Novocaine (instructions for use in ampoules) is a solution for local anesthesia. Novocaine - instructions, use, indications, contraindications, action, side effects, analogues, dosage, composition

Name:

Novocain (Novocainum)

Pharmacological
action:

Local anesthetic with moderate anesthetic activity and wide latitude therapeutic action.
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 impulses in the endings of sensory nerves and the conduction of impulses along nerve fibers.
Changes action potential in membranes nerve cells without a pronounced effect on the resting potential. Suppresses the conduction of not only pain, but also impulses of other modalities.
Upon entering the systemic circulation reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic endings (has a weak ganglion-blocking effect), eliminates spasm of smooth muscles, reduces the excitability of the myocardium and motor areas of the cerebral cortex.
Compared to lidocaine and bupivacaine, procaine has a less pronounced anesthetic effect and, therefore, has relatively low toxicity and greater therapeutic breadth.

Pharmacokinetics
Poorly absorbed through mucous membranes.
At parenteral administration well absorbed, quickly hydrolyzed by plasma and tissue esterases to form two main pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilating effect) and PABC. T1/2 - 0.7 min.
Excreted primarily by the kidneys in the form of metabolites - 80%.

Indications for
application:

Infiltration, conduction, epidural and spinal anesthesia;
- intraosseous anesthesia;
- anesthesia of mucous membranes (in ENT practice); vagosympathetic and perinephric blockade;
- circular and paravertebral blockades for eczema, neurodermatitis, ischalgia.

IV: to potentiate the action of basic anesthetics; for cupping pain syndrome of various origins.
V/m: to dissolve penicillin in order to extend its duration of action; as aid for some diseases that are more common in old age, incl. endarteritis, atherosclerosis, arterial hypertension, spasms coronary vessels and cerebral vessels, joint diseases of rheumatic and infectious origin.
Rectally: hemorrhoids, spasms of intestinal smooth muscles, anal fissures.
Procaine as an adjuvant used intravenously and orally for arterial hypertension, late toxicosis of pregnant women with hypertensive syndrome, spasms blood vessels, phantom pain, peptic ulcer stomach and duodenum, NUC, itching, neurodermatitis, eczema, keratitis, iridocyclitis, glaucoma.

Mode of application:

With infiltration anesthesia the highest doses at the beginning of the operation are no more than 500 ml of a 0.25% solution or 150 ml of a 0.5% solution, then for 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 use 1-2% solutions, with epidural(administered local anesthetic into the epidural space spinal canal for the purpose of anesthetizing areas innervated spinal nerves) -20-25 ml of 2% solution, for spinal- 2-3 ml of 5% solution, with perirenal block- 50-80 ml of 0.5% solution, with vagosympathetic blockade- 30-100 ml of 0.25% solution, as a local anesthetic and antispasmodic(relieving spasms) means the drug is used in suppositories of 0.1 g.

Side effects:

Maybe: arterial hypotension, collapse, dizziness, weakness, urticaria, allergic reactions, anaphylactic shock.

Contraindications:

Individual intolerance.
It should be taken into account that when carrying out local anesthesia when using the same total dose the toxicity of procaine is higher, the more concentrated the solution used.
Procaine penetrates slowly through intact mucous membranes and is therefore not very effective for superficial anesthesia.

The ability to influence the reaction speed when driving a vehicle or working with other mechanisms.
During the treatment period, care must be taken when managing vehicles and activities potentially dangerous species activities requiring increased concentration attention and speed of psychomotor reactions.

Interaction
other medicinal
by other means:

Prolongs the neuromuscular blockade caused by suxamethonium (since both drugs are hydrolyzed by plasma cholinesterase).
Use simultaneously with MAO inhibitors (furazolidone, procarbazine, selegeline) increases the risk of developing arterial hypotension . The toxicity of procaine is increased by anticholinesterase drugs (suppressing its hydrolysis).
Procaine metabolite (para-aminobenzoic acid) is a competitive antagonist sulfa drugs and can weaken them antimicrobial effect.
When treating the local anesthetic injection site with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of pain and swelling increases.
Potentiates the effect of direct anticoagulants.
The drug reduces the effect anticholinesterase drugs on neuromuscular transmission.
Cross-sensitization possible.

Pregnancy:

Use during pregnancy is possible provided it is well tolerated.
During breastfeeding, the use of the drug is possible after a preliminary careful assessment of the expected benefits of therapy for the mother and the potential risk for the baby.
When used during childbirth, bradycardia, apnea, and convulsions may develop in the newborn.

Overdose:

This is only possible when novocaine is used in high doses.
Symptoms: pallor skin and mucous membranes, dizziness, nausea, vomiting, increased nervous excitability, “cold” sweat, tachycardia, decreased blood pressure almost to collapse, tremor, convulsions, apnea, methemoglobinemia, respiratory depression, sudden cardiovascular collapse.
The effect on the central nervous system is manifested by a feeling of fear, hallucinations, convulsions, and motor agitation. In cases of overdose, administration of the drug should be stopped immediately. When performing local anesthesia, the injection site can be injected with adrenaline.
Treatment: are common resuscitation measures which include oxygen inhalation and, if necessary, artificial ventilation lungs. If convulsions continue for more than 15-20 seconds, they are stopped intravenous administration thiopental (100-150 mg) or diazepam (5-20 mg). For arterial hypotension and/or myocardial depression, ephedrine (15-30 mg) is administered intravenously; severe cases– detoxification and symptomatic therapy.
If intoxication develops after injection of novocaine into the muscles of the leg or arm, it is recommended to urgently apply a tourniquet to reduce the subsequent entry of the drug into the general bloodstream.

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 reticular formation 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 acute blood loss; conditions accompanied by decreased hepatic blood flow (for example, chronic failure, liver diseases); progression cardiovascular failure(usually due to the development of heart block and shock); inflammatory diseases or infection of the injection site; pseudocholinesterase deficiency; ; childhood from 12 to 18 years old, elderly age(over 65 years old); 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 outside of cardio-vascular system: increase or decrease in blood pressure, peripheral vasodilation, collapse, bradycardia, arrhythmias, .

From the hematopoietic organs: methemoglobinemia.

Allergic reactions: itchy 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, please 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. Action on the central nervous system 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 medicines, 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 cardiovascular system functions, respiratory system and the 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.

If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

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 package.

Novocaine— 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 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 able to suppress many interoceptive reflexes (from the circulatory, respiratory, intestinal, Bladder) due to blockade of excitation transmission 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

What is novocaine? Unique in its composition medical drug synthetic origin, which is usually classified as a group of agents for local anesthesia. It has a direct analgesic effect, which is observed after the drug is absorbed into the blood. A solution administered intravenously in the form of injections, with a volume of about five mg, also allows it to have an anti-inflammatory effect, and also act as an analgesic that can somewhat reduce the occurrence and development of spasms in smooth muscles.

What is noteworthy is novocaine, injections of which are carried out intravenously in accordance with the regulations medical standards, provides general decline excitability of the heart muscle. Unlike the similar anesthetic drug cocaine, it has slightly less toxicity, but also has less impact, which should be taken into account. The difference is observed in terms of approximately 10 times and this key difference drugs.

Features of application

Novocaine injection solution, which is taken based on the norm of five injections, is used according to medical practice for direct local anesthesia, as well as a number of anesthesia, such as Zakharyin-Ged zones, in dentistry and other situations. It is customary to use the drug intramuscularly, which will allow the composition to be easily delivered to the human body and ensure subsequent pain relief. In particular, intravenous novocaine is relevant when performing spinal anesthesia, which is the most difficult for a potential patient who consults a doctor. Current this drug and during tissue infiltration surgery, when performing general anesthesia, when injections of novocaine in a dosage of five mg are designed to provide the necessary effect with minimal side effects.

Rules of use, individual characteristics, doctor’s prescription

Some have been developed and installed specific features, according to which five mg novocaine injections are used intramuscularly. However, all the basic definitions and specifics of use are worked out directly by the attending physician. For this reason, before using novocaine in the form of mg injections, you will definitely need to undergo appropriate consultation. You can select following features the use of novocaine, through which it is important to distribute rationing and subsequent supply of components in the required quantity.

The following order of supply and normalization of the drug is determined:

• If it is necessary to provide mg of novocaine when performing anesthesia of the corresponding Zakharyin-Ged zone, it is customary to use a solution in a ratio of 0.25-0.5%. A similar dosage is used when carrying out a mandatory novocaine blockade, which will eliminate the occurrence of side effects and painful sensations.
• If spinal anesthesia is necessary, the mg dose is increased slightly, ranging from 2-5%.
• Dentists also use novocaine injections, and a mg injection solution is taken in a percentage of no more than 2%.
• Conductive as well as sacral anesthesia will require the use of a mg solution within 1-2%, depending on the complexity of the situation.

This decision and injection solution is made by the attending physician, who uses the results of pre-compiled tests. What is noteworthy is that there is a procedure for enhancing the effect of novocaine, as well as prolonging the effect of the drug for local anesthesia, which, therefore, will guarantee an excellent painless effect. In this case, adrenaline is used as an additional component, their ratio is one drop of the drug per injection solution of approximately 10 milliliters of the novocaine component. In a similar way and in the appropriate dosage, novocaine is actively used in therapy, which has made it an important component of treatment. The drug solution has no side effects, provided all instructions are followed. necessary standards and conditions, dosage.

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In this article you can find instructions for use medicinal product Novocaine. Feedback from site visitors - consumers - is presented of this medicine, as well as the opinions of specialist doctors on the use of Novocaine in their practice. We kindly ask you to actively add your reviews about the drug: whether the medicine helped or did not help get rid of the disease, what complications and side effects were observed, perhaps not stated by the manufacturer in the annotation. Analogues of Novocain, if available structural analogues. Use for anesthesia, blockades and dilution of drugs in adults, children, as well as during pregnancy and lactation.

Novocaine- 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 plasma and liver esterases 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 antimicrobial effect). It is excreted primarily by the kidneys in the form of metabolites; no more than 2% are excreted unchanged.

Indications

• infiltration (including intraosseous) anesthesia;
• for diluting medications and reducing the pain effect of administered medications;
• vagosympathetic cervical, perinephric, circular and paravertebral blockades.

Release forms

Solution for injection (injections in ampoules) 0.25%, 0.5% and 2%.

Rectal suppositories 100 mg.

Instructions for use and dosage

Only for procaine solution (active ingredient of the drug Novocaine) 5 mg/ml (0.5%).

For infiltration anesthesia, 350-600 mg (70-120 ml) is administered. Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation - no more than 0.75 g (150 ml), then during each hour of the operation - no more than 2 g (400 ml) of solution.

With perinephric blockade (according to Vishnevsky), 50-80 ml are injected into the perinephric tissue.

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

To reduce absorption and prolong the effect of local anesthesia, an additional 0.1% solution of epinephrine hydrochloride is administered - 1 drop per 2-5-10 ml of procaine solution.

The maximum dose for use in children over 12 years of age is 15 mg/kg.

Side effect

• headache;
• dizziness;
• drowsiness;
• weakness;
• increase or decrease in blood pressure;
• peripheral vasodilation;
• collapse;
• bradycardia;
• arrhythmias;
• chest pain;
• itchy skin;
• skin rash;
• other anaphylactic reactions (including anaphylactic shock);
• urticaria (on the skin and mucous membranes).

Contraindications

• hypersensitivity (including to para-aminobenzoic acid and other local anesthetic esters);
• for anesthesia using the creeping infiltrate method - pronounced fibrous changes in the tissues.

Use during pregnancy and breastfeeding

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.

If it is necessary to use the drug during lactation, the issue of stopping breastfeeding should be decided.

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.

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, enoxaparin 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 (furazolidone, 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.

Novocaine 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.

Analogues of the drug Novocain

Structural analogues according to active substance:

• Novocaine Bufus;
• Novocain-Vial;
• Novocaine base;
• Novocaine solution for injection;
• Procaine hydrochloride.

If there are no analogues of the drug for the active substance, you can follow the links below to the diseases for which the corresponding drug helps, and look at the available analogues for the therapeutic effect.