolong the local anesthetic effect;
  • Narcotic analgesics - lead to an additive effect, which is used in epidural and spinal anesthesia(at the same time, there is an increase in respiratory depression);
  • Ecothiopata iodide, demecarium bromide, thiotepa, cyclophosphamide, antimyasthenic drugs (cholinesterase inhibitors) - reduce the rate of drug metabolism.

The effect of Novocain on concomitantly taken substances / drugs:

  • Muscle relaxant drugs - prolongs and enhances their action;
  • Medicines for general anesthesia, sedatives, sleeping pills, tranquilizers - exacerbates the depressing effect on the central nervous system;
  • Antimyasthenic drugs - reduces their effectiveness (requires correction of myasthenia therapy);
  • Sulfonamides - weakens the antibacterial effect, since the procaine metabolite (para-aminobenzoic acid) belongs to sulfonamide antagonists.

Terms and conditions of storage

Store in a place protected from light, out of the reach of children: solution for injection - at a temperature not exceeding 25 ° C; rectal suppositories - not higher than 20 ° C.

The shelf life of the solution is 3 years, suppositories - 2 years.

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

Synonyms: Aethocain, Allocaine, Ambocain, Aminocaine, Anesthocaine, Atoxicain, Cerocain, Chemocain, Citocain, Ethocaine, Genocaine, Herocaine, Isocain, Jenacain, Marecaine, 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. Let's very easily dissolve in water (1:1), we will easily dissolve in alcohol (1:8). Aqueous solutions sterilized at + 100 C for 30 minutes. Solutions of novocaine are easily hydrolyzed into alkaline environment. To stabilize, add 0.1 N. hydrochloric acid solution to pH 3.8 - 4.5.

Novocaine was synthesized in 1905. long time he 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 the 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 phenomena.

In addition to the local anesthetic effect, novocaine, when absorbed and directly injected into the bloodstream, has overall influence on the body: reduces the formation of acetylcholine and reduces the excitability of peripheral cholinergic 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.

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

Breakdown products of novocaine - pharmacologically active substances. para-Aminobenzoic acid (vitamin H 1) is an integral part of the molecule folic acid; it is also included in the bound state in other compounds found in plant and animal tissues. Para-aminobenzoic acid is a "growth factor" for bacteria. By chemical structure it is similar to part of the sulfonamide molecule; entering into competitive relations with the latter, para-aminobenzoic acid weakens their antibacterial action (see Sulfanilamide preparations). Novocaine as a derivative of para-aminobenzoic acid, it also has an antisulfanilamide effect. Diethylaminoethanol has moderate vasodilating properties.

Novocaine widely used for local anesthesia - mainly for infiltration; for surface anesthesia, it is of little use, as it slowly penetrates intact mucous membranes. Novocaine is widely prescribed for therapeutic blockades.

For infiltration anesthesin, 0.25 - 0.5% solutions are used; for anesthesia according to the method of A.V. 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 the mucous membranes, novocaine is sometimes used in otorhinolaryngology. To obtain a surface anesthetic effect, 10-20% solutions are required.

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

It should be noted that for the same total dose drug toxicity is higher, the more concentrated is the solution used.

To reduce the absorption and lengthen the action 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 also recommended for the treatment various diseases. Novocaine blockade aims to weaken the reflex reactions that occur during the development pathological processes. With pararenal 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 perirenal tissue, and with vagosympathetic blockade - 30 - 100 ml of 0.25% solution.

Solutions of novocaine are also used intravenously and orally (for hypertension, late toxicosis of pregnant women with hypertension, spasms blood vessels, phantom pains, peptic ulcer stomach and duodenum, non-specific 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. Enter slowly, preferably in isotonic solution sodium chloride. The number of injections (sometimes up to 10 - 20) depends on the severity of the disease and the effectiveness of the 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% solution nicotinic acid and 10,000 units of heparin. Enter intraarterially.

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 postoperative period(to relieve pain and spasms).

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

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

Candles (rectal) with novocaine are used as a local anesthetic and antispasmodic for spasms of the smooth muscles of the intestine.

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 of 2-5 ml is injected into a vein up to 4-5 times. More effective and specifically acting antiarrhythmic drugs are local anesthetics lidocaine and trimecaine and a derivative of novocaine - novocainamide (see).

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

Novocaine also assigned in the form intramuscular injections with some diseases that are more common in old age (endarteritis, atherosclerosis, hypertonic disease, spasms of the coronary and cerebral vessels, diseases of the joints of rheumatic and infectious origin, etc.). Treatment is carried out in a hospital. A 2% solution of novocaine, 5 ml, is injected into the muscles 3 times a week; for a course of 12 injections, after which they take a 10-day break. During the year, the course of treatment is repeated up to 4 times. The effect is seen mainly in early stages diseases associated with functional disorders of the central nervous system.

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

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

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

Release form: powder; 0.25% and 0.5% solutions in ampoules of 1; 2; five; 10 and 20 ml and 1% and 2% solutions 1 each; 2; 5 and 10 ml; 0.25% and 0.5% sterile solutions of novocaine in vials of 200 and 400 ml; 5% and 10% ointment; candles containing 0.1 g of novocaine.

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

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

Rp:. Sol. Novocaini 0.25% 200ml

D.S. For infiltration anesthesia

Rp.: Sol. Novocaini 1% 10ml

D.t.d. N. 5 in amp.

S. For conduction anesthesia

Rp.: Novocaini 1, 25

Natrii chloridi 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. Inside 1 tablespoon

Rp.: Sol. Novocaini 2% 5ml

D.t.d. N. 6 in amp.

S. 5 ml into the muscles 1 time in 2 days