Active substanceOndansetronOndansetron
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  • Dosage form: & nbsp

    film-coated tablets

    Composition:

    1 A film coated tablet contains:

    active substance: ondansetron hydrochloride dihydrate in terms of ondansetron - 4 mg and 8 mg;

    Excipients: lactose (milk sugar), cellulose microcrystalline, potato starch, povidone (polyvinylpyrrolidone), silicon dioxide colloid (aerosil), magnesium stearate;

    composition of the shell: hypromellose (hydroxypropylmethyl cellulose), povidone (polyvinylpyrrolidone), polysorbate (tween-80), titanium dioxide, dye azorubin or cantoxanthine.

    Description:

    The tablets covered with a film cover, light pink color, round, biconcave. On the cross-section, two layers are visible, the outer layer is light pink, the inner layer is white or almost white.

    Pharmacotherapeutic group:An antiemetic, a serotonin receptor antagonist
    ATX: & nbsp

    A.04.A.A.01   Ondansetron

    Pharmacodynamics:

    Ondansetron is a selective antagonist of 5-HTZ receptors (serotonin). Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in the level of serotonin, which, by activating vagal afferent fibers containing 5-HTZ receptors, causes a vomiting reflex.Selectively blocks serotonin 5-HT3 receptors of neurons of the central and peripheral nervous system, endings 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 oral administration, the maximum concentration (TСmах) ondansetron in the blood plasma is achieved after about 1.5 hours. The binding to plasma proteins is. 70-76%. The volume of distribution is 140 liters. Half-life (T1/2) is 3 hours, in elderly patients can reach 5 hours, and with severe hepatic insufficiency, 15-20 hours. Absence of enzyme CYP2D6 does not affect the pharmacokinetics of ondansetron. Unchanged in the urine is displayed less 5% of the administered dose. 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 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.

    Indications:

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

    - prevention and relief of nausea and vomiting in the postoperative period.

    Contraindications:

    - hypersensitivity to ondansetron or other components of the drug;

    - pregnancy and the period of breastfeeding;

    - Children's age up to 3 years (for this dosage form).

    Pregnancy and lactation:Safety of ondansetron during pregnancy is not established.
    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 daily dose, as a rule, is 8-32 mg, the following regimens are recommended:

    With moderately-emetogenic chemotherapy or radiotherapy:

    8 mg ondansetron inside for 1-2 hours before the start of the main therapy with subsequent 8 mg orally through 12 h.

    With highly emeticogenic chemotherapy:

    The recommended dose of ondansetron is 24 mg concurrently with dexamethasone inside at a dose 12 mg for 1-2 hours before the start of chemotherapy.

    To prevent late or prolonged vomiting that occurs after 24 hours, continue taking ondansetron in a dose 8 mg twice daily for 5 days.

    Children

    Children older than 3 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 prescribe 16 mg orally 1 hour before the onset of general anesthesia.

    Children to prevent postoperative nausea and vomiting ondansetron is used exclusively parenterally.

    Patients of elderly growth

    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 violations of liver function, the clearance of ondansetron significantly decreases,This increases the half-life of it from the plasma, so it is not recommended for such patients to prescribe more 8 mg ondansetron per day.

    Side effects:
    Allergic reactions: urticaria, bronchospasm, laryngospasm, angioedema edema, anaphylaxis.

    From the digestive system: hiccough, dry mouth, diarrhea, constipation, asymptomatic transient increase in aminotransferases in blood serum.

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

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

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

    Overdose:In cases of suspected overdose, symptomatic therapy is indicated. The specific antidote is unknown. 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, glutetimide, griseofulvin, dinitrogen 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, estrogen-containing oral contraceptives, diltiazem, disulfiram, valproic acid and its salts, erythromycin, fluconazole, fluoroquinolones, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil.

    Special instructions:

    Patients who had previously had allergic reactions to other selective 5HT3 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 regular monitoring.

    Form release / dosage:

    Tablets, film-coated, 4 mg and 8 mg.

    Packaging:By 5, 6 or 10 tablets in a planar cell pack. For 10 tablets in a jar or bottle of polymer materials. Each bank or bottle, or 1 contour squamous packaging together with instructions for use in a pack of cardboard.
    Storage conditions:

    Store at a temperature not higher than 30 ° C. Keep out of the reach of children!

    Shelf life:

    3 of the year.

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

    Terms of leave from pharmacies:On prescription
    Registration number:P N002944 / 01
    Date of registration:14.08.2008 / 08.10.2015
    Expiration Date:Unlimited
    The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia
    Manufacturer: & nbsp
    Information update date: & nbsp01.02.2017
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