Emetron

Emetron is an antiemetic drug that helps relieve nausea.

Indications Emetrona

It is used to eliminate vomiting with nausea that occurs due to radiotherapy or cytostatic chemotherapy procedures, and also to prevent and eliminate vomiting with nausea that develops after surgical operations.

Release form

It is released in the form of a solution, in ampoules of 4 ml. There are 5 such ampoules inside the box.

Pharmacodynamics

Ondansetron is a highly selective antagonist of endings (5-HT3). There is no precise information regarding the mechanism that allows the drug to reduce vomiting with nausea. Chemotherapeutic drugs of a cytostatic nature, as well as radiotherapy, can lead to an increase in serotonin levels in the small intestine. And this element, activating the vagus fibers of the afferent type, which contain endings of 5-HT3, stimulates the vomiting reflex. The drug prevents the development of this reflex.

As a result of the excitation of the activity of afferent fibers in the vagus nerve area, it is possible to increase serotonin levels in the area postrema, located in the lower region of the 4th cerebral ventricle. This process, through the 5-HT3 endings, also provokes vomiting. The antagonistic effect exerted by ondansetron on the 5-HT3 endings located inside the neurons of the central and peripheral nervous systems prevents the development of vomiting. This mechanism is similar to that which acts in the treatment or prevention of the development of postoperative vomiting or nausea (under the influence of cytostatics).

The medicinal element does not affect plasma prolactin levels.

Pharmacokinetics

The distribution of the drug after oral administration, intravenous administration, or intramuscular administration has the same parameters. The terminal half-life is approximately 3 hours, and the equilibrium distribution volume is approximately 140 liters.

The level of synthesis with plasma protein is approximately 70-76%.

Excretion of the substance from the systemic circulation occurs through multiple metabolic processes involving enzymes, primarily within the liver. Less than 5% of the unchanged component is excreted in the urine.

The absence of the CYP2D6 enzyme (polymorphism in relation to the cleavage of debrisoquine) does not affect the pharmacokinetic characteristics of ondansetron. Changes in these parameters are not observed with repeated injection of the drug.

Efficacy tests in children involving 21 children aged 3 to 12 years who underwent planned surgery under anesthesia showed that after a single dose of the drug (2 mg for children aged 3 to 7 years, and 4 mg for 8 to 12 years), there was a decrease in the distribution volume and absolute clearance values. The magnitude of these changes was determined by the patient's age, and the clearance values varied from 300 ml/minute (12-year-old children) to 100 ml/minute (3-year-old children). The distribution volume in 12-year-old patients was 75 l, and in 3-year-olds - 17 l. Portions selected taking into account weight (0.1 mg/kg, no more than 4 mg) help to balance such differences and stabilize the systemic exposure of the drug in children.

In people with moderate renal impairment (creatinine clearance is 15-60 ml/minute), the distribution volume and systemic clearance are reduced, which results in a slight increase in the elimination half-life (up to 5.4 hours).

In individuals with severe liver failure, a significant decrease in the systemic clearance of ondansetron was observed, resulting in an increase in the elimination half-life (by 15-32 hours).

Dosing and administration

Use after radiotherapy or cytostatic chemotherapy procedures.

Adults.

The dose size of the drug is determined by the emetogenic activity of the treatment course. Often, 8 mg is required per day. If necessary, this dosage can be increased to 32 mg in the following cases:

• use of an emetogenic substance or radiotherapy procedure - before using a cytostatic drug, 8 mg of the drug should be administered intravenously at a slow rate. To prevent attacks of delayed or late vomiting, after the first 24 hours, the drug should be taken in tablet form;
• use of highly emetogenic drugs (for example, large doses of cisplatin) - before using the cytostatic agent, the patient is administered 8 mg of the drug intravenously at a slow speed.

A portion that exceeds 8 mg (but not more than 32 mg) may only be administered intravenously by infusion. In this case, the required portion of Emetron is dissolved in a suitable infusion solution (50-100 ml). The prepared solution is administered at a slow rate over at least 15 minutes.

There is also an alternative method - before the procedure of introducing a cytostatic drug, an intravenous injection of 8 mg of the drug is given (at a slow speed). Then another 2 portions of the drug (8 mg) can be administered by infusion, making intervals of 2-4 hours, or a continuous infusion lasting 24 hours can be performed (the rate will be 1 mg/hour).

The dosage is selected based on the severity of vomiting. When using highly emetogenic cytostatics, the effect of ondansetron can be increased by a single intravenous injection of GCS (for example, 20 mg of dexamethasone), which is administered before the start of cytostatic treatment.

To prevent late vomiting that occurs 24 hours after the use of moderately or highly emetogenic cytostatics, it is necessary to take the drug in tablets (8 mg twice a day) for 5 days.

Children.

Children with a body surface area >1.2 ^m2 should be given 8 mg of the drug (initial dose) intravenously before chemotherapy. The patient should then take Emetron tablets (8 mg) at 12-hour intervals. After completion of therapy, the tablets should be taken in a dose of 8 mg twice a day for up to 5 days.

Prevention of nausea and vomiting in the period after surgery.

Adults.

To prevent attacks of vomiting with nausea caused by surgical interventions, it is necessary to administer 4 mg of the drug intravenously (slowly) or intramuscularly during the introduction of the patient into anesthesia. To eliminate nausea with vomiting, the same dosages and methods of administration should be used.

Children.

To prevent the occurrence of vomiting with nausea after surgery under general anesthesia, it is necessary to administer the medication in doses of 0.1 mg/kg (maximum 4 mg once) at a slow rate - before the application of anesthesia or after the start of its administration.

There is very little information about the safe use of drugs in infants under 2 years of age.

Use in liver pathologies.

Since liver disorders result in a significant decrease in the clearance of ondansetron, its half-life in the blood plasma is extended, which requires reducing the daily dose of the drug to 8 mg.

Use of medication for infusion.

The solution is prepared immediately before the administration of the medicine. If necessary, the prepared mixture can be stored at a temperature of 2-8°C, but not longer than 24 hours. The prepared medicine retains its properties stable when kept in conditions of light.

When dissolving a medicinal substance, it is permissible to use the following solutions:

• 0.9% sodium chloride solution;
• 10% mannitol solution;
• 5% glucose solution;
• Ringer's solution,
• 0.3% KCl solution together with 0.9% NaCl solution;
• 0.3% KCl solution together with 5% glucose solution.

It is prohibited to dissolve Emetron in other infusion mixtures. Also, the medicine is prohibited to be mixed in one syringe with other drugs. The infusion of the drug is administered at a rate of 1 mg/hour.

At drug concentrations of 16-160 mcg/ml (for example, 8 mg/0.5 l or 8 mg/50 ml), it can be administered using a Y-shaped mechanism of infusion devices with similar agents.

Use of cisplatin: to a concentration of 0.48 mg/ml (for example, 240 mg/0.5 l), during drug administration over 1-8 hours.

Use of 5-fluorouracil: to a concentration of 0.8 mg/mL (e.g. 2.4 g/3 L or 0.4 g/0.5 L) when administered at a rate of at least 20 mL/hour (0.5 L/24 hours). When using high concentrations of fluorouracil, precipitation of Emetron may occur. The fluorouracil solution may contain no more than 0.045% magnesium chloride along with other common elements.

Use of carboplatin: to a concentration level of 0.18-9.9 mg/mL (e.g. 90 mg/0.5 L or 990 mg/0.1 L) during injection over 10-60 minutes.

Etoposide administration: to a concentration level of 0.144-0.25 mg/ml (e.g. 72 mg/0.5 l or 0.25 g/1 l) when administered over 0.5-1 hour.

Use of ceftazidime: to concentration values of 0.25-2 g, after dissolution in distilled water, following the instructions (for example, 0.25 g / 2.5 ml or 2 g / 10 ml), during jet injection over 5 minutes.

Use of cyclophosphamide: to a concentration level of 0.1-1 g after dissolution with distilled water for injection (e.g. 0.1 g/5 ml), following the instructions, during administration for 5 minutes.

Doxorubicin administration: to a concentration of 10-100 mg, after dissolution using distilled injection liquid (for example, 10 mg / 5 ml), following the instructions, during jet injection for 5 minutes.

Application of dexamethasone: the substance in a dose of 20 mg is administered at a slow rate intravenously, over 2-5 minutes, by means of a Y-shaped mechanism of the infusion apparatus, through which Emetron (in a portion of 8-32 mg) dissolved in infusion fluid (0.05-0.1 l) is administered over 15 minutes.

It is prohibited to sterilize ampoules containing medication using an autoclave.

Use Emetrona during pregnancy

Animal tests have shown that ondansetron is not teratogenic. However, there is no information about the absence of teratogenic effects on humans, so Emetron is prohibited during pregnancy (especially in the first trimester).

Ondansetron can be excreted in breast milk, which is why breastfeeding is prohibited when using it.

Contraindications

Contraindication is intolerance to medicinal elements.

Side effects Emetrona

The use of the drug usually causes the development of the following side effects:

• immune disorders: occasionally, immediate symptoms of hypersensitivity develop (this includes anaphylaxis);
• lesions affecting the functioning of the nervous system: headaches often occur. Convulsions, extrapyramidal disorders (such as dystonic manifestations or oculomotor crisis), and dizziness (with rapid administration of a medicinal injection) are occasionally observed;
• problems with visual function: occasionally, transient deterioration of vision (for example, its clouding) and temporary blindness (usually with intravenous injection) are observed, which often disappears within 20 minutes after the completion of the procedure;
• disturbances in the functioning of the heart: bradycardia or arrhythmia occasionally develops, as well as pain in the sternum (with or without depression of the ST interval);
• vascular dysfunction: hot flashes and a feeling of warmth, as well as redness, are often observed. A decrease in blood pressure may occasionally be observed;
• disturbances in the functioning of the lungs, as well as the mediastinum and sternum: hiccups are occasionally observed;
• disorders affecting digestive function: constipation is occasionally observed (because ondansetron prolongs the period of passage of feces in the colon);
• lesions affecting the hepatobiliary system: transient increases in serum transaminase levels are often observed, occurring without symptoms (usually in people treated with cisplatin);
• systemic disorders: symptoms often appear at the injection site.

Overdose

There is very little information available regarding Emetron intoxication. Typically, the symptoms are similar to the side effects listed above.

The drug has no antidote, so in case of overdose, symptomatic and supportive measures should be taken.

Interactions with other drugs

There is no data that the drug can block or induce metabolic processes of other drugs that are used in combination with it.

Specific test data showed that the drug does not interact with the substances furosemide, propofol, as well as tramadol and temazepam, and also with alcoholic beverages.

In individuals who used a strong CYP3A4 inducer (such as carbamazepine, phenytoin or rifampicin) in combination with oral administration of the drug, an increase in the clearance of the active drug element was observed, while its levels in the blood, on the contrary, decreased.

Data based on tests conducted in a limited number of patients have shown that Emetron may reduce the analgesic properties of tramadol.

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Storage conditions

Emetron should be kept in a place protected from sunlight and small children. Temperature indicators are within 30°C.

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Shelf life

Emetron can be used for 4 years from the date of manufacture of the drug.

Application for children

The medicine is approved for use (to eliminate vomiting and nausea that occurs after surgery) in children over 2 years of age.

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Analogues

The following drugs are analogs of the drug: Vero-Ondansetron, Zofran and Atossa with Domegan, and also Ondansetron, Latran with Lazaran VM and Ondansetron-Altpharm, as well as Ondazan and Ondansetron-ESCOM. The list also includes Ondansetron-LENS, Ondasol, Ondansetron-Teva, Setronon with Osetron and Ondantor, and also Ondansetron-Ferein and Emeset.