medicalmeds.eu Medicines Antiemetic, serotoninovy receptors antagonist. Setronon

Setronon

Producer: Teva (Tev) Israel

Code of automatic telephone exchange: A04AA01

Release form: Firm dosage forms. Tablets.

General characteristics. Structure:

Active agent: ондансетрон 4 mg or 8 mg (in the form of a dihydrate hydrochloride).
excipients: magnesium stearate, cellulose microcrystallic, starch corn, lactoses monohydrate;
structure of a cover: titanium dioxide, macrogoal/polyethyleneglycol 4000, gipromelloza 15 Wednesday, lactoses monohydrate, sodium citrate dihydrate

Description
Tablets on 4 mg: round, biconvex tablets of white or almost white color, film coated;
Tablets on 8 mg: round, biconvex tablets of white or almost white color, film coated

Pharmacological properties:

Antiemetic drug, the selection antagonist of serotoninovy 5HT3-receptors. Medicines for cytostatic chemotherapy and radiotheraphy can cause increase in level of serotonin which by activation of the vagal afferent fibers containing serotoninovy 5HT3-receptors causes an emetic reflex. Ondansetron slows down emergence of an emetic reflex by blockade of serotoninovy 5HT3-receptors at the level of TsNS neurons, and a peripheral nervous system.

Apparently, the prevention and treatment postoperative and caused cytostatic himio-and radiotheraphy of vomiting and nausea is based on this mechanism of action.

Ondansetron does not influence concentration of prolactin in blood serum.

Pharmacokinetics
Absorption

After intake of Cmax of an ondansetron in a blood plasma it is reached approximately in 1.5 h. Absolute bioavailability after intake makes about 60%.

At introduction in oil Cmax is defined within 10 min. after an injection.

Distribution

Linkng with proteins of plasma makes 70-76%. Distribution of an ondansetron identical at in oil and in introduction.

Metabolism and removal

Ondansetron is metabolized in a liver.

Both after intake, and at parenteral administration of T1/2 makes about 3 h. At elderly patients of T1/2 reaches 5 h. With urine in not changed look less than 5% are removed.

Pharmacokinetics in special clinical cases

At the expressed liver failure of T1/2 reaches 15-22 h.

At damage of kidneys (KK <15 ml/min.) of T1/2 increases by 4-5 h, but this increase has no clinical value.

Indications to use:

— prevention and stopping of nausea and vomiting, caused by cytostatic chemotherapy and radiotheraphy;

— prevention and stopping of postoperative nausea and vomiting.

Route of administration and doses:

Prevention and stopping of nausea and vomiting at cytostatic therapy

The choice of the mode of dosing is defined by expressiveness of emetogenny action of the carried-out antineoplastic therapy.

For adults the daily dose, as a rule, makes 8-32 mg. The following modes of dosing are recommended.

At moderate emetogenny chemotherapy or radiotheraphy:

- in/in struyno slowly or in oil 8 mg in a dose just before the beginning of therapy;

- inside in a dose of 8 mg for 1-2 h prior to therapy, then 8 more mg inside in 12 h later began therapies.

At vysokoemetogenny chemotherapy:

- in/in struyno (slowly) in a dose of 8 mg just before the beginning of chemotherapy, then 2 more injections in/in struyno on 8 mg, each of which is carried out in 2-4 h;

- continuous 24-hour 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 the form of 15-minute infusion, 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; at intake for strengthening of effect the single dose can be increased to 24 mg and is appointed along with 12 mg of dexamethasone for 1-2 h prior to carrying out chemotherapy.

For the prevention of the delayed vomiting arising in 24 h after the beginning himio-or radiotheraphy, it is recommended to continue drug use inside on 8 mg 2 within 5 days.

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 in a dose of 4 mg in 12 h; after the termination of chemotherapy it is recommended to continue administration of drug inside on 4 mg 2 within 5 days.

Prevention of postoperative nausea and vomiting

The adult enter a single dose of 4 mg in oil or in/in struyno slowly at the beginning of an anesthesia, or appoint inside in a dose 16 mg for 1 h prior to the beginning of an anesthesia.

At children 2 years ондансетрон are more senior it is applied exclusively parenterally in a single dose of 100 mkg/kg (as much as possible to 4 mg) in the form of slow in/in an injection in time or after anesthesia.

Stopping of postoperative nausea and vomiting

It is recommended to adults in oil or in/in slow administration of drug in a dose of 4 mg. In oil into the same body part ондансетрон it can be entered in the dose which is not exceeding 4 mg.

To children 2 years are more senior it is recommended in/in slow administration of drug in a single dose of 100 mkg/kg (as much as possible to 4 mg).

It is not required to patients of advanced age of dose adjustment.

At a renal failure correction of the mode of dosing is not required.

At an abnormal liver function the clearance of an ondansetron substantially decreases, at the same time its T1/2 from plasma therefore at this category of patients it is not necessary to exceed a daily dose of 8 mg increases.

It is possible to apply 0.9% to cultivation of injection solution 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% solution of potassium of chloride and 5% dextrose solution.

Features of use:

At patients at whom earlier at use of other selection antagonists of serotoninovy 5NT3 receptors hypersensitivity reactions were observed at use of an ondansetron similar reactions can also develop.

Since ондансетрон causes a lock, patients with signs of impassability of intestines after use of drug need 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 during 24 h at a temperature from 2 ° up to 8 °C. 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 artificial lighting.

In the presence of a lactose intolerance it is necessary to consider that contains in 1 tablet of Setronon of 4 mg 59.25 mg of lactose, 8 mg - 118.5 mg of lactose.

Influence on ability to driving of motor transport and to control of mechanisms

Setronon does not possess sedation and does not break ability to control of motor transport and work with moving mechanisms.

Side effects:

Allergic reactions: small tortoiseshell, bronchospasm, laryngospasm, Quincke's disease, anaphylaxis.

From the alimentary system: a hiccups, dryness in a mouth, diarrhea, a lock, sometimes asymptomatic passing increase in level of aminotransferases in blood serum.

From cardiovascular system: thorax pains, in some cases with a depression of a segment of ST, arrhythmia, bradycardia, decrease in the ABP.

From TsNS and peripheral nervous system: headache, dizziness, spontaneous motive frustration and spasms.

Local reactions: pain, burning and reddening in an injection site.

Others: rush of blood to the person, feeling of heat, temporary disturbance of visual acuity; seldom - a hypopotassemia (connection with administration of drug is unambiguously not established).

Interaction with other medicines:

Ondansetron is metabolized in a liver by CYP450 system isoenzymes therefore perhaps medicinal interaction with inductors of isoenzymes of CYP2D6 and CYP3A, including with barbiturates, carbamazepine, karizoprodoly, glutetimidy, griseofulvin, nitrous oxide, a papaverine, phenylbutazone, Phenytoinum (it is probable also with other hydantoins), rifampicin, Tolbutamidum; with inhibitors of isoenzymes of CYP2D6 and CYP3A, including with Allopyrinolum, antibiotics - macroleads, antidepressants - MAO inhibitors, chloramphenicol, Cimetidinum, the oral contraceptives containing estrogen, diltiazem, Disulfiramum, valproic acid, sodium Valproatum, erythromycin, flukonazoly, ftorkhinolona, an isoniazid, ketokonazoly, lovastatiny, metronidazole, omeprazoly, propranolol, quinidine, quinine, verapamil).

Setronon does not enter interaction with ethanol, temazepam, furosemide, tramadoly and propofoly.

Ondansetron in concentration of 16-160 mkg/ml pharmaceutical is compatible to the following medicines which can be entered through a Y-shaped injector:

- Cisplatinum (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 settling out 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.);

- a ceftazidime (in a dose of 0.25-2 g in a look in a bolyusny injection within 5 min.);

- cyclophosphamide (in a dose from 0.1-1 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 slowly within 2-5 min. are possible in/in introduction in a dose. Dexamethasone and Setronon it is possible to enter through one dropper, at the same time in solution of concentration of dexamethasone of sodium of phosphate can make from 32 mkg/ml to 2.5 mg/ml, an ondansetron - from 8 mkg/ml to 1 mg/ml.

Contraindications:

— pregnancy;

— lactation (breastfeeding);

— children's age up to 2 years (safety and efficiency are not studied);

— hypersensitivity to drug components.

Use of drug CETPOHOH at pregnancy and feeding by a breast
Use at pregnancy and in the period of a lactation (breastfeeding) is contraindicated.

Use at abnormal liver functions
At an abnormal liver function the clearance of an ondansetron substantially decreases, at the same time its T1/2 from plasma therefore at this category of patients it is not necessary to exceed a daily dose of 8 mg increases.

Use at renal failures
At a renal failure correction of the mode of dosing is not required.

Use for elderly patients
It is not required to patients of advanced age of dose adjustment.

Use for children
Use for children under 2 years is contraindicated (safety and efficiency of use are not studied).

Overdose:

In cases of alleged overdose symptomatic therapy is shown. The specific antidote is not known.

Storage conditions:

List B. Drug should be stored in the place, unavailable to children. Tablets should be stored at a temperature not above 30 °C. A period of validity - 3 years.