Active substanceProcainProcain
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  • Dosage form: & nbsprectal suppositories
    Composition:

    1 suppository contains:

    active substance: procaine hydrochloride 0.1 g;

    auxiliary substance: solid fat - a sufficient amount to obtain a suppository with a mass of 1.1 g.

    Description:

    Suppositories white or white with a yellowish hue of color, torpedo-shaped.

    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, 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.

    Pharmacokinetics:

    It is subject to complete systemic absorption. 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 sulfonamide chemotherapeutic drugs and can weaken their antimicrobial effect.

    Indications:As a local anesthetic for hemorrhoids and fissures of the anus.
    Contraindications:

    Hypersensitivity (including para-aminobenzoic acid and other local anesthetic esters), children's age (under 18 years).

    Carefully:

    Emergency operations accompanied by acute blood loss, conditions accompanied by a decrease in hepatic blood flow (eg, in chronic heart failure, liver diseases), progression of cardiovascular insufficiency (usually due to the development of heart block and shock), proctitis, pseudocholinesterase deficiency, renal failure, in the elderly patients (over 65 years), seriously ill, weakened patients, pregnancy, childbirth.

    Pregnancy and lactation:

    During pregnancy and lactation, the drug should be used when the benefit to the mother exceeds the risk to the fetus or the baby.

    Dosing and Administration:

    Rectally.

    The suppository is injected deep into the anus (after cleansing enema or spontaneous bowel movement), having previously released the candle from the contoured package with scissors (cutting the package along the contour of the candle). Apply to 1 suppository 1-2 times a day.

    The duration of treatment as a local anesthetic is not more than 5 days. If the painful phenomena persist, you should consult your doctor.

    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), paralysis of the respiratory muscles, impaired sensory and motor conduction, respiratory paralysis center 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: skin itching, skin rash, other anaphylactic reactions (including anaphylactic shock), urticaria (on the skin and mucous membranes), dizziness, weakness, lowering blood pressure. In these cases, stop using the drug and consult a doctor.

    Local Reactions: in the first days of the drug, there may be urges for defecation and a feeling of discomfort, which later pass independently and do not require the drug to be withdrawn. Rarely, hyperemia and itching in the anal area (when used in high doses).

    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 ventilation with oxygen inhalation, intravenous administration of short-acting drugs for general anesthesia, in severe cases - detoxification and symptomatic therapy.

    Interaction:

    Local anesthetics increase the inhibitory effect on the central nervous system of other drugs.

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

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

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

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

    Cholinesterase inhibitors (antimiasthenic drugs, cyclophosphamide, democaria bromide, eco-iodide iodide, thiotepa) reduce the metabolism of locally anesthetic drugs. Metabolite procaine (paraaminobenzoic acid) is an antagonist of sulfonamides, which leads to a weakening of the antimicrobial effect.

    Special instructions:

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

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

    Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and taking other potentially hazardousActivities that require increased concentration and speed of psychomotor reactions.
    Form release / dosage:

    Suppositories rectal, 100 mg.

    Packaging:

    5 suppositories are placed in a contour mesh package from a polyvinyl chloride film.

    Two contour mesh packages together with the instruction for use are placed in a pack of cardboard.

    Storage conditions:

    In a dry, dark place at a temperature of no higher than 20 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:Without recipe
    Registration number:P N000353 / 01
    Date of registration:06.09.2011 / 28.02.2018
    Expiration Date:Unlimited
    The owner of the registration certificate:BIOSINTEZ, PAO BIOSINTEZ, PAO Russia
    Manufacturer: & nbsp
    Representation: & nbspBIOSINTEZ JSC BIOSINTEZ JSC Russia
    Information update date: & nbsp24.06.2018
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