Tropisetron

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[edit] BRAND NAMES

[edit] STRUCTURE

Tropisetron.jpg

[edit] MECHANISM OF ACTION

Tropisetron is an antinauseant and antiemetic agent. It acts as a selective serotonin 5-HT3 receptor antagonist.

Cancer chemotherapy may be associated with a high incidence of nausea and vomiting, particularly when certain agents, such as cisplatin, are used. 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema. It is thought that chemotherapeutic agents produce nausea and vomiting by releasing serotonin from the enterochromaffin cells of the small intestine and that the released serotonin then activates 5-HT3 receptors located on vagal afferents to initiate the vomiting reflex.

Postoperative nausea and vomiting is influenced by multiple patient,surgical and anesthesia related factors and is triggered by release of serotonin in a cascade of neuronal events involving both the central nervous system and the gastrointestinal tract. The 5-HT3 receptor has been demonstrated to selectively participate in the emetic response.

[edit] INDICATIONS

  • Prevention of nausea and vomiting induced by cancer chemotherapy
  • Treatment and prevention of post-operative nausea and vomiting in adults.

[edit] DOSAGE

Prevention of nausea and vomiting induced by cancer chemotherapy: Tropisetron is recommended as six-day courses of 5 mg per day, given intravenously on Day 1 immediately before cancer chemotherapy either as an infusion given over 15 minutes or as a slow injection (not less than 1 minute), followed by oral administration on Days 2 to 6. Oral Tropisetron should be taken with water in the morning immediately upon rising at least one hour before food intake. If Tropisetron alone produces insufficient antiemetic control, its therapeutic efficacy may be enhanced by the addition of dexamethasone.

Treatment and prevention of post-operative nausea and vomiting in adults: Tropisetron is recommended as a 2 mg dose given intravenously either as an infusion or as a slow injection (not less than 30 seconds). In the case of prevention of post-operative nausea and vomiting, Tropisetron should be administered shortly before the induction of anaesthesia.

[edit] CONTRAINDICATIONS

[edit] PRECAUTIONS

  • In patients with uncontrolled hypertension, daily doses of Navoban higher than 10 mg should be avoided since they may cause a further increase in blood pressure

[edit] INTERACTIONS

As a prolongation of the QTc interval has been observed in patients on tropisetron, care should be taken when other drugs that are likely to prolong the QT interval are taken concomitantly with it.

[edit] PREGNANCY AND LACTATION

Pregnancy Category B3 (australia) Tropisetron is contraindicated during pregnancy and lactation

[edit] SIDE EFFECTS

The most frequently reported adverse reaction at the 2 mg dose was headache. At the 5 mg dose, constipation and, less frequently, dizziness, fatigue, somnolence, and gastrointestinal disorders, such as abdominal pain, diarrhoea and anorexia were observed as well.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Antiemetics
5-HT3 receptor antagonists Dolasetron   Granisetron   Ondansetron   Palonosetron   Tropisetron
Dopamine antagonists Alizapride   Bromopride   Clebopride   Domperidone   Metoclopramide   Prochlorperazine   Thiethylperazine
H1 antagonists Dimenhydrinate   Meclizine
NK1 receptor antagonists‎ Aprepitant   Fosaprepitant   Maropitant
Motion sickness‎ Cinnarizine   Dimenhydrinate   Meclizine   Meclizine/Pyridoxine   Scopolamine (Patch)
Pregnancy Meclizine/Pyridoxine   Ondansetron
Veterinary Maropitant