Tropisetron

General characteristics. Structure:

1 capsule contains a tropisetron of a hydrochloride in terms of 100% трописетрон - 0,005 g;
Excipients: lactoses monohydrate, starch corn, to silicon dioxide colloid anhydrous, to magnesium stearate.

Pharmacological properties:

Pharmacodynamics. Tropisetron represents the highly active selection competitive antagonist of peripheral and central serotoninovy 5-HT3 receptors. Blocking these receptors, трописетрон prevents emergence of the emetic reflex caused by reception of chemotherapeutic antineoplastic drugs which stimulate emission of serotonin from enterokhromaffinny cells in a mucous membrane of a digestive tract. Besides, трописетрон oppresses the central links
emetic reflex, blocking 5-HT3 - receptors in TsNS, in particular, in area postrema (a bottom of the IV ventricle).

Pharmacokinetics. After intake drug more than for 95% is soaked up from a digestive tract (the period of semi-absorption averages about 20 min.). The maximum concentration in blood is reached within 3 hours. Absolute bioavailability depends on a dose and reaches about 60% after reception of 5 mg, increasing to 100% after reception of 45 mg. Linkng with proteins of plasma makes 71%, distribution volume - 7,9 l/kg. Drug is metabolized in a liver by a hydroxylation with the subsequent conjugation with glucuronic or sulfuric acids and removed with urine or with bile. At persons, with undisturbed metabolism, the elimination half-life of a tropisetron makes 8 hours, at persons with a low speed of metabolism, the elimination half-life can increase to 43 h. The general clearance of a tropisetron makes about 1 l/min, about 10% are the share of renal clearance. It is brought out of an organism slowly.
At patients with the broken metabolism, the general clearance is reduced to 0,1 - 0,2 l/min at not changed renal clearance.

Indications to use:

Prevention of nausea and vomiting when carrying out antineoplastic chemotherapy and in the postoperative period (prevention and treatment).

Route of administration and doses:

It is applied inside. Tropisetron appoint courses for 5 days. To children the recommended dose is more senior than two years makes 0,2 mg/kg of body weight, the maximum dose - to 5 mg a day; scheme of treatment such: after preliminary intravenous drop or jet administration of injection solution of the drug administered in the first day of treatment (solution for injections, by 1 mg/ml, ampoules on 5 ml), in the next days (2 – the 6th is used) drug is accepted inside in capsules (contents of the capsule are mixed with orange juice or with drink like Coca). The daily dose for adults makes 5 mg. Capsules are appointed from the 2nd to the 6th day after preliminary intravenous drop or jet administration of injection solution of the drug administered in the first day of treatment (solution for injections, by 1 mg/ml, ampoules on 5 ml is used). Capsules should be accepted in the morning, directly after awakening or for an hour till a breakfast, washing down with water. With the lowered ability to metabolism reduction of a standard daily dose is not required from persons. Duration of action of Tropisetron makes 24 h that allows to apply it once a day. Purpose of drug throughout multiple cycles of chemotherapy does not influence its efficiency. The wide therapeutic index of Tropisetron causes lack of need for change of a dose at patients of advanced age, at persons with disturbance of functions of a liver or kidneys.

Features of use:

Patients with uncontrollable arterial hypertension need to avoid purpose of the daily doses of Tropisetron exceeding 10 mg.

Side effects:

Drug is well transferred. Disturbances are possible from TsNS: headache, dizziness, feeling of fatigue; from a digestive tract: abdominal pain, locks, diarrhea. Reactions of immediate hypersensitivity are in rare instances noted (face reddening, widespread
small tortoiseshell, feeling of shortage of air, asthma, acute bronchospasm); seldom or never - a collapse, a stop of cordial activity, but exact interrelation with Tropisetron it is not established. Some of side effects can be caused by at the same time carried out chemotherapy or a basic disease.

Interaction with other medicines:

The rifampicin, phenobarbital and other drugs inducing activity of enzymes of a liver reduce Tropisetron's concentration in a blood plasma that can result in need of increase in a dose at persons
with active metabolism whereas at the lowered speed of metabolism of it it is not required. The drugs inhibiting microsomal enzymes of a liver have no significant effect on Tropisetron's concentration in a blood plasma. The therapeutic effectiveness of drug amplifies dexamethasone. Reception together with food can increase several Tropisetron's bioavailability that has no clinical value. To store in the place, unavailable to children.

Contraindications:

Hypersensitivity to Tropisetron, pregnancy, a lactation (for the period of reception it is necessary to suspend breastfeeding), children's age up to 2 years.

Overdose:

At repeated reception of very high doses the following symptoms are possible: visual hallucinations, increase in the ABP (at patients with arterial hypertension). A symptomatic treatment (in the conditions of monitoring of the vital functions and attentive observation of a condition of the patient).

Storage conditions:

Period of validity - 3 years. It is forbidden to use medicine after the termination of date of term
the validity specified on packaging. Visual signs of unfitness of drug: deformation of capsules. To store in the dry, protected from light place at a temperature from 15 °C to 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Capsules on 0,005 g No. 5 in the blister, 1 blister in a pack.