Tropisetron: an Update of Its Use in the Prevention of Chemotherapy-induced Nausea and Vomiting

Overview

Journal Drugs

Specialty Pharmacology

Date 2000 Jul 6

PMID 10882164

Citations 26

Authors

K Simpson

C M Spencer

K J McClellan

Affiliations

Soon will be listed here.

Abstract

Unlabelled: Tropisetron is a serotonin (5-hydroxytryptamine; 5-HT) antagonist that is primarily used in the prevention of chemotherapy-induced nausea and vomiting. Antagonism of 5-HT3 binding sites in the peripheral and central nervous system is the probable mechanism of prevention of acute nausea and vomiting. Effects on delayed nausea and vomiting are less well understood as these are probably not mediated solely by 5-HT3 receptors. Tropisetron monotherapy is effective for the control of acute, and to a lesser extent delayed, nausea and vomiting in patients receiving moderately to severely emetogenic chemotherapy. The combination of dexamethasone and tropisetron is more effective than monotherapy. Complete control of cisplatin-induced nausea and vomiting was obtained in 69 to 97% of patients receiving the combination compared with 46 to 80% receiving tropisetron monotherapy in randomised trials. There were generally no significant differences between the control of acute or delayed nausea and vomiting provided by tropisetron, ondansetron or granisetron in randomised, comparative trials. The antiemetic efficacy of tropisetron was maintained over multiple cycles of chemotherapy. Most comparative studies showed tropisetron monotherapy to be more effective than metoclopramide in controlling acute nausea and vomiting, with the exception of 1 study which showed similar efficacy. However, high dose metoclopramide plus dexamethasone provided similar control of delayed emesis to tropisetron plus dexamethasone. Tropisetron is also effective in children, including those who responded poorly to previous antiemetic treatment. Tropisetron and ondansetron generally have similar efficacies in this population. The drug enhanced patients' quality of life and was well tolerated by adults and children alike. The recommended oral and IV dosage of tropisetron is 5 mg once daily; there is no increase in efficacy with doses >5 mg.

Conclusions: Tropisetron is similar to other 5-HT3 receptor antagonists for the prevention of chemotherapy-induced nausea and vomiting in both adults and children. It is suitable as first-line therapy (combined with a corticosteroid) for the prevention of acute nausea and vomiting in patients treated with moderately to severely emetogenic chemotherapeutic agents. This combination is also moderately effective in the prevention of delayed nausea and vomiting.

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References

Massidda B, Ionta M . Prevention of delayed emesis by a single intravenous bolus dose of 5-HT3-receptor-antagonist in moderately emetogenic chemotherapy. J Chemother. 1996; 8(3):237-42. DOI: 10.1179/joc.1996.8.3.237. View

Sorbe B, Andersson H, Schmidt M, Soderberg M, Hogberg T, Wernstedt L . Tropisetron (Navoban) in the prevention of chemotherapy-induced nausea and vomiting--the Nordic experience. Support Care Cancer. 1994; 2(6):393-9. DOI: 10.1007/BF00344055. View

de Bruijn K . The development of tropisetron in its clinical perspective. Ann Oncol. 1993; 4 Suppl 3:19-23. DOI: 10.1093/annonc/4.suppl_3.s19. View

Garcia-Del-Muro X, Vadell C, Perez Manga G, Bover I, Rifa J, Beltran M . Randomised double-blind study comparing tropisetron alone and in combination with dexamethasone in the prevention of acute and delayed cisplatin-induced emesis. Eur J Cancer. 1998; 34(1):193-5. DOI: 10.1016/s0959-8049(97)00367-5. View

Kris M, Pendergrass K, Navari R, Grote T, Nelson A, Thomas V . Prevention of acute emesis in cancer patients following high-dose cisplatin with the combination of oral dolasetron and dexamethasone. J Clin Oncol. 1997; 15(5):2135-8. DOI: 10.1200/JCO.1997.15.5.2135. View

Bleiberg H, Hulstaert F, Buyse M, De Keyser P . Tropisetron in the prevention of acute and delayed nausea and vomiting over six courses of emetogenic chemotherapy. Anticancer Drugs. 1998; 9(9):773-7. DOI: 10.1097/00001813-199810000-00005. View

Malik I, Moid I, Khan Z, Hussain M . Prospective randomized comparison of tropisetron with and without dexamethasone against high-dose metoclopramide in prophylaxis of acute and delayed cisplatin-induced nausea and vomiting. Am J Clin Oncol. 1999; 22(2):126-30. DOI: 10.1097/00000421-199904000-00004. View

Jantunen I, Muhonen T, Kataja V, Flander M, Teerenhovi L . 5-HT3 receptor antagonists in the prophylaxis of acute vomiting induced by moderately emetogenic chemotherapy--a randomised study. Eur J Cancer. 1993; 29A(12):1669-72. DOI: 10.1016/0959-8049(93)90101-k. View

Roila F, Tonato M, Cognetti F, Cortesi E, Favalli G, Marangolo M . Prevention of cisplatin-induced emesis: a double-blind multicenter randomized crossover study comparing ondansetron and ondansetron plus dexamethasone. J Clin Oncol. 1991; 9(4):675-8. DOI: 10.1200/JCO.1991.9.4.675. View

10.

Lee C, Plosker G, McTavish D . Tropisetron. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential as an antiemetic. Drugs. 1993; 46(5):925-43. DOI: 10.2165/00003495-199346050-00009. View

11.

Wymenga A, van der Graaf W, Wils J, Siegenbeek van Heukelom L, VAN DER LINDEN G, Nooy M . A randomized, double-blind, multicentre study comparing daily 2 and 5 mg of tropisetron for the control of nausea and vomiting induced by low-dose cisplatin- or non-cisplatin-containing chemotherapy. Ann Oncol. 1996; 7(5):505-10. DOI: 10.1093/oxfordjournals.annonc.a010640. View

12.

Bruntsch U, Rufenacht E, Parker I, Drechsler S, de Bruijn K . Tropisetron in the prevention of chemotherapy-induced nausea and vomiting in patients responding poorly to previous conventional antiemetic therapy. Ann Oncol. 1993; 4 Suppl 3:25-9. DOI: 10.1093/annonc/4.suppl_3.s25. View

13.

de Bruijn K . Tropisetron. A review of the clinical experience. Drugs. 1992; 43 Suppl 3:11-22. DOI: 10.2165/00003495-199200433-00005. View

14.

Gralla R, Osoba D, Kris M, Kirkbride P, Hesketh P, Chinnery L . Recommendations for the use of antiemetics: evidence-based, clinical practice guidelines. American Society of Clinical Oncology. J Clin Oncol. 1999; 17(9):2971-94. DOI: 10.1200/JCO.1999.17.9.2971. View

15.

Anderson H, Thatcher N, Howell A, Logan K, Sage T, de Bruijn K . Tropisetron compared with a metoclopramide-based regimen in the prevention of chemotherapy-induced nausea and vomiting. Eur J Cancer. 1994; 30A(5):610-5. DOI: 10.1016/0959-8049(94)90530-4. View

16.

Yalcin S, Tekuzman G, Baltali E, Ozisik Y, Barista I . Serotonin receptor antagonists in prophylaxis of acute and delayed emesis induced by moderately emetogenic, single-day chemotherapy: a randomized study. Am J Clin Oncol. 1999; 22(1):94-6. DOI: 10.1097/00000421-199902000-00023. View

17.

Zhang P, Sun Y, Zhang H . [A randomized trial of tropisetron in the prophylaxis of nausea and vomiting induced by chemotherapy]. Zhonghua Zhong Liu Za Zhi. 1996; 18(2):154-6. View

18.

Roila F, Ballatori E, Tonato M, Del Favero A . 5-HT3 receptor antagonists: differences and similarities. Eur J Cancer. 1997; 33(9):1364-70. DOI: 10.1016/s0959-8049(97)00003-8. View

19.

Lofters W, Pater J, Zee B, Dempsey E, Walde D, Moquin J . Phase III double-blind comparison of dolasetron mesylate and ondansetron and an evaluation of the additive role of dexamethasone in the prevention of acute and delayed nausea and vomiting due to moderately emetogenic chemotherapy. J Clin Oncol. 1997; 15(8):2966-73. DOI: 10.1200/JCO.1997.15.8.2966. View

20.

Adams M, Soukop M, Barley V, Yosef H, Anderson H, Boesen E . Tropisetron alone or in combination with dexamethasone for the prevention and treatment of emesis induced by non-cisplatin chemotherapy: a randomized trial. Anticancer Drugs. 1995; 6(4):514-21. DOI: 10.1097/00001813-199508000-00004. View