Emetron

Emetron - an antiemetic drug that helps to eliminate nausea.

Indications of the emetron

It is used to eliminate vomiting with nausea that arise from radiotherapy or chemotherapy procedures of a cytostatic nature, and in addition to preventing and eliminating vomiting with nausea developing after performing surgical operations.

Release form

The release takes place in the form of a solution, in ampoules of 4 ml. Inside the box there are 5 such ampoules.

Pharmacodynamics

Ondansetron is an end antagonist (5-HT3), which has a high selectivity. There is no precise information on the mechanism allowing the drug to reduce vomiting with nausea. Chemotherapeutic drugs of a cytostatic nature, as well as radiotherapy, can lead to an increase in serotonin values within the small intestine. And this element, activating the vagal fibers of the afferent type, in which the endings of 5-HT3 are contained, stimulates a gag reflex. Medication prevents the development of this reflex.

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

The medicinal element has no effect on the plasma indices of prolactin.

Pharmacokinetics

The distribution of the drug after its administration inside or in / in or / m introduction has the same indicators. Term terminal half-life is approximately 3 hours, and the equilibrium distribution volume is about 140 liters.

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

Excretion of the substance from the systemic blood flow occurs through multiple metabolic processes involving enzymes - mainly within the liver. Less than 5% of the unchanged component is excreted in the urine.

The absence of the CYP2D6 enzyme (polymorphism with respect to cleavage of debrisoquin) has no effect on the pharmacokinetic characteristics of ondansetron. Changes in these parameters are not observed with repeated injections of drugs.

Tests of the effectiveness of the drug in children, which were performed with the participation of the 21st child at the age of 3-12 years who underwent a planned surgical operation under anesthesia, showed that after a single dose of medicines (2 mg for 3-7-year-olds, and also 4 mg for 8-12-year-olds) there was a decrease in the distribution volume and absolute clearance rates. The magnitude of these changes was determined by the patient's age, and the clearance values ranged from 300 ml / minute (12-year-olds) to 100 ml / minute (3-year-olds). The indicator of distribution volume in 12-year-old patients was 75 liters, and in 3-year-old patients - 17 liters. Portions selected with weight (0.1 mg / kg, not more than 4 mg), help balance these differences and stabilize the indicator of systemic exposure of drugs in children.

In people with moderate kidney failure (QC values of 15-60 ml / minute) the level of distribution volume and system clearance is lowered, which causes a slight increase in the elimination half-life (up to 5.4 hours).

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

Dosing and administration

Application after radiotherapy or chemotherapy procedures of cytostatic nature.

Adults.

The size of the portion of the drug is determined by the emetogenic activity of the treatment course. Often, 8 mg is required per day. If there is a need, this dosage is allowed to be increased to 32 mg in such cases:

• use of an emetogenic substance or a procedure for radiotherapy - before applying the cytotoxic drug, you must inject, at a slow speed, 8 mg of the drug. To prevent the appearance of attacks of delayed or late vomiting, after the first 24 hours it is necessary to use medicines in tablets;
• use of highly emetic drugs (for example, large portions of cisplatin) - before the application of the cytostatic agent, 8 mg of LS in the IV method, at a slow speed, is administered to the patient.

A portion that exceeds 8 mg (but not more than 32 mg), in / in the method is allowed to enter only infuzionno. The required portion of Emetron is dissolved in a suitable solution for infusions (50-100 ml). Ready solution is introduced at a slow speed, for at least 15 minutes.

There is also an alternative method - before the procedure for the administration of cytotoxic drugs, an 8 mg dose of medication (at a slow speed) is injected iv. Then 2 more servings of medicinal product (8 mg) are allowed to be infused, making intervals of 2-4 hours, or to perform a continuous infusion of 24 hours (speed is 1 mg / hour).

The size of the dosage is selected based on the degree of vomiting. When using highly emeticogenic cytostatics, the effect of ondansetron can be increased with a single intravenous injection of GCS (eg, 20 mg of dexamethasone), which is administered before the cytostatic treatment is initiated.

To prevent late vomiting that occurs 24 hours after the application of medium-or high-emetic cytotoxic drugs, it is necessary to take the drug in tablets (8 mg twice a day) for 5 days.

Children.

Children whose body surface size is> 1.2 m ² should be given an IV injection in a way of 8 mg LS (initial dose) before performing chemotherapy. The patient should then take Emetron tablets (8 mg) at intervals of 12 hours. After the end of therapy, taking 8 mg of tablets takes place twice a day, and lasts up to 5 days.

Preventing the appearance of nausea with vomiting in the period after surgery.

Adults.

To prevent attacks of nausea with nausea caused by surgical interventions, it is necessary to inject IV slowly or IV using 4 mg of the drug during the patient's admission to anesthesia. To remove nausea with vomiting, you should use the same dosages and methods of administration.

Children.

To prevent the occurrence of vomiting with nausea after an operation under general anesthesia, it is required to administer the drug in a dose of 0.1 mg / kg (maximum 4 mg once) at a slow speed - before applying anesthesia, or even after the beginning of its injection.

About safe use of drugs for babies under 2 years of age, there is very little information.

Use in hepatic pathologies.

Since in hepatic disorders there is a significant decrease in clearance of ondansetron, the time of its half-life inside the blood plasma is prolonged - because of this it is required to reduce the daily portion of the drug to 8 mg.

Use of medicament for infusion.

Preparation of the solution is carried out immediately before the administration of the drug. If necessary, the prepared mixture is allowed to be stored at 2-8 ° C, but not longer than 24 hours. The finished medicine retains its properties stable when kept in conditions of presence of light.

When dissolving a drug substance, it is allowed to use such solutions:

• 0.9% solution of sodium chloride;
• 10% solution of mannitol;
• 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.

Other infusion mixtures Emetron dissolve is prohibited. Also, the medicine should not be mixed inside one syringe with other drugs. Infusion of the drug is administered at a rate of 1 mg / h.

With medication concentrations of 16-160 μg / ml (eg 8 mg / 0.5 l or 8 mg / 50 ml), it can be administered using the Y-shaped mechanism of infusion devices with similar means.

The use of cisplatin: to a concentration of 0.48 mg / ml (eg, 240 mg / 0.5 L), during the administration of drugs for 1-8 hours.

Use of 5-fluorouracil: to a concentration of 0.8 mg / ml (eg, 2.4 g / 3 liters or 0.4 g / 0.5 liter), at the time of administration at a rate of at least 20 ml / h ( 0.5 l / 24 hours). With the use of high concentrations of fluorouracil, precipitation of Emetron is possible. Inside the solution, fluorouracil can 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 (eg, 90 mg / 0.5 L or 990 mg / 0.1 L), during the injection for 10-60 minutes .

The use of etoposide: to a concentration index of 0.144-0.25 mg / ml (eg, 72 mg / 0.5 L or 0.25 g / 1 L), during administration for 0.5-1 hour .

The use of ceftazidime: to a concentration value of 0.25-2 g, after dissolution in distilled water, following the instructions (eg 0.25 g / 2.5 ml or 2 g / 10 ml), during an inkjet injection during 5 minutes.

Use cyclophosphamide: to a concentration level of 0.1-1 g, after dissolving with distilled injectable water (eg 0.1 g / 5 mL), following the instructions, during the administration for 5 minutes.

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

The use of dexamethasone: the substance in a dose of 20 mg is administered at a slow speed intravenously, for 2-5 minutes, by means of the Y-shaped mechanism of the infusion apparatus, through which, for 15 minutes, the dissolved in the infusion fluid (0.05-0 , 1 L) Emetron (in the dose of 8-32 mg).

It is forbidden to sterilize with the help of an autoclave the ampoules in which the medicine is contained.

Use of the emetron during pregnancy

Animal tests demonstrated the lack of teratogenic properties in ondansetron. But there is no information on the absence of teratogenic effects on humans, therefore, during pregnancy, Emetron is banned (especially in the 1st trimester).

Ondansetron is excreted with human milk, which is why it is forbidden to breast-feed while using it.

Contraindications

Contraindication is intolerance with regard to medicinal elements.

Side effects of the emetron

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

• Immune disorders: Occasionally, immediate symptoms of increased sensitivity develop (this includes anaphylaxis);
• lesions affecting the work of the National Assembly: headaches often occur. Occasionally, convulsions, extrapyramidal disorders (such as dystonic manifestations or oculomotor crisis), and dizziness (with the rapid administration of a drug injection) are observed;
• problems with visual function: occasionally there is a transient visual impairment (eg, its turbidity) and temporary blindness (usually with / in injection), which often occurs 20 minutes after completion of the procedure;
• disorders in the work of the heart: occasionally develops bradycardia or arrhythmia, as well as pain in the sternum (with or without ST depression);
• disorders of vascular function: often marked by hot flashes and a feeling of warmth, as well as redness. Occasionally there may be a decrease in blood pressure;
• violations of the lungs, as well as mediastinum and sternum: occasionally there is a hiccough;
• disorders affecting the function of digestion: occasionally there is constipation (because ondansetron lengthens the period of passage of feces inside the colon);
• lesions affecting the work of the hepatobiliary system: often there is a transient increase in the level of transaminases inside the blood serum, taking place without symptoms (usually in people who are treated with cisplatin);
• systemic disorders: often there are symptoms at the injection site.

Overdose

Now there is very little information about Emetron's intoxication. Usually in this case, the manifestations are similar to the above-mentioned side-effects.

The drug has no antidote, which is why in case of an overdose, symptomatic and supportive measures should be performed.

Interactions with other drugs

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

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

In persons who used a powerful inducer of the element CYP3A4 (such as carbamazepine, phenytoin or rifampicin) in patients who used oral medication, an increase in the clearance of the active element of the drug was noted, and its indices inside the blood, on the contrary, decreased.

Data based on tests conducted with the participation of a limited number of patients showed that Emetron is able to weaken the analgesic properties of tramadol.

[1], [2], [3]

Storage conditions

Emetron should be kept in a place that is closed from penetration of sunlight, as well as small children. The temperature is within 30 ° C.

[4]

Shelf life

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

Application for children

The medicine is allowed for use (elimination of vomiting that occurs after surgery with nausea) in children over 2 years of age.

[5], [6]

Analogues

Analogues of the medication are such drugs: Vero-Ondansetron, Zofran and Atossa with Domeganom, and besides Ondansetron, Latran with Lazaran VM and Ondansetron-Altpharm, and Ondazan and Ondansetron-ESCOM. The list includes Ondansetron-LENS, Ondasol, Ondansetron-Teva, Stronon with Stsetron and Ondantor, and besides Ondansetron-Ferein and Emeset.