Active substanceOndansetronOndansetron
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  • Dosage form: & nbsp

    - solution for intravenous and intramuscular injection

    - film coated tablets

    Composition:
    1 ml of solution contains: active substance: ondansetron 2.0 mg (as ondansetron hydrochloride dihydrate). auxiliary substances: citric acid anhydrous - 0.46 mg, trisodium citrate dihydrate - 0.33 mg, sodium chloride - 8.3 mg, water for injection - q.s.

    1 tablet film-coated 4 mg contains: active substance: ondansetron 4.0 mg (as ondansetron hydrochloride dihydrate). Excipients: microcrystalline cellulose - 22.0 mg, starch - 15.5 mg, lactose - 47.0 mg, magnesium stearate - 0.5 mg, hypromellose - 2.07 mg. shell: titanium dioxide 0.77 mg, talc 0.43 mg, propylene glycol 0.36 mg.

    Description:

    Solution: clear, colorless solution.

    Tablets of 4 mg: white or almost white, round, biconvex tablets, covered with a film sheath, with a squashed "4" on one side.

    Tablets of 8 mg: white or almost white, round, biconvex tablets, covered with a film shell, with a squashed "8" on one side and a fault line on the other.

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

    A.04.A.A.01   Ondansetron

    Pharmacodynamics:

    Ondansetron is a selective antagonist of the 5HT3 (serotonin) receptor.Drugs 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 postoperative and induced by cytostatic chemotherapy and radiotherapy of 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. Binding to plasma proteins is. 70- 76%. Unchanged in the form of unchanged, less than 5% of the drug is excreted.

    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 radiotherapy, as well as 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: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 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, just before the start of chemotherapy.

    The effectiveness of Ameset® can be increased by a single intravenous injection of a glucocorticosteroid (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 in the same part of the body, Emeset® can be administered at a dose not exceeding 4 mg!

    Children To prevent postoperative nausea and vomiting, Emeset® is used exclusively parenterally in 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 renal lesions.

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

    With liver damage Ameset's clearance is significantly reduced, and the half-life of it is increased from the plasma, therefore, the daily dose of 8 mg should not be exceeded.

    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.

    In case of an overdose of Emeset® tablets, it is not recommended that ipecacuanas be used, since it is unlikely that this drug will be effective during the antiemetic activity of ondansetron.

    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, nitrous 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 have previously experienced other hypersensitivity reactions with other selective 5HT3 receptor antagonists, similar reactions may occur with the use of Emeseta.

    As ondansetron 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:Tablets coated with a film coat of 4 mg and 8 mg.
    Packaging:

    Solution for intravenous and intramuscular injection 2 mg / ml. At 4 mg / 2 ml in ampoules with a blue line and 8 mg / 4 ml in ampoules with a red line.

    For 5 ampoules in a plastic pallet along with instructions for use in a cardboard bundle.

    Tablets coated with a film coat of 4 mg and 8 mg.

    For 6 tablets in a strip from AL / AL. 1 strip with instructions for use in a cardboard bundle. For 10 packs in a cardboard box.

    Storage conditions:

    Tablets, film-coated, stored at a temperature of no higher than 25 ° C in a dark place.

    The solution for intravenous and intramuscular administration should be stored at a temperature of no higher than 30 ° C in a dark place. Keep out of the reach of children.
    Shelf life:

    The solution for intravenous and intramuscular injection is 3 years.

    The tablets covered with a film cover - 3 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:П N013675 / 01
    Date of registration:18.09.2008
    The owner of the registration certificate:Cipla Ltd.Cipla Ltd. India
    Manufacturer: & nbsp
    Information update date: & nbsp01.07.2011
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