Tropisetron - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Antiemetic drugs

Serotonergic agents

Included in the formulation

Tropindole®

capsules inwards

VEROPHARM SA Russia

Tropindole®

solution in / in

LENS-PHARM, LLC Russia

АТХ:

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

A.04.A.A.03 Tropisetron

Pharmacodynamics:

Selective blockade of serotonin 5-HT₃receptors, peripheral receptors (nervous end of the vagus nerve in the intestine) and neurons of the central nervous system (in the bottom of the IV ventricle) that regulate the gag reflex.

Pharmacokinetics:

Absorption is dose-dependent, in a dose of 45 mg almost 100%. Connection with blood plasma proteins - 70%. Biotransformation in the liver with the participation of the cytochrome P450 system with the formation of inactive metabolites. Half-life is 8 h, for slow acetylates increases 4-5 times. Elimination by the kidneys (8% unchanged, 70% in the form of metabolites) and with feces 15% (in the form of metabolites).

Indications:

Prevention and treatment of nausea and vomiting that occur during antitumor chemotherapy.
Prevention and treatment of postoperative nausea and vomiting.

ICD-10

XVIII.R10-R19.R11 Nausea and vomiting

XXI.Z40-Z54.Z51.1 Chemotherapy for neoplasm

Contraindications:

Hypersensitivity, pregnancy (with the exception of cases to prevent postoperative nausea and vomiting during medical abortion), breast-feeding, children's age (up to 2 years).

Carefully:

Arterial hypertension.Patients with uncontrolled hypertension should avoid the use of a dose of more than 10 mg per day.

Pregnancy and lactation:

Adequate and well-controlled studies in humans and animals have not been conducted. There is no information on the penetration into breast milk. Do not apply!

Dosing and Administration:

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

Prevention of nausea and vomiting arising from antitumor chemotherapy.

Children. The recommended dose for children older than 2 years is 0.2 mg / kg; the maximum daily dose is 5 mg. On the first day in a short period of time before the application of antitumor chemotherapy, the drug is administered intravenously. On the 2nd to the 6th day, the drug is administered orally, in a dose of 0.2 mg / kg; the maximum daily dose is 5 mg.

Adults. Adults are recommended to prescribe the drug in the form of 6-day courses at a dose of 5 mg per day. On the first day, the drug is administered intravenously for a short period of time before the use of antitumor chemotherapy. From the 2nd to the 6th day, the drug is administered orally.

If a satisfactory antiemetic effect is not achieved with the use of troposetron, dexamethosone can additionally be prescribed to achieve a clinical effect.

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

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

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 was also observed, and less often - dizziness, fatigue, abdominal pain, diarrhea.

Allergic reactions ("tide" of blood to the skin of the face, urticaria, a sense of heaviness behind the sternum, shortness of breath, bronchospasm) were rare in the use of troposetron, very rarely - collapse, fainting, cardiac arrest (cause and effect with troposetron application not established).

Overdose:

Symptoms: visual hallucinations, in patients with prior arterial hypertension - increased blood pressure.

Treatment: symptomatic.

Interaction:

Antiarrhythmic drugs, β-blockers - it is possible to increase the QT interval, apply with caution.

Barbiturates, rifampicin, tricyclic antidepressants, phenylbutazone, phenytoin, ethanol (inducers of microsomal oxidation) - a decrease in the concentration of tropospheric in plasma (dose adjustment is required).

Dexamethasone is an increase in troposetron effectiveness.

Inhibitors of microsomal oxidation - an increase in the concentration of tropisetron in plasma (dose adjustment is not required).

Special instructions:

Granisetron is more effective than tropositrone when used to treat and prevent nausea and vomiting caused by chemotherapy in children.

Granisetron, ondansetron and tropospheric are equally effective in the use for the prevention and treatment of nausea and vomiting during chemotherapy.

During the treatment period, care must be taken when driving vehicles, working with complex mechanisms and engaging in any potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Caution should be exercised while simultaneously applying funds for general anesthesia in patients with heart rhythm disorders and conduction in the background of treatment with antiarrhythmics and β-blockers.

Instructions

Tropisetron (Tropisetronum)