Emetron - instructions for use, dose, side effects, contraindications

Excipients: silicon dioxide colloidal -0,60 mg, magnesium stearate - 1.30 mg, talc - 7.10 mg, pregelatinized starch - 18,0 mg, microcrystalline cellulose - 40,0 mg, corn starch -54,50 mg, anhydrous lactose -118,50 mg;

composition of the shell: silicon dioxide colloid - 0.07 mg, iron dye oxide yellow 0.12 mg, titanium dioxide 0.27 mg, macrogol 6000 0.79 mg, sepilated film 003 8.75 mg (Macrogol-40 stearate (mono and diesters of stearic acid and PEG-40) (E431) - 8.00 - 12,0 %, microcrystalline cellulose (E460) - 35,0 - 45,00 %, hypromellose (E464) - 45.00 - 55.00%)

Description:

Film coated tablets. 8 mg: round biconvex tablets coated with a film sheath, yellow, engraved "8" on one side and "RG" - another. On the cross-section, two layers are visible, the color of the inner layer is white or almost white.

Pharmacotherapeutic group:Antiemetic, serotonin receptor antagonist.

ATX: & nbsp

A.04.A.A.01 Ondansetron

Pharmacodynamics:

Ondansetron is a selective antagonist 5HT3 - receptors (serotonin).Drugs for cytostatic chemotherapy and radiotherapy can cause an increase in the serotonin concentration, which by activation of the afferent fibers of the vagus nerve, containing receptors 5-HTs, causes a vomitive reflex. Selectively blocks serotonin 5-HTZ - receptors of central neurons (vomiting center) and peripheral (gastrointestinal tract) of the nervous system that regulate the vomiting reflex. Does not disrupt the coordination of movements, does not cause sedation and reduced efficiency. Does not change the concentration of prolactin in the plasma.

Pharmacokinetics:

After oral administration ondansetron completely absorbed in the gastrointestinal tract and subjected to the effect of "first passage" through the liver. The maximum concentration of ondansetron in the blood plasma is reached about 1.5 after oral administration and is approximately 30 ng / ml after taking the drug at a dose of 8 mg. Absolute bioavailability is about 60%. Bioavailability of ondansetron slightly increases with simultaneous intake with food, but does not change when taking antacids.

Binding to plasma proteins is 70-76%.With kidneys, unchanged, less than 5% of ondansetron is excreted.

The distribution of ondansetron when administered orally, intravenously or intramuscularly is the same. The volume of distribution when an equilibrium state is reached is about 140 liters. Binding to blood plasma proteins - 70-76%.

Ondansetron is eliminated from the body, mainly as a result of liver metabolism involving several microsomal isozymes (CYP1A2, CYP2D6, CYP3A4). Lack of isoenzyme CYP2D6 does not affect the pharmacokinetics of ondansetron. Less than 5% of the administered dose is excreted by the kidneys unchanged.

Both after oral administration, and with parenteral administration, the elimination half-life is about 3 hours. The pharmacokinetic parameters of ondansetron do not change when it is repeated.

Pharmacokinetics in special clinical cases

In children, the values of clearance and volume of distribution depend on age. Correction of the dose taking into account the body weight of patients (from 0.1 mg / kg to 4 mg maximum) compensates for these changes and normalizes the system exposure of ondansetron in children.

In patients with moderate renal insufficiency (creatinine clearance 15-60 ml / min) systemic clearance and volume of distribution are reduced,which leads to a small and clinically insignificant increase in the half-life (T1 / 2- 5.4 hours).

In patients with severe impairment of renal function on hemodialysis, the pharmacokinetics of ondansetron is virtually unchanged.

In patients with severe hepatic insufficiency significantly decreases the clearance of ondansetron, resulting in a half-life increases (up to 15-32 h), and oral bioavailability reaches 100 % due to a decrease in presystemic metabolism.

In elderly patients there is a slight increase in bioavailability to 65% and a half-life of up to 5 hours.

The distribution of ondansetron depends on sex, women have a higher intake absorption, as well as a lower systemic clearance and volume of distribution.

Indications:

Prevention and management of nausea and vomiting caused by cytotoxic chemo- or radiotherapy.

Prevention and relief of nausea and vomiting in the postoperative period.

Contraindications:

- Hypersensitivity to any component of the drug.

- Pregnancy and lactation.

- Children under 12 years (for a dosage of 8 mg).

Carefully:

Patients with hereditary lactose intolerance, congenital lactase deficiency or glucose-galactose malabsorption.

Dosing and Administration:

Cytostatic therapy

The choice of the dosage regimen is determined by the severity of the emetogenic effect of the antitumor therapy.

For adults and children over 12 years of age, the daily dose, as a rule, is 8-24 mg, the following regimens are recommended:

With moderate expression of the emetogenic effect of chemotherapy or radiotherapy:

- 8 mg orally for 1 to 2 hours before the start of therapy, then another 8 mg orally 12 hours after the start therapy.

If the emetogenic effect of chemotherapy or radiotherapy is high: The recommended adult dose (no data for use in children) is 24 mg concomitantly with dexamethasone orally at a dose of 12 mg 1-2 hours before the start of chemotherapy.

When taken orally to enhance the effect of a single dose can be increased to 24 mg and is prescribed concomitantly with 12 mg of dexamethasone 1-2 hours before the start of chemotherapy. Prevention of postoperative nausea and vomiting

- adults prescribe 16 mg orally 1 hour before the onset of general anesthesia;

- children for preventing and arresting postoperative nausea and vomiting ondansetron only applied parenterally.

Elderly patients

A dose change is not required.

Patients with impaired renal function

Change the usual daily dose and the frequency of taking the drug is not required.

Patients with impaired hepatic function

The daily dose should not exceed 8 mg per day.

Patients with a slow metabolism of sparteine / debrisoquine Correction of a daily dose or frequency of ondansetron is not required.

Side effects:

From the immune system: urticaria, bronchospasm, laryngospasm, angioedema, immediate-type hypersensitivity reactions, sometimes severe, including anaphylaxis.

From the nervous system: headache, dizziness, convulsions, spontaneous movement disorders, including extrapyramidal disorders (dystonic reactions, oculogic crisis, dyskinesia), which are reversible and do not lead to persistent clinical consequences.

From the cardiovascular system: pain in the chest, in some cases with depression of the segment S-T, arrhythmias, bradycardia, lowering blood pressure.

From the digestive system: hiccough, dry mouth, diarrhea, constipation, asymptomatic transient increase in the activity of "liver" enzymes.

Other: sensation of fever and redness of the skin of the face, hypokalemia, hypercreatininaemia; temporary reduction of visual acuity.

Overdose:

Symptoms: visual impairment, constipation, lowering of blood pressure and vasovagal episode with transient atrioventicular blockade of II degree. In all cases, the phenomena are completely reversible.

Treatment: conduct symptomatic and supportive therapy, a specific antidote is not known.

Interaction:

As ondansetron is metabolized by the enzyme system (cytochrome P450) of the liver, caution is required when combined:

- with inducers of cytochrome P450 (isozymes CYP2D6 and CYP3A) (barbiturates,

carbamazepine, carisoprodol, glutetimide, griseofulvin, dinitrogen oxide, papaverine, phenylbutazone, phenytoin (probably other hydantoins), rifampicin, tolbutamide;

- with inhibitors of cytochrome P450 (isozymes CYP2D6 and CYP3A) (allopurinol, macrolide antibiotics, antidepressants - MAO inhibitors, chloramphenicol, cimetidine, oral contraceptives containing estrogens, diltiazem, disulfiram, valproic acid, valproat seminary, erythromycin, fluconazole, fluoroquinolones, isoniazid, ketoconazole, lovastatin, metronidazole, omeprazole, propranolol, quinidine, quinine, verapamil).

- does not interact with alcohol, temazepam, furosemide, tramadol and propofol.

Special instructions:Ondansetron should not be administered to children with body surface area less than 0.6 m² . Ondansetron It can not be used to prevent and treat postoperative nausea and vomiting in children after surgery on the abdominal organs. In patients who had previously used other selective 5HT3 antagonists-receptors, there were reactions of hypersensitivity, with the application of ondansetron, similar reactions can also develop. As ondansetron slows the bowel motility, patients with signs of intestinal obstruction after using the drug require regular monitoring of the doctor.

Effect on the ability to drive transp. cf. and fur:

In case of adverse reactions from the nervous system, patients are advised to refrain from driving and othermechanisms, as well as activities that require concentration of attention, stress of psychomotor functions.

Form release / dosage:Tablets coated with a film coat of 8 mg.

Packaging:

10 tablets in a blister of PVC and aluminum foil. 1 blister in a cardboard box with instructions for use.

Storage conditions:

Store at a temperature not exceeding 30 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N012102 / 01

Date of registration:02.06.2010

The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary

Manufacturer: & nbsp

GEDEON RICHTER, Ltd. Hungary

Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary

Information update date: & nbsp18.06.2015

Illustrated instructions

Instructions

Emetron® (Emetron®)