Ameset

Emeset has antiemetic properties. It is included in the group of antagonists of 5HT3 serotonin endings.

[1], [2]

Indications of the ameseta

It is used to prevent and eliminate emesis with nausea arising from radiotherapy and chemotherapy procedures of a cytostatic nature, and in addition to vomiting with nausea arising after surgical interventions.

Release form

The release is carried out in the form of a therapeutic solution for injections. Inside the blister contains 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. Carrying out procedures of radiotherapy and chemotherapy of a cytostatic nature can lead to an increase in serotonin values - as a result of irritation of the small intestine and stomach mucosa. This effect causes the activation of the action of vagal fibers of the afferent type, inside which there are 5HT3 endings, provoking a vomiting reflex. If these fibers are irritated, the serotonin index within the area postrema located in the lower region of the 4th cerebral ventricle can also increase. This effect also causes vomiting, because it stimulates the endings of 5HT3 located there.

Ondansetron slows the onset of the emetic reflex, antagonizing the 5HT3 endpoints located in the neuronal region of the PNS and CNS. It seems that this particular mechanism provides the prevention and elimination of nausea with vomiting, caused by cytostatic therapy and surgical intervention.

Pharmacokinetics

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

Most of the portion used is metabolized inside the liver.

Less than 5% of unchanged substance is excreted in urine. Half-life is approximately 3 hours (in elderly people this figure is 5 hours, and in the case of hepatic pathology in a severe degree - 15-32 hours).

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Dosing and administration

The emetogenic potential for the treatment of cancer varies with the size of dosages, as well as a combination of radiotherapy and chemotherapy. Selection of the treatment scheme depends on the strength of the expression of the emetogenic effect.

Radiation and chemotherapy of an emetic nature.

The recommended amount for IM or IV injection is 8 mg (slow injection rate). The procedure is carried out immediately before the start of therapy.

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

Emetogenic chemotherapy with a powerful effect.

People who undergo high-emetic chemotherapy (for example, the use of cisplatin in large portions), ondansetron can be administered in the amount of 8 mg once (IM or IV), immediately before the chemotherapeutic procedure. Portions exceeding 8 mg (maximum 32 mg) are allowed to be used exclusively in the form of IV infusion (the substance is dissolved in 0.9% isotonic solution (50-100 ml) or other appropriate solvent). This infusion lasts at least 15 minutes.

Another method is in / m or IV injection of 8 mg of medication at a slow speed, which is performed immediately before the start of chemotherapy. Then follows a two-time IV or IM injection of 8 mg of the drug (after 2 and 4 hours), or a continuous infusion takes place, lasting 24 hours (dosage of 1 mg / hour).

The effectiveness of the Emset effect in chemotherapy of a highly emetic nature can be increased by an additional single intravenous injection of dexamethasone (a dose of 20 mg) before the chemotherapy procedure.

Use in children.

Children older than 4 years of age, whose body surface area is 0.6-1.2 m², can be prescribed a one-time injection of LS in a dose of 5 mg / m ², which is administered immediately before the chemotherapy procedure. Further, after 12 hours, Emeset tablets are used in a dose of 4 mg. Ingestion can last for another 5 days after the end of the therapeutic course.

Children who have a body surface area greater than 1.2 m² should be administered iv injection at an initial dose of 8 mg before starting chemotherapy. Further, after 12 hours, the patient should take the tablet in a dose of 8 mg. The consumption of 8 mg twice a day can be continued for another 5 days after the end of the course.

As an alternative medicine in a dose of 0.15 mg / kg (maximum 8 mg) is used in the form of a single injection before the start of the chemotherapy procedure. This portion is allowed to repeat at intervals of 4 hours, but a maximum of 3 times. Oral administration of 4 mg of the drug twice a day can last for another 5 days after the end of therapy.

Recommended adult dosages can not be exceeded.

To prevent or eliminate nausea after surgery, children under 4 years of age who are under general anesthesia are allowed to take a medication in a dose of 0.1 mg / kg (maximum 4 mg) with a slow infusion - before, during , and also after induction of anesthesia.

Vomiting with nausea, appearing after operations.

To prevent the occurrence of postoperative vomiting with nausea (an adult), one-time IV / m or slow iv injection of 4 mg of medication is required during the patient's injection into anesthesia. To remove already appeared above described unpleasant symptoms, you also need to enter the above methods, 4 mg of the drug.

Persons with liver failure.

In people with functional hepatic disorders of moderate or severe nature, the ondansetron clearance rate significantly decreases, and the half-life of blood serum increases on the contrary. Such patients should not administer more than 8 mg of medication per day.

Intramuscularly in the same area of the body, the drug is allowed to be administered momentarily exclusively in a dose not exceeding 2 ml.

Infusion solution is required to be administered immediately after its manufacture. To dissolve the drug, the following solvents can be used:

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

The drug is not allowed to dissolve with other infusion agents.

Use of the ameseta during pregnancy

It is forbidden to appoint Emeset to nursing mothers or pregnant women.

Contraindications

Hypersensitivity to the components of the drug.

Side effects of the ameseta

The use of a medicine can cause the appearance of certain side-effects:

• manifestations of allergy: symptoms of intolerance of the immediate type, having a different degree of severity. Occasionally anaphylaxis develops;
• disorders in the CNS: the appearance of extrapyramidal disorders (eg, oculogic crisis), headaches, dystonic symptoms without persistent complications, as well as seizures. Occasionally there is dizziness (in case of rapid injection);
• disturbances of visual function: after intravenous injection there is a transient weakening of vision. Temporary blindness develops occasionally (it is usually observed in people who received chemotherapy with cisplatin, the duration of which was a maximum of 20 minutes);
• lesions in the CCC region: the appearance of pain in the heart (with or without depression in the ST segment), arrhythmias, facial hyperemia, bradycardia and a feeling of heat, and in addition, a decrease in pressure;
• problems with respiratory function: the appearance of hiccups;
• digestive disorders: development of constipation;
• disturbances in the function of the hepatobiliary system: an increase in the functional values of the liver, proceeding without symptoms. Similar effects are usually observed in people who use chemotherapy as a substance with cisplatin;
• systemic disorders: appearance of local symptoms at the site of injection.

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Overdose

Intoxication is treated as follows - you need to monitor the patient's condition in time to determine the development of symptoms of the disorder, and then perform symptomatic procedures with regard to their focus. Emeseth has no antidote.

Interactions with other drugs

Ondansetron does not have a slowing or accelerating effect on the metabolism of other drugs when combined with them. Special tests showed that the drug does not interact with substances such as furosemide, propofol, temazepam, as well as tramadol, and also with alcoholic beverages.

Metabolism of ondansetron occurs with the participation of different enzymes of the hemoprotein P450, and in addition the elements CYP3A4 and CYP2D6 with CYP1A2. The variety of metabolic enzymes allows, in case of a decrease or slowdown in the activity of any of them (for example, genetic deficiency of CYP2D6 substance) under standard conditions to compensate it with other enzymes, due to what it almost does not affect the overall QC values.

People who use therapy with potentially CYP3A4-inducing agents (such as carbamazepine and phenytoin with rifampicin) have increased ondansetron clearance with decreased blood counts.

The information obtained after some clinical tests shows that Emeset can weaken the analgesic effect of tramadol.

[5], [6]

Storage conditions

The emulsion should be kept in a dark place, closed from the access of children. Temperature values are not higher than 25 ° C.

[7]

Shelf life

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

Application for children

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

Analogues

Analogues of the drug are the following drugs: Domegan and Granitron with Zofran and Zoltem, and in addition Zofetron, Omstron and Navoban with Isotron, and Ondansetron and Tropisetron. In addition, the list includes Osetron, Emetron, Stronon, and Emtron with Emesteron.

[8]

Reviews

Emeset has a highly effective effect, eliminating vomiting with nausea that occur after chemotherapy procedures. The reviews of many patients indicate that the drug really helps to eliminate these disorders.