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

Locally anesthetizing agents with moderate anesthetic activity and a large breadth of therapeutic effect. Being a weak base, it blocks Na+ -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 carrying out not only pain, but also impulses of another modality.

With absorption and direct vascular injection into the blood flow 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.

With intravenous administration, analgesic, hypotensive and antiarrhythmic action (increases the effective refractory period, reduces excitability, automatism and conductivity), in large doses can disrupt neuromuscular conduction.

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:

It is subject to complete systemic absorption. The degree of absorption depends on the site (degree of vascularization and blood flow velocity in the area of administration), route of administration and total dosage. It is rapidly hydrolyzed by plasma and liver esterases with the formation of two basic pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilating effect) and para-aminobenzoic acid (a competitive antagonist of sulfanilamide chemotherapeutic drugs and can weaken their antimicrobial effect).

The half-life is 30-50 s, in the neonatal period is 54-114 s. It is excreted mainly by kidneys in the form of metabolites, in an unchanged form, no more than 2% is excreted.

Indications:

Infiltration, conductive, epidural anesthesia.

Vagosympathetic cervical, paranephalic, circular and paravertebral blockades.

Contraindications:

Hypersensitivity (incl.to para-aminobenzoic acid and other local anesthetics), children under 12 years of age.

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

For epidural anesthesia: atrioventricular blockade, marked decrease in blood pressure, shock, infection of the site of the lumbar puncture, septicemia.

Carefully:

Emergency operations, accompanied by acute blood loss; conditions accompanied by a decrease in hepatic blood flow (eg, in chronic heart failure, liver disease): progression of cardiovascular failure (usually due to the development of heart block and shock); pseudocholinesterase deficiency; kidney failure; children's age (from 12 to 18 years) and in elderly patients (over 65 years); seriously ill patients; pregnancy and childbirth.

Dosing and Administration:

For infiltration anesthesia, solutions of 2.5 mg / ml, 5 mg / ml; for anesthesia by the method of Vishnevsky (tight creeping infiltration) solutions - 1.25 mg / mg, 2.5 mg / ml. To reduce the absorption and lengthening of the action with local anesthesia, an additional 0.1% solution of epinephrine hydrochloride is added - 1 drop per 2-5-10 ml of procaine solution.

With paranephric blockade (according to AV Vishnevsky) 50-80 ml of a solution of 5 mg / ml or 100-150 ml of a solution of 2.5 mg / ml are injected into the peritoneal cellulose.

With vagosympathetic blockade - 30-100 ml of a solution of 2.5 mg / ml.

For circular or paravertebral blockades intradermally injected solution 2.5 mg / ml or 5 mg / ml.

Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation - no more than 500 ml of a solution of 2.5 mg / ml or 150 ml of a solution of 5 mg / ml. Further, during each hour of operation - no more than 1000 ml of a solution of 2.5 mg / ml or 400 ml of a solution of 5 mg / ml.

The maximum dose for use in children older than 12 years is 15 mg / kg.

For conductive anesthesia - solutions of 10 mg / ml, 20 mg / ml (up to 25 ml); for epidural - a solution of 20 mg / ml (20-25 ml).

Side effects:

From the central and peripheral nervous system: headache, dizziness, drowsiness, weakness, motor anxiety, loss of consciousness, convulsions, trismus, tremor, visual and auditory disorders, nystagmus, cauda equina syndrome (paralysis of the legs, paresthesia), respiratory muscle paralysis, motor and sensory block, respiratory paralysis more often develops with subarachnoid anesthesia.

From the side of 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 (including 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 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 for general anesthesia, hypnotics and sedatives, narcotic analgesics and tranquilizers.

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

When treating the injection site of a local anesthetic with disinfectants

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, selegiline) increases the risk of developing hypotension.

Strengthen and prolong the action of muscle relaxants.

In the appointment of procaine, together with narcotic analgesics, an additive effect is noted that is used in 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, 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:

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

It is necessary to abolish MAO 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; does not provide a superficial anesthesia for dermal application.

Effect on the ability to drive transp. cf. and fur:During the period of treatment 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, 2.5 mg / ml, 5 mg / ml, 10 mg / ml and 20 mg / ml.

Packaging:

1 ml, 2 ml, 5 ml, 10 ml into neutral glass ampoules of grade HC-1 or HC-3.

For 10 ampoules, together with the instructions for use and a knife for opening ampoules or a scarifier ampoule are placed in a cardboard box.

5 ampoules into the contour cell package. 2 contour squares with instructions for use and a knife for opening ampoules or an ampoule scarifier are placed in a cardboard pack.

Storage conditions:

In a dark place out of the reach of children.

Shelf life:

3 years.

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

Terms of leave from pharmacies:On prescription

Registration number:P N001052 / 01

Date of registration:22.01.2008

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Representation: & nbspDALHIMFARM, OJSCDALHIMFARM, OJSC

Information update date: & nbsp03.09.2015

Illustrated instructions

Instructions

Novocaine (Novocaine)