Emesetron-Zdorovye, tab. of 4 mg No. 10

General characteristics. Structure:

International and chemical names: ondansetron; (+–)-1,2,3,9 – tetragidro-9-metil-3-[(2-methyl-1H-imidazole-1-silt) - methyl] - 4H - a carbazole - 4 - it (in the form of a dihydrate monohydrochloride); main physical and chemical properties: tablets, coated, light yellow color with a nacreous shade; structure: 1 tablet contains an ondansetron of a hydrochloride (in terms of ондансетрон) – 4 mg or 8 mg; auxiliary substances: lactoses monohydrate, cellulose microcrystallic, potato starch, magnesium stearate, povidone (polyvinylpirrolidone low-molecular medical), aerosil, titanium dioxide, кандурин (silver gloss), gipromeloz (gidroksipropilmetiltsellyuloz), Sepispers Dry Yellow R dye.

Pharmacological properties:

Pharmacodynamics. Antiemetic. The mechanism of action is caused by competitive high-selection blockade of the central and peripheral 5-HT3-retseptorov of serotonin (receptors of a trigger zone, the emetic center). Suppresses an emetic reflex, eliminating and warning vomiting at use of cytotoxic chemotherapeutic means, radiation therapy, in the postoperative period. At repeated use slows down a peristaltics and passing of contents on intestines.

Pharmacokinetics. Drug is well absorbed in digestive tract, bioavailability makes about 60%, in connection with effect of "the first passing" through a liver. The maximum concentration of an ondansetron in blood is reached in 1,5–1,7 h. Meal extends the absorption period for 17%, without influencing the maximum concentration. Linkng with proteins of plasma of 70-76%. The main part of the entered dose (85–90%) is hydroxylated in a liver with participation of P450 cytochrome before connections of an indole cycle, and then conjugates with glucuronic and sulfuric acids. The total amount of distribution makes 1,9 l/kg, an elimination half-life of 3,5-5,5 h (depending on age), the general clearance - 5,9 ml/(min.). Drug is excreted from an organism by kidneys, at the same time 5% of the entered dose are removed in not changed look. Pharmacokinetic parameters of an ondansetron do not change at its repeated introduction.

At children, and also at persons with damages of a liver the general clearance decreases, at patients of advanced age the elimination half-life and the general clearance of drug increases. At patients with a moderate renal failure (clearance of creatinine of 15-60 ml/min.) the system clearance and volume of distribution of an ondansetron what insignificant clinically small increase in an elimination half-life of drug is result of are reduced. Women have a level of the maximum concentration and bioavailability of drug is higher, and the clearance and level of distribution are lower, than at men.

Indications to use:

Prevention and elimination of nausea and vomiting at cytotoxic chemotherapy (initial and repeated courses, including use of high doses of Cisplatinum) and radiation therapy (radiation of all body surface, partial single high-dose or daily exposition of abdominal area) in oncology. Prevention and elimination of nausea and vomiting in the postoperative period at adults and children are more senior than 12 years.

Route of administration and doses:

When performing cytostatic therapy the mode of dosing is set individually depending on degree of manifestation of emetic reaction.
To adults and teenagers 12 years at moderate emetogenny chemotherapy and radiation therapy are more senior inside appoint: originally on 8 mg in 1–2 hours prior to antineoplastic therapy with the subsequent reception of 8 more mg in 8–12 hours. For prevention of late or long nausea and vomiting after the first 24 hours it is necessary to continue administration of drug on 8 mg each 12 hours. At partial high-dose radiation of abdominal area on 8 mg each 8 hours. Drug is accepted during all course himio-and radiation therapy, and also 1–2 days (in need of 3–5 days) after its termination.
At vysokoemetogenny chemotherapy to adults and teenagers 12 years inside are more senior appoint 24 mg of an ondansetron (along with sodium dexamethasone phosphate) in 1–2 hours prior to the beginning of chemotherapy. For prevention of late vomiting in the next days on 8 mg 2 times a day during all course of chemotherapy, and also 5 days after its termination. Instead of intake it is possible to appoint ондансетрон in the form of solution for injections.
At chemotherapy at children of 4-12 years inside appoint: originally on 4 mg 3 times a day (in 30 minutes prior to the beginning of a course, then in 4 and 8 hours). For prevention of late vomiting on 4 mg each 8 hours 1-2 days, then on 4 mg 2 times a day or on 4 mg 2 times a day during all course, and also 5 days after its termination.
For prevention of postoperative nausea and vomiting: to adults and children 12 years on 16 mg in 1 hour prior to anesthesia are more senior. For treatment of nausea and vomiting in the postoperative period parenteral use of an ondansetron is recommended.
The maximum daily dose of an ondansetron at adults makes 32 mg, patients with the expressed abnormal liver functions have 8 mg.

Features of use:

During treatment ondansetrony feeding by a breast needs to be stopped.
At very expressed emetic reaction as a result of chemotherapy efficiency of drug can be increased by one-time intravenous administration of glucocorticoids (for example, 20 mg of dexamethasone of sodium of phosphate) prior to the beginning of chemotherapy.
With care to appoint to the patients having in the anamnesis of reaction of hypersensitivity to other selection antagonists of serotoninovy 5HT3-receptors. With care and under careful medical observation patients should appoint drug with signs of subacute impassability of intestines.

Side effects:

From the central nervous system can be: headache, dizziness, spontaneous motive frustration, attacks of spasms, oppression of the central nervous system, paresthesia, weakness, extrapyramidal symptomatology, syncope;
from cardiovascular system are possible: feeling of heat and rush of blood to the person, arrhythmia, tachycardia or bradycardia, hypotension or hypertensia;
from the alimentary system can appear: a lock, diarrhea, a hiccups, dryness in a mouth, tranzitorny increase in activity of aminotransferases, insufficiency of function of a liver;
allergic reactions are possible: a small tortoiseshell, a bronchospasm, in isolated cases – anaphylactic reactions;
others: can there will be cough, thorax pains (anginous type).

Interaction with other medicines:

Simultaneous use of inhibitors of microsomal liver enzymes of system of P450 cytochrome (Allopyrinolum, chloramphenicol, Cimetidinum, diltiazem, флуконазол, кетоконазол, metronidazole, омепразол, propranolol, quinidine, verapamil) can increase time of semi-removal and reduce the general clearance of drug.
At simultaneous use with inductors of microsomal liver enzymes of system of P450 cytochrome (barbiturates, carbamazepine, каризопродол, глютетимид, griseofulvin, nitrous oxide, a papaverine, phenylbutazone, Phenytoinum and other hydantoins, rifampicin, Tolbutamidum) decrease in clinical performance of drug is possible.

Contraindications:

Insufficiency of function of a liver, pregnancy (especially I trimester), feeding period breast, children's age: at himio-and radiation therapy up to 4 years; at anesthesia up to 12 years, hypersensitivity to drug components.

Overdose:

At overdose the aggravation of the symptoms described in the section "Side effect" is possible. Treatment: the drug withdrawal and symptomatic therapy directed to maintenance of the vital functions. There is no specific antidote.

Storage conditions:

In the dry, protected from light place at a temperature from 15 °C to 30 °C. To store in the place, unavailable to children.
Period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging; No. 10 in a pack.