LATRAN AMPOULES 0,2% 2ML

After oral administration, Tcmax - 1.5 hours. After rectal administration of 16 mg, ondansetron is determined in plasma in 15-60 minutes. The concentration of the active substance increases linearly, TCmax is reached in about 6 hours and is 20-30 ng / ml. The decrease in plasma concentration occurs at a slower rate than after ingestion (due to continued absorption). Absolute bioavailability with rectal administration is approximately 60% and does not depend on gender. After i / m administration TCmax - 10 min. The volume of distribution, both after ingestion and after parenteral administration, is 140 liters. Communication with plasma proteins - 70-76%.Metabolized in the liver with the participation of microsomal enzymes (cytochrome P450). Both after oral administration and after parenteral administration, T1 / 2 is 3 hours. After rectal administration, T1 / 2 is determined by the rate of ondansetron absorption, not by systemic clearance, and is approximately 6 hours. Less than 5% of the injected doses. The pharmacokinetic parameters of ondansetron do not change with its repeated administration. In patients with moderate renal insufficiency (CC 15–60 ml / min), both systemic clearance and volume of distribution are reduced, resulting in a small and clinically insignificant increase in T1 / 2. The pharmacokinetics of ondansetron practically does not change in patients with severe impaired renal function on chronic hemodialysis (the studies were conducted in the intervals between hemodialysis sessions). In patients with severe impaired liver function T1 / 2 - 15-20 hours. With a slow metabolism of spartein and debrisoquine, T1 / 2 of ondansetron does not change regardless of the route of administration. In elderly patients after oral administration or parenteral administration, T1 / 2 may increase up to 5 hours.

Indications and usage

Nausea and vomiting caused by cytotoxic chemotherapy or radiotherapy; postoperative nausea and vomiting - prevention and treatment.

Contraindications

Hypersensitivity, pregnancy, lactation. With care - children's age (up to 2 years - the lack of sufficient experience).

The choice of dosing regimen is determined by the emethogenicity of antitumor therapy. For adults, the daily dose is 8-32 mg / day, the following regimens are recommended: For moderately emethogenic chemotherapy or radiotherapy, 8 mg IV jet stream slowly or intramuscularly, immediately before the start of therapy. In case of high-efficacy chemotherapy: 8 mg is introduced into a jet stream slowly 8 mg immediately before the start of chemotherapy, and then 8 mg every 2–4 hours; or iv drip continuously at a rate of 1 mg / h for 24 h; or drip directly before chemotherapy at a dose of 16-32 mg, diluted in 50-100 ml of the appropriate infusion solution, for 15 minutes. The effectiveness of odanetron can be increased by a single intravenous injection of GCS (for example, 20 mg of Dexamethasone sodium phosphate) before the start of chemotherapy. To prevent delayed vomiting that occurs after 24 hours from the start of chemotherapy or radiotherapy, it is recommended to take the drug in pill form when using highly emetic and moderate emetic therapy. For oral administration: Adults, for the prevention of nausea and vomiting on the background of chemotherapy or radiotherapy, ondansetron is prescribed at 8 mg for 1-2 hours before the start of antitumor therapy followed by further 8 mg orally after 12 hours. For the prevention of late (after 24 hours ) or prolonged vomiting should continue taking 8 mg 2 times a day for 5 days after the end of the course of antitumor therapy. To enhance the effect, a single dose can be increased to 24 mg and administered simultaneously with 12 mg of dexamethasone phosphate (in the form of sodium salt) 1-2 hours before the start of chemotherapy.Children older than 2 years: Assign IV body dose of 5 mg / m2 immediately before chemotherapy, followed by oral administration at a dose of 4 mg after 12 hours. After completing the course of chemotherapy, ondansetron should be continued at a dose of 4 mg 2 times a day within 5 days. Prevention of postoperative nausea and vomiting: Adults are administered during the initial anesthesia in an IM or IV (slow) dose of 4 mg. For the treatment of nausea and vomiting, it is recommended IM or IV slow injection of 4 mg of the drug. V / m in one the same area of ​​the body ondansetron can be administered in a dose not exceeding 4 mg. For the prevention of postoperative nausea and vomiting, ondansetron is used exclusively for parenteral children, in a single dose of 0.1 mg / kg (up to a maximum of 4 mg) slowly intravenously before or after anesthesia. For the treatment of developed postoperative nausea and vomiting in children, a slow intravenous dose of 0.1 mg / kg (up to a maximum of 4 mg) is recommended. With regard to the prevention and treatment of postoperative nausea and vomiting in children under 2 years of age, there is not enough experience. With kidney damage and in elderly patients, the correction of the usual daily dose and frequency of drug administration is not required. If the liver is damaged, the ondansetron clearance is significantly reduced, its T1 / 2 from plasma increases, and the dose is reduced to 8 mg / day.

Adverse reactions

Allergic reactions: urticaria, bronchospasm, laryngism, angioedema, anaphylaxis. Local reactions: hyperemia, pain, burning at the injection site.On the part of the digestive system: hiccups, dry mouth, diarrhea, constipation, sometimes asymptomatic transient increases in serum aminotransferase levels. Since the cardiovascular system: pain in the chest, in some cases with ST depression, arrhythmias, bradycardia, decreased blood pressure. Nervous system disorders: headache, dizziness, spontaneous motor disorders, and convulsions. Others: flushing, feeling hot, temporary visual acuity, hypokalemia, hypercreatininemia.

Special notes

Patients who have previously had allergic reactions to other selective antagonists of 5HT3 receptors have an increased risk of their development against ondansetron. Ondansetron can slow down the motility of the large intestine, and therefore its administration to patients with signs of intestinal obstruction requires special observation. Infusion solution is prepared immediately before use. If necessary, it can be stored for 24 hours at a temperature of 2-8 degrees C in normal light. No protection from light is required during the infusion; The diluted injection solution maintains its stability for at least 24 hours in natural light or normal light. The following solutions can be used for preparing an infusion solution: 0.9% sodium chloride solution, 5% dextrose solution, 10% mannitol solution, Ringer's solution, 0.3% potassium chloride solution and 0.9% sodium chloride solution, 0.3% potassium chloride solution and 5% dextrose.Lingual pills contain aspartame; this must be considered when prescribing patients with phenylketonuria.

Drug Interactions

It requires caution when used together: with inducers of cytochrome P450 (CYP2D6 and CYP3A) - barbiturates, Carbamazepine, carisoprodol, glutethimide, Griseofulvin, nitrous oxide, papaverine, phenylbutazone, phenytoin (probably, hydantoins, hyphentoins, ripheverin, nitrified acid, papaverine, phenybutazone, phenytoin (probably also other hydantoins, nitrous oxide, papaverine, phenylbutazone, phenytoin (probably also other hydantoins), intodispants, intoxico); with the P450 inhibitors (CYP2D6) and alpurinol, macrolide antibiotics, antidepressants, MAO, chloramphenicol and omega, anesthetics, lovastatin, Metronidazole, Omeprazole, propranolol, quinidine, quinine, Verapamil . Ondansetron at a concentration of 16-160 µg / ml is pharmaceutically compatible and can be administered via a Y-shaped injector in / in a drip together with the following drugs: cisplastin (at a concentration of 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 of 5-fluorouracil may cause precipitation of odninetron); carboplatin (at a concentration of 0.18–9.9 mg / ml for 10–60 min); etoposide (at a concentration of 0.14–0.25 mg / ml for 30–60 min; ceftazidime (at a dose of 0.25–2 g, in the form of iv bolus injection for 5 min); cyclophosphamide (at a dose of 0.1–1 g, as a iv bolus injection over 5 min; doxorubicin (at a dose of 10-100 mg, as a iv bolus injection over 5 min); dexamethasone — possibly i.v. administration of 20 mg of dexamethasone sodium phosphate, slowly, for 2-5 minutesThey can be administered through a single dropper, while in a solution the concentrations of dexamethasone phosphate (in the form of sodium salt) can be from 32 μg to 2.5 mg / ml, ondansetron - from 8 μg to 1 mg / ml.

In the dark place at a temperature of no higher than 25 ° C. Shelf life - 3 years.

Latran