Universal reference book for medicines
Product name: OSETRON ® (OSETRON)

Active substance: ondansetron

Type: Antiemetic medication of central action blocking serotonin receptors

Manufacturer: DR.
REDDY`S LABORATORIES (India)
Composition, form of production and packaging
The tablets covered with a film shell of
white or almost white color, round, biconcave, embossed "Rx" on one side and a smooth surface on the other side.

1 tab.

ondansetron hydrochloride dihydrate 5 mg,

which corresponds to the content of ondansetron 4 mg

Excipients: corn starch, microcrystalline cellulose (Ultra-102), lactose, silicon dioxide colloid, magnesium stearate.

4 things.
- Strips (1) - packs of cardboard.
10 pieces.
- Strips (1) - packs of cardboard.
The tablets covered with a film shell of white or almost white color, round, biconcave, embossed "Rx" on one side and a smooth surface on the other side.

1 tab.

ondansetron hydrochloride dihydrate 9.976 mg,

which corresponds to the content of ondansetron 8 mg

Excipients: corn starch, microcrystalline cellulose (Ultra-102), lactose, silicon dioxide colloid, magnesium stearate.

4 things.
- Strips (1) - packs of cardboard.
10 pieces.
- Strips (1) - packs of cardboard.
The solution for intravenous and / or injection is clear, colorless.

1 ml of 1 amp.

ondansetron hydrochloride dihydrate 2.494 mg 4.988 mg,

which corresponds to the content of ondansetron 2 mg 4 mg

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

2 ml - ampoules of colorless glass (2) - blisters (1) - packs of cardboard.

2 ml - ampoules of colorless glass (5) - blisters (2) - packs cardboard.

2 ml - ampoules of colorless glass (5) - blisters (10) - packs of cardboard.

The solution for intravenous and / or injection is clear, colorless.

1 ml of 1 amp.

ondansetron hydrochloride dihydrate 2.494 mg 9.976 mg,

which corresponds to the content of ondansetron 2 mg 8 mg

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

4 ml - ampoules of colorless glass (2) - blisters (1) - packs of cardboard.

4 ml - ampoules of colorless glass (5) - blisters (2) - packs of cardboard.

4 ml - ampoules of colorless glass (5) - blisters (10) - packs of cardboard.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2013.

PHARMACHOLOGIC EFFECT

Antiemetic drug of central action.
Ondansetron is a selective antagonist of serotonin 5HT 3 receptors.
Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in the level of serotonin, which, by activating vagal afferent fibers containing 5HT 3receptors, causes a vomiting reflex.
Selectively blocks serotonin 5HT 3 receptors of neurons of the central and peripheral nervous system, endings of the vagus nerve in the intestine and in the centers of the central nervous system (mainly the bottom of the IV ventricle), regulating the implementation of emetic reflexes.
Does not disrupt the coordination of movements, does not cause sedation and reduced efficiency.
It has anxiolytic activity. Does not change the concentration of prolactin in the plasma.
PHARMACOKINETICS

After ingestion, the time to reach C max is 1.5 h. After the / m introduction, the time to reach C max is 10 min.

Binding to plasma proteins is 70-76%.

Metabolised in the liver with the participation of microsomal enzymes (CYP2D6).
The absence of the CYP 2D6 enzyme (debrisoquine polymorphism) does not affect the pharmacokinetics of ondansetron.
Both after ingestion and after parenteral administration, T 1/2 is 3 hours. In unchanged form, less than 5% of the administered dose is excreted in the urine.

The pharmacokinetic parameters of ondansetron do not change with its repeated administration.

In patients with moderate renal insufficiency (CK 15-60 ml / min), both systemic clearance and V d are reduced, resulting in a small and clinically insignificant increase in T 1/2 .
The pharmacokinetics of ondansetron practically does not change in patients with severe renal dysfunction in chronic hemodialysis (studies were conducted in between hemodialysis sessions).
In patients with severe impairment of liver function, the systemic clearance of ondansetron drastically decreases, resulting in an increase in T 1/2 to 15-20 hours. T 1/2 of ondansetron does not depend on the mode of administration.

In elderly patients after ingestion or parenteral administration, T 1/2 may increase to 5 hours.

INDICATIONS

- prevention and elimination of nausea and vomiting caused by cytotoxic chemotherapy or radiotherapy;

- prevention and elimination of nausea and vomiting in the postoperative period.

DOSING MODE

Nausea and vomiting caused by cytostatic therapy

The choice of dosage regimen is determined by the emetogenicity of antitumor therapy.

For adults, the daily dose of Osetron is on average 8-32 mg.

With moderately emetogenic chemotherapy or radiotherapy , 8 mg of ondansetron is administered internally 1-2 hours before the start of the main therapy, followed by another 8 mg at 12 hours, or 8 mg IV slowly or immediately before the start of therapy.

With highly emetogenic chemotherapy , 24 mg of Osetron is administered concomitantly with 12 mg of dexamethasone 1-2 hours before the start of chemotherapy.
To prevent late or prolonged vomiting that occurs after 24 hours, continue taking ondansetron in a dose of 8 mg 2 times / day for 5 days.
For parenteral administration, the following regimens are recommended:

- 8 mg IV slowly before the start of chemotherapy, and then 2 more IV injections of 8 mg, each of which is carried out in 2-4 hours;

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

- 16-32 mg, diluted in 50-100 ml of the appropriate infusion solution, in the form of a 15-minute infusion, immediately before the start of chemotherapy.

The efficacy of ondansetron can be increased by a single intravenous injection of glucocorticosteroids (eg, 20 mg dexamethasone) prior to chemotherapy.

For children older than 2 years, the drug is prescribed at a dose of 5 mg / m 2 of the surface of the body iv, immediately before the start of chemotherapy, followed by ingestion of 4 mg after 12 hours;
treatment is recommended to continue at a dose of 4 mg 2 times / day inside for 5 days.
Postoperative nausea and vomiting

To prevent postoperative nausea and vomiting to adults
inject the drug in a single dose of 4 mg IM or IV in a jet (slow) at the beginning of anesthesia or appoint 16 mg orally for 1 hour before the onset of general anesthesia.
For relief of nausea and vomiting , a / m or slow iv injection of 4 mg of the drug is recommended.

In / m in the same area of ​​the body, ondansetron can be administered at a dose not exceeding 4 mg!

To prevent postoperative nausea and vomiting in children, ondansetron is used exclusively parenterally in a single dose of 0.1 mg / kg (maximum to 4 mg) in the form of a slow intravenous injection before or after anesthesia.

To treat the development of postoperative nausea and vomiting in children, slow IV administration of the drug in a single dose of 0.1 mg / kg (maximum to 4 mg) is recommended.

In the prevention and treatment of postoperative nausea and vomiting in children under 2 years of age, there is no sufficient experience.

Elderly patients are not required to change the dosage.

Patients with impaired renal function change the usual daily dose and the frequency of administration of the drug is not required.

With moderate or severe impairment of liver function, the clearance of ondansetron is significantly reduced, while its T 1/2 increases, so it is not recommended for such patients to prescribe ondansetron at a dose of more than 8 mg / day.

To dilute the injection solution, the following solutions can be used: 0.9% sodium chloride solution, 5% dextrose solution, Ringer's solution, 0.3% potassium chloride solution and 0.9% sodium chloride solution, 0.3% potassium chloride solution and 5% dextrose solution.

SIDE EFFECT

Allergic reactions: urticaria, bronchospasm, laryngospasm, angioedema, anaphylaxis.

On the part of the digestive system: hiccough, dry mouth, constipation or diarrhea;
sometimes - an asymptomatic transient increase in the activity of aminotransferases in the blood serum.
From the cardiovascular system: pain in the chest, in some cases with ST segment depression, arrhythmias, bradycardia, lowering blood pressure.

From the nervous system: headache, dizziness, spontaneous movement disorders and convulsions.

Local reactions: hyperemia, pain, burning at the injection site.

Other: a rush of blood to the skin of the face, a feeling of heat, a temporary disturbance of visual acuity, hypokalemia, hypercreatinemia.

CONTRAINDICATIONS

- Pregnancy;

- the period of lactation (breastfeeding);

- Children under 2 years;

- Hypersensitivity to ondansetron or other components of the drug.

PREGNANCY AND LACTATION

Safety of ondansetron during pregnancy is not established.

Contraindicated the use of the drug Osetron ® during pregnancy and lactation.

APPLICATION FOR FUNCTIONS OF THE LIVER

Patients with impaired renal function change the usual daily dose and the frequency of administration of the drug is not required.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

With moderate or severe impairment of liver function, the clearance of ondansetron is significantly reduced, while its T 1/2 increases, so it is not recommended for such patients to prescribe ondansetron at a dose of more than 8 mg / day.

APPLICATION FOR CHILDREN

It is used in children older than 2 years.

Contraindicated in children under 2 years.

APPLICATION IN ELDERLY PATIENTS

Elderly patients are not required to change the dosage.

SPECIAL INSTRUCTIONS

Patients who had previously had allergic reactions to other selective 5HT 3 receptor blockers have an increased risk of developing them with ondansetron.

Ondansetron can slow the motility of the large intestine, and therefore its appointment to patients with signs of intestinal obstruction requires regular monitoring.

The infusion solution should be prepared immediately before use.
If necessary, the ready-made infusion solution can be stored for up to 24 hours at a temperature of 2-8 ° C at normal illumination.
During the infusion, protection from light is not required;
The diluted injection solution retains its stability for at least 24 hours under natural light or normal light.
OVERDOSE

In cases of suspected overdose, symptomatic therapy is indicated.
The specific antidote is unknown. In case of an overdose of ondansetron, the use of ipecacuanas is not recommended. It is unlikely that this drug will be effective in the period of the antiemetic effect of ondansetron.
DRUG INTERACTION

Because
ondansetron is metabolized by the enzyme system (cytochrome P450) of the liver, caution is required when combined:
- with inducers of cytochrome P450 isoenzymes (CYP2D6 and CYP3A) - barbiturates, carbamazepine, carisoprodol, glutetimide, griseofulvin, dinitrogen oxide, papaverine, phenylbutazone, phenytoin (probably other hydantoins), rifampicin, tolbutamide;

- with inhibitors of isoenzymes P450 (CYP2D6 and CYP3A) - allopurinol, macrolide antibiotics, antidepressants (MAO inhibitors), chloramphenicol, cimetidine, estrogen-containing oral contraceptives, diltiazem, disulfiram, valproic acid and its salts, erythromycin, fluconazole, fluoroquinolones, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil.

Ondansetron at a concentration of 16-160 μg / ml is pharmaceutically compatible and can be injected through the Y-shaped injector intravenously with the following drugs:

- cisplastin (concentration up to 0.48 mg / ml) for 1-8 hours;

- 5-fluorouracil (at a concentration of up to 0.8 mg / ml at a rate of 20 ml / h - higher concentrations may cause precipitation of ondansetron);

- carboplatin (at a concentration of 0.18-9.9 mg / ml for 10-60 min);

- etoposide (in the concentration of 0.14-0.25 mg / ml for 30-60 minutes);

- ceftazidime (in a dose of 0.25-2.0 g in the form of IV bolus injection for 5 minutes);

- cyclophosphamide (in a dose of 0.1-1.0 g as an IV bolus injection for 5 minutes);

- doxorubicin (at a dose of 10-100 mg in the form of IV bolus injection for 5 minutes);

- dexamethasone (possibly iv injection of 20 mg dexamethasone slowly for 2-5 min).
Drugs can be administered through a single dropper, while in a solution, dexamethasone concentrations can range from 32 μg to 2.5 mg / ml, ondansetron from 8 μg to 0.1 mg / ml.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

List B. The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 3 years.
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