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

    1 ampoule solution contains:

    active substance: ondansetron 8 mg (equivalent to 10.00 mg ondansetron hydrochloride dihydrate);

    Excipients: sodium citrate - 1.60 mg, citric acid monohydrate - 2.20 mg, sorbitol - 192.00 mg, water for injection - up to 4.00 ml.

    Description:

    transparent, colorless or almost colorless solution.

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

    A.04.A.A.01   Ondansetron

    Pharmacodynamics:

    Ondansetron is a selective antagonist of serotonin 5-HTZ receptors.

    - Medicines for cytostatic chemotherapy and radiotherapy can cause

    g

    an increase in serotonin concentration, which, by activating the afferent fibers of the vagus nerve, containing 5-HT3 receptors, causes a vomiting reflex. Selective


    blocks serotonin 5-HTZ receptors of central neurons (vomiting center) and peripheral (gastrointestinal tract) of the nervous system that regulates the gag reflex. Does not disrupt 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, peak plasma concentrations are achieved within 10 minutes. The distribution of 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 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 were 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, which are on chronic hemodialysis. In patients with severe impairment of liver function, the systemic clearance of ondansetron drastically decreases, which increases the half-life of the liver (up to 15-32 h).

    Indications:

    • Preventing and arresting nausea and vomiting caused by cytotoxic chemotherapy or radiotherapy.
    • Prevention and relief of nausea and vomiting in the postoperative period.

    Contraindications:

    - Hypersensitivity to any component of the drug.

    - Pregnancy and lactation.

    - Children under 2 years.

    Pregnancy and lactation:it is contraindicated.
    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 corresponding infusion solution, as a 15-

    minute infusion, immediately before the start of chemotherapy.

    The efficacy of ondansetron 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.

    Patents of elderly growth Dosage adjustments are not required.

    Patents with impaired renal function

    Change the usual daily dose and the frequency of administration of the drug is not required.

    Patients with a violation of liver 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:

    Currently, there is not enough information about an overdose of ondansetron. The most frequent symptoms that are noted in patients with overdose ondansetron: visual impairment, constipation, lowering of arterial pressure, vasovagal reaction with transient atrioventicular blockade of the II degree. All symptoms are completely reversible.

    Treatment: conduct symptomatic and supportive therapy, a 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 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

    medicinal products:

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

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

    concentrations may cause ondansetron precipitation);

    - 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,

    5 6 2 9 1

    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 intestinal obstruction 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.

    Effect on the ability to drive transp. cf. and fur:

    In case of adverse reactions from the nervous system, patients are advised to refrain from controlling the car and other mechanisms, as well as activities that require concentration of attention, stress - psychomotor functions

    Form release / dosage:

    Solution for intravenous and intramuscular injection, 2 mg / ml: 4 ml solution in colorless glass ampoules.

    Packaging:For 5 ampoules in a cardboard box with instructions for use.
    Storage conditions:

    Store in a dark place at a temperature of 15 to 30 ° C.

    Keep out of the reach of children!

    Shelf life:

    4 years.

    Do not use after expiry date.

    Terms of leave from pharmacies:On prescription
    Registration number:П N012102 / 02
    Date of registration:21.06.2010
    The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary
    Manufacturer: & nbsp
    Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary
    Information update date: & nbsp22.06.2015
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