Active substanceParacetamolParacetamol
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  • Dosage form: & nbspsolution for infusions
    Composition:

    One ml of the solution contains:

    Active substances:

    Paracetamol-10 mg;

    One 100 ml bottle contains:

    Active substances:

    Paracetamol - 1000 mg;

    Excipients: Mannitol - 3,850 mg, cysteine ​​hydrochloride monohydrate - 25 mg, sodium hydrogen phosphate dihydrate-13 mg, sodium hydroxide - up to pH 5.5, hydrochloric acid concentrated - to pH 5.5, water for injection - up to 100 ml.

    Description:Transparent colorless or slightly yellowish solution.
    Pharmacotherapeutic group:analgesic non-narcotic remedy
    ATX: & nbsp

    N.02.B.E   Anilides

    N.02.B.E.01   Paracetamol

    Pharmacodynamics:

    Paracetamol has an analgesic and antipyretic effect.

    The action of the drug Perfalgan® occurs within 5-10 minutes. and reaches a maximum after 1 hour; duration of action - from 4 to 6 hours.

    The drug Perfalgan® blocks cyclooxygenase I and II mainly in the CNS, affecting the centers of pain and thermoregulation. In inflamed tissues cellular peroxidase neutralize the effect of paracetamol on the cyclo-oxygenase, which explains the almost complete absence of his anti-inflammatory effect. The absence of influence on the synthesis of prostaglandins in peripheral tissues causes the absence of a negative influence on the water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract.

    Pharmacokinetics:

    The maximum plasma concentration is reached 15 minutes after intravenous infusion of Perfalgan® at a dose of 500 mg or 1 g and is 15 or 30 μg / ml, respectively. The volume of distribution is 1 l / kg. Paracetamol weakly binds to plasma proteins. Penetrates through the blood-brain barrier; 20 minutes after intravenous infusion of a dose of 1 g in the cerebrospinal fluid, a significant concentration of paracetamol (about 1.5 μm / ml) is detected.

    Metabolized in the liver with the formation of glucuronides and sulfates. A small part (4%) of the drug is metabolized by cytochrome P450 to form an active intermediate metabolite (N-acetylbenzoquinonimine), which under normal conditions is quickly neutralized by reduced glutathione and is excreted in the urine after binding to cysteine ​​and mercaptopuric acid. However, with massive intoxication, the amount of this toxic metabolite increases. The half-life in adults is 2.7 hours, in children 1.5-2 hours, the total clearance is 18 liters per hour. Paracetamol is excreted mainly in the urine; 90% of the accepted dose is excreted by the kidneys within 24 hours, mainly in the form of glucuronide (60-80%) and sulfate (20-30%). Less than 5% is displayed unchanged. In severe renal failure (clearance of creatinine below 10-30 ml / min) excretion of paracetamol somewhat slows down, and the half-life is 2-5.3 hours. The rate of elimination of glucuronide and sulfate in patients with severe renal insufficiency is 3 times less than in healthy patients.
    Indications:

    - Pain syndrome of moderate intensity, especially after surgical interventions;

    - Feverish syndrome on the background of infectious and inflammatory diseases;

    - The drug is indicated for rapid relief of pain and febrile syndrome, including when the oral route of administration is difficult.

    Contraindications:

    - Hypersensitivity to paracetamol or propacetamol hydrochloride (prodrug paracetamol) or any other component of the drug.

    - Severe hepatic impairment or decompensated liver disease in the active phase.

    - Newborn period ™ (up to 1 month).

    Carefully:

    - severe renal failure (creatinine clearance <30 ml / min),

    - benign hyperbilirubinemia (including Gilbert's syndrome, viral hepatitis, alcoholic liver damage),

    - chronic alcoholism,

    - chronic malnutrition,

    - anorexia,

    - bulimia,

    - cachexia,

    - hypovolemia,

    - dehydration,

    - the period of breastfeeding,

    - elderly age,

    - deficiency of glucose-6-phosphate dehydrogenase.

    If you have any of these diseases, consult a doctor before taking the drug.

    Pregnancy and lactation:
    The drug should be used during pregnancy, only if the expected The benefits exceed the possible risk for mother and fetus.
    When taking paracetamol inside it small amounts are excreted in breast milk. The appearance of the rash was aboutIt is found in children whose mothers used paracetamol during breastfeeding.
    Nevertheless, paracetamol can be used during breastfeeding, but caution should be exercised when taking the drug during this period.
    Dosing and Administration:Intravenous single infusion in for 15 minutes.
    The drug should not be mixed in one vial for infusion with other medicinal preparations.
    ANDNfusion should be administered immediately after opening the vial; unused remedy destroy. Before starting the infusion the vial with the drug should be carefully to inspect for the absence of visible mechanical particles and discoloration solution.
    Additional dilution is allowed 0.9% solution of sodium chloride or 5% solution of dextrose, in addition to 1/10 of the original volume.
    The diluted solution should be used within an hour after preparation, including the infusion time.
    For infusion, use a needle with a diameter of 0.8 mm, which is injected into the vial in a place marked on the rubber stopper, holding the bottle strictly vertically.
    As with other solutions for infusions supplied in glass containers, in order to avoid embolism with air bubbles, respect the special
    caution, especially at the end of the infusion, regardless of the type of vein the drug is injected into.
    Unintentional surplus recommended doses can lead to a serious impairment of liver function, including fatal outcome. When determining the dose, individual factors risk hepatotoxicity present in the patient: hepatic insufficiency, chronic alcoholism, chronic eating disorders, dehydration.
    Doses are calculated based on the patient's body weight.

    Weight

    bodies

    the patient

    Dose

    paracetamol

    for one

    application of

    (solution of 10 mg / ml)

    Minimalth interval

    between

    receptions

    Maximum

    daily

    dose*

    > 50 kg

    1 g, i.e. 1 vial (100 ml)

    up to 4 times a day

    4 hours

    Not more than 4 g

    > 33 kg - <50 kg

    15 mg / kg, i.e. 1.5 ml / kg up to 4 times a day

    4 hours

    <60 mg / kg, but not more than 3 g

    > 10 kg - <33 kg

    15 mg / kg, i.e. 1.5 ml / kg up to 4 times a day

    4 hours

    <60 mg / kg, but not more than 2 g

    <10 kg **

    7.5 mg / kg, i.e. 0.75 ml / kg up to 4 times a day

    4 hours

    <30 mg / kg, the maximum daily dose is not more than 30 mg / kg

    * The maximum daily dose, taking into account the intake of all drugs containing paracetamol or propacetamol.

    ** Safety and efficacy of the drug for premature infants are not established.

    When the drug is administered to children and adolescents, the vial with the drug can not be suspended as an infusion vessel due to the small volume of the drug administered.

    To avoid mistakes in the calculation of doses for children with a body weight of less than 10 kg, it is recommended to specify the volume for a single injection in milliliters (ml), while in this group of patients introduced amount medicinal product Perfalgan® solution for infusions of 10 mg / ml should not exceed 7.5 ml per infusion.

    Patients with a lower body weight require the introduction of smaller volumes of the drug.

    In order to measure the dose of the drug with taking into account the body weight of the child and the volume, use syringes volume of 5 ml or 10 ml.

    The volume required for administration to the patient should be removed from the bottle and diluted in 0.9% solution of sodium chloride or in a 5% solution of dextrose in ratio of one to ten (one volume preparation in nine volumes of the solution for and enter into the patient for 15 minutes. In severe violations of kidney function (creatinine clearance <30 mL / min) interval between drug administration should not less than 6 hours.

    With chronic liver disease or compensated liver disease in active stage in adults, in particular with hepatic insufficiency, and patients with chronic alcoholism, eating disorders or dehydration, the daily dose should not exceed 3 g. Dose adjustments for elderly patients are not it takes.

    Side effects:Frequency of side effects is given in according to the following scale: very often - 1/10 appointments (> 10%); often - 1/100 appointments (> 1% and <10%); infrequently - 1/1000 appointments (> 0.1% and <1%); rarely - 1/10 000 appointments (> 0.01% and <0,1%); very rare - 1/10 000 (<0.01%).
    From the skin:
    Rarely: redness of the skin, itching, rash on the skin and mucous membranes (usually erythematous or urticarum).
    From the side of the liver and bile-excreting ways:
    Rarely: increased activity "liver" enzymes, usually without development of jaundice.
    From the side of cardiovascular system:
    Rarely: lowering of blood pressure;
    Rarely: tachycardia
    From the hematopoiesis:
    Very rarely: thrombocytopenia
    General Characteristics:
    Rarely: malaise.
    The following side effects also were observed in post-marketing application of the drug, however their frequency not installed:
    Allergic reactions: reactions hypersensitivity, anaphylactic shock, anaphylaxis, angioedema.
    From the skin: acute generalized exanthematous pustulosis (AGEP), Stevens-Johnson syndrome, toxic epidermal necrolysis.
    From the side of the liver and bile-excreting ways: fulminant hepatitis, necrosis liver, liver failure, increased activity of "hepatic" enzymes.
    From the gastrointestinal side tract: nausea, vomiting;
    Local reactions: soreness and burning sensation at the site of injection.
    If any of the instructions specified in the instruction side effects are aggravated, or you noticed any other side effects effects not listed in the instructions, tell your doctor.
    Overdose:

    In case of an overdose, liver damage (fulminant hepatitis, hepatic insufficiency, cholestatic hepatitis, cytolytic hepatitis), especially in elderly patients, children, patients with liver diseases (caused by chronic alcoholism), in patients with eating disorders, as well as in patients taking enzyme inducers .

    The clinical picture of acute overdose develops within 24 hours after taking paracetamol.

    Symptoms: gastrointestinal disorders (nausea, vomiting, decreased appetite, abdominal discomfort and / or abdominal pain), pale skin. With the simultaneous administration of 7.5 g or more to adults or children over 140 mg / kg, cytolysis of hepatocytes occurs with complete and irreversible necrosis of the liver, the development of hepatic insufficiency, metabolic acidosis and encephalopathy, which can lead to coma and fatal outcome. Across 12-48 hours after the introduction of paracetamol, there was an increase in the activity of "hepatic" transaminases, lactate dehydrogenase, bilirubin level and a decrease in the level of prothrombin.

    Clinical symptoms of liver damage are manifested after 2 days after drug overdose and reach a maximum of 4-6 days.

    Treatment:

    - Immediate hospitalization;

    - Determination of the quantitative content of paracetamol in blood plasma before treatment at the earliest possible time after an overdose;

    - Introduction donators SH-groups and precursors of the synthesis of glutathione-methionine and N - Acetylcysteine ​​- within 10 hours after an overdose. The need for additional therapeutic measures (further introduction of methionine, iv administration N - acetylcysteine) is determined depending on the concentration of paracetamol in the blood, as well as on the time elapsed after its administration;

    - Symptomatic treatment;

    - Hepatic tests should be performed at the beginning of treatment and then every 24 hours. In most cases, the activity of liver transaminases is normalized within 1 to 2 weeks. In very serious cases, liver transplantation may be required.

    Interaction:
    Probenecid almost twice reduces clearance of paracetamol, inhibiting process its conjugation with glucuronic acid.
    With simultaneous application should consider lowering the dose paracetamol.
    Inductors of microsomal enzymes liver (eg, ethanol, barbiturates, isoniazid, rifampicin, anticoagulants, zidovudine, amoxicillin + clavulanic acid, phenytoin) increase the production of hydroxylated active metabolites, which makes it possible to develop severe intoxication with small overdoses. Phenytoin reduces the effectiveness of paracetamol and increases the risk of hepatotoxicity. Patients receiving phenytoin, paracetamol should be avoided in high doses and / or for a long time. It is necessary to monitor the condition of such patients for the development of signs of hepatotoxicity.
    Ethanol promotes the development of acute pancreatitis.
    Inhibitors of microsomal liver enzymes (incl. cimetidine) reduce the risk of hepatotoxic effects.
    Long-term use of barbiturates reduces the effectiveness of paracetamol.
    Long-term combined use of paracetamol and other non-steroidal anti-inflammatory drugs (salicylamide) increases the risk of developing analgesic nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure.
    Simultaneous long-term use paracetamol in high doses and salicylates increases the risk of cancer kidney or bladder.
    Salicylamide increases half-life paracetamol.
    Simultaneous application of paracetamol in infusions (4 g / day, not less than 4 days) and coumarins, including warfarin, can lead to a slight change international normalized relationship (INR). It should be controlled INR during treatment and during the week after stopping infusions of paracetamol.
    Special instructions:

    It is recommended to transfer the patient to oral administration painkillers drugs, as soon as such a opportunity.

    The risk of liver damage increases when the recommended doses are exceeded (in including the simultaneous use of the drug Perfalgan® and other drugs, containing paracetamol), as well as patients with chronic alcoholism.

    When taking Perfalgan® develop serious skin reactions, such as acute generalized exanthematous pustulosis (AGEP), Stevens-Johnson syndrome, toxic epidermal necrolysis, which can lead to death. Patients should be informed of the signs of severe skin reactions. The drug should be discontinued at the first manifestations of skin reactions or any other signs of hypersensitivity.

    To avoid the risk of overdose, simultaneous use of Perfalgan® and other preparations containing paracetamol (both prescription and non-prescription medicines).Distorts the results of quantitative determination of uric acid in the plasma.

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

    Has no influence.

    Form release / dosage:Solution for infusions 10 mg / ml.
    Packaging:

    To 50 ml or 100 ml of the drug in a bottle of clear, colorless glass type II, sealed with a bromobutyl rubber stopper with a silicone coating, coated with an aluminum cap with a protective plastic cover.

    Twelve bottles, covered with polyethylene, with instructions for use are placed in a cardboard box (for hospitals).

    Storage conditions:

    At a temperature of 15-30 ° C.

    Keep out of the reach of children!

    Shelf life:

    2 of the year.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N016008 / 01
    Date of registration:06.10.2009
    The owner of the registration certificate:BRISTOL-MIYERS SQUIPB BRISTOL-MIYERS SQUIPB USA
    Manufacturer: & nbsp
    Information update date: & nbsp07.10.2015
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