SETRONON

Active material: Ondansetron
When ATH: A04AA01
CCF: Antiemetic drugs of the central action, blocking serotonin receptors
ICD-10 codes (testimony): R11
When CSF: 11.06.01
Manufacturer: PLIVA HRVATSKA d.o.o. (Croatia)

Pharmaceutical form, composition and packaging

Pills, coated (film) white or nearly white, round, lenticular.

Excipients: magnesium stearate, microcrystalline cellulose, corn starch, lactose monohydrate.

The composition of the shell: Titanium dioxide, macrogol (polyethylene glycol) 4000, hypromellose 15sR, lactose monohydrate, sodium citrate dihydrate.

10 PC. – blisters (1) – packs cardboard.

Solution for in / and the / m clear, colorless.

Excipients: sodium citrate, citric acid monohydrate, sodium chloride, water d / and.

2 ml – colorless glass vials (5) – packs cardboard.

Solution for in / and the / m clear, colorless.

Excipients: sodium citrate, citric acid monohydrate, sodium chloride, water d / and.

4 ml – colorless glass vials (5) – packs cardboard.

Pharmacological action

Antiemetics, selective serotonin 5HT₃-receptors. Medicines for cytostatic chemotherapy and radiotherapy can cause an increase in serotonin levels, which by activating vagal afferent fibers, containing serotonin 5HT₃-receptors, induces a gag reflex. Ondansetron inhibits the onset of the gag reflex by blocking serotonin 5HT₃-receptors at the level of neurons in the central nervous system, and peripheral nervous system.

Apparently, prevention and treatment of postoperative and induced cytostatic chemotherapy is based on this mechanism of action.- and radiotherapy for vomiting and nausea.

Ondansetron does not affect serum prolactin concentration.

Pharmacokinetics

Absorption

After oral administration, C_max ondansetron in blood plasma is reached after about 1.5 no. Absolute bioavailability after oral administration is about 60%.

With i / m introduction C_max determined during 10 min after injection.

Distribution

Plasma protein binding is 70-76%. The distribution of ondansetron is the same with intramuscular and intravenous administration.

Metabolism and excretion

Ondansetron is metabolized in the liver.

As after ingestion, and with parenteral administration T_1/2 is about 3 no. Older patients T_1/2 reaches 5 no. With urine in an unmodified form appears less 5%.

Pharmacokinetics in special clinical situations

With severe liver failure, T_1/2 reaches 15-22 no.

With kidney damage (CC < 15 ml / min) T_1/2 increases by 4-5 no, but this increase has no clinical significance.

Testimony

- prevention and relief of nausea and vomiting, caused by cytostatic chemotherapy and radiotherapy;

- prevention and relief of postoperative nausea and vomiting.

Dosage regimen

Prevention and relief of nausea and vomiting during cytostatic therapy

The choice of the dosage regimen is determined by the severity of the emetogenic effect of the antitumor therapy..

For adults daily dose, usually, is 8-32 mg. The recommended dosing regimens.

For mild emetogenic chemotherapy or radiotherapy:

– i / v jet slowly or i / m at a dose 8 mg immediately before starting therapy;

– oral dose 8 mg for 1-2 h before the start of therapy, then another 8 mg inside through 12 hours after the start of therapy.

With highly emetogenic chemotherapy:

– w / jet (slowly) dose 8 mg immediately before starting chemotherapy, then another 2 intravenous injection by jet 8 mg, each of which is carried out through 2-4 no;

– continuous 24-hour infusion of the drug in a dose 24 mg at a speed 1 mg / h;

– 16-32 mg, divorced in 50-100 ml of the appropriate infusion solution, as a 15 minute infusion, just before starting chemotherapy.

The effectiveness of ondansetron can be increased by a single intravenous administration of corticosteroids (eg, 20 mg dexamethasone) before chemotherapy; when taken orally to enhance the effect, a single dose can be increased to 24 mg and prescribed simultaneously with 12 mg dexamethasone for 1-2 h before chemotherapy.

To prevent delayed vomiting, emerging through 24 h after the start of chemotherapy- or radiotherapy, it is recommended to continue using the drug inside by 8 mg 2 times / day for 5 days.

Children over 2 years the drug is prescribed in a dose 5 mg / m² body surface i / v, immediately before starting chemotherapy followed by oral administration in a dose 4 mg after 12 no; after the end of chemotherapy, it is recommended to continue taking the drug inside by 4 mg 2 times / day for 5 days.

Prevention of postoperative nausea and vomiting

Adults enter a single dose 4 mg IM or IV jet slowly at the beginning of anesthesia, or is administered orally in a dose 16 mg for 1 h before the onset of anesthesia.

In older children 2 years ondansetron is used exclusively parenterally in a single dose 100 mg / kg (a maximum of 4 mg) as a slow intravenous injection during or after anesthesia.

Relief of postoperative nausea and vomiting

Adults recommended intramuscular or intravenous slow administration of the drug in a dose 4 mg. In / m in the same area of ​​the body ondansetron can be administered in a dose, not exceeding 4 mg.

Children over 2 years recommended intravenous slow administration of the drug in a single dose 100 mg / kg (a maximum of 4 mg).

Elderly patients dose adjustment is required.

If the kidney function It does not require correction dosing regimen.

If abnormal liver function the clearance of ondansetron decreases significantly, at the same time, its T_1/2 plasma, therefore, in this category of patients, the daily dose should not be exceeded 8 mg.

For diluting the injection solution It may be used 0.9% sodium chloride solution, 5% Dextrose, Ringer, 0.3% solution of potassium chloride and 0.9% sodium chloride solution, 0.3% solution of potassium chloride and 5% Dextrose.

Side effect

Allergic reactions: hives, bronchospasm, laringospazm, angioedema, anaphylaxis.

From the digestive system: Ikotech, dry mouth, diarrhea, constipation, sometimes asymptomatic, transient elevation of serum aminotransferase levels.

Cardio-vascular system: chest pain, in some cases with ST segment depression, Arrhythmia, bradycardia, decrease in blood pressure.

From the central and peripheral nervous system: headache, dizziness, spontaneous movement disorders and seizures.

Local reactions: pain, burning and redness at the injection site.

Other: flushing, feeling the heat, temporary visual impairment; rarely – kaliopenia (the connection with taking the drug has not been clearly established)

Contraindications

- Pregnancy;

- Lactation (breast-feeding);

- Children up to age 2 years (safety and efficacy have not been studied);

- Hypersensitivity to the drug.

Pregnancy and lactation

Contraindicated for use in pregnancy and lactation (breast-feeding).

Cautions

Patients, in whom previously with the use of other selective antagonists of serotonin 5HT₃– receptor hypersensitivity reactions were observed, when using ondansetron, similar reactions may also develop.

Unnecessarily. ondansetron causes constipation, patients with signs of intestinal obstruction after using the drug require regular monitoring.

The infusion solution should be prepared immediately before use. If necessary, the solution is ready for infusion may be stored prior to use as much as possible during the 24 hours at a temperature of from 2 ° to 8 ° C.. During infusion light shielding is not required; diluted injectable solution remains stable for at least 24 h in natural light or artificial light.

If you have lactose intolerance, consider, what in 1 Setronon's tablet 4 mg contains 59.25 Lactose mg, 8 mg – 118.5 Lactose mg.

Effects on ability to drive vehicles and management mechanisms

Setronon does not have a sedative effect and does not impair the ability to drive vehicles and work with moving mechanisms.

Overdose

In cases of suspected overdose, symptomatic therapy is indicated.. Spetsificheskiy no known antidote.

Drug Interactions

Ondansetron is metabolized in the liver by isoenzymes of the CYP450 system, therefore, drug interaction with inducers of isoenzymes CYP2D6 and CYP3A is possible, incl. barbiturates, karʙamazepinom, karizoprodol, glutetimidom, griseofulvin, nitrous oxide, papaverine, phenylbutazone, phenytoin (probably with other hydantoins), rifampicin, tolʙutamidom; with inhibitors of isoenzymes CYP2D6 and CYP3A, incl. with allopurinol, antibiotics – macrolides, antidepressants – MAO inhibitors, chloramphenicol, cimetidine, oral contraceptives, containing estrogens, diltiazemom, disulьfiramom, valproic acid, sodium valproate, Erythromycin, fluconazole, ftorxinolonami, izoniazidom, ketoconazole, lovastatin, metronidazolom, omeprazole, propranolol, quinidine, xininom, verapamil).

Setronone does not interact with ethanol, temazepamom, furosemidom, tramadolom and propofolom.

Ondansetron in concentration 16-160 μg / ml pharmaceutically compatible with the following drugs, which can be injected through the Y-shaped injector:

– cisplatin (at a concentration of 0.48 mg / ml) during 1-8 no;

– 5-ftoruracil (at a concentration of 0.8 mg / ml at a rate 20 ml / h – higher concentrations may precipitate ondansetron);

– carboplatin (concentration 0.18-9.9 mg / ml for 10-60 m);

– etoposide (concentration 0.14-0.25 mg / ml for 30-60 m);

– ceftazidime (dose 0.25-2 g as an intravenous bolus injection during 5 m);

– cyclophosphamide (in a dose of 0.1-1 g as an intravenous bolus injection during 5 m);

– doxorubicin (dose 10-100 mg, a / in a bolus injection over a 5 m);

– Dexamethasone – possible intravenous administration in a dose 20 mg slowly over 2-5 m. Dexamethasone and Setronone can be administered through a single dropper, wherein the concentration of dexamethasone in the solution of sodium phosphate may be from 32 ug / ml to 2.5 mg / ml, ondansetrona – from 8 ug / ml to 1 mg / ml.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored out of reach of children.

Solution for injection should be stored in a dark place at a temperature not exceeding 25 ° С. Shelf life – 3 year.

The tablets should be stored at a temperature not exceeding 30 ° C.. Shelf life – 3 year.