Active substanceOndansetronOndansetron
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  • Dosage form: & nbsp

    solution for intravenous and intramuscular administration.

    Composition:Active substance: ondansetron hydrochloride dihydrate (in terms of ondansetron) 2.0 mg. flapExcipients: citric acid monohydrate - 0.5 mg, sodium citrate dihydrate - 0.25 mg, sodium chloride - 9.0 mg, water for injection - up to 1.0 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 5-HT3 receptor antagonist (serotonin). Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in the level of serotonin, which, by activation of vagal afferent fibers containing 5-HTs receptors, causes a vomiting reflex. Selectively blocks serotonin 5-HTZ receptors of neurons of the central and peripheral nervous system, n.vagus in the intestine and in the centers of the central nervous system (mainly the bottom of the IV ventricle), which regulate the exercise of vomitive reflexes. Does not disrupt the coordination of movements, does not cause sedation and reduced efficiency. It has anxiolytic activity.Does not change the concentration of prolactin in the plasma.

    Pharmacokinetics:

    After intramuscular injection, the time to reach the peak concentration in plasma (Tcmax) - 10 min. The volume of distribution is 140 liters. The connection with plasma proteins is 70-76%. After parenteral administration, the elimination half-life (T1 /2) is 3 hours. The absence of an enzyme CYP2D6 (debrisoquine polymorphism) 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 with its repeated administration.

    In patients with moderate renal insufficiency (creatinine clearance 15-60 ml / min), both systemic clearance and volume of distribution are reduced, resulting in a small and clinically insignificant increase T1 / 2. The pharmacokinetics of ondansetron practically does not change in patients with severe renal dysfunction in chronic hemodialysis (studies were conducted in between hemodialysis sessions). In patients with severe impairment of liver function, the systemic clearance of ondansetron is sharply reduced,as a result of which the half-life of it increases to 15-20 hours.1/2 ondansetron does not depend on the mode of administration. In elderly patients after parenteral administration of T1/2 can increase up to 5 hours.

    Indications:

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

    prevention and relief of nausea and vomiting in the postoperative period.
    Contraindications:

    -increased sensitivity to ondansetron or other components of the drug.

    -pregnancy and the period of breastfeeding.

    -children under 2 years old

    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 adults The daily dose is 8-32 mg / day, the following regimens are recommended. With moderately-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, 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, as a 15-minute infusion, immediately before the start of chemotherapy.

    The efficacy of Odansetron can be increased by a single intravenous injection of glucocorticosteroids (eg, 20 mg dexamethasone) prior to chemotherapy.

    To prevent delayed vomiting that occurs 24 hours after the onset of chemo- or radiotherapy - both with the use of high-emetogenic therapy, and with moderate-emetogenic therapy - it is recommended to continue using the drug inside as tablets at 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 / m2 the surface of the body intravenously, immediately before the start of chemotherapy, followed by ingestion of 4 mg after 12 hours; treatment is recommended to continue at a dose of 4 mg 2 times a day inside 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.

    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 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.

    In 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 impaired renal function

    Change the usual daily dose and the 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% 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, constipation or diarrhea, sometimes an asymptomatic transient increase in serum aminotransferase activity. From 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: hyperemia, pain, burning at the injection site.

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

    Overdose:

    In the event of an alleged overdose, symptomatic therapy is indicated. The specific antidote is not known.In case of an overdose of ondansetron, the use of ipecacuanas is not recommended, as it is unlikely that this drug will be effective during the antiemetic activity of ondansetron.

    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 (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 (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-HT3 receptor blockers have an increased risk of developing them against ondansetron. Ondansetron can slow the motility of the large intestine, in connection with which its appointment to patients with signs of an obstruction of the intestine requires special observation.

    Safety of ondansetron during pregnancy is not established.

    The infusion solution is prepared immediately before use. If necessary, it can be stored for 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 of 4 mg / 2 ml or 8 mg / 4 ml (2 mg / ml).


    Packaging:For 5 or 10 ampoules in contour cell packs from a polyvinyl chloride film. For 1 or 2 contour pack together with instructions for medical use in a cardboard box.
    Storage conditions:In the dark place at a temperature of no higher than 30 ° C. Keep out of the reach of children.
    Shelf life:

    3 years.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LSR-003484/09
    Date of registration:08.05.2009
    The owner of the registration certificate:ESKOM NPK, OAO ESKOM NPK, OAO Russia
    Manufacturer: & nbsp
    Representation: & nbspESKOM NPK, OAOESKOM NPK, OAO
    Information update date: & nbsp30.06.2011
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