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

    Composition per 1ml of solution

    Active substance

    Paracetamol 10.0 mg

    Excipients: propylene glycol 8.0 mg, citric acid monohydrate 0.47 mg, sodium disulfite 0.50 mg, sodium hydrogen phosphate dihydrate 0.89 mg, sodium chloride 2.00 mg, water for injection - sk. up to 1 ml

    Description:

    Clear solution from colorless to light yellow color

    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 drug blocks cyclooxygenase I and II mainly in the central nervous system, 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 paracetamol negative influence on water-salt metabolism (sodium and water retention) and the mucous membrane of the gastrointestinal tract.
    Pharmacokinetics:

    The maximum concentration in the blood plasma is reached after 15 minutes. and is 15-30 μg / ml. The volume of distribution is 1l / kg. Paracetamol weakly binds to plasma proteins, penetrates the hemato-encephalic barrier.

    Metabolized in the liver with the formation of gljuronids and sulfates. A small part (4%) of the drug is metabolized by cytochrome P450 with the formation of an 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, in newborns 3.5 hours, total clearance -

    18 l / h. Paracetamol is excreted mainly with urine; 90% of the 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 (creatinine clearance 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 failure is 3 times less than in healthy patients.

    Indications:

    Pain syndrome of mild and moderate intensity, especially after surgical interventions. Feverish syndrome on the background of infectious and inflammatory diseases. The drug is indicated for the rapid relief of pain and febrile syndrome, especially in cases where the oral route of administration is difficult.

    Contraindications:

    - hypersensitivity to paracetamol or propacetamol hydrochloride (paracetamol prodrug) or any other component included in the formulation;

    - severe liver dysfunction;

    - children under 1 year.

    Carefully:

    - severe renal failure (creatinine clearance <30 mL / min);

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

    - chronic alcoholism;

    - severe liver dysfunction;

    - deficiency of glucose-6-phosphate dehydrogenase.

    - elderly age.

    Pregnancy and lactation:

    The drug should be used only if the expected benefit exceeds the possible risk to the mother and fetus.

    Dosing and Administration:

    Intravenous single infusion for 15 min.

    An open and unused vial of the drug should be destroyed. Additional dilution is possible with 0.9% sodium chloride solution, maximum - in 10 times. Such a diluted solution should be used within 1 hour after its preparation (including the infusion time).

    Children from 1 year to 11 years (with a body weight of 34 kg):

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

    The minimum interval between administrations should be at least 4 hours. The maximum daily dose of paracetamol should not exceed 60 mg / kg.

    Adolescents (over 12 years) and adults with a body weight of 35 to 50 kg: 15 mg / kg paracetamol per infusion, i.e. 1.5 ml / kg. The minimum interval between introductions should be at least 4 hours.

    The maximum daily dose of paracetamol should not exceed 60 mg / kg.

    Adolescents (over 12 years) and adults weighing more than 50 kg: the maximum single dose is 1 g of paracetamol, i.e. 1 bottle (100 ml).The minimum interval between administrations should be 4 hours. The maximum daily dose is 4 g.

    In patients with impaired hepatic or renal function, with Gilbert's syndrome and in the elderly, the interval between injections should be at least 8 hours, with the daily dose of paracetamol should be reduced.
    Side effects:

    From the gastrointestinal tract: increased activity of hepatic enzymes (usually without the development of jaundice).

    From the side of the cardiovascular system: arterial hypotension.

    On the part of the organs of hematopoiesis: thrombocytopenia, and leukopenia.

    Allergic reactions: skin itching, rashes on the skin and mucous membranes (usually erythematous or urticaria), anaphylactic shock, Quincke's edema.

    Overdose:

    The clinical picture of an acute overdose develops in the first 24 hours after the administration of high doses of paracetamol. Symptoms of chronic overdose appear after 12-96 hours after increasing the dose of the drug.

    Symptoms of acute overdose: diarrhea, decreased appetite, nausea, vomiting, discomfort and / or abdominal pain, pale skin. With the simultaneous introduction of paracetamol to adults at a dose of 7.5 g or more,and children more than 140 mg / kg cytolysis of hepatocytes occurs with complete and irreversible necrosis of liver development of hepatic insufficiency, metabolic acidosis and encephalopathy, which may lead to coma and death. Twelve hours after the administration of paracetamol, an increase in liver transaminases, lactate dehydrogenase and bilirubin levels, as well as a decrease in the level of prothrombin, was noted.

    Symptoms of chronic overdose: developing hepatotoxic effect, characterized common symptoms (pain, fatigue, weakness, sweating), and specific symptoms characterizing liver damage may occur as a result gepatonekroz. Hepatotoxic effects of acetaminophen can be complicated by development of hepatic encephalopathy (thought disorder, central nervous system depression, anxiety or stupor), the occurrence of seizures, respiratory depression, coma, cerebral edema, hypoglycemia, metabolic acidosis, arrhythmias, collapse. Rarely, liver function abnormalities develop with lightning speed and can be complicated by renal failure (tubular necrosis).

    Treatment: introduction of donators SH-band and the precursors of the synthesis of glutathione - methionine 8-9 hours after an overdose and N-acetylcysteine ​​after 10 hours. The need for additional therapeutic measures (further introduction of methionine, intravenous administration N- acetylcysteine) is determined by the concentration of paracetamol in the blood plasma, as well as by the time elapsed after its administration.

    Interaction:

    Inductors of microsomal liver enzymes (phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants) increase the production of hydroxylated active metabolites of paracetamol, which allows the development of severe intoxication with a slight overdose of paracetamol.

    Ethanol increases the likelihood of developing acute pancreatitis.

    Inhibitors of microsomal liver enzymes (incl. cimetidine) reduce the risk of hepatotoxic effects of paracetamol. Long-term use of barbiturates reduces the effectiveness of paracetamol.

    Probenecid lowers paracetamol clearance, so when combined, the dose of paracetamol should be reduced.

    Long-term combined use of paracetamol with other non-steroidal anti-inflammatory drugs increases the risk of developing analgesic nephropathy and renal papillary necrosis, the onset of the terminal stage of renal failure.

    Simultaneous long-term use of paracetamol in high doses and salicylates increases the risk of developing kidney or bladder cancer.

    Diflunisal increases the concentration of paracetamol in the blood plasma by 50% and increases the risk of hepatotoxic reactions.

    Special instructions:

    The risk of liver damage increases in patients with alcoholic hepatosis. Paracetamol distorts the levels of uric acid in the blood plasma.

    When the drug is used for a long time, it is necessary to monitor the pattern of peripheral blood and the functional state of the liver.

    Effect on the ability to drive transp. cf. and fur:During the period of treatment, care must be taken when driving vehicles and when engaging in other potentially hazardous activities requiring increased attention and speed of psychomotor reactions (hypotension, dizziness).
    Form release / dosage:
    Solution for infusions 10 mg / ml.
    Packaging:50 ml or 100 ml in a glass bottle (USP, type 1), ukuporenny brombutilovoy rubber stopper with a silicone coating, coated with an aluminum cap with a protective plastic cover.
    One bottle with the instruction for use and the bottle holder is placed in a cardboard bundle or 100 ml per bottle of low-density polyethylene, sealed with a snap-on cap.
    One bottle with instructions for use is placed in a cardboard box.
    Storage conditions:Store at a temperature not exceeding 30 ° C.
    Shelf life:

    2 years. Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-000900
    Date of registration:18.10.2011
    The owner of the registration certificate:Unik Pharmaceutical Laboratories Unik Pharmaceutical Laboratories India
    Manufacturer: & nbsp
    Representation: & nbsp"UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")""UNIC PHARMACEUTICAL LABORATORY (branch of the company" JB Chemicals and Pharmaceuticals Ltd. ")"India
    Information update date: & nbsp02.10.2015
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