Tropindole® (Tropindol®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceTropisetronTropisetron
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  • Tropindole®
    capsules inwards 
    VEROPHARM SA     Russia
  • Tropindole®
    solution in / in 
    LENS-PHARM, LLC     Russia
    • Dosage form: & nbspsolution for intravenous administration
    Composition:

    Active substance:

    Tropisetron hydrochloride in terms of troposetron or Tropindol® (Tropisetron) 1.00 mg

    Excipients:

    Sodium citrate 4.30 mg

    Citric acid monohydrate 2.25 mg

    Water for injection up to 1.0 ml
    Description:

    Transparent colorless liquid.

    Pharmacotherapeutic group:antiemetics - serotonin receptor antagonist
    ATX: & nbsp

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

    A.04.A.A.03   Tropisetron

    Pharmacodynamics:

    Tropisetron is a highly selective competitive antagonist of 5-HT3receptors (a subclass of receptors for serotonin) located on peripheral neurons and in the central nervous system. Some chemotherapeutic agents can promote the release of serotonin (5-HT) from enterochromaffin-like cells located in the mucous membrane of the gastrointestinal tract (GIT), which contributes to the development of a vomiting reflex and nausea. Tropisetron selectively blocks excitation of presynaptic 5-HT3-receptors on peripheral neurons taking part in the onset of this reflex, and may also have an additional direct effect on 5-HT3-receptors located in the central nervous system and mediating the influence of the vagus nerve on area postrema. It is believed that these effects are the basis of the anti-emetic mechanism of troposetron.

    The duration of the action of troposetron is 24 hours, which allows one to use it once a day. Does not cause extrapyramidal disorders. When carrying out repeated courses, the effectiveness is maintained.

    Pharmacokinetics:The connection with plasma proteins (mainly with a-glycoproteins) is 70%. Metabolism of tropospeter is carried out mainly in the liver. Metabolites are inactive and practically do not participate in the realization of the pharmacological action of troposetron. The degree of metabolism varies depending on the individual characteristics of the patient, in particular with genetically determined polymorphism of sparteine ​​/ debrisoquine metabolism. In individuals with a high level of metabolism of troposetron, the elimination half-life is about 8 hours; at a slow metabolism, the half-life period is prolonged and can be 30-45 hours. The drug is excreted mainly by the kidneys (70% in the form of metabolites, about 8% unchanged), about 15% of the drug is metabolized through the intestine.

    Indications:

    - Prevention and treatment of nausea and vomiting that occur during antitumor chemotherapy;

    - Prevention and treatment of postoperative nausea and vomiting.

    Contraindications:

    Hypersensitivity to troprissetron, other 5-HT antagonists3-receptors or to other components of the drug.

    Pregnancy (with the exception of surgical interventions for medical abortion).

    Breastfeeding period

    Children up to 2 years.

    Carefully:Tropindole should be administered with caution in cases of concomitant use of anesthesia in patients with cardiac rhythm and conduction disorders, as well as with antiarrhythmic drugs or beta-blockers (the experience of simultaneous application of Tropindol and anesthesia in such cases is limited); with arterial hypertension.
    Dosing and Administration:

    Intravenous drip (for 15 minutes) or slowly struino (at least 1 minute).

    Prevention of nausea and vomiting due to antitumor chemotherapy

    On the first day, the drug is administered intravenously for a short time before the beginning of antitumor therapy to adults at a dose of 5 mg per day, to children at a dose of 0.2 mg / kg (maximum daily dose of 5 mg).In the next 5 days, to prevent delayed nausea and vomiting, Tropindol is administered orally (see instructions for use of Tropindol capsules).

    If a satisfactory antiemetic effect is not achieved with the application of Tropindole, in order to achieve a clinical effect, dexamethasone.

    Elimination and prevention of nausea and vomiting that occur in the postoperative period

    Adults tropindol recommended to use intravenously in a dose of 2 mg shortly before the onset of anesthesia.

    Rules for the preparation of a solution for infusions.

    The contents of one vial (5 mg / 5 ml) for intravenous infusion are diluted in 100 ml of a 0.9% solution of sodium chloride or 5 % solution of dextrose. With jet injection, if necessary, the contents of 1 bottle can be diluted in 15 ml of the above solutions.

    Side effects:

    When using the drug at a dose of 2 mg, the most common reported development of headache; in a dose of 5 mg, constipation and, less often, dizziness, fatigue, abdominal pain, diarrhea were also observed.

    Rarely with the use of tropositrone, there were allergic reactions ("tide" of blood to the skin of the face, hives, a feeling of heaviness behind the sternum, shortness of breath,bronchospasm), extremely rare - collapse, fainting, cardiac arrest (cause-and-effect relationship with the use of troposetron is not established).

    Overdose:

    In cases of repeated use of Tropindol in doses far exceeding therapeutic, visual hallucinations may occur; In patients with hypertension, blood pressure may increase.

    Treatment is symptomatic. A specific antidote to tropisetron is not known.

    Interaction:

    The simultaneous use of tropindole with phenytoin, ethanol, barbiturates, rifampicin, phenylbutazone, tricyclic antidepressants or other drugs that induce microsomal enzymes of the liver, leads to a decrease in its concentration in the plasma.

    Inhibitors of microsomal oxidation with simultaneous administration with tropindol slightly increase its concentration in plasma (correction of doses is not required).

    Special instructions:

    In persons with a low level of sparteine ​​/ debrisoquine metabolism, the half-life of tropospirae is elongated (4-5 times, compared to individuals with a high level of sparteine ​​/ debrisoquine metabolism).However, during the 6-day course of treatment of patients, classified as those with low-sparteine ​​metabolism / debrizohina, the need to reduce the usual dose formulation is 5 mg, does not arise.

    Patients with cirrhosis of the liver or renal function tropisetron concentration in plasma may increase, but the application tropisetron such patients as the recommended 6-day course in a dose of 5 mg / day, the drug dosing regimen correction is required.

    Some side effects of the drug, such as dizziness and fatigue can adversely affect driving ability and the performance of potentially hazardous activities that require high concentration and speed of psychomotor reactions
    Form release / dosage:Solution for intravenous administration.
    Packaging:

    Solution for intravenous administration of 5 mg / 5 ml (1 mg / ml) in vials. 1 bottle with instructions for use in a pack of cardboard. For 50, 85, 100 vials with instructions for use, based on one instruction for 10 bottles, in a box of cardboard (for hospitals).

    Storage conditions:In the dark place at a temperature of 5 to 25 ° C.
    Shelf life:

    2 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:P N001073 / 01
    Date of registration:09.02.2009
    The owner of the registration certificate:LENS-PHARM, LLC LENS-PHARM, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp24.10.2015
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