Composition, form of production and packaging
Tablets 1 tab.
ondansetron 4 mg
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings without cell contour (1) - packs cardboard.
Solution for intravenous and / m introduction 1 ml
ondansetron (in the form of hydrochloride dihydrate) 2 mg
2 ml - ampoules of colorless glass (5) - packings contour mesh (1) - packs cardboard.
4 ml - ampoules of colorless glass (5) - packings contour mesh (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Ondansetron is a selective 5HT 3 receptor antagonist (serotonin). Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in the level of serotonin, which, by activating vagal afferent fibers containing 5-HT 3 receptors, causes a vomiting reflex. Ondansetron inhibits the appearance of a vomiting reflex by blocking the 5-HT 3 receptors at the level of the neurons of both the central and peripheral nervous system.
This mechanism of action is based on the prevention and treatment of post-operative and cytostatic chemo- and radiotherapy-induced vomiting and nausea.
PHARMACOKINETICS
With intramuscular injection, C max in plasma is achieved within 10 minutes. The distribution of ondansetron is the same for intramuscular and intravenous administration. After ingestion C max of ondansetron in the blood plasma is achieved after about 1.5 hours. Absolute bioavailability is about 60%. The drug is metabolized in the liver. The binding with plasma proteins is 70-76%. Less than 5% of the drug is excreted unchanged in urine.
Both after ingestion and parenteral administration, T 1/2 is about 3 hours, in elderly patients it can reach 5 hours, and with severe hepatic insufficiency - 15-20 hours. In case of kidney damage (renal clearance less than 15 ml / min) T 1/2 increases by 4-5 h, but this increase is not clinically significant.
INDICATIONS
- prevention and elimination of nausea and vomiting caused by cytostatic chemotherapy and / or radiotherapy, as well as postoperative nausea and vomiting.
DOSING MODE
Cytostatic therapy
The choice of the dosage regimen is determined by the severity of the emetogenic effect of the antitumor therapy.
For adults, the daily dose, as a rule, is 8-32 mg, the following regimens are recommended:
With moderate emetogenic chemotherapy or radiotherapy:
- 8 mg intravenously struino slowly or intramuscularly, immediately before the start of therapy;
- 8 mg orally for 1 to 2 hours before the start of therapy, then 8 mg orally 12 hours after the start of therapy.
With highly emeticogenic chemotherapy:
- 8 mg intravenously slowly before the start of chemotherapy, and then two further intravenous 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 Lazaran BM can be increased by a single intravenous glucocorticoid (eg, 20 mg dexamethasone) prior to chemotherapy; when ingested to enhance the effect of a single dose can be increased to 24 mg and administered simultaneously with 12 mg of dexamethasone 1-2 hours before the start of chemotherapy. To prevent delayed (occurring after 24 hours after the initiation of chemotherapy or radiotherapy) vomiting, it is recommended to continue the use of the drug in the form of tablets 8 mg twice a day for 5 days.
Children
Children older than 2 years of the drug is administered at a dose of 5 mg / m2 body surface intravenously, immediately before the start of chemotherapy, followed by oral administration in the vine 4 mg after 12 hours; after the end of chemotherapy, it is recommended to continue treatment at 4 mg twice daily for 5 days.
Prevention of postoperative nausea and vomiting
Adults injected a single dose of 4 mg intramuscularly or intravenously slowly at the beginning of anesthesia, or prescribed 16 mg orally 1 hour prior to the onset of anesthesia.
For relief of nausea and vomiting, intramuscular or slow intravenous administration of 4 mg of the drug is recommended.
Intramuscularly into the same site of the body, Lazaran BM can be administered at a dose not exceeding 4 mg!
For children to prevent postoperative nausea and vomiting, Lazaran BM is used exclusively parenterally at a single dose of 0.1 mg / kg (maximum 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 intravenous administration of a single dose of the drug 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
Dosage adjustments are not required.
Patients with kidney and liver lesions
With renal damage, the usual daily dose and frequency of administration of the drug is not required.
With liver damage, the clearance of Lazaran BM significantly decreases, and the half-life of it is increased from the plasma, therefore, do not exceed the daily dose of 8 mg per 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, diarrhea, constipation, sometimes asymptomatic transient increase in the level of aminotransferases in the blood serum.
From the side of 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: pain, burning and redness at the injection site.
Other: a rush of blood to the face, a feeling of heat, a temporary disturbance of visual acuity, hypokalemia.
CONTRAINDICATIONS
- pregnancy and the period of breastfeeding;
- Children under 2 years of age (safety and efficacy have not been studied;
- Hypersensitivity to ondansetron or any other component of the drug.
PREGNANCY AND LACTATION
Contraindicated in pregnancy and during lactation.
APPLICATION FOR FUNCTIONS OF THE LIVER
With renal damage, the usual daily dose and frequency of administration of the drug is not required.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With liver damage, the clearance of Lazaran BM decreases, and the half-life of it is increased from the plasma, so do not exceed the daily dose of 8 mg per day.
APPLICATION FOR CHILDREN
Contraindicated in children under 2 years.
APPLICATION IN ELDERLY PATIENTS
In elderly patients, dosage changes are not required.
SPECIAL INSTRUCTIONS
In patients who previously had other sensitivity selective antagonists of 5HT 3 receptors, reactions of increased sensitivity were observed, similar reactions may also occur with the use of Lazaran BM.
Since Lazaran VM slows the bowel motility, patients with signs of intestinal obstruction after using the drug require special observation. 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 В° C.
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. In case of an overdose of ondansetron tablets, the use of ipecacuanas is not recommended, since it is unlikely that this drug will be effective during the antiemetic activity of the drug. The specific antidote is not known.
DRUG INTERACTION
Since ondansetron is metabolized by the enzyme system (cytochrome P450) of the liver, caution is required when combined:
- with enzymatic inducers P450 (CYP2D6 and CYP3A) - barbiturates, carbamazepine, carisoprodol, glutetimide, griseofulvin, dinitrogen oxide, papaverine, phenylbutazone, phenytoin (probably other hydantoins), rifampicin. tolbutamide;
- with inhibitors of enzymes P450 (CYP2D6 and CYP3A) - allopurinol. macrolide antibiotics, antidepressants - MAO inhibitors, chloramphenicol, cymidine, oral contraceptives containing estrogens, diltiazem, disulfiram, valproic acid, sodium valproate, erythromycin, fluconazole, fluoroquinolones, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, nerapamil,
Lazaran BM at a concentration of 16-160 Ојg / 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 Lazaran BM);
- 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, as an intravenous bolus injection for 5 minutes);
- cyclophosphamide (in a dose of 0.1-1.0 g, as an intravenous bolus injection for 5 minutes);
- doxorubicin (in a dose of 10-100 mg, as an intravenous bolus injection for 5 minutes);
- dexamethasone: possible intravenous administration of 20 mg dexamethasone slowly, for 2-5 minutes. Drugs can be administered through a single dropper, while the concentration of dexamethasone sodium phosphate in the solution can range from 32 Ојg to 2.5 mg / ml, Lazaran BM from 8 Ојg to 1 mg / ml.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
List B. Tablets: at a temperature of 15 to 25 В° C in a dry, dark place out of the reach of children. Solution for intravenous and intramuscular administration: at a temperature of 15 to 25 В° C in a dark place out of the reach of children.
Shelf life of the tablets is 3 years, the solution for intravenous and intramuscular injection is 2 years.
