Domegan - instructions for use, dose, side effects, contraindications

active substance: ondansetron (in the form of ondansetron hydrochloride dihydrate) 2 mg Excipients: sodium chloride, citric acid monohydrate, sodium citrate dihydrate, water for injection.

Description:

Clear colorless liquid

Pharmacotherapeutic group:antiemetics, serotonin receptor antagonist.

ATX: & nbsp

A.04.A.A.01 Ondansetron

Pharmacodynamics:

Ondansetron is a selective receptor antagonist 5HT3 (serotonin). Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in the level of serotonin, which by activation of vagal afferent fibers containing receptors 5-HTs, causes a vomitive reflex. Ondansetron inhibits the appearance of a vomiting reflex by blockade of receptors 5-HTZ at the level of neurons of both the central and peripheral nervous system.

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

Pharmacokinetics:

With intramuscular injection, the peak concentration in plasma is reached within 10 minutes.The distribution of ondansetron is the same for intramuscular and intravenous administration. 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.

Half-life with parenteral administration is about 3 hours, in elderly patients can reach 5 hours, and with severe hepatic insufficiency - 15-20 hours. With kidney damage (renal clearance less than 15 ml / min), the elimination half-life increases by 4-5 hours, but this increase is not clinically significant.

Indications:

- Prevention and elimination of nausea and vomiting caused by cytostatic chemotherapy and radiotherapy

- Prevention and treatment of postoperative nausea and vomiting.

Contraindications:

- Hypersensitivity to any component of the drug

- Pregnancy and lactation.

Carefully:children's age up to 2 years (lack of sufficient experience of application)

Pregnancy and lactation:contraindicated

Dosing and Administration:

The drug is administered intravenously or intramuscularly.

Cytostatic therapy

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

For adults the daily dose, as a rule, is 8-32 mg, the following regimens are recommended:

With moderately-emetogenic chemotherapy or radiotherapy:

-8 mg intravenously struino slowly or intramuscularly, immediately before the start of therapy;

With highly emeticogenic chemotherapy:

- 8 mg intravenously struino slowly just before the start of chemotherapy, and then two more 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, as a 15-minute infusion, immediately before the start of chemotherapy.

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

Children

Children older than 2 years of the drug is administered at a dose of 5 mg / m² surface of the body intravenously, immediately before the start of chemotherapy.

Prevention of postoperative nausea and vomiting

Adults Introduce a single dose of 4 mg intramuscularly or intravenously struino (slowly) at the beginning of anesthesia.

For relief of nausea and vomiting it is recommended intramuscular or slow intravenous injection of 4 mg of the drug.

Intramuscularly in the same body region ondansetron can be administered at a dose not exceeding 4 mg!

Children to prevent postoperative nausea and vomiting 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, a slow intravenous injection of a single dose of the drug 0.1 mg / kg (maximum 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 renal lesions

With renal damage, the usual daily dose and frequency of administration of the drug is not required.

With liver damage significantly reduces the clearance of ondansetron, and the half-life of it is increased from the plasma, so it is necessary to reduce the dose to 8 mg per day.

To dilute the injection solution, the following solutions can be used:

0.9% solution of sodium chloride,

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 effects:

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

From the digestive system: hiccough, dry mouth, constipation or diarrhea, sometimes an asymptomatic transient increase in serum aminotransferase activity.

From the cardiovascular system: pain in the chest, in some cases with depression of the segment S-T, 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: "tide" of blood to the face, a feeling of heat, a temporary violation of visual acuity, hypokalemia.

Overdose:

In cases of suspected overdose, symptomatic therapy is indicated. The specific antidote is unknown.

Interaction:

As 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, glutethimide, 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, cimetidine, oral contraceptives containing estrogens, diltiazem, disulfiram, valproic acid, sodium valproate, 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 administered via Y-injector intravenously (IV) drip along with the following drugs (LC):

- cisplatin (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 may cause precipitation of ondansetron);

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

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

- ceftazidime (in a dose of 0.25-2 g, as an IV bolus injection for 5 minutes);

- cyclophosphamide (in a dose of 0.1-1 g, as an IV bolus injection for 5 minutes);

- doxorubicin (in a dose of 10-100 mg, as an IV bolus injection for 5 minutes);

- dexamethasone: possible iv injection of 20 mg dexamethasone slowly, for 2-5 minutes. LC can be administered through a single dropper, while in the solution the concentrations of dexamethasone can range from 32 μg to 2.5 mg / ml, ondansetron - from 8 μg to 0.1 mg / ml.

Special instructions:

In patients who have previously experienced other hypersensitivity reactions with other selective 5HT3 receptor antagonists, similar reactions may also occur with the use of Domegan.

Since the Domegan slows the bowel motility, 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 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.

Form release / dosage:A solution for intravenous and intramuscular injection of 4 mg / 2 ml or 8 mg / 4 ml (2 mg / ml) in bottles of dark glass, ukuporennyh rubber lid, obkatannye aluminum cap and closed with a plastic lid.

Packaging:

5 vials with instructions for use in a cardboard pack.

Storage conditions:

In the dark place at a temperature of 15 to 30 ° C. Do not freeze Keep out of the reach of children!

Shelf life:

2 years.

The drug should not be used after the expiry date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003330/09

Date of registration:30.04.2009

The owner of the registration certificate: Genfa Medica S.A. Genfa Medica S.A. Switzerland

Manufacturer: & nbsp

GENFA MEDICA, S.A. Canada

Representation: & nbspHEAD OF MEDICA SAHEAD OF MEDICA SASwitzerland

Information update date: & nbsp30.04.2009

Illustrated instructions

Instructions

Domegan (Domegan)