Active substanceOndansetronOndansetron
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  • Dosage form: & nbsp

    solution for intravenous and intramuscular administration

    Composition:

    1 ml of the solution contains:

    active substance: ondansetron hydrochloride dihydrate in terms of 100% ondansetron - 2 mg

    Excipients: chlorobutanol anhydrous, water for injection.

    Description:

    Solution: a clear, colorless or almost colorless liquid.

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

    A.04.A.A.01   Ondansetron

    Pharmacodynamics:

    Ondansetron is a selective 5HT receptor antagonist3 (serotonin). Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in serotonin levels, which by activation of vagal afferent fibers containing 5-H receptorsT3, causes a vomitive reflex. Ondansetron inhibits the appearance of a vomiting reflex by blockade of 5-HT receptors3 at the level of neurons of both the central and peripheral nervous system.

    This mechanism of action is based on the prevention and treatment of post-operative and cytostatic chemo- and radiotherapy-induced vomiting and nausea.

    Pharmacokinetics:

    With intramuscular injection, the peak concentration in plasma is reached within 10 minutes. The distribution of ondansetron is the same for intramuscular and intravenous administration.After oral administration, the maximum concentration of ondansetron in the blood plasma is reached after about 1.5 hours. Absolute bioavailability is about 60%. 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.

    Both after oral administration and with parenteral administration, the elimination half-life is about 3 hours, in elderly patients it 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 / or radiotherapy, as well as postoperative nausea and vomiting.

    Contraindications:

    - Hypersensitivity to ondansetron or any other component of the drug.

    - Pregnancy and lactation.

    - Children under 2 years of age (safety and efficacy not studied)

    Dosing and Administration:

    Cytostatic therapy

    The choice of the dosage regimen is determined by the severity of the emetogenic effect of the 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;

    - 8 mg orally 1 to 2 hours before the start of therapy, then another 8 mg orally 12 hours after the start of therapy.

    With highly emeticogenic chemotherapy:

    - 8 mg intravenously struino slowly just before chemotherapy, and then two further intravenous jet 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 efficacy of Lazaran BM can be increased by a single intravenous glucocorticoid (eg, 20 mg dexamethasone) prior to chemotherapy; when ingested to enhance the effect of a single dose can be increased to 24 mg and administered simultaneously with 12 mg of dexamethasone 1-2 hours before the start of chemotherapy.

    To prevent delayed (occurring after 24 hours after the initiation of chemotherapy or radiotherapy) vomiting, it is recommended to continue using the drug inside as tablets 8 mg twice a day for 5 days.

    Children

    Children older than 2 years of the drug is administered at a dose of 5 mg / m2 body surface intravenously, immediately before the start of chemotherapy, followed by oral administration at a dose of 4 mg after 12 hours; after the end of chemotherapy, it is recommended to continue treatment at 4 mg twice daily for 5 days.

    Prevention of postoperative nausea and vomiting

    Adults inject a single dose of 4 mg intramuscularly or intravenously slowly at the onset of anesthesia, or prescribe 16 mg orally 1 hour prior to the onset of anesthesia.

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

    Intramuscularly into the same site of the body, Lazaran BM can be administered at a dose not exceeding 4 mg!

    Children To prevent postoperative nausea and vomiting, Lazaran BM is used exclusively parenterally at a single dose of 0.1 mg / kg (max. 4 mg) as 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 the clearance of Lazaran BM significantly decreases, and the half-life of it is increased from the plasma, therefore, do not exceed the daily dose of 8 mg per day.

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

    0.9% solution of sodium chloride,

    5% 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 blood 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 rush of blood to the face, a feeling of heat, a temporary violation of visual acuity, hypokalemia.

    Overdose:

    In cases of suspected overdose, symptomatic therapy is indicated.

    In case of an overdose of ondansetron tablets, the use of ipecacuanas is not recommended, since it is unlikely that this drug will be effective during the antiemetic activity of the drug. 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 also other hydantoins), rifampicin, tolbutamide;

    - with enzyme inhibitors R450 (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.

    Lazaran BM at a concentration of 16-160 μg / ml is pharmaceutically compatible and can be administered via Y-injector intravenously drip with the following drugs:

    - cisplastin (at a concentration of up to 0.48 mg / ml) for 1-8 hours;

    - 5-fluorouracil (at a concentration of up to 0.8 mg / ml at a rate of 20 ml / h - higher

    concentrations may cause precipitation of Lazaran BM);

    - carboplatin (at a concentration of 0.18-9.9 mg / ml for 10-60 min);

    - etoposide (in a concentration of 0.14-0.25 mg / ml for 30-60 minutes);

    - ceftazidime (at a dose of 0.25-2.0 g, as an intravenous bolus injection for 5 min);

    - cyclophosphamide (in a dose of 0.1 -1.0 g, as an intravenous bolus injection for 5 minutes);

    - doxorubicin (at a dose of 10-100 mg, as an intravenous bolus injection for 5 min);

    - dexamethasone: possible intravenous administration of 20 mg dexamethasone slowly, for 2-5 minutes. Drugs can be administered through a single dropper, while the concentration of dexamethasone sodium phosphate in the solution can range from 32 μg to 2.5 mg / ml, Lazaran BM from 8 μg to 1 mg / ml.

    Special instructions:

    In patients who previously used other selective antagonists 5HT3-receptors, reactions of increased sensitivity were observed, when using Lazaran BM, similar reactions may also develop.

    Since Lazaran VM slows the bowel motility, patients with signs of intestinal obstruction after using the drug require special observation.

    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.

    Form release / dosage:Solution for injection in ampoules of dark glass at 4 mg / 2 ml and 8 mg / 4 ml.
    Packaging:

    5 ampoules in blisters; 1 blister in a cardboard box with the attached instructions for use.

    Storage conditions:

    List B.

    Solution for intravenous and intramuscular administration: at a temperature of 15 to 25 ° C in a dark place out of the reach of children.

    Shelf life:

    The solution for intravenous and intramuscular injection is 2 years.

    The drug should not be used after the expiry date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LS-000817
    Date of registration:10.08.2010
    Expiration Date:Unlimited
    The owner of the registration certificate:Simen LaboratoriesSimen Laboratories India
    Manufacturer: & nbsp
    Representation: & nbspPERMFARMACY, OJSCPERMFARMACY, OJSC
    Information update date: & nbsp09.02.2018
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