Осетрон®

General characteristics. Structure:

Tablets, film coated white or almost white color, round, biconvex, with a stamping of "Rx" on one party and a smooth surface on other party.
1 таб.
ondansetrona of a hydrochloride dihydrate of 5 mg,
what corresponds to the maintenance of an ondansetron of 4 mg
Excipients: starch corn, cellulose microcrystallic (Ultra_102), lactose, silicon dioxide colloid, magnesium stearate.
4 pieces – strips (1) – packs cardboard.
10 pieces – strips (1) – packs cardboard.
Tablets, film coated white or almost white color, round, biconvex, with a stamping of "Rx" on one party and a smooth surface on other party.
1 таб.
ondansetrona of a hydrochloride dihydrate of 9.976 mg,
what corresponds to the maintenance of an ondansetron of 8 mg
Excipients: starch corn, cellulose microcrystallic (Ultra_102), lactose, silicon dioxide colloid, magnesium stearate.
4 pieces – strips (1) – packs cardboard.
10 pieces – strips (1) – packs cardboard.
Solution for in/in and introductions in oil transparent, colourless.
1 ml 1 amp.
ondansetrona of a hydrochloride dihydrate of 2.494 mg 4.988 mg,
what corresponds to the maintenance of an ondansetron of 2 mg 4 mg
Excipients: citric acid monohydrate, sodium citrate, sodium chloride,
water for and.
2 ml – ampoules of colourless glass (2) – blisters (1) – packs cardboard.
2 ml – ampoules of colourless glass (5) – blisters (2) – packs cardboard.
2 ml – ampoules of colourless glass (5) – blisters (10) – packs cardboard.
Solution for in/in and introductions in oil transparent, colourless.
1 ml 1 amp.
ondansetrona of a hydrochloride dihydrate of 2.494 mg 9.976 mg,
what corresponds to the maintenance of an ondansetron of 2 mg 8 mg
Excipients: citric acid monohydrate, sodium citrate, sodium chloride,
water for and.
4 ml – ampoules of colourless glass (2) – blisters (1) – packs cardboard.
4 ml – ampoules of colourless glass (5) – blisters (2) – packs cardboard.
4 ml – ampoules of colourless glass (5) – blisters (10) – packs cardboard.

Pharmacological properties:

Antiemetic drug of the central action. Ondansetron is the selection antagonist 5HT3 (serotoninovy) receptors.
Medicines for cytostatic chemotherapy and radiotheraphy can cause increase in level of serotonin which by activation of the vagal afferent fibers containing 5HT3 receptors causes an emetic reflex. Selectively blocks serotoninovy 5HT3 receptors of neurons of the central and peripheral nervous system, the termination of a vagus nerve in intestines and in the TsNS centers (is preferential a bottom of the IV ventricle) regulating implementation of emetic reflexes.
Does not break coordination of movements, does not cause sedation and decrease in working capacity. Has anxiolytic activity. Does not change concentration of prolactin in plasma.

Indications to use:

The prevention and elimination of nausea and vomiting, caused by cytotoxic Himio-or radiotheraphy; the prevention and elimination of nausea and vomiting in the postoperative period.

Route of administration and doses:

The nausea and vomiting caused by cytostatic therapy
The choice of the mode of dosing is defined by an emetogennost of antineoplastic therapy.
For adults a daily dose Sturgeon averages 8-32 mg.
At умеренно&эметогенной chemotherapy or radiotheraphy appoint in 8 mg of an ondansetron for 1_2 h prior to performing the main therapy with the subsequent reception 8 more mg in 12 h, or 8 mg in/in struyno slowly or therapies, in oil just before the beginning. At vysokoemetogenny chemotherapy appoint in 24 mg Sturgeon along with 12 mg of dexamethasone for 1_2 h prior to carrying out chemotherapy. For prevention of the late or long vomiting arising in 24 h it is necessary to continue reception of an ondansetron in a dose of 8 mg of 2 times/days within 5 days.
For parenteral administration the following modes are recommended:
– 8 mg in/in struyno slowly just before the beginning of chemotherapy, and then 2 more in/in an injection on 8 mg, each of which is carried out in 2_4 h;
– continuous 24_chasovaya infusion of drug in a dose of 24 mg with a speed of 1 mg/h;
– 16_32 mg divorced in 50_100 ml of the corresponding infusion solution in a look
15_minutnoy infusions, just before the beginning of chemotherapy.
Efficiency of an ondansetron can be increased in the way one-time in/in introductions of GKS (for example, 20 mg of dexamethasone) prior to the beginning of chemotherapy.
To children 2 years drug are more senior appoint in a dose 5 mg/sq.m of a body surface in/in, just before the beginning of chemotherapy, with the subsequent intake of 4 mg in 12 h; treatment is recommended to continue in a dose 4 mg of 2 times/days inside within 5 days.
Postoperative nausea and vomiting
For the warning of postoperative nausea and vomiting to adults administer the drug in a single dose of 4 mg in oil or in/in struyno (slowly) at the beginning of an anesthesia or appoint 16 mg inside for 1 h prior to the beginning of the general anesthesia.
For stopping of the arisen nausea and vomiting 4 mg of drug, in oil or slow in/in introduction, are recommended.
Intramusculary into the same body part ондансетрон it can be entered in the dose which is not exceeding 4 mg!
To prevention of postoperative nausea and vomiting at children ондансетрон it is applied exclusively parenterally in a single dose of 0.1 mg/kg (as much as possible to 4 mg)
in the form of slow in/in an injection to or after anesthesia.
For treatment of the developed postoperative nausea and vomiting at children it is recommended slow in/in administration of drug in a single dose of 0.1 mg/kg (as much as possible to 4 mg).
Concerning prevention and treatment of postoperative nausea and vomiting children under 2 years have no sufficient experience.
It is not required to patients of advanced age of change of a dosage.
To change patients with a renal failure a usual daily dose and frequency
administration of drug is not required.
At a moderate or heavy abnormal liver function the clearance of an ondansetron substantially decreases, at the same time its T1/2 therefore such patients are not recommended to appoint ондансетрон in a dose more than 8 mg/days increases.
The following solutions can be applied to cultivation of injection solution: 0.9% solution of sodium of chloride, 5% dextrose solution, Ringer's solution, 0.3% solution of potassium of chloride and 0.9% solution of sodium of chloride, 0.3% chloride potassium solution i5%rastvor Dextrosums.

Features of use:

The patients who had earlier allergic reactions to other selection blockers 5nt3_retseptorov have the increased risk of their development against the background of use of an ondansetron. Ondansetron can slow down motility of a large intestine in this connection its appointment as the patient with signs of impassability of intestines demands regular observation. Infusion solution has to be prepared just before use. In case of need ready infusion solution can be stored before use as much as possible within 24 hours at a temperature of 2-8 °C at usual illumination. During performing infusion of protection against light it is not required; divorced injection solution keeps the stability at least during 24 h at natural light or normal lighting.

Side effects:

Allergic reactions: small tortoiseshell, bronchospasm, laryngospasm, Quincke's disease, anaphylaxis.
From the alimentary system: a hiccups, dryness in a mouth, locks or diarrhea, sometimes – asymptomatic passing increase in activity of aminotransferases in blood serum.
From outside сердечно&сосудистой systems: thorax pains, in some cases with a depression of a segment of ST, arrhythmia, bradycardia, decrease in the ABP.
From a nervous system: headache, dizziness, spontaneous motive frustration and spasms.
Local reactions: a hyperemia, pain, burning in an injection site.
Others: rush of blood to face skin, feeling of heat, temporary disturbance of visual acuity, a hypopotassemia, a hypercreatinemia.

Interaction with other medicines:

As ондансетрон it is metabolized by fermental system (P450 cytochrome) of a liver, care at combined use is required:
with inductors of enzymes of P450 cytochrome (CYP2D6 and CYP3A) – barbiturates, carbamazepine, каризопродол, глютетимид, griseofulvin, a dinitrogene oxide, a papaverine, phenylbutazone, Phenytoinum (it is probable also other hydantoins), rifampicin, Tolbutamidum; with P450 inhibitors (CYP2D6 and CYP3A) – Allopyrinolum, makrolidny antibiotics, antidepressants (MAO inhibitors), chloramphenicol, Cimetidinum, estrogensoderzhashchy oral contraceptives, diltiazem, Disulfiramum, valproic acid and its salts, erythromycin, флуконазол, ftorkhinolona, an isoniazid, кетоконазол, ловастатин, metronidazole, омепразол, propranolol, quinidine, quinine, verapamil.
Ondansetron in concentration of 16_160 mkg/ml pharmaceutical is compatible and can be entered through a Y-shaped injector in/in kapelno jointly with the following medicines:
cisplates (in concentration to 0:48 mg/ml) during 1_8 h;
5-ftoruratsit (in concentration to 0.8 mg/ml with a speed of 20 ml/h – higher concentration can cause precipitation of an ondansetron);
карбоплатин (in concentration of 0.18_9.9 mg/ml within 10_60 min.);
этопозид (in concentration of 0.14_0.25 mg/ml within 30_60 min.);
ceftazidime (in a dose of 0.25_2.0 g in a look in a bolyusny injection within 5 min.);
cyclophosphamide (in a dose from 0.1_1.0 g in a look in a bolyusny injection within 5 min.);
doxorubicine (in a dose of 10_100 mg in a look in a bolyusny injection within 5 min.);
dexamethasone (20 mg of dexamethasone slowly within 2-5 min. are possible in/in introduction). The drugs can be administered through one dropper, at the same time in solution of concentration of dexamethasone can make from 32 mkg to 2.5 mg/ml, an ondansetron from 8 mkg to 0.1 mg/ml.

Contraindications:

Pregnancy; period of a lactation (breastfeeding); children's age up to 2 years; hypersensitivity to an ondansetron or other components of drug.

PREGNANCY AND LACTATION
Safety of use of an ondansetron at pregnancy is not established.
Use of the drug Osetron® at pregnancy and in the period of a lactation is contraindicated.

Overdose:

In cases of alleged overdose symptomatic therapy is shown. The specific antidote is unknown. 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:

List B. Drug should be stored in dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C. A period of validity – 3 years.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 4 mg and 8 mg. According to 4 or 10 tab. in a strip. On 1 strip in a cardboard pack.

Solution for intravenous and intramuscular administration, 2 mg/ml. On 2 or 4 ml in ampoules from colourless glass. On 2 ampoules in PVC / алюмниевом the blister; on 1 blister in a cardboard pack. On 5 ampoules in PVC / алюмниевом the blister; on 2 or 10 blisters in a cardboard pack.