Active substanceOndansetronOndansetron
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  • Dosage form: & nbspsolution for intravenous and intramuscular administration
    Composition:

    1 ampoule (2 ml) of the solution contains ondansetron hydrochloride dihydrate (in terms of ondansetron base) as active ingredient - 4.0 mg;


    Excipients: lemon

    acid monohydrate 1.1 mg, sodium citrate pentasecylhydrate 0.66 mg or sodium citrate dihydrate 0.55 mg, sorbitol 96.0 mg, water for injection 2.0 ml.

    1 ampoule (4 ml) of the solution contains ondansetron hydrochloride dihydrate (in terms of ondansetron base) as active ingredient - 8.0 mg;

    Excipients: citric acid monohydrate 2.2 mg, sodium citrate pentasecvhydrate 1.32 mg or sodium citrate dihydrate 1.1 mg, sorbitol 192.0 mg, water for injection 4.0 ml.


    Description:

    colorless or almost colorless transparent or with light opalescence liquid.

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

    A.04.A.A.01   Ondansetron

    Pharmacodynamics:

    Ondansetron is a selective 5-HTZ receptor antagonist (serotonin). Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in the serotonin level, which by activation of the afferent fibers of the vagus nerve, containing 5-HT receptors3, causes a vomitive reflex.


    Ondansetron selectively blocks serotonin 5-HTZ receptors of central neurons (vomiting center) and

    peripheral (gastrointestinal tract) of the nervous system, regulating the gag reflex.


    Does not violate the coordination of movements, does not cause sedation and reduced efficiency. Does not change the concentration of prolactin in the plasma.
    Pharmacokinetics:With intramuscular injection, the peak concentration (TCmOh) in plasma is achieved within 10 minutes. Distribution

    ondansetron is the same for oral, intramuscular and intravenous administration. Bioavailability is about 60%. The drug is metabolized in the liver. The binding with plasma proteins is 70-76%. The volume of distribution is 140 liters. The half-life (T1/2) is 3 hours, in elderly patients can reach 5 hours, and with severe hepatic insufficiency - 15-20 hours. From the systemic blood flow is eliminated mainly as a result of liver metabolism, which occurs with the participation of several microsomal liver enzymes (CYP1A2, CYP2D6, CYP3A4). Absence of isoenzyme CYP2D6 does not affect the pharmacokinetics of ondansetron.In the unchanged form, less than 5% of the administered dose is excreted in the urine. The pharmacokinetic parameters of ondansetron do not change when it is repeated. In patients with moderate renal insufficiency (creatinine clearance 15-60 ml / min), both systemic clearance and volume of ondansetron distribution are reduced, resulting in a small and clinically insignificant increase T1 / 2 (up to 5.4 hours).


    The pharmacokinetics of ondansetron practically does not change in patients with severe renal dysfunction.
    Indications:

    - prevention and relief of nausea and vomiting caused by cytostatic chemotherapy, cytostatic radiotherapy;

    - prevention and management of postoperative nausea and vomiting.

    Contraindications:

    - hypersensitivity to any component of the drug;

    - pregnancy and lactation;

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

    Pregnancy and lactation:contraindicated
    Dosing and Administration:

    Cytostatic therapy

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

    For adults The daily dose, as a rule, is 8-32 mg.

    The following modes 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, just before the start of chemotherapy. The efficacy of ondansetron can be increased by a single intravenous injection of a glucocorticoid (eg, 20 mg dexamethasone) before the onset


    chemotherapy.

    To prevent delayed vomiting. arising after 24 hours from the beginning chemotherapy or radiotherapy - as with the use of highly emetogenic therapy, and with moderately-emetogenic therapy - it is recommended to continue the use of the drug inside in the form of tablets of 8 mg 2 times a day for 5 days.

    Children

    Children older than 2 years of the drug is administered at a dose of 5 mg / m body surface 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 is used exclusively parenterally in a single dose of 0.1 mg / kg (maximum to 4 mg) in the form of a slow intravenous injection before, during 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.

    Patents with impaired renal function

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

    Patients with impaired hepatic function

    With moderate or severe impairment of liver function, the clearance of ondansetron is significantly reduced, while the half-life of it is increased from the plasma, so it is not recommended for such patients to prescribe more than 8 mg of ondansetron per day.

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

    - 0.9% solution of sodium chloride,

    - 5% glucose solution,

    - Ringer's solution,

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

    - 0,3 % potassium chloride solution and 5% glucose solution.

    Side effects:

    From the digestive system: hiccough, dry mouth, diarrhea or constipation, sometimes an asymptomatic transient increase in serum aminotransferase levels.

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

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

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

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

    Other: "tide" of blood to the face, a feeling of heat, a temporary violation of visual acuity, hypokalemia, hypercreatininaemia.

    Overdose:

    Symptoms: in most cases are similar to adverse reactions when the drug is used in the recommended doses.

    Treatment: there is no specific antidote. In cases of suspected overdose, symptomatic and supportive therapy is indicated.

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

    Ondansetron at a concentration of 16-160 μg / ml is pharmaceutically compatible and can be administered via Yinjector intravenously drip together 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 ondansetron); carboplatin (in 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 (in a dose of 0.25-2 g, as an intravenous bolus injection for 5 minutes);

    cyclophosphamide (in a dose of 0.1-1 g, as an intravenous bolus injection for 5 minutes);

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

    dexamethasone: possible intravenous administration of 20 mg dexamethasone sodium phosphate slowly, for 2-5 minutes. The drug can be administered through a single dropper, while the concentration of dexamethasone sodium phosphate in the solution can range from 32 to 2500 μg / ml, ondansetron - from 8 to 100 μg / ml.


    Special instructions:

    Patients who had previously had allergic reactions to other selective 5-HT blockers3-receptors, have an increased risk of their development against the background of ondansetron. Ondansetron can slow the motility of the large intestine in connection, with which its appointment to patients with signs of intestinal obstruction requires 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 at normal illumination. 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 intravenous and intramuscular injection 4 mg / 2 ml or 8 mg / 4 ml (2 mg / ml).


    Packaging:

    By 2 ml or 4 ml in ampoules of colorless neutral glass with a color fracture ring or with a colored dot and a notch. One, two or three color rings and / or a two-dimensional bar code, and / or alphanumeric coding or without additional color rings, a two-dimensional barcode, alphanumeric coding are applied to ampoules.

    5 ampoules in the outline of the cell.For 1 or 2 contour mesh packages together with instructions for use in a pack of cardboard.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    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:LS-001020
    Date of registration:16.12.2010
    The owner of the registration certificate:FarmSirma Soteks, ZAO FarmSirma Soteks, ZAO Russia
    Manufacturer: & nbsp
    Representation: & nbspPharm Company Sotex CJSC Pharm Company Sotex CJSC Russia
    Information update date: & nbsp25.08.2011
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