Emetron, 2 mg/ml 4 ml 5 pcs

Pharmacodynamics

The anti-emetic drug of central action. Ondansetron is a selective serotonin 5NT3 receptor antagonist. Cytostatic chemotherapy drugs and radiotherapy may increase serotonin levels which, by activation of vagal afferent fibers containing serotonin 5NT3 receptors, causes the gag reflex. Ondansetron inhibits the onset of the gag reflex by blockade of serotonin 5NT3 receptors at the neuronal level of both the central and peripheral nervous system.

This mechanism of action appears to be the basis for the prevention and treatment of postoperative vomiting and nausea caused by cytostatic chemotherapy and radiotherapy.

Pharmacokinetics

Introduction Cmax is measured within 10 min of injection. The distribution of ondansetron is the same when administered v/m and intravenously. After oral administration Cmax of ondansetron in blood plasma is reached after about 1.5 hours. Absolute bioavailability after oral administration is about 60%. The drug is metabolized in the liver. Binding with plasma proteins is 70-76%. With urine, less than 5% of the drug is excreted unchanged.

After oral and parenteral administration T1/2 is about 3 hours, in elderly patients it can be up to 5 hours, and in case of severe hepatic insufficiency – 15-22 hours. In renal impairment (renal clearance less than 15 ml/min) the T1/2 is increased by 4-5 hours, but this increase is of no clinical significance.

Indications

Active ingredient

Composition

1 ml (1 ampoule) contains:

Active ingredients:

ondansetron hydrochloride dihydrate 2.5 mg (10 mg), corresponding to ondansetron 2 mg (8 mg).

Auxiliary substances:

sodium citrate – 1.6 mg,

citric acid monohydrate – 2.2 mg,

How to take, the dosage

Cytostatic therapy

The choice of dosing regimen is determined by the severity of the emetogenic effects of the antitumor therapy being given.

For adults, the daily dose is usually 8-32 mg; the following regimens are recommended.

In moderate emetogenic chemotherapy or radiotherapy: 8 mg w/v slow-acting or v/m, immediately before therapy; or 8 mg orally 1-2 hours before therapy, then another 8 mg orally 12 hours after therapy begins.

In high-emetogenic chemotherapy: 8 mg by IV jet (slow) immediately before the start of chemotherapy, followed by 2 more IV jet injections of 8 mg, each 2-4 h later; or a continuous 24-hour infusion of the drug at a dose of 24 mg at 1 mg/h; or 16-32 mg diluted in 50-100 ml of an appropriate infusion solution, as a 15-minute infusion, immediately before the start of chemotherapy.

The efficacy of ondansetron may be increased by a single intravenous glucocorticoid (e.g., 20 mg dexamethasone) before chemotherapy; if given orally, the single dose may be increased to 24 mg and administered simultaneously with 12 mg dexamethasone 1-2 h before chemotherapy to enhance the effect.

In order to prevent delayed vomiting occurring 24 hours after the start of chemotherapy or radiotherapy, it is recommended that oral administration of 8 mg twice daily be continued for 5 days.

In children over 2 years of age, the drug is administered in a dose of 5 mg/m2 body surface w/in, immediately before the start of chemotherapy followed by an oral dose of 4 mg 12 hours later; after completion of chemotherapy it is recommended to continue treatment at 4 mg 2 times/day orally for 5 days.

Prevention of postoperative nausea and vomiting

Adults are given a single dose of 4 mg in m/m or IV by IV stream, slowly at the start of anesthesia, or 16 mg orally 1 hour before anesthesia.

To relieve nausea and vomiting that occurs, 4 mg of the drug is recommended as a single dose in m/m or a slow IV infusion.

Into the same area of the body, ondansetron may be administered in a dose not exceeding 4 mg.

In children, to prevent postoperative nausea and vomiting, ondansetron is used exclusively parenterally in a single dose of 0.1 mg/kg (up to a maximum of 4 mg) as a slow IV injection during or after anesthesia.

In order to treat developed postoperative nausea and vomiting in children, a slow IV single dose of the drug of 0.1 mg/kg (up to a maximum of 4 mg) is recommended. There is insufficient experience with regard to the prevention and treatment of postoperative nausea and vomiting in children under 2 years of age.

Elderly patients do not require dosage changes.

In patients with renal impairment, there is no need to change the usual daily dose and frequency of administration of the drug.

In liver damage, ondansetron clearance is significantly decreased and T1/2 from plasma is increased, so the daily dose of 8 mg/day should not be exceeded.

The following solutions may be used for dilution of the injection solution: 0.9% sodium chloride solution, 5% dextrose solution, Ringer’s solution, 0.3% potassium chloride solution and 0.9% sodium chloride solution, 0.3% potassium chloride solution and 5% dextrose solution.

Interaction

Because ondansetron is metabolized by the liver enzyme system (cytochrome P450), caution is required when used together:

It does not interact with ethanol, temazepam, furosemide, tramadol and propofol.

Ondansetron at a concentration of 16-160 µg/ml is pharmaceutically compatible with the following drugs, which can be administered via a Y-injector:

Special Instructions

Patients who have previously had hypersensitivity reactions when using other selective serotonin 5HT3 receptor antagonists may also develop similar reactions when using ondansetron.

Because ondansetron causes constipation, patients with signs of bowel obstruction require regular monitoring after using the drug.

The infusion solution should be prepared immediately prior to use. If necessary, the prepared infusion solution may be stored for a maximum of 24 h at 2-8°C prior to use.

At the time of infusion, protection from light is not required; the diluted infusion solution remains stable for at least 24 h in natural light or artificial light.

In the case of lactose intolerance, note that the 4 mg tablet contains 59.25 mg of lactose and the 8 mg tablet contains 118.5 mg, respectively.

Impact on the ability to drive vehicles and other mechanisms requiring increased concentration

It does not have a sedative effect and does not affect the psychomotor abilities required for driving and other mechanisms.

Contraindications

Side effects

Allergic reactions: urticaria, bronchospasm, laryngospasm, angioedema, anaphylaxis.

Digestive system disorders: hiccups, dry mouth, diarrhea, constipation; sometimes – asymptomatic transient increase in serum aminotransferase levels.

Cardiovascular system disorders: chest pain, in some cases with ST-segment depression, arrhythmias, bradsardia, BP decrease.

CNS disorders: headache, dizziness, spontaneous motor disorders and seizures. Local reactions: pain, burning and redness at the injection site.

Others: rush of blood to the face, fever, temporary visual acuity impairment; rarely – hypokalemia (relationship with taking the drug has not been clearly established).

Overdose

In cases of suspected overdose symptomatic therapy is indicated. A specific antidote is not known.

Pregnancy use

It is contraindicated in pregnancy and lactation.

Similarities