Ondansetron-Borimed

General characteristics. Structure:

Active ingredient: 4 mg or 8 mg of an ondansetron (in the form of an ondansetron of a hydrochloride) in 1 ampoule.

Excipients: sodium citrate for injections, sodium chloride, citric acid monohydrate, water for injections.

Pharmacological properties:

Pharmacodynamics. Antiemetic drug. The selection antagonist serotoninovy 5HT3 - receptors. Has strong antiemetic effect which mechanism is finally not installed. The drugs used for chemotherapy and radiological influence can cause release of serotonin in a small bowel, starting thereby an emetic reflex through activation serotoninovy 5HT3 - receptors and initiation of the afferent terminations of a vagus nerve. Ondansetron blocks releasers of this reflex.

Activation of the afferent terminations of a vagus nerve, in turn, can cause emission of serotonin in the zone a post-rheme which is at the bottom of the IV ventricle and, therefore, to start an emetic reflex via the central mechanism. Suppression of nausea and vomiting, provoked by cytotoxic chemotherapy and radiotheraphy, apparently, is carried out thanks to antagonistic action of an ondansetron on serotoninovy 5HT3 - receptors of neurons of the central and peripheral nervous system.

At psychomotor testing it is shown what ондансетрон does not worsen working capacity and has no sedative effect. Drug does not influence concentration of prolactin in a blood plasma.

Pharmacokinetics. Absorption. After introduction in oil Cmax is reached in 10 min.

Distribution. The volume of distribution (Vd) after parenteral administration makes 140 l. Linkng with proteins of plasma - 70-76%.

Metabolism. It Biotransformirutsya in a liver.

Removal. The drug elimination half-life after parenteral administration (T1/2) makes 3 h.

In not changed view with urine less than 5% of the entered dose are removed.

Pharmacokinetic parameters of an ondansetron do not change at its repeated introduction.

Pharmacokinetics in special clinical cases. At patients with a moderate renal failure (the clearance of creatinine (CC) of 15 - 60 ml/min.) both the system clearance, and Vd of an ondansetron are reduced, it small and clinically insignificant increase is result of it T 1/2. The pharmacokinetics of an ondansetron practically does not change at the patients with a heavy renal failure who are on a chronic hemodialysis (researches were conducted in breaks between hemodialysis sessions).

Lack of CYP2D6 enzyme (polymorphism of debrisoquine) does not influence pharmacokinetic parameters of an ondansetron.

At patients of advanced age after parenteral administration of the drug T1/2 can increase to 5 h.

Indications to use:

Route of administration and doses:

The Emetogenny effect at therapy of malignant tumors changes depending on doses and combinations of the applied schemes himio-and radiotheraphy. The route of administration and doses of an ondansetron should be regulated in the range of 8 - 32 mg/days according to the criteria provided below.

The adult at the nausea and vomiting caused emetogenny himio-and radiotheraphy, the recommended dose of an ondansetron for in/in or introductions in oil makes 8 mg just before carrying out himio-or radiotheraphy; the drug should be administered slowly.

At the nausea and vomiting caused by vysokoemetogenny chemotherapy (for example in case of use of Cisplatinum in high doses), ондансетрон it is possible to appoint in the form of single in oil or in/in (slowly) injection in a dose of 8 mg just before administration of emetogenny drug.

According to other scheme of treatment ондансетрон appoint in a dose 8 mg in the form of in oil or in/in (slowly) injection just before chemotherapy. Further appoint 2 injections in/in or in oil 8 mg in a dose, each of which is carried out in 2-4 h; or enter in the form of continuous infusion with a speed of 1 mg/h during 24 h. Efficiency of an ondansetron can be increased by additional introduction (prior to the beginning of chemotherapy) phosphate dexamethasone (in the form of sodium salt) in a dose of 20 mg in/in, once.

Children ондансетрон can appoint in/in in the form of an injection in a dose of 5 mg/sq.m just before the beginning of chemotherapy with the subsequent (in 12 h) intake (in the form of tablets, lingvalny tablets or syrup).

For prevention and treatment of postoperative nausea and vomiting by the adult ондансетрон enter into the period of an introduction anesthesia in oil or in/in (slowly) in a dose of 4 mg. For stopping of the developed postoperative nausea and vomiting it is recommended in oil or in/in (slowly) single administration of drug in a dose of 4 mg.

Children for prevention of postoperative nausea and vomiting ондансетрон are recommended to appoint in/in (slowly) in a dose of 0,1 mg/kg (as much as possible to 4 mg) to, in time or after an introduction anesthesia.

For stopping of the developed postoperative nausea and vomiting ондансетрон appoint in/in (slowly) in a dose of 0,1 mg/kg (as much as possible up to 4 mg).

Ondansetron it is possible to enter in/in with a speed of 1 mg/hour through a dropper or the piston pump.

At patients with abnormal liver functions of a moderate and heavy current the clearance of an ondansetron is significantly reduced, and the elimination half-life is significantly increased therefore use of an ondansetron in doses more than 8 mg/days is not recommended.

At patients with abnormal liver functions of a moderate and heavy current the clearance of an ondansetron is significantly reduced, and the elimination half-life is significantly increased therefore it is not necessary to appoint drug in doses more than 8 mg/days, and also use of other dosage forms is recommended.

Features of use:

Pregnancy and lactation. Safety of use of an ondansetron at pregnancy is not established.

In pilot studies it is established what ондансетрон has no direct or indirect adverse effect on development of an embryo and fruit, the course of pregnancy, and also on perinatal and post-natal development. However, as by results of researches at animals it is not always possible to predict precisely the nature of action at the person, drug is not recommended to use at pregnancy.

In need of purpose of drug in the period of a lactation it is necessary to stop breastfeeding.

Special instructions. At the patients receiving the previous treatment by other selection antagonists 5HT3 - receptors, being followed by hypersensitivity reactions, at use of an ondansetron hypersensitivity reactions are also possible.

As ондансетрон increases time of passing of contents on a large intestine, in case of use of an ondansetron for patients with symptoms of subacute intestinal impassability regular observation is necessary.

Patients of advanced age have an experience of use of an ondansetron for prevention and treatment of nausea and vomiting in the postoperative period is limited. Patients are more senior than 65 years receiving chemotherapy well transfer ондансетрон; special changes of a dose, frequency of reception or a way of administration of drug are not required.

At people with slow metabolism of sparteine and debrisoquine (lack of CYP2D6 enzyme) the elimination half-life of an ondanserton is not changed. Therefore, at repeated administration of drug to such patients of its concentration in plasma will not differ from those in the general population. Therefore it is not required to such patients of correction of a daily dose or frequency of reception of an ondansteron.

Patients with a renal failure do not need correction of a daily dose, frequency or a way of introduction of an ondansetron.

Influence on ability to driving of motor transport and to control of mechanisms. Ondansetron does not render sedation.

Side effects:

From cardiovascular system: a caumesthesia or rush of blood to a face and the head; seldom - thorax pains, arrhythmia, arterial hypotension, bradycardia.

From the alimentary system: a lock, a hiccups, tranzitorny asymptomatic increase in activity of transaminases in a blood plasma.

From TsNS: the headache, spasms (passing afterwards).

Allergic reactions: seldom - allergic reactions of immediate type, in some cases - a heavy current, up to an anaphylaxis.

Local reactions: seldom - local reactions in the field of an injection.

Interaction with other medicines:

At simultaneous use with the drugs which are inductors (barbiturates, carbamazepine, rifampicin, Phenytoinum, phenylbutazone) or inhibitors (Cimetidinum, Allopyrinolum, Disulfiramum) of microsomal enzymes of a liver – P450 cytochrome isoenzymes, change of clearance of an ondansetron is possible.

Pharmaceutical interaction. Ondansetron in the form of solution for injections is compatible to the following infusion solutions: 0,9% solution of sodium of chloride, 5% solution of glucose, 10% Mannitolum solution, Ringer's solution, 0,3% solution of potassium of chloride and 0,9% solution of sodium of chloride, 0,3% solution of potassium of chloride and 5% glucose solution.

Solution of an ondansetron is compatible to solution of dexamethasone of phosphate and they can be entered through one dropper, at the same time in solution of concentration of dexamethasone of phosphate (in the form of sodium salt) can make from 32 mkg to 2,5 g in 1 ml, an ondansetron - from 8 mkg to 1 mg in 1 ml.

Contraindications:

Hypersensitivity to drug.

Overdose:

Now data on overdose of an ondansetron are limited.

Symptoms. At two patients who received doses of 84 mg and 145 mg in/in only easy side effects which are not demanding medicamentous therapy were observed.

Treatment. In cases of alleged overdose symptomatic therapy is shown. At overdose of an ondansetron use of an ipecacuanha as it is improbable that this drug will be effective during antiemetichesky action of an ondansetron is not recommended.

Storage conditions:

Issue conditions:

According to the recipe

Packaging:

On 2 ml in an ampoule, in packaging No. 10; No. 10х1; on 4 ml in an ampoule, in packaging No. 10; No. 5х2.