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

A local anesthetic with moderate anesthetic activity and a large breadth of therapeutic effect. Being a weak base, it blocks sodium channels, prevents the generation of pulses in the endings of the sensory nerves and impulses along nerve fibers. Changes the action potential in the membranes of nerve cells without a pronounced effect on the resting potential. Suppresses the carrying out not only painful, but also impulses of other modality.

When absorbed, it reduces the excitability of peripheral cholinergic systems, reduces the formation and release of acetylcholine from preganglionic endings (possesses some ganglion-blocking action), eliminates spasm of smooth muscles, reduces the excitability of the myocardium and motor cortex areas of the brain.

Eliminates the descending inhibitory effects of the reticular formation of the brain stem. Oppresses polysynaptic reflexes. In large doses can cause seizures. Has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 h).

Pharmacokinetics:

Subject to complete systemic absorption.The degree of absorption depends on the site and route of administration (especially on vascularization and blood flow velocity in the area of administration) and the final dose (amount and concentration). It is rapidly hydrolyzed by plasma and liver esterases with the formation of two basic pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilator effect) and para-aminobenzoic acid (a competitive antagonist of sulfanilamide chemotherapeutic drugs and can weaken their antimicrobial effect). The half-life is 30-50 seconds, in the neonatal period - 54-114 s. It is excreted mainly by the kidneys in the form of metabolites, in the unchanged form, no more than 2%.

Indications:

- Infiltration anesthesia;

- paranephalic, circular and paravertebral blockades.

Contraindications:

- Hypersensitivity (including to para-aminobenzoic acid and other local anesthetics);

- children's age till 12 years;

- pronounced fibrotic changes in the tissues (for anesthesia using the creeping infiltrate method).

Carefully:

- Emergency operations, accompanied by acute blood loss;

- conditions accompanied by a decrease in hepatic blood flow (for example,with chronic heart failure, liver disease), the progression of cardiovascular failure (usually due to the development of heart block and shock);

- inflammatory diseases or infection of the injection site;

- Pseudocholinesterase deficiency;

- kidney failure;

- Children's age (from 12 to 18 years);

- in elderly patients (over 65 years);

- Weakened patients.

Pregnancy and lactation:

During pregnancy, the prescription of the drug is possible with good tolerability if the potential benefit to the mother exceeds the possible risk to the fetus.

During breastfeeding, the drug can be used after a preliminary thorough evaluation of the expected benefit of therapy for the mother and the potential risk to the baby.

Dosing and Administration:

Intramuscularly, intradermally, subcutaneously.

For infiltration anesthesia Novocaine solution 5 mg / ml is used. Higher doses for adults: the first single dose at the beginning of the operation - no more than 150 ml of the solution, in future - no more than 2.0 g of a solution of 5 mg / ml (ie 400 ml of solution) is injected for each hour of the operation.

To reduce the absorption and lengthening of the action with local anesthesia, an additional 0.1% solution of epinephrine is injected - 1 drop per 2-5-10 ml of Novocain solution.The maximum dose for injection without a vasoconstrictor is 500 mg. Higher single doses with intramuscular injection: 0.1 g (20 ml solution 5 mg / ml).

For circular or paravertebral blockades Novocaine solution 5 mg / ml is administered intracutaneously.

With paranephric blockade (according to AV Vishnevsky) 50-80 ml of a solution of Novocaine 5 mg / ml are injected into the peritoneal cellulose.

With vagosympathetic cervical blockade in the perivascular tissue injected 30-40 ml of Novocaine solution 5 mg / ml.

Doses for children depending on age and body weight are not developed. The maximum dose for use in children older than 12 years with all methods of anesthesia is 15 mg / kg.

Side effects:

From the central and peripheral nervous system: headaches, dizziness, drowsiness, weakness, motor anxiety, loss of consciousness, convulsions, trismus, tremor, visual and auditory disorders, nystagmus, cauda equina syndrome (paralysis of legs, paresthesia), paralysis of the respiratory muscles, motor block and sensitive.

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

From the urinary system: involuntary urination.

From the digestive system: nausea, vomiting, involuntary defecation.

From the side of the blood: methemoglobinemia.

Allergic reactions: itching of the skin, skin rash, other anaphylactic reactions (in that body anaphylactic shock), urticaria (on the skin and mucous membranes).

Other: return pain, persistent anesthesia, hypothermia, impotence; with anesthesia in dentistry: numbness and paresthesia of the lips and tongue, lengthening of anesthesia.

Overdose:

Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, "cold" sweat, quickening of the breath, tachycardia, lowering of blood pressure, including collapse, apnea, methemoglobinemia. Action on the central nervous system (CNS) is manifested by a feeling of fear, hallucinations, convulsions, motor excitement.

Treatment: maintenance of adequate pulmonary ventilation, detoxification and symptomatic therapy.

Interaction:

Strengthens the depressing effect on the central nervous system of funds for general anesthesia, hypnotics and sedatives, narcotic analgesics and tranquilizers.

Anticoagulants (ardeparin sodium, dalteparin sodium, sodium danaparoid, sodium enoxaparin, heparin, warfarin) increase the risk of bleeding.

When treating the site of injection of a local anesthetic with disinfectant solutions containing heavy metals, the risk of developing a local reaction in the form of tenderness and swelling increases.

Use with monoamine oxidase inhibitors (furazolidone, procarbazine, selegiline) increases the risk of lowering blood pressure.

Strengthen and prolong the action of muscle relaxants.

With the simultaneous use of procaine in conjunction with narcotic analgesics, there is an additive effect, which is used for spinal and epidural anesthesia, and respiratory depression is increased.

Vasoconstrictors (epinephrine, methoxamine, phenylephrine) extend the local anesthetic effect.

Procaine reduces the anti-myasthenic action of drugs (LS), especially when used in high doses, which requires an additional correction of the treatment of myasthenia gravis.

Cholinesterase inhibitors (antimiasthenic drugs, cyclophosphamide, democaria bromide, eco-iodide iodide, thiotepa) reduce the metabolism of procaine.

Metabolite procaine (paraaminobenzoic acid) is a sulfonamide antagonist.

Special instructions:

Indication of the features of the drug during the first admission or when it is withdrawn

Patients need control over the functions of the cardiovascular, respiratory and central nervous systems.

It is necessary to cancel monoamine oxidase inhibitors 10 days before the introduction of a local anesthetic.

Before use, mandatory sampling for individual sensitivity to the drug.

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

It is not absorbed from the mucous membranes, it does not provide a superficial anesthesia for the dermal application.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Solution for injection, 5 mg / ml.

Packaging:

5 ml in the ampoule.

For 10 ampoules with instructions for use and a knife ampoule or scarifier ampullum in a cardboard box.

Storage conditions:

Store in a dark place at a temperature not exceeding 30 FROM.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000347 / 01

Date of registration:02.12.2011 / 22.09.2016

Expiration Date:Unlimited

The owner of the registration certificate:ORGANICS, JSC ORGANICS, JSC Russia

Manufacturer: & nbsp

ORGANICS, JSC Russia

Information update date: & nbsp24.06.2018

Illustrated instructions

Instructions

Novocaine (Novocaine)