Emeset

Emeset has antiemetic properties. It belongs to the group of 5HT3 serotonin ending antagonists.

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Indications Emeseta

It is used to prevent and eliminate vomiting with nausea that occurs due to radiation therapy and cytostatic chemotherapy procedures, as well as vomiting with nausea that occurs after surgical interventions.

Release form

The release is carried out in the form of a medicinal solution for injections. Inside the blister there are 5 ampoules with a capacity of 2 or 4 ml. Inside the box - 1 blister with ampoules.

Pharmacodynamics

Ondansetron is a highly selective antagonist of serotonin 5HT3 endings. Conducting radiotherapy and chemotherapy procedures of a cytostatic nature can lead to an increase in serotonin values - as a result of irritation of the mucous membranes of the small intestine and stomach. This effect causes activation of the action of vagal fibers of the afferent type, which contain 5HT3 endings that provoke a gag reflex. When these fibers are irritated, the serotonin level can also increase inside the area postrema, located in the lower region of the 4th cerebral ventricle. Such an effect also causes vomiting, because it stimulates the 5HT3 endings located there.

Ondansetron slows the onset of the gag reflex by antagonistically acting on 5HT3 endings located in the area of neurons of the PNS and CNS. It seems that this mechanism provides the prevention and elimination of nausea and vomiting caused by cytostatic therapy and surgical intervention.

Pharmacokinetics

After intravenous injection, peak plasma levels are observed after 10 minutes. The level of protein synthesis inside the plasma is 70-76%.

Most of the dose taken is metabolized within the liver.

Less than 5% of the unchanged substance is excreted in the urine. The half-life is approximately 3 hours (in the elderly this figure is 5 hours, and in the case of severe liver disease - 15-32 hours).

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Dosing and administration

The emetogenic potential of cancer treatment varies depending on the dosages and the combination of radiation and chemotherapy regimens used. The choice of treatment regimen depends on the severity of the emetogenic effect.

Radiation and chemotherapy of an emetogenic nature.

The recommended dose for intramuscular or intravenous administration is 8 mg (slow injection rate). The procedure is performed immediately before the start of therapy.

To prevent the development of delayed or prolonged vomiting, the drug should be administered for a maximum of 5 days (rectally or orally) after the first 24 hours.

Emetogenic chemotherapy with a powerful effect.

For individuals undergoing highly emetogenic chemotherapy (e.g., use of cisplatin in large doses), ondansetron may be administered in a single dose of 8 mg (IM or IV) immediately before the chemotherapy procedure. Doses exceeding 8 mg (maximum 32 mg) are permitted to be administered only in the form of an IV infusion (the substance is dissolved in 0.9% isotonic solution (50-100 ml) or another appropriate solvent). Such infusion continues for at least 15 minutes.

Another method is an intramuscular or intravenous injection of 8 mg of the drug at a slow rate, which is carried out immediately before the start of chemotherapy. This is followed by a two-time intravenous or intramuscular administration of 8 mg of the drug (after 2 and 4 hours), or a continuous infusion is carried out lasting 24 hours (dosage 1 mg/hour).

The efficacy of Emeset in highly emetogenic chemotherapy can be increased by an additional single intravenous injection of dexamethasone (20 mg dose) before the chemotherapy procedure.

Use in children.

Children over 4 years of age, whose body surface area is 0.6-1.2 m², may be prescribed a single injection of the drug in a dose of 5 mg/m ², which is administered immediately before the chemotherapy procedure. Then, 12 hours later, Emeset tablets are used in a dose of 4 mg. Oral administration can continue for another 5 days after the end of the therapeutic course.

For children with a body surface area greater than 1.2 m², an initial 8 mg dose should be administered intravenously before the start of chemotherapy. Then, 12 hours later, the patient should take 8 mg tablets. Oral 8 mg doses twice a day can be continued for another 5 days after the end of the course.

Alternatively, the drug in a dose of 0.15 mg/kg (maximum 8 mg) is used as a single injection before the start of the chemotherapy procedure. This dose can be repeated at intervals of 4 hours, but a maximum of 3 times. Oral administration of 4 mg of the drug twice a day can continue for another 5 days after the end of therapy.

Recommended adult dosages should not be exceeded.

To prevent or eliminate postoperative vomiting with nausea in children over 4 years of age who undergo surgery under general anesthesia, the medication is allowed to be administered in doses of 0.1 mg/kg (maximum 4 mg) by slow infusion - before, during, and after the induction of anesthesia.

Vomiting with nausea that occurs after surgery.

To prevent postoperative vomiting with nausea (for adults), a single intramuscular or slow intravenous injection of 4 mg of the drug is required during the process of putting the patient under anesthesia. To remove the unpleasant symptoms described above that have already appeared, 4 mg of the drug must also be administered using the methods indicated above.

Persons with liver failure.

In patients with moderate or severe functional liver disorders, the clearance rate of ondansetron is significantly reduced, while the half-life from blood serum is increased. Such patients should not be administered more than 8 mg of the drug per day.

The drug may be administered intramuscularly into the same area of the body at one time only in doses no greater than 2 ml.

The infusion solution must be administered immediately after its preparation. The following solvents can be used to dissolve the drug:

• 0.9% sodium chloride solution;
• 5% glucose solution;
• Ringer's solution;
• 10% solution of mannitol;
• 0.3% KCl solution with 0.9% sodium chloride infusion solution;
• 0.3% KCl solution with 5% glucose solution.

The medication must not be dissolved using other infusion agents.

Use Emeseta during pregnancy

Emeset should not be administered to nursing mothers or pregnant women.

Contraindications

Hypersensitivity to the components of the drug.

Side effects Emeseta

The use of the drug may cause the occurrence of certain side effects:

• manifestations of allergy: symptoms of immediate intolerance, varying in severity. Anaphylaxis occasionally develops;
• CNS disorders: occurrence of extrapyramidal disorders (for example, oculogyric crisis), headaches, dystonic symptoms without persistent complications, as well as seizures. Dizziness occasionally occurs (in case of rapid injection);
• visual impairment: after intravenous injection, transient visual impairment is observed. Temporary blindness develops occasionally (usually observed in people who received chemotherapy with cisplatin, the duration of which was a maximum of 20 minutes);
• lesions in the cardiovascular system: the appearance of painful sensations in the heart (with or without depression in the ST segment), arrhythmia, facial hyperemia, bradycardia and a feeling of heat, as well as a decrease in pressure;
• problems with respiratory function: the appearance of hiccups;
• digestive disorders: development of constipation;
• hepatobiliary dysfunction: increased functional values of the liver, occurring without symptoms. Such effects are usually observed in people using chemotherapy agents containing cisplatin;
• systemic disorders: appearance of local symptoms at the injection site.

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Overdose

Intoxication is treated as follows: it is necessary to monitor the patient's condition in order to determine the development of symptoms of the disorder in time, and then perform symptomatic procedures taking into account their direction. Emeset has no antidote.

Interactions with other drugs

Ondansetron does not slow down or accelerate the metabolism of other drugs when combined with them. Special tests have shown that the drug does not interact with such substances as furosemide, propofol, temazepam, and tramadol, as well as with alcoholic beverages.

Ondansetron is metabolized by various enzymes of the P450 hemoprotein, as well as elements of CYP3A4 and CYP2D6 with CYP1A2. The diversity of metabolic enzymes allows, in case of a decrease or slowdown in the activity of any of them (for example, a genetic deficiency of the CYP2D6 substance), to compensate for it under standard conditions with other enzymes, due to which this has almost no effect on the overall indicators of CC.

In individuals receiving therapy with agents that potentially induce the CYP3A4 element (such as carbamazepine and phenytoin with rifampicin), an increase in the clearance of ondansetron is observed along with a decrease in its levels in the blood.

Evidence from some clinical tests suggests that Emeset may reduce the pain-relieving effects of tramadol.

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Storage conditions

Emeset should be kept in a dark place, out of reach of children. Temperature indicators should not exceed 25°C.

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Shelf life

Emeset can be used for 3 years from the date of release of the drug.

Application for children

There are only limited data on the use of drugs in children under 4 years of age.

Analogues

The following medications are analogs of the drug: Domegan and Granitron with Zofran and Zoltem, and in addition to this Zofetron, Omtron and Navoban with Isotron, as well as Ondansetron and Tropisetron. In addition, the list includes Osetron, Emetron, Setronon and Emtron with Emesetron.

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Reviews

Emeset has a highly effective effect, eliminating vomiting and nausea that occur after chemotherapy procedures. Reviews from many patients indicate that the drug really helps eliminate these disorders.