Novocaine release form in ampoules. Intravenous use of novocaine. Application for violations of kidney function

Tradename: Novocaine

International non-proprietary name:

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 at 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. 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. When administered intravenously, it 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), children under 12 years of age.
For anesthesia by the creeping infiltrate method: pronounced fibrotic changes in the tissues. For epidural anesthesia: atrioventricular block, marked decrease in 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.
The maximum dose for use in children over 12 years old is 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 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: maintaining 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, trimethaphan, the risk of a sharp decrease in blood pressure and bradycardia increases.
Anticoagulants (ardeparin, dalteparin, danaparoid, enoxaparin, heparin, warfarin) increase the risk of bleeding. When treating the injection site of a local anesthetic with 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 hazardous activities that require an 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:

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 is used as a local anesthetic and is included in the list of the most important medical pharmaceuticals. This drug has an average anesthetic effect, reduces the conductivity of the motor areas of the brain, myocardium, relieves spasms of smooth muscles. When the drug is administered intravenously, it is able to lower blood pressure, is taken with arrhythmias, and removes from shock. In case of an overdose, Novocaine disrupts muscle conduction and causes convulsions. Intramuscularly, the drug is effective for disorders of the nervous system in the elderly.

The drug is produced in the form of a solution for injections in ampoules of rectal suppositories, Novocain5 ointment.

Indications

The medication is prescribed for the following types of anesthesia:

• retrobulbar;
• epidural conduction;
• spinal terminal;
• infiltration.

And also for vagosympathetic or pararenal neck blockade. Rectal suppositories are prescribed for the treatment of anal fissures and hemorrhoids. The ointment is effective for relieving itching in dermatosis, neurodermatitis, eczema.

Instructions for use

1. Infiltration anesthesia - solution 0.25-0.5% - 350-600 mg.
2. Tight creeping infiltration according to Vishnevsky - a solution of 0.125-0.25%.
3. Conduction anesthesia - a solution of 1-2% - is injected up to 25 ml.
4. Epidural anesthesia - solution 2% 20-25ml.
5. Spinal anesthesia - solution Novocain 5% 2 or 3 ml.
6. Otorhinolaryngology. Local anesthesia - solution 10-20%.
7. Electrophoresis with novocaine - solution 10%.
8. Blockade according to Vishnevsky - solution 0.25% up to 100-150 ml or 0.5% up to 50-80 ml.
9. Vagosympathetic blockade - solution 0.25% up to 100 ml.
10. Children - no more than 15 mg per kg of body weight.
11. Suppositories are administered rectally after defecation or cleansing by means of an enema 1-2 times a day.
12. The ointment is applied to areas of the skin prone to disease up to two times a day.

Side effects

After taking Novocain, the following may appear:

• headache;
• convulsions;
• drowsiness;
• dizziness;
• loss of consciousness;
• weaknesses;
• tremor;
• paresthesia;
• pain in the sternum;
• respiratory paralysis;
• bradycardia;
• paralysis of the legs;
• collapse;
• pressure surges;
• arrhythmias;
• involuntary bowel movements;
• skin rashes;
• vomiting;
• hypothermia;
• impotence.

Overdose manifests itself:

• pale skin and mucous membranes;
• nausea;
• dizziness;
• rapid breathing;
• hallucinations;
• motor excitement;
• convulsions;
• apnea;
• vomiting.

Eliminate the consequences by administering short-acting general anesthesia drugs intravenously, maintain ventilation of the lungs artificially with the help of oxygen inhalation. If intoxication is severe enough, detoxification and symptomatic treatment is carried out.

When using novocaine ointment, local allergic manifestations may develop.

Contraindications

When anesthetizing according to the method of creeping infiltrate, the existing fibrotic changes are a contraindication. With subarachnoid anesthesia, the following contraindications are septicemia, shock, hypotension, bleeding.

The instructions for the drug warns to use it with caution during operations when the patient has acute blood loss, as well as in renal failure and progressive cardiovascular insufficiency. Care should be taken to prescribe the drug in the presence of inflammatory diseases and in conditions accompanied by a violation of the blood supply to the liver. Enhanced medical supervision requires the use of the drug by the elderly over 65 years of age and children under 18 years of age, as well as by weakened, severe patients during pregnancy or during childbirth.

Interaction with certain drugs

The combination of Novocain with anticoagulants increases the risk of bleeding. Anticoagulants: danaparoid, warfarin, ardeparin, dalteparin, enoxaparin, heparin. If you take the drug simultaneously with trimetafan, mecamylamine, guanadrel, guanethidine, bradycardia and pressure reduction may develop. The following drugs lower blood pressure in combination with Novocain: furazolidone, procarbazine, selegiline. The local anesthetic effect of Novocain is increased by epinephrine, methoxamine, phenylephrine.

It is important to remind readers that this drug, like other medicinal pharmaceutical preparations, as well as the appropriate treatment for them, is prescribed only by a qualified doctor according to indications. Self-medication can greatly harm not only health, but also life.

Novocain is an injection solution that is used as a local anesthetic. The use of the product is possible in dentistry, surgery and dermatology. The drug can be used externally as a compress. The drug has a number of contraindications that must be identified in the patient in advance in order to avoid the development of side effects.

The drug has several forms of release: suppositories and Novocaine solution. The liquid form and suppositories contain one active ingredient - procaine. Additional components (solid fat, distilled water, aqueous hydrogen chloride solution) may vary depending on the manufacturer.

Solution (0.25%, 0.5%, 2%) is a colorless (rarely yellowish) transparent liquid, poured into glass ampoules of 10 ml, 5 ml or 2 ml. There is a scarifier in the cardboard box. Torpedo-shaped suppositories are sold in plastic pallets of 10 pcs. in everyone.

Pharmacological properties

Novocaine intravenously as an anesthetic has moderate activity. The drug stops pain attacks and impulses of different modality. When released into the blood, the main component reduces the rate of release and production of choline derivatives. With absorption, the degree of excitability of cholinergic neurons decreases.

The drug is able to smooth out the muscles, lowers the level of excitability of the motor areas of the brain and myocardium. Polysynaptic reflexes are inhibited, any inhibitory downward influences are eliminated. Novocaine used in high doses can cause convulsions.

Duration of action - no more than 60 minutes. Anesthetic activity is short-term. The main component is completely absorbed. The level of absorption depends on the place of administration (intramuscularly, in a vein or by means of a dropper) and the dose of the drug. Hydrolysis is fast, in the process para-aminobenzoic acid and diethylaminoethanol are formed. The latter has a slight vasodilating effect.

Indications and contraindications

The use of injections with Novocain is possible with the following types of anesthesia:

• spinal;
• conductive;
• epidural;
• intraosseous;
• infiltration.

A 0.5% solution is used in otolaryngology for anesthesia of the mucous membranes of the nose and mouth. With its help, blockade is carried out:

• circular;
• paravertebral;
• vagosympathetic cervical;
• pararenal.

The drug for anesthesia is combined with the main anesthetic drugs. When administered intramuscularly, the drug accelerates the dissolution of penicillin. Novocaine is used for the following pathologies:

• rheumatic and infectious diseases of the joints;
• high blood pressure (hypertension);
• vascular spasms;
• endarteritis;
• atherosclerosis.

The medicine is effective for toothache. You can use a solution for compresses for diseases of the skin. Suppositories help with anal fissures and hemorrhoids.

The drug has a number of absolute and relative contraindications for use. The absolute ones are:

• individual intolerance to procaine;
• childhood;
• kidney failure;
• inflammatory pathologies;
• lack of pseudocholinesterase;
• progressive cardiovascular insufficiency;
• slow blood flow in the liver;
• emergency operations accompanied by blood loss.

Relative contraindications include pregnancy, a tendency to allergic reactions and old age.

Application instruction of Novocaine in ampoules

The use of the drug should be carried out only according to the instructions. Before administering the medication, the doctor should ask the patient in detail about possible contraindications. The treatment regimen, course and dosage are selected individually, taking into account the age of the patient.

How to breed?

The pure solution does not need to be diluted with anything. If necessary, antibiotics are diluted with Novocaine.

Dosage and administration

For children over 12 years of age, the maximum daily dose is 5 mg/kg body weight. To prolong the effect and reduce the absorption rate of Novocain during anesthesia, epinephrine hydrochloride 0.1% (one drop per 5-10 ml). With paravertebral and circular blockade, the solution is administered intradermally (5-10 ml each). With vagosympathetic blockade, the rate is increased by 3-4 times (once no more than 40 ml).

Pararenal blockade involves the introduction of a solution into the perirenal zone (no more than 80 ml once). With infiltration anesthesia, Novocain 0.5% is used, the maximum dose is 600 ml. Before surgery, adult patients are injected with 150 ml of solution. During the operation (every hour) another 400 ml is poured through a dropper.

Side effects and overdose

The risk of developing side effects increases if an individually selected treatment regimen is not followed. They come from:

1. Cardiovascular system: aching chest pain, collapse, arrhythmia, peripheral vasodilation, bradycardia, blood pressure surges.
2. Hematopoietic systems: methemoglobinemia.
3. Central nervous system: weakness, drowsiness, dizziness, prolonged headaches.

Most often, patients complain of the appearance of characteristic allergy symptoms, which include urticaria, itching, and skin rashes. In rare cases, anaphylactic shock is possible. Side effects are reversible, they disappear on their own after stopping treatment.

Symptoms of an overdose appear when the daily norm is repeatedly exceeded. Main features:

• motor excitation;
• auditory and visual hallucinations;
• feeling of fear and anxiety;
• apnea;
• a sharp drop in blood pressure;
• respiratory failure (up to asthma attacks);
• tachycardia;
• increased sweating ("cold" sweat);
• uncontrolled vomiting;
• dizziness (up to fainting);
• bouts of nausea;
• pallor of the skin.

Gastric lavage will not help in this case. Symptomatic treatment is required: the patient should be immediately taken to the nearest medical facility, where doctors are able to maintain pulmonary ventilation and, if necessary, prescribe detoxification therapy.

special instructions

The solution is not recommended to be instilled into the eyes without the consent of the attending physician. If the patient was prescribed electrophoresis for osteochondrosis, then the procedure is carried out only after the diagnosis has been clarified and under the supervision of a specialist. During the period of treatment, it is recommended to refuse to drive a car and other vehicles: the drug can reduce concentration. Procaine does not penetrate well through intact mucous membranes, therefore, with its help, superficial anesthesia is not performed.

2 weeks before the start of treatment, monoamine oxidase inhibitors should be discontinued. The systematic use of novocaine requires regular monitoring of the functions of the respiratory and nervous system, heart and blood vessels. Before administering the solution to the patient, it is necessary to conduct an individual test for sensitivity. The drug is incompatible with alcohol. 7 days before the start of treatment, the patient must completely refrain from drinking alcohol (including low alcohol).

Appointment during pregnancy and lactation

Before prescribing Novocaine to a pregnant or breastfeeding woman, the doctor must calculate the possible risks in advance. In the postpartum period, a careful reception is necessary: ​​injections are placed under the supervision of a doctor. If there is a need for a breastfeeding woman to use the drug, then lactation should be stopped.

Interaction with other drugs

Cholinesterase inhibitors can slow down the metabolism of Novocaine. The metabolite of procaine (para-aminobenzoic acid) is considered a sulfonamide antagonist. Under the influence of novocaine, the degree of anti-myasthenic effects of some drugs decreases, so it may be necessary to correct therapy for myasthenia gravis. Vasoconstrictors (methoxamine, epinephrine, phenylephrine) prolong the anesthetic effect.

Under the influence of Novocaine, muscle relaxant drugs increase their bioavailability. The drug has a negative compatibility with monoamine oxidase inhibitors due to the high likelihood of a sharp decrease in blood pressure. The injection site of the solution cannot be treated with disinfectant solutions: they contain heavy metals, so the risk of bruising increases.

Novocaine can not be combined with anticoagulants: internal bleeding may open. The drug enhances the effect of analgesics, tranquilizers, hypnotics and sedatives.

Terms of sale and storage

Novocaine as a local anesthetic can only be purchased with a doctor's prescription, written in Latin on a special endorsed form. Approximate cost - from 25 rubles. for packing. Opened boxes with ampoules and suppositories must be properly stored so that the medicine does not lose its properties. Shelf life - no more than 36 months. The storage location must be dry and dark. The drug should be protected from children, fire, sunlight and pets.

Analogues (briefly)

In the pharmacy, you can purchase a number of medicines that provide the same therapeutic effect as the original drug. These include:

1. Dekain. A local anesthetic in the form of a solution quickly anesthetizes the mucous membranes, reducing the sensitivity of the nerve endings. It is used in otolaryngology and ophthalmology. If the patient has contraindications to amide anesthetics, the drug is used for spinal anesthesia. Price - from 45 rubles.
2. Anestezin. The tablet form of the drug provides local anesthesia. Contains benzocaine. Tablets are dissolved in liquid and used as directed. Oral administration is possible for pathologies of the digestive tract. The cost is from 50 rubles.
3. Pyromecaine. Produced in the form of a gel, it is used mainly in dentistry. The active ingredients are methyluracil and bumecaine. The drug provides local anesthesia for stomatitis, erythema and periodontitis. Price - from 220 rubles.
4. mepivacaine. Amide anesthetic is sold in the form of a solution. The main element is the substance of the same name in the form of hydrochloride. There are no vasoconstrictor components in the composition. The drug is used in surgery, otolaryngology and dentistry. The cost is from 140 rubles.

Generics have contraindications, which the doctor must take into account when prescribing. Self-selection of medication is strictly prohibited.

Means for local anesthesia. Esters of aminobenzoic acid.
ATX code N01BA02.

Pharmacological properties

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 at 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 a different modality.
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. Eliminates the descending inhibitory influences of the reticular formation of the brain stem. Inhibits polysynaptic reflexes.
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 (especially on the degree of vascularization and blood flow velocity in the injection site), the route of administration and the final dose (amount and concentration). It is rapidly hydrolyzed by plasma and liver esterases to form two 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. It is excreted mainly by the kidneys in the form of metabolites, unchanged - no more than 2%.

Indications for use

Infiltration anesthesia and therapeutic blockades.

Dosage and administration

Method of administration:
Slowly inject into tissue for anesthesia; repeated administration should avoid accidental intravenous administration.
Dosage:
The concentration, amount and method of administration of novocaine is used depending on the indications and prescriptions of the doctor. Novocaine should be used at the lowest dose that results in an anesthetic effect to avoid excessively high plasma concentrations that can lead to side effects.

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 (then there are 150 ml).
The recommended daily dose is a maximum of 7.0 mg/kg body weight (approximately 500 mg at an average body weight of 70 kg) or 50 ml of a 1% solution. mg of novocaine (80 ml of a 2.5 mg / ml solution or 40 ml of a 5 mg / ml solution) for 2 hours. In elderly and debilitated patients, when using novocaine in the head and neck (in anatomical proximity to the cerebral vessels), a lower dosage is recommended.

Contraindications

Hypersensitivity to the active substance or any of the excipients;
- hypersensitivity to local anesthetics such as ether, the possibility of cross-allergic reactions to p-aminobenzoic acid derivatives (parabens) and sulfonamides;
- myasthenia gravis;
- deficiency of cholinesterase and pseudocholinesterase;
- simultaneous treatment with sulfonamides and cholinesterase inhibitors;
- severe forms of bradycardia, AV block II and III degree and other conduction disorders;
- decompensated heart failure;
- severe arterial hypotension;
- purulent-inflammatory processes, cicatricial changes in the tissue at the injection site.
Novocaine is not intended for intra-arterial and intravenous administration, epidural or spinal anesthesia.
Children The drug is not used in children.

Precautionary measures

Infiltration anesthesia and therapeutic blockades should be performed by a qualified specialist who knows the methods of emergency care and in conditions of immediate (if necessary) access to resuscitation equipment (ventilator, defibrillator) and drugs used in shock (plasma substitutes, adrenaline, prednisolone, diazepam , atropine, etc.).
Special care is required when using novocaine for the following categories of patients:
- Patients with bleeding disorders. It should be noted that an increased bleeding tendency can be expected during treatment with blood clotting inhibitors (anticoagulants such as heparin), NSAIDs or plasma expanders. In addition, the injection can lead to serious bleeding due to accidental damage to the vessel. Additionally, it is necessary to conduct tests for blood clotting time, activated partial thromboplastin time (APTT), thrombin and platelet count.
- patients taking antiarrhythmic drugs. In some cases, ECG monitoring is necessary in patients taking class III antiarrhythmic drugs (eg, amiodarone);
- patients with partial or complete blockade of the conduction system of the heart, due to the fact that local anesthetics can suppress the conduction of excitation through the atrioventricular junction.
- patients with renal or hepatic dysfunction (due to the risk of cumulation);
- Elderly and debilitated patients.
Before local anesthesia, it is recommended to provide conditions for infusion therapy. Existing hypovolemia must be corrected. The dose of anesthetic used should be the minimum that provides an analgesic effect.
It is recommended to find out a possible allergic history in relation to novocaine and other local anesthetics.
Patients with a known allergy to novocaine may simultaneously be allergic to other local anesthetics of the ester group and related compounds, including sulfonamides, oral antidiabetic agents (group paraallergy). With a known allergy to sulfonamides, a cross-allergy to novocaine is not excluded.
In patients with pseudocholinesterase deficiency or with significantly reduced enzyme activity, there is an increase in toxic symptoms when novocaine is used.
To prevent adverse reactions, a tolerance test should first be carried out.. Intolerance is evidenced by swelling and redness of the injection site. With a positive reaction, novocaine should not be used!
It is recommended to avoid intravascular administration of novocaine solution.
Do not inject into the area of ​​inflammation.
When used in the head and neck area, there is an increased risk of toxicity and overdose.
If the first signs of side effects are detected, the administration of novocaine should be stopped immediately.

Side effect

Significant dose-dependent side effects develop mainly from the side of the central nervous system and the cardiovascular system. They are usually the result of errors in application (incorrectly selected concentration), exceeding the maximum dose, accidental intravascular administration, accelerated resorption (for example, in abundantly perfused tissues), in patients with hepatic or renal insufficiency with impaired metabolism and elimination of novocaine.
A drop in blood pressure may be the first sign of a relative overdose due to cardiac depression.
The toxic effect on the central nervous system is manifested by a number of symptoms, such as nausea, vomiting, restlessness, tremor, confusion, blurred vision, drowsiness, tinnitus, speech disorder, muscle twitching with the development of convulsions, coma and central respiratory paralysis.
In severe forms of intoxication with local anesthetics, the prodromal period may be very short or absent, and the patient quickly enters a coma.
When listing the following side effects, the frequency of manifestation is determined as follows:
Very often (>1/10)
Often (<1/100, <1/10)
Sometimes (>1/1000,<1/100)
Rare (>1/10000,<1/1000)
Very rarely (<1/10000)
Not known (cannot be estimated from available data):
From the immune system:
Rarely allergic reactions (urticaria, laryngeal edema, bronchospasm, in extreme cases, anaphylactic shock).
From the nervous system:
Paresthesia, dizziness, drowsiness.
Signs and symptoms of CNS toxicity (convulsions, parasthesia of the orbicular muscle of the mouth, numbness of the tongue, hypercausia, visual disturbances, tremor, tinnitus, dysarthria, CNS depression).
From the side of the heart:
Bradycardia, tachycardia.
Cardiac arrest, cardiac arrhythmias.
From the vascular side:
Hypotension, hypertension.
From the organs of the chest and mediastinum:
Respiratory depression, shortness of breath (see immune system disorders).
From the gastrointestinal tract:
Nausea, vomiting.

Overdose

Overdose symptoms
In low doses, novocaine acts as a stimulant of the central nervous system, in high doses it leads to depression of the functions of the central nervous system. Intoxication with novocaine hydrochloride proceeds in 2 phases:
1. Stimulation
- CNS: paresthesia of the eyelids, numbness of the tongue, anxiety, delirium, convulsions (tonic-clonic).
- Cardiovascular system: increased cardiac output, increased blood pressure, skin redness.
2. Depression
- CNS: coma, respiratory arrest.
- Cardiovascular system: the pulse is not palpable, pallor of the skin, cardiac arrest.
Patients in the first stage of intoxication with local anesthetics show symptoms of arousal. They are restless, complain of dizziness, blurred vision, hearing, tingling and paresthesia, especially in the area of ​​the tongue and lips. Paresthesia of the tongue, chills, and muscle cramps are harbingers of impending generalized seizures. Plasma concentrations of novocaine that do not reach the seizure initiation threshold also often lead to drowsiness and sedation of the patient. In the first stage of intoxication, tonic-clonic convulsions develop. With progressive CNS intoxication, dysfunction of the brain stem develops with respiratory depression, symptoms of coma, which can lead to death.
A drop in blood pressure is often the first sign of toxic effects on the cardiovascular system. Hypotension is mainly due to depression or blockade of cardiac conduction. However, toxic effects on the cardiovascular system are clinically of relatively little importance.
In the case of an accidental general spinal anesthesia, intoxication is manifested by initial signs of anxiety, then drowsiness, which can turn into unconsciousness and respiratory arrest.
Overdose treatment:
In the event of the appearance of symptoms of the toxic effect of novocaine on the central nervous system or the cardiovascular system, it is necessary:
- immediate cessation of the introduction of novocaine;
- ensuring the patency of the respiratory tract;
- if necessary, inhalation of oxygen or artificial respiration;
- careful monitoring of blood pressure, pulse and pupil diameter;
- in case of an acute and threatening drop in blood pressure, the patient is transferred to the so-called. "anti-shock" position (lying horizontally, with the head below the level of the legs), slowly intravenous injection of beta-adrenergic agents (adrenaline). In addition, crystalloid solutions are administered to replenish volume;
- with an increase in the tone of the vagus nerve with the development of bradycardia, atropine is administered (0.5 mg to 1.0 mg intravenously);
- in case of suspected cardiac arrest, it is necessary to perform appropriate resuscitation measures;
- with the development of seizures, diazepam is administered (about 0.1 mg / kg intravenously).
Analeptics of central action are contraindicated in case of intoxication with local anesthetics!

Use during pregnancy and during breastfeeding

Interaction with other medicinal products and other forms of interaction

The antibacterial activity of sulfonamides decreases.
Cholinesterase inhibitors (eg, physostigmine) and acetazolamide can inhibit the degradation of novocaine and increase its effectiveness.
Vasoconstrictors prolong the action of local anesthetics. The effect of non-depolarizing muscle relaxants is prolonged.
When used simultaneously with other antiarrhythmic drugs, beta-blockers and calcium channel blockers increase the inhibitory effect on the AV connections and intraventricular stimulus propagation and contraction force.
The use simultaneously with MAO inhibitors increases the risk of arterial hypotension.
Anticoagulants (sodium ardeparin, sodium dalteparin, sodium danaparoid, sodium enoxaparin, heparin, warfarin) increase the risk of bleeding. With the simultaneous use of novocaine with anticoagulants, it is recommended to monitor the following indicators of hemostasis - APTT and prothrombin index (or INR). These studies should be carried out in patients at risk, as well as in the case of the use of low molecular weight heparins (prophylactic treatment with a blood clotting inhibitor (heparin) at a low dose). If possible, stop anticoagulant therapy as soon as possible.
When treating the injection site of a local anesthetic with antiseptic solutions containing salts of heavy metals, the risk of developing a local reaction in the form of pain and swelling increases. For hospitals: glass bottles of 100 ml in package No. 35 and 200 ml in package No. 24 are packed in polyethylene film and, together with 1-2 instructions for medical use, are placed in cardboard boxes
or glass bottles of 100 ml, 200 ml in packaging No. 20 or No. 40, together with 1-2 instructions for medical use, are placed in cardboard boxes with partitions or corrugated cardboard grids.

Manufacturer, country
Produced by OAO "Nesvizh Plant of Medical Preparations";
222603, pos. Alba, st. Factory, 1;
Nesvizh district, Minsk region;
Republic of Belarus.

Novocaine (active substance - procaine) is among those medicines, the effect of which is known to almost any person who is not particularly knowledgeable in medicine. And this is true: the pronounced local anesthetic effect of this drug and its large range of therapeutic activity (read: a small risk of being subjected to its toxic effects) led to the widest use of novocaine in surgical, dental and urological practice, and the phrase "novocaine blockade" has firmly entered the lexicon the average layman. Being a weak base (in the chemical sense of the word), novocaine blocks membrane sodium channels, displaces calcium from their receptors, and prevents the generation and conduction of impulses in nerve (mostly in non-myelin) fibers. As a result of these physiological metamorphoses, the action potential changes in the membranes of neurons, while the resting potential, on the contrary, remains practically in its original form. When administered intravenously, it reduces the sensitivity of receptors in peripheral cholinergic synapses, thereby inhibiting the secretion of acetylcholine, relieves spasms of smooth muscles, and reduces the excitability of the heart muscle and motor areas of the cerebral cortex. It has an analgesic, hypotonic and antiarrhythmic effect, in high concentrations it can inhibit neuromuscular conduction. Antiarrhythmic activity is associated with an extension of the effective refractory period, a decrease in the excitability and automatism of the heart muscle.

Large doses of the drug can provoke convulsions. The analgesic effect of novocaine is short-lived: for example, with infiltration anesthesia, it remains active for 0.5–1 h. Prolonging the effect of the drug, as well as reducing its toxicity, is achieved by the combined use of vasoconstrictors (for example, adrenaline).

Novocaine is available as a solution for intravenous and intramuscular administration and rectal suppositories. The concentration of the injected solution depends on the type of anesthesia: infiltration (blocking pain at the level of receptors and small nerves) anesthesia requires 0.25–0.5% novocaine solution, conductive (blocking pain at the level of the nerve plexus or trunk) - 1–2%, epidural (extinguishing pain at the level of the spinal roots when injected into the epidural space) - 2%, spinal (different from the epidural injection site) - 5%. When using novocaine anesthesia, control over the functions of the central nervous system, cardiovascular and respiratory systems is shown. Before the first administration of the drug, it is recommended to pass a test for individual sensitivity to it.

Novocaine in the form of rectal suppositories is used as a local anesthetic for the relief of pain in hemorrhoids or intestinal colic. Multiplicity of use - 1-2 times a day with deep introduction into the anus after a cleansing enema.

Pharmacology

A local anesthetic with moderate anesthetic activity and a wide range of therapeutic effects. 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 at 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 a different modality. When released into the systemic circulation, it reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic endings (it has a weak ganglion-blocking effect), eliminates smooth muscle spasm, and reduces the excitability of the myocardium and motor areas of the cerebral cortex.

Compared with lidocaine and bupivacaine, procaine has a less pronounced anesthetic effect and, therefore, has a relatively low toxicity and a greater therapeutic breadth.

Pharmacokinetics

Release form

Solution for injection is clear, colorless.

5 ml - polymer ampoules (5) - packs of cardboard.
5 ml - polymer ampoules (10) - packs of cardboard.
10 ml - polymer ampoules (5) - packs of cardboard.
10 ml - polymer ampoules (10) - packs of cardboard.

Dosage

Individual, depending on the type of anesthesia, route of administration, indications.

Interaction

When administered intravenously, it enhances the inhibitory effect on the central nervous system of general anesthesia, hypnotics, sedatives, narcotic analgesics and tranquilizers.

The procaine metabolite PABA is a competitive antagonist of sulfonamides and may weaken their antimicrobial activity.

Side effects

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

Indications

Infiltration, conduction, epidural and spinal anesthesia, intraosseous anesthesia, anesthesia of the mucous membranes (in ENT practice); vagosympathetic and pararenal blockade. Circular and paravertebral blockade in eczema, neurodermatitis, ischalgia.

In / in: to potentiate the action of the main means for anesthesia; for the relief of pain syndrome of various origins.

V / m: to dissolve penicillin in order to lengthen its duration; as an adjuvant for certain diseases that are more common in old age, incl. endarteritis, atherosclerosis, arterial hypertension, spasms of the coronary vessels and brain vessels, diseases of the joints of rheumatic and infectious origin.

Rectally: hemorrhoids, intestinal smooth muscle spasms, anal fissures.

Contraindications

Hypersensitivity to procaine.

Application features

special instructions

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

Procaine penetrates slowly through intact mucous membranes, so it is not very effective for surface anesthesia.

As an adjuvant, procaine is used intravenously and orally for arterial hypertension, late toxicosis of pregnant women with hypertensive syndrome, spasms of blood vessels, phantom pains, peptic ulcer of the stomach and duodenum, UC, itching, neurodermatitis, eczema, keratitis, iridocyclitis, glaucoma.