Tropindole® (Tropindol®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
Read on
Active substanceTropisetronTropisetron
Similar drugsTo uncover
  • Tropindole®
    capsules inwards 
    VEROPHARM SA     Russia
  • Tropindole®
    solution in / in 
    LENS-PHARM, LLC     Russia
    • Dosage form: & nbspcapsules
    Composition:Active substance - tropindole hydrochloride in terms of tropindole 5 mg.
    Excipients: lactose, corn starch, povidone, talc, calcium stearate.
    Description:Hard gelatin capsules No. 4 in white. Contents of capsules - a mixture of powder and granules white or white with a creamy shade of color.
    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 potent and highly selective competitive antagonist of central and peripheral 5-HT3receptors. Effectively prevents and eliminates the nausea and vomiting that occur during antitumor chemotherapy and in the postoperative period. The mechanism of antiemetic action of troposetron is based on the blockade of peripheral presynaptic 5-HT3receptors. which prevents the release of serotonin from enterochromaffin cells of the gastrointestinal mucosa. Tropisetron, in addition, has a direct blocking effect on 5-HT3-receptors located in the central nervous system, including in area postrema, thereby blocking the effect of the vagus nerve on this region.

    The duration of action of Tropindole is 24 hours, which allows it to be applied once a day. The effectiveness of the drug persists for multiple cycles of chemotherapy. Tropindole does not cause extrapyramidal side effects.

    Pharmacokinetics:

    Suction. Tropindole is absorbed from the gastrointestinal tract almost completely (more than 95%). The half-life period averages about 20 minutes; the time to reach the maximum concentration is about 3 hours. The bioavailability of the drug is about 60% for a dose of 5 mg. With increasing dose, bioavailability increases, reaching almost 100% for a dose of 45 mg.

    Distribution. Nonspecific binding of tropospira to plasma proteins (predominantly with alpha-1-glycoproteins) is 71%. The volume of distribution in adults ranges from 400 to 600 liters; in children aged 3 to 6 years - about 145 liters. in children aged 7 to 15 years - about 265 liters.

    Metabolism. Tropisetron metabolized in the liver by hydroxylation reactions followed by glucuronation or sulfation. Metabolites are pharmacologically inactive.At repeated appointments of Tropindol in doses exceeding the therapeutic dose (10 mg twice a day), a dose-dependent increase in tropisetron levels in the plasma is possible due to a decrease in its metabolism associated with saturation of the enzyme system of the liver. However, if the recommended dosage regimen is followed, the concentrations of the drug in the plasma do not exceed the tolerable values.
    Metabolism of tropisetron has a connection with the genetically determined polymorphism of sparteine ​​/ debrisoquine.

    Excretion. Tropisetron is excreted primarily by the kidneys - 70% (in the form of metabolites) and 8% (unchanged), through the intestine - 15% (in the form of metabolites). The proportion of unchanged drug in urine is higher in "slow oxidants." The ratio of metabolites in urine and feces is 5: 1. In persons with fast metabolism of tropospira ("fast oxidizers"), the half-life (beta-phase) is about 8 hours, slow oxidizers ", this index can be extended to 45 hours. The total clearance of troposetron is about 1 L / min, while the renal clearance is about 10% of this value. In" slow oxidants "the total clitoris is reduced to 0.1-0.2 l / min (due to reduction of the out-of-card clearance),which leads to a 4-5-fold elongation of the half-life and to a 5-7-fold increase in the values AUC, while such indicators as the maximum concentration and volume of distribution do not change.

    Have children The values ​​of such indicators as bioavailability and the final half-life are similar to those of adult healthy volunteers.

    Indications:

    - Prevention of nausea and vomiting due to antitumor chemotherapy;

    - Elimination of nausea and vomiting that occur in the postoperative period;

    - Prevention of nausea and vomiting that occur after gynecological intra-abdominal surgery.

    Contraindications:

    Hypersensitivity to troprissetron, other antagonists of 5-HT3-receptors or any other components that make up the drug.

    Tropindole should not be used during pregnancy and lactation.

    Carefully:Arterial hypertension.
    Pregnancy and lactation:

    Tropindole should not be administered during pregnancy, as its use in this contingent of patients has not been studied.

    It is not known whether the blood is excreted tropospheric in breast milk in humans, so patients taking Tropindol should not breast-feed.

    Dosing and Administration:

    Prevention of nausea and vomiting due to antitumor chemotherapy

    Children. In children older than 2 years, the recommended dose of Tropindol is 0.2 mg / kg, with a maximum daily dose of 5 mg.

    Adults. Adults tropindol recommended in the form of 6-day courses of 5 mg / day. Capsules should be taken in the morning, washed down with water, immediately after getting up, 1 hour before meals.

    Side effects:

    When the drug is used in recommended doses, the undesirable effects are transitory. When using Tropindol in a dose of 2 mg, the most common reported development of headache. When using the drug at a dose of 5 mg, constipation was often noted and less often - dizziness, increased fatigue and disorders of the gastrointestinal tract (abdominal pain and diarrhea).

    As with other 5-HT antagonists3-receptors, hypersensitivity reactions were rarely observed ("reactions Itype "), characterized by one or more of the following symptoms: a sense of blood flow to the face and / orgeneralized urticaria, a feeling of heaviness behind the sternum, shortness of breath, acutely developing bronchospasm, arterial hypotension.

    Very rare cases of collapse, fainting, or cardiac arrest have been reported, but the causal relationship of these phenomena with the use of Tropindol has not been established. Some of them could be caused by concomitant therapy or a major disease.

    Interaction:

    Taking the capsule of the drug along with food results in a slight increase in bioavailability of troposis terone (approximately from 60% to 80%), which is not clinically relevant.

    The simultaneous use of tropindole with rifampicin or with other drugs inducing enzyme systems of the liver (for example, with phenobarbital), leads to a decrease in concentrations of tropospira in plasma. Therefore, patients who are "fast oxidants" need to increase the dose of Tropindol ("slow oxidizers" do not need this). The effect of drugs inhibiting the enzymatic system of cytochrome P450, for example, cimetidine, on the concentration of troposetron in the plasma is negligible, so there is no need to change the dosage of Tropindole in such cases.

    Studies of the interaction of Tropindol with funds for anesthesia have not been conducted.

    Interval lengthening QTc was noted in several patients who received tropindole in combination with drugs that elongated this interval. At the same time, in those studies where only one Tropindole was used in therapeutic doses, the lengthening of the interval QTc was not noted. Nevertheless, caution should be exercised with the simultaneous use of tropindol and drugs that cause lengthening of the interval QTc.

    Special instructions:

    Use in persons belonging to the category of "slow oxidizers" sparteine ​​/ debrisoquine

    In patients belonging to this category (they constitute about 8% of the population of Caucasians), the half-life of tropospheric is longer (4-5 times, compared with those who metabolize sparteine ​​/ debrisoquine intensively). However, with intravenous administration of Tropindol twice a day at doses up to 40 mg for 7 days, healthy volunteers, classified as "slow oxidants," did not observe serious adverse events. These observations indicate that in the 6-day course of treatment of patients,in the category of "slow oxidants", there is no need to reduce the usual daily dose of the drug of 5 mg.

    Use in patients with impaired liver function or kidney function

    Patients with acute hepatitis or fatty liver dystrophy have no change in the pharmacokinetics of tropospitron. In contrast, in patients with cirrhosis of the liver or impaired renal function, concentrations of tropospheric in plasma may exceed (as much as 50 %) those indices that are detected in healthy volunteers belonging to the group intensively metabolizing sparteine ​​/ debrisoquine. Nevertheless, if such patients are prescribed in the form of recommended 6-day courses of 5 mg / day, no dose reduction is required.

    Use in patients with arterial hypertension

    In patients with uncontrolled hypertension should be avoided Tropindola at daily doses exceeding 10 mg, as this may lead to a further increase in blood pressure.

    Use in patients with heart disease

    Care should be taken in patients with heart rhythm and conduction disorders, as well as in patients,which is treated with antiarrhythmic drugs or beta-blockers, since the available experience of simultaneous use and funds for anesthesia in such cases is limited.

    Use in children

    It was noted that in children older than 2 years tolerance of Tropindol was good.

    Use in elderly patients

    There is no evidence that older patients (in comparison with younger patients) require the use of other doses of Tropindol, or that. that they may experience any other adverse reactions.

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

    Data on the influence of Tropindol on the ability to drive a car is not available. It is necessary to take into account the existence of such side effects as dizziness and fatigue.

    Form release / dosage:Capsules to 0,005 g.
    Packaging:

    For 5 or 10 capsules in a contour mesh package. For 5 or 10 capsules in a jar of orange glass. Each jar or 1 circuit cell pack together with instructions for use in the pack.

    Storage conditions:

    List B. In a dry, protected from light and inaccessible to children place.

    Shelf life:

    2 years.

    Terms of leave from pharmacies:On prescription
    Registration number:P N002673 / 01
    Date of registration:10.09.2008
    The owner of the registration certificate:VEROPHARM SA VEROPHARM SA Russia
    Manufacturer: & nbsp
    Information update date: & nbsp24.10.2015
    Illustrated instructions
      Instructions
      Up