Active substanceOndansetronOndansetron
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  • Dosage form: & nbsp

    solution for intravenous and intramuscular administration

    Composition:
    Active substance:

    ondansetron hydrochloride dihydrate in terms of base - 2 mg

    Excipients: sodium chloride 9 mg, 1 M hydrochloric acid solution to pH 3.0-4.0, water for injection up to 1 ml.

    Description:

    Transparent colorless or slightly colored liquid.

    Pharmacotherapeutic group:antiemetics, serotonin receptor antagonist
    ATX: & nbsp

    A.04.A.A.01   Ondansetron

    Pharmacodynamics:

    Ondansetron is a selective antagonist of the 5HT3 (serotonin) receptor. Medicines for cytostatic chemotherapy and radiotherapy can cause an increase in the level of serotonin, which, by activating vagal afferent fibers containing 5-HTs receptors, induces a vomiting reflex. Ondansetron inhibits the appearance of a vomitive reflex by blocking the receptors of 5-HTs at the level of neurons of both the central and peripheral nervous system.

    Apparently, this mechanism of action is based on the prevention and treatment of post-operative and cytotoxic chemo- and radiotherapy-induced vomiting and nausea.

    Pharmacokinetics:

    With intramuscular injection, the peak concentration in plasma is reached within 10 minutes.The drug is metabolized in the liver. The binding with plasma proteins is 70-76%. Less than 5% of the drug is excreted unchanged in urine.

    Half-life is about 3 hours, in elderly patients can reach 5 hours, and with severe hepatic insufficiency - 15-20 hours. With kidney damage (renal clearance less than 15 ml / min), the elimination half-life increases by 4-5 hours, but this increase is not clinically significant.

    Indications:

    Prevention and elimination of nausea and vomiting caused by cytostatic chemotherapy and radiotherapy, as well as postoperative nausea and vomiting.

    Contraindications:

    - Hypersensitivity to ondansetron or any other component of the drug

    - Pregnancy and lactation.

    - Children up to 2 years of age (lack of sufficient experience).

    Pregnancy and lactation:contraindicated
    Dosing and Administration:

    Enter the drug intravenously or intramuscularly.

    Cytostatic therapy

    The choice of dosage regimen is determined by the emetogenicity of antitumor therapy.

    For of adults The daily dose, as a rule, is 8-32 mg, the following regimens are recommended With moderate emetogenic chemotherapy or radiotherapy:

    - 8 mg intravenously struino slowly or intramuscularly, immediately before the start of therapy;

    With highly emeticogenic chemotherapy:

    - 8 mg intravenously struino slowly just before the start of chemotherapy, and then two more intravenous injections of 8 mg, each of which is carried out in 2-4 hours;

    continuous 24-hour infusion of the drug at a dose of 24 mg at a rate of 1 mg / h;

    - 16-32 mg, diluted in 50-100 ml of the appropriate infusion solution, in the form of a 15-minute infusion, immediately before the start of chemotherapy.

    The effectiveness of the drug can be increased by a single intravenous glucocorticoid (eg, 20 mg dexamethasone) prior to chemotherapy.

    Children

    Children older than 2 years of the drug is administered at a dose of 5 mg / m2 surface of the body intravenously, immediately before the start of chemotherapy.

    Prevention of postoperative nausea and vomiting

    Adults introduce a single dose of 4 mg intramuscularly or intravenously struino, slowly at the beginning of anesthesia.

    For relief of nausea and vomiting it is recommended intramuscular or slow intravenous injection of 4 mg of the drug.

    Intramuscularly in the same body region ondansetron can be administered at a dose not exceeding 4 mg!

    Children to prevent postoperative nausea and vomiting ondansetron It is applied parenterally in a single dose of 0.1 mg / kg (maximum to 4 mg) in the form of a slow intravenous injection before or after anesthesia.

    To treat the development of postoperative nausea and vomiting in children, a slow intravenous injection of a single dose of the drug 0.1 mg / kg (maximum 4 mg) is recommended.

    With regard to the prevention and treatment of postoperative nausea and vomiting in children under 2 years of age there is no sufficient experience.

    Elderly patients

    Dosage adjustments are not required.

    Patients with kidney and liver lesions

    With renal damage, the usual daily dose and frequency of administration of the drug is not required.

    With liver damage significantly reduces the clearance of ondansetron, and the half-life of it is increased from the plasma, so it is necessary to reduce the dose to 8 mg per day.

    To dilute the injection solution, the following solutions can be used:

    0.9% solution of sodium chloride,

    5% dextrose solution, Ringer's solution,

    0.3% potassium chloride solution and 0.9% sodium chloride solution,

    0.3% potassium chloride solution and 5% dextrose solution.

    Side effects:

    Allergic reactions: urticaria, bronchospasm, laryngospasm, angioedema, anaphylaxis.

    From the digestive system: hiccough, dry mouth, diarrhea, constipation, sometimes asymptomatic transient increase in the level of aminotransferases in the serum.

    From the side of the cardiovascular system: pain in the chest, in some cases with depression of the segment ST, arrhythmias, bradycardia, lowering blood pressure.

    From the nervous system: headache, dizziness, spontaneous movement disorders and convulsions.

    Local reactions: pain, burning and redness at the injection site,

    Other: a flood of blood to the face, a feeling of heat, a temporary disturbance of visual acuity, hypokalemia.
    Overdose:

    In cases of suspected overdose, symptomatic therapy is indicated.

    The specific antidote is not known.

    Interaction:

    As ondansetron is metabolized by the enzyme system (cytochrome P450) of the liver, caution is required when combined:

    - with enzymatic inducers P450 (CYP2D6 and CYP3A) (barbiturates, carbamazepine, carisoprodol, glutethimide, griseofulvin, dinitrogen oxide, papaverine, phenylbutazone, phenytoin (probably other hydantoins), rifampicin, tolbutamide);

    - with inhibitors of enzymes P450 (CYP2D6 and CYP3A) (allopurinol, macrolide antibiotics, antidepressants - MAO inhibitors, chloramphenicol, cimetidine, oral contraceptives containing estrogens, diltiazem, disulfiram, valproic acid, sodium valproate, erythromycin, fluconazole, fluoroquinolones, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil).

    Special instructions:

    In patients who previously had other sensitivity selective 5HT receptor antagonists, reactions of increased sensitivity were observed, and similar reactions may occur with ondansetron.

    As ondansetron can cause constipation, patients with signs of intestinal obstruction after using the drug require regular monitoring.

    The infusion solution should be prepared immediately before use. If necessary, the ready-made infusion solution can be stored for up to 24 hours at a temperature of 2-8 ° C.

    During the infusion, protection from light is not required; The diluted injection solution retains its stability for at least 24 hours under natural light or normal light.

    Effect on the ability to drive transp. cf. and fur:
    No information.
    Form release / dosage:

    Solution for intravenous and intramuscular injection 2 mg / ml. 2 ml or 4 ml into neutral glass ampoules.

    Packaging:

    For 3, 5 or 10 ampoules with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a box of cardboard.


    1 ampoule with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a packet with cardboard partitions.

    By 1, 3, 5 or 10 ampoules per contour cell packaging from a polyvinyl chloride film or polyethylene terephthalate tape and aluminum foil or paper with a polyethylene coating or without foil, or without paper.

    For 1 or 2 contour squares with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a pack of cardboard.


    When you pack the ampoules with a break ring or break point, the ampoule opener or ampoule scapper is not put in.
    Storage conditions:

    At a temperature of 15 ° Сдо25 ° С in the dark place.

    Keep 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:LSR-001525/08
    Date of registration:14.03.2008
    The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia
    Manufacturer: & nbsp
    Representation: & nbspNOVOSIBHIMFARM, OJSCNOVOSIBHIMFARM, OJSC
    Information update date: & nbsp22.10.2013
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