Emetron, 2 mg/ml 4 ml 5 pcs

Pharmacodynamics

The anti-emetic drug of central action. Ondansetron is a selective serotonin 5NT3 receptor antagonist. Cytostatic chemotherapy drugs and radiotherapy may increase serotonin levels which, by activation of vagal afferent fibers containing serotonin 5NT3 receptors, causes the gag reflex. Ondansetron inhibits the onset of the gag reflex by blockade of serotonin 5NT3 receptors at the neuronal level of both the central and peripheral nervous system.

This mechanism of action appears to be the basis for the prevention and treatment of postoperative vomiting and nausea caused by cytostatic chemotherapy and radiotherapy.

Pharmacokinetics

Introduction Cmax is measured within 10 min of injection. The distribution of ondansetron is the same when administered v/m and intravenously. After oral administration Cmax of ondansetron in blood plasma is reached after about 1.5 hours. Absolute bioavailability after oral administration is about 60%. The drug is metabolized in the liver. Binding with plasma proteins is 70-76%. With urine, less than 5% of the drug is excreted unchanged.

After oral and parenteral administration T1/2 is about 3 hours, in elderly patients it can be up to 5 hours, and in case of severe hepatic insufficiency – 15-22 hours. In renal impairment (renal clearance less than 15 ml/min) the T1/2 is increased by 4-5 hours, but this increase is of no clinical significance.

Indications

Prevention and elimination of nausea and vomiting caused by cytostatic chemotherapy and radiotherapy, as well as postoperative nausea and vomiting.

Pharmacological effect

Pharmacodynamics

Centrally acting antiemetic drug. Ondansetron is a selective serotonin 5HT3 receptor antagonist. Cytostatic chemotherapy drugs and radiotherapy can cause an increase in serotonin levels, which, by activating vagal afferent fibers containing serotonin 5HT3 receptors, causes the gag reflex. Ondansetron inhibits the appearance of the gag reflex by blocking the serotonin 5HT3 receptor at the level of neurons in both the central and peripheral nervous systems.

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

Pharmacokinetics

With intramuscular administration, Cmax is measured within 10 minutes after injection. The distribution of ondansetron is the same with IM and IV administration. After oral administration, Cmax of ondansetron in the blood plasma is reached in approximately 1.5 hours. Absolute bioavailability after oral administration is about 60%. The drug is metabolized in the liver. Plasma protein binding is 70-76%. Less than 5% of the drug is excreted unchanged in the urine.

Both after oral administration and with parenteral administration, T1/2 is about 3 hours, in elderly patients it can reach 5 hours, and with severe liver failure – 15-22 hours. With kidney damage (renal clearance less than 15 ml/min), T1/2 increases by 4-5 hours, but this increase has no clinical significance.

Special instructions

Patients who have previously experienced hypersensitivity reactions when using other selective serotonin 5HT3 receptor antagonists may also develop similar reactions when using ondansetron.

Because Ondansetron causes constipation; patients with signs of intestinal obstruction after using the drug require regular monitoring.

The infusion solution must be prepared immediately before use. If necessary, the prepared infusion solution can be stored until use for a maximum of 24 hours at a temperature of 2-8°C.

No protection from light is required during the infusion; The diluted injection solution remains stable for at least 24 hours in natural light or artificial light.

If you have lactose intolerance, please note that a 4 mg tablet contains 59.25 mg of lactose, 8 mg – 118.5 mg, respectively.

Impact on the ability to drive vehicles and other mechanisms that require increased concentration

Does not have a sedative effect and does not affect the psychomotor abilities necessary to drive a car and other mechanisms.

Active ingredient

Ondansetron

Composition

1 ml (1 ampoule) contains:

Active ingredients:

ondansetron hydrochloride dihydrate 2.5 mg (10 mg), which corresponds to the content of ondansetron 2 mg (8 mg).

Excipients:

sodium citrate – 1.6 mg,

citric acid monohydrate – 2.2 mg,

sorbitol – 192 mg,

water for d/i – up to 4 ml.

The ampoule contains 4 ml of solution.

There are 5 ampoules in a cardboard package.

Pregnancy

Contraindicated during pregnancy and breastfeeding.

Contraindications

Pregnancy;
lactation period;
children under 2 years of age (safety and effectiveness of use have not been studied);
hypersensitivity to any component of the drug.

Side Effects

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

From the digestive system: hiccups, dry mouth, diarrhea, constipation; sometimes – an asymptomatic transient increase in the level of aminotransferases in the blood serum.

From the cardiovascular system: chest pain, in some cases with ST segment depression, arrhythmias, bradysardia, decreased blood pressure.

From the central nervous system: headache, dizziness, spontaneous movement disorders and convulsions. Local reactions: pain, burning and redness at the injection site.

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

Interaction

Because Ondansetron is metabolized by the enzyme system (cytochrome P450) of the liver, caution is required when used together:

with P450 enzymatic inducers (CYP2D6 and CYP3A) (barbiturates, carbamazepine, carisoprodol, glutethimide, griseofulvin, nitrous oxide, papaverine, phenylbutazone, phenytoin (probably other hydantoins), rifampicin, tolbutamide);
with inhibitors of P450 enzymes (CYP2D6 and CYP3A) (allopurinol, macrolide antibiotics, antidepressants – MAO inhibitors, chloramphenicol, cimetidine, oral contraceptives containing estrogens, diltiazem, disulfiram, valproic acid, sodium valproate, erythromycin, fluconazole, fluoroquinolopes, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil).

Does not interact with ethanol, temazepam, furosemide, tramadol and propofol.

Ondansetron at a concentration of 16-160 mcg/ml is pharmaceutically compatible with the following drugs that can be administered through a Y-shaped injector:

cisplastin (at a concentration of up to 0.48 mg/ml) for 1-8 hours;
5-fluorouracil (at concentrations up to 0.8 mg/ml at a rate of 20 ml/h – higher concentrations may cause ondansetron to precipitate);
carboplatin (at a concentration of 0.18-9.9 mg/ml for 10-60 minutes);
etoposide (at a concentration of 0.14-0.25 mg/ml for 30-60 minutes);
ceftazidime (at a dose of 0.25-2 g, as an intravenous bolus injection over 5 minutes); cyclophosphamide (in a dose of 0.1-1 g, as an intravenous bolus injection over 5 minutes);
doxorubicin (at a dose of 10-100 mg, as an intravenous bolus injection over 5 minutes);
dexamethasone: it is possible to administer 20 mg of dexamethasone slowly over 2-5 minutes. Medicines can be administered through one dropper, and in solution the concentration of dexamethasone sodium phosphate can range from 32 μg to 2.5 mg/ml, ondansetron – from 8 μg to 1 mg/ml.

Overdose

In cases of suspected overdose, symptomatic therapy is indicated. A specific antidote is not known.

Storage conditions

The solution for injection is stored at a temperature of 15-30°C in a place protected from light, out of reach of children.

Shelf life

4 years.

Manufacturer

Gedeon Richter, Hungary