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Is there a pharmacological basis for differences in 5-HT3-receptor antagonist efficacy in refractory patients?

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Abstract

5-HT3-receptor antagonists are the current antiemetic ‘gold standard’ for chemotherapy- and radiotherapy-induced nausea and vomiting. Interestingly, studies have shown that patients experiencing poor control of acute chemotherapy-induced nausea and vomiting with one antiemetic therapy may respond well to another agent, including a drug of the same class. This review examines pharmacological differences between the 5-HT3-receptor antagonists in order to determine potential reasons for their differing efficacy, particularly in relation to refractory emesis. Differences in drug metabolism by the cytochrome P450 system, inadequate dosing of the respective agents, differences in onset and duration of action, and effects on serotonin release and reuptake are discussed.

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Acknowledgements

This manuscript was supported by Roche.

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Authors and Affiliations

  1. Rotterdam Cancer Institute, Groene Hilledijk 301, 3075, Rotterdam, The Netherlands

    Ronald de Wit

  2. Clinique de Genolier, 1272, Genolier, Switzerland

    Matti Aapro

  3. Poole House, Great Yeldham, Halstead, Essex, CO9 4HP, UK

    Peter R Blower

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  1. Ronald de Wit
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  2. Matti Aapro
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  3. Peter R Blower
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Correspondence to Ronald de Wit.

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de Wit, R., Aapro, M. & Blower, P.R. Is there a pharmacological basis for differences in 5-HT3-receptor antagonist efficacy in refractory patients?. Cancer Chemother Pharmacol 56, 231–238 (2005). https://doi.org/10.1007/s00280-005-1033-0

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  • DOI: https://doi.org/10.1007/s00280-005-1033-0

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