Active substanceProcainProcain
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  • Dosage form: & nbspinjection
    Composition:

    1 ml of the solution contains:

    0,25% solution:

    active substances: procaine 2.5 mg;

    Excipients: hydrochloric acid solution to pH 3.8-4.5, water for injection.

    0.5% solution:

    active substances: procaine 5 mg;

    Excipients: hydrochloric acid solution to pH 3.8-4.5, water for injection.

    Description:

    Transparent colorless liquid.

    Pharmacotherapeutic group:Local anesthetic
    ATX: & nbsp

    N.01.B.A   Ethers of aminobenzoic acid

    N.01.B.A.02   Procain

    Pharmacodynamics:

    A local anesthetic with moderate anesthetic activity and a large breadth of therapeutic effect. 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 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.

    Has a short anesthetic activity (the duration of infiltration anesthesia is 0.5-1 h).

    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.

    When administered intravenously, it has analgesic, antishock,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.

    Pharmacokinetics:

    Poorly absorbed through mucous membranes for external application. When parenteral administration is well absorbed, rapidly hydrolyzed by esterases of plasma and tissues with the formation of two major pharmacologically active metabolites: diethylaminoethanol (has a moderate vasodilator action) and para-aminobenzoic acid (it is a competitive antagonist of sulfanilamide chemotherapeutic drugs and can weaken their antimicrobial effect).

    The elimination half-life is 0.7 min. It is excreted mainly by kidneys in the form of metabolites - 80%.

    Indications:

    Infiltration (including intraosseous), conductive, epidural, spinal anesthesia; anesthesia of mucous membranes (in otorhinolaryngology); vagosympathetic and paranephalic blockade.

    To prepare for anesthesia, during general anesthesia and in the postoperative period (to relieve pain and spasms).

    To dissolve penicillin.

    Contraindications:

    Hypersensitivity, children under 14 years.

    Emergency operations, accompanied by acute blood loss.

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

    Dosing and Administration:

    For infiltration anesthesia - 0.25-0.5% solutions; for anesthesia by the method of Vishnevsky (tight creeping infiltration) - 0,125-0,25% solutions.

    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 parainal blockade (according to AV Vishnevsky), 50-80 ml of a 0.5% solution or 100-150 ml of a 0.25% solution is administered to the peritoneal cellulose, and with vagosympathetic blockade - 30-100 ml of 0.25% solution.

    Higher doses of procaine (for adults):

    - single when taken orally - 0.25 g, intravenously 0.25% solution - 0.05 g (20 ml);

    - daily when taken orally - 0.75 g, intramuscularly and intravenously - 0.1 g.

    Higher doses for infiltration anesthesia for adults: the first single dose at the beginning of the operation is not higher than 1.25 g of a 0.25% solution (with a 0.25% solution of 500 ml) and 0.75 g of a 0.5% solution (150 ml).Further, during each hour of operation - no more than 2.5 g (1000 ml for 0.25% solution) and 2 g (400 ml for 0.5% solution).

    Side effects:

    Dizziness, weakness, low blood pressure, collapse, shock, allergic reactions (dermatitis, skin peeling).

    Overdose:

    Symptoms: pallor of the skin and mucous membranes, dizziness, nausea, vomiting, cold sweats, increased respiration, tachycardia, lowering blood pressure until collapse. Action on the central nervous system is manifested by a feeling of fear, hallucinations, convulsions, motor excitement.

    Treatment: maintenance of adequate pulmonary ventilation with inhalation of oxygen, intravenous administration of short-acting agents for general anesthesia, in severe cases - detoxification and symptomatic therapy.

    Interaction:

    With intravenous injection, it increases the inhibitory effect on the central nervous system of means for general anesthesia, hypnotics, sedatives, narcotic analgesics and tranquilizers.

    Metabolite procaine (paraaminobenzoic acid) is a sulfonamide antagonist.

    Special instructions:It is not absorbed from the mucous membranes; does not provide a superficial anesthesia for dermal application.
    Form release / dosage:Solution for injection, 0.25% and 0.5%.
    Packaging:

    In bottles of 200 and 400 ml of solution.

    Each bottle with the instruction is placed in a pack of cardboard.

    Storage conditions:

    In a place protected from light, inaccessible to 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:П N015659 / 01
    Date of registration:14.05.2009
    Expiration Date:Unlimited
    The owner of the registration certificate:NESVIZH FACTORY OF MEDICAL PREPARATIONS, RUP NESVIZH FACTORY OF MEDICAL PREPARATIONS, RUP Republic of Belarus
    Manufacturer: & nbsp
    Information update date: & nbsp25.06.2018
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