Active substancePalonosetronPalonosetron
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  • Onitsit®
    solution in / in 
  • Dosage form: & nbspsolution for intravenous administration
    Composition:

    AT 1 ml of solution contains:

    active substance: palonosetron hydrochloride (in terms of palonosetron) 0.05 mg;

    Excipients: mannitol 41.5 mg; disodium edetate dihydrate 0.5 mg; sodium citrate dihydrate 3.7 mg; citric acid monohydrate 1.56 mg; sodium hydroxide solution and / or hydrochloric acid solution to pH = 5.0 ± 0.5; water for injection up to 1,0 ml.

    Description:Clear, colorless solution without foreign particles.
    Pharmacotherapeutic group:An antiemetic, a serotonin receptor antagonist
    ATX: & nbsp

    A.04.A.A   Antagonists of serotonin 5HT3 receptors

    A.04.A.A.05   Palonosetron

    Pharmacodynamics:Onicit® (palonosetron) - highly selective serotonin receptor antagonist. The mechanism of action is associated with the suppression of the emetic reflex by blockade of serotonin 5HT3receptors at the level of neurons of the central and peripheral nervous system. This mechanism is based on the prevention and treatment of nausea and vomiting caused by cytotoxic chemotherapy and radiotherapy associated with an increase in the serotonin content, which by activation of vagal afferents containing 5HT3-receptors of fibers cause a vomiting reflex.Onitsit® does not inhibit or stimulate cytochrome isoenzymes R450.
    Pharmacokinetics:

    When administered intravenously at the recommended doses in the blood plasma, the concentration of the drug slowly decreases by elimination from the body. The half-distribution period is 40 hours, the average plasma concentration is usually proportional to the applied dose.

    Palonosetron is well distributed in tissues. The volume of distribution is 6.9-7.9 l / kg. Binding to blood plasma proteins - 62 %.

    The drug is excreted by the kidneys, approximately 50% in the form of metabolites, the activity of which is less than 1% of the activity of palonosetron.

    So, PAfter a single intravenous introducedof palonosetron at a dose of 10 μg / kg, approximately 80% of the drug is found in the urine for 144 hours.

    After a single bolus administration, the total clearance is 173 ± 73 ml / min, the renal clearance is 53 ± 29 ml / min and the half-life can be more than 100 hours (10% of patients).

    Pharmacokinetics in different patient groups.

    Patients with renal insufficiency.

    Correction of the dose in patients with renal insufficiency is not required.

    Patients with hepatic insufficiency.

    Dose adjustment in patients with hepatic insufficiency is not required.

    Children.

    Data on the use of the drug in children under 18 years are absent.

    Patients of advanced age.

    Correction of dose in elderly patients is not required.

    Indications:

    Prevention and elimination of nausea and vomiting caused by conduction cytostatic chemotherapy or radiotherapy (moderately and highly emetic).

    Contraindications:

    - Hypersensitivity to palonosetron, or to other components of the drug;

    - Children under 18 years;

    - Pregnancy and lactation.

    Carefully:It should be used with caution in patients with a tendency to increase the interval QT.
    Dosing and Administration:

    The drug Onitsit® is administered intravenously for at least 30 seconds at a dose of 0.25 mg approximately 30 minutes before the start of chemotherapy.

    Do not administer the drug for the next seven days.

    The effect of the drug on preventing nausea and vomiting caused by chemotherapy increases with the simultaneous administration of glucocorticosteroids.

    Side effects:

    The incidence of adverse reactions listed below was determined by the following criteria: very often (not less than 1/10), often (more than 1/100, less than 1/10); infrequently (more 1/1000, less than 1/100); rarely (more than 1/10000, less than 1/1000); very rarely (less than 1/10000), including individual messages.

    The most common adverse reactions: headache - up to 9%; constipation - up to 5%.

    Infrequently observed adverse reactions:

    from the cardiovascular system: tachycardia, bradycardia, extrasystoles, myocardial ischemia, sinus tachycardia, sinus arrhythmia, supraventricular extrasystoles, lowering of blood pressure (BP), increased blood pressure, lengthening of the interval QT, varicose veins, varicose veins veins;

    from the nervous system: headache, dizziness, drowsiness, insomnia, paresthesia, peripheral sensory neuropathy, anxiety, euphoria;

    from the digestive system: constipation, diarrhea, abdominal pain dry mucosa membranes of the mouth, flatulence, anorexia, hiccough;

    with the side of the urinary system: retention of urine;

    from the skin and skin appendages: allergic dermatitis, itching, rash;

    from the musculoskeletal system: arthralgia;

    from the senses: increased sensitivity of the eyes - irritation, diplopia, amblyopia, impaired coordination of movements, tinnitus;

    change laboratory indicators: increased activity of "hepatic" transaminase, hypo- or hyperkalemia, hypocalcemia, hyperglycemia, hyperbilirubinemia, glucosuria, metabolic acidosis;

    Other: increased fatigue, weakness, increased body temperature, hot flashes - a feeling of "heat", flu-like syndrome.

    Very rare reactions occur at the injection site (burning, tightening, pain).

    Overdose:

    Until now, there have been no cases of overdose, however, if any of these side effects increase, symptomatic therapy is necessary.

    Interaction:

    Palonosetron is mainly metabolized by isoenzyme CYP2D6, with the participation of isoenzymes CYP3A4 and CYP1A2. In the concentrations used palonosetron Does not inhibit or stimulate the formation of cytochrome R450.

    Metoclopramide: in clinical studies, there was no interaction of palonosetron with metoclopramide, which is an inhibitor of the isoenzyme CYP2D6.

    Inhibitors and inducers of isoenzyme CYP2D6: possibly combined use with dexamethasone and rifampicin (isoenzyme inducers CYP2D6), and amiodarone, tauxoxib, chlorpromazine, cimetidine, doxorubicin, fluoxetine, haloperidol, paroxetine, quinidine, ranitidine, ritonavir, sertraline and terbinafine (isoenzyme inhibitors CYP2D6).

    Glucocorticosteroids: joint use with glucocorticosteroids is safe.

    Other medicines: it is possible to use together with analgesics, antispasmodic, anticholinergic drugs, other antiemetics.

    Antineoplastic agents: palonosetron does not reduce the activity of antitumor drugs (cisplatin, cyclophosphamide, cytarabine, doxorubicin, mitomycin).

    Special instructions:Onitsit® can cause an increase in the time of passage of the contents through the intestine. Therefore, special control of the condition of patients with signs of intestinal obstruction is required.
    Effect on the ability to drive transp. cf. and fur:

    Since the use of Onitsit® can cause undesirable effects such as dizziness, drowsiness, increased fatigue, with driving car and other potentially dangerous activities that require increased concentration and speed of psychomotor reactions, care must be taken.

    Form release / dosage:

    Solution for intravenous administration 0.25 mg / 5 ml.

    Packaging:

    For 5 ml of the solution in a vial of transparent glass, ukuporenny rubber stopper with aluminum obakkoy and protective cap.

    1 bottle with the instruction for use is placed in a cardboard box.

    Storage conditions:

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

    Keep out of the reach of children!

    Shelf life:

    5 years.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:PL-000716
    Date of registration:29.09.2011
    Expiration Date:29.09.2016
    The owner of the registration certificate:Helsins Bayrex Pharmaceuticals Ltd.Helsins Bayrex Pharmaceuticals Ltd. Ireland
    Manufacturer: & nbsp
    Representation: & nbspCBS CJSC LTDCBS CJSC LTDItaly
    Information update date: & nbsp07.06.2017
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