Setronon (Tablets) Instructions for Use

ATC Code

A04AA01 (Ondansetron)

Active Substance

Ondansetron (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Centrally acting antiemetic drug blocking serotonin receptors

Pharmacotherapeutic Group

Antiemetic agent – serotonin receptor antagonist

Pharmacological Action

Antiemetic agent. It effectively prevents and relieves nausea and vomiting occurring during anticancer chemotherapy or radiation therapy, as well as in the postoperative period.

The mechanism of action is due to the ability of ondansetron to selectively block serotonin 5-HT₃ receptors.

It is believed that stimulation of afferent fibers of the vagus nerve by serotonin released from enterochromaffin cells of the gastrointestinal mucosa plays an important role in the occurrence of nausea and vomiting during anticancer therapy.

By blocking 5-HT₃ receptors, Ondansetron prevents the occurrence of the vomiting reflex.

Furthermore, Ondansetron suppresses the central links of the vomiting reflex by blocking 5-HT₃ receptors in the floor of the IV ventricle (area postrema).

Pharmacokinetics

Ondansetron undergoes a significant first-pass effect through the liver.

Protein binding is high (70-76%).

It is biotransformed in the liver, mainly by hydroxylation.

The mean T_1/2 in adult patients is about 4 hours.

Indications

Prevention of nausea and vomiting during anticancer chemotherapy or radiation therapy; prevention and treatment of nausea and vomiting in the postoperative period.

ICD codes

Dosage Regimen

Determine the dosage individually based on indication, patient age, and emetogenic potential of the therapy.

For highly emetogenic chemotherapy, administer 24 mg orally as a single dose 30 minutes before the start of chemotherapy.

For moderately emetogenic chemotherapy or radiotherapy, administer 8 mg orally 30 minutes before therapy, followed by 8 mg doses 8 hours after the first dose, then 8 mg every 12 hours for 1 to 2 days after therapy completion.

For postoperative nausea and vomiting prevention, administer 16 mg as a single oral dose 1 hour before anesthesia induction.

For postoperative nausea and vomiting treatment, administer 8 mg orally every 12 hours as needed.

For pediatric patients (aged 4-11 years) receiving chemotherapy, administer 4 mg orally 30 minutes before chemotherapy, followed by 4 mg doses 4 and 8 hours after the first dose, then 4 mg every 8 hours for 1 to 2 days after therapy completion.

Do not exceed a maximum daily dose of 24 mg in pediatric patients aged 4-11 years.

For patients with severe hepatic impairment (Child-Pugh score ≥10), do not exceed a single daily dose of 8 mg due to significantly reduced clearance.

Adjust the dosing schedule for patients with renal impairment is not usually required.

Adverse Reactions

Immune system disorders: rarely – immediate-type hypersensitivity reactions (urticaria, bronchospasm, laryngospasm, angioedema), in some cases severe, including anaphylaxis.

Nervous system disorders: very common – headache; uncommon – seizures, movement disorders (including extrapyramidal symptoms such as dystonia, oculogyric crisis, and dyskinesia); rarely – dizziness, predominantly during rapid IV administration.

Eye disorders: rarely – transient visual disturbances (e.g., blurred vision, transient blindness), mainly during IV administration.

Cardiac and vascular disorders: common – feeling of warmth or flushing; uncommon – arrhythmia, chest pain, both accompanied and not accompanied by ST segment depression, bradycardia, decreased blood pressure; rarely – QT interval prolongation (including torsades de pointes-type ventricular tachycardia).

Gastrointestinal disorders: common – constipation; uncommon – hiccups, dry oral mucosa; frequency unknown – diarrhea.

Hepatobiliary disorders: uncommon – asymptomatic increase in ALT, AST activity (mainly in patients receiving cisplatin chemotherapy).

Skin and subcutaneous tissue disorders: very rare – toxic skin rash, including toxic epidermal necrolysis.

Metabolism and nutrition disorders: rarely – hypokalemia, hypercreatininemia.

Local reactions: with IV administration – burning at the injection site; with use of suppositories – burning sensation in the anus and rectum.

Contraindications

Hypersensitivity to ondansetron; concomitant use of ondansetron with apomorphine; pregnancy, lactation (breastfeeding); pediatric age – depending on the indications and dosage form; congenital long QT syndrome.

Use with caution in patients with hypersensitivity to other 5HT₃ receptor antagonists, with cardiac rhythm and conduction disorders, with significant water-electrolyte balance disturbances; in patients with prolonged or at risk of QTc prolongation, including patients with water-electrolyte balance disorders, chronic heart failure, bradyarrhythmia, or in patients taking other medications that can cause QT interval prolongation, water-electrolyte balance disturbances, or decreased heart rate; in patients receiving antiarrhythmic agents and beta-blockers; in patients with subacute intestinal obstruction; with concomitant use of other serotonergic drugs.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding). If use during lactation is necessary, breastfeeding should be discontinued.

Use in Hepatic Impairment

In patients with moderate and severe hepatic impairment, the clearance of ondansetron is significantly reduced, and the half-life is significantly increased.

Pediatric Use

Can be used in children of appropriate age categories strictly according to indications, in recommended doses and dosage forms. It is necessary to strictly follow the instructions in the ondansetron drug labels regarding contraindications for the use of specific ondansetron dosage forms in children of different ages.

Special Precautions

There are reports of hypersensitivity reactions to ondansetron in patients with a history of hypersensitivity to other selective 5HT₃ receptor antagonists.

It is known that Ondansetron increases the transit time of contents through the large intestine. When using ondansetron in patients with symptoms of subacute intestinal obstruction, regular monitoring of such patients is necessary.

Hypokalemia and hypomagnesemia should be corrected before using ondansetron.

It has been established that the combined use of ondansetron and other serotonergic drugs increases the risk of developing serotonin syndrome. If the use of such a combination is clinically justified, regular monitoring of the patient’s condition is necessary.

Effect on ability to drive vehicles and operate machinery

During the use of ondansetron, patients should exercise caution when driving vehicles and operating machinery, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Since Ondansetron is metabolized in the liver by enzymes of the cytochrome P450 system, concomitant use with drugs that are inducers or inhibitors of this enzyme system may lead to changes in the clearance and T_1/2 of ondansetron.

In patients receiving strong inducers of the CYP3A4 isoenzyme (phenytoin, carbamazepine, and rifampicin), the clearance of ondansetron increases, and the blood concentration of ondansetron decreases.

There is evidence that Ondansetron may reduce the analgesic effect of tramadol.

When ondansetron is used concomitantly with other serotonergic drugs, including selective serotonin reuptake inhibitors and serotonin and norepinephrine reuptake inhibitors, the risk of developing serotonin syndrome increases.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.