Emesetron-Zdorovye, 0,2% 2 ml No. 5/0,2 of % of 4 ml No. 5

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: transparent colourless or slightly yellowish solution; structure: 1 ml of solution contains an ondansetron of a hydrochloride (in terms of ондансетрон) – 2 mg;
excipients: citric acid monohydrate, sodium citrate, dinatrium эдетат (Trilonum of B), sorbitol, 0,1 M hydroxide sodium solution, water for injections.

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. At intravenous administration in a dose of 0,15 mg/kg adult 75 years are younger the maximum concentration in blood averages about 100 ng/ml, at persons 75 years – 170 ng/ml are more senior. At intramuscular introduction the maximum concentration of an ondansetron in blood is registered in 10 min. after an injection and makes about 25 ng/ml. 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 3,5–5,5 hours (depending on age). 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 clinically insignificant 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.

Route of administration and doses:

The drug is administered intravenously struyno or kapelno, and also intramusculary. For infusional introduction can be applied to preparation of solution of an ondansetron: 0,9% solution of sodium of chloride, 5% glucose solution, Ringer's solution. Solution of an ondansetron for infusional introduction is prepared just before introduction; in case of need it is possible to store it before full use no more than 24 hours at a temperature 2-8os. During performing infusion protection against light at normal lighting is not required.
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 for primary prevention of nausea and vomiting at moderate emetogenny chemotherapy and radiation therapy are more senior – 3 options of introduction are possible:
I – once 8 mg intravenously slowly just before the beginning of a course;
II – once 32 mg divorced in 50–100 ml of normal saline solution, infusionally within not less than 15 minutes in 30 minutes prior to the beginning of a course;
III – on 0,15 mg/kg infusionally 3 times – in 30 minutes prior to the beginning of chemotherapy and then in 4 hours and 8 hours.
The adult for primary prevention of nausea and vomiting at vysokoemetogenny chemotherapy – 3 options of introduction are possible:
I – once 8 mg intravenously slowly just before the beginning of a course;
II - on 8 mg intravenously slowly just before the beginning of a course, then repeatedly on 8 mg intravenously slowly two times with an interval of 2 - 4 hours or on 1 mg/h intravenously kapelno with breaks within 24 hours.
III – once 32 mg divorced in 50–100 ml of normal saline solution, infusionally within not less than 15 minutes just before the beginning of a course.
In the next days ондансетрон apply to prevention of vomiting inside in the form of tablets.
At children from 4 to 12 years for primary prevention of nausea and vomiting at emetogenny chemotherapy: once intravenously 5 mg/sq.m just before the beginning of a course with the subsequent reception of an ondansetron inside in the form of tablets.
For prevention of postoperative nausea and vomiting: the adult – on 4 mg intramusculary or intravenously struyno slowly at the beginning of carrying out the general anesthesia; to children 2 years – 0,1 mg/kg (as much as possible to 4 mg) intravenously slowly to (not less, than in 30 seconds) or after an introduction anesthesia are more senior.
For stopping of the developed postoperative nausea and vomiting: adult – 4 mg intramusculary or intravenously, to children – 0,1 mg/kg (to 4 mg) intravenously slowly.
Intramusculary the dose which is not exceeding 4 mg of an ondansetron can be in one step entered into the same body part.
The highest daily dose of an ondansetron for adults makes 32 mg, patients with the expressed abnormal liver functions have 8 mg (as much as possible at single infusional introduction within 15 minutes).

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 appoint to the patients having in the anamnesis of reaction of hypersensitivity on 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 are possible: a headache, dizziness, temporary disturbance of visual acuity (at bystry intravenous administration), spontaneous motive frustration, attacks of spasms, oppression of the central nervous system, paresthesia, weakness, extrapyramidal symptomatology, a 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: there can be cough, thorax pains (anginous type), reddening and burning in the place of an injection.

Interaction with other medicines:

For cultivation use only the recommended infusion solutions (see the section "Route of Administration and Doses").
Drug in the form of infusion solution at concentration of an ondansetron of 16-160 mkg/ml (8 mg / 500 ml and 8 mg / 50 ml) can be entered through a Y-shaped catheter jointly with the following drugs:
– Cisplatinum in concentration to 0,48 mg/ml within 1–8 hours;
– карбоплатин in concentration of 0,18-9,9 mg/ml within 10–60 minutes;
– 5-ftoruratsit in concentration up to 0,8 mg/ml with a speed not less than 20 ml/h, at the same time it is necessary to consider that higher concentration of a 5-ftoruratsil can cause precipitation of an ondansetron;
– этопозид in concentration of 0,14-0,25 mg/ml within 30–60 minutes;
– the ceftazidime in a dose of 0,025 - 2 g divorced water for injections according to recommendations of the producer in the form of an intravenous bolyusny injection within 5 minutes;
– the cyclophosphamide in a dose of 0,1 - 1 divorced water for injections according to recommendations of the producer in the form of an intravenous bolyusny injection within 5 minutes;
– doxorubicine in a dose of 10 - 100 mg divorced water for injections according to recommendations of the producer in the form of an intravenous bolyusny injection within 5 minutes;
– sodium dexamethasone phosphate in a dose of 20 mg intravenously slowly within 2–5 minutes through a Y-shaped catheter together with 8–32 mg of an ondansetron in 50–100 ml of solution.
Drug should not be used in one syringe or in one dropper 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), lactation period, children's age: at himio-and radiation therapy – up to 4 years; at anesthesia – up to 2 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:

To store in the place protected from light 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 2 ml and on 4 ml in ampoules; No. 5 in a pack.