01 October 2005
Cytochrome P450 2D6 metabolism and 5-hydroxytryptamine type 3 receptor antagonistsfor postoperative nausea and vomiting.
Piotr K JanickiMed Sci Monit 2005; 11(10): RA322-328 :: ID: 430339
Abstract
Postoperative nausea and vomiting (PONV) affects approximately one thirdof patients and may lead to aspiration, dehiscence, esophageal rupture, and increased treatment costsif inadequately controlled. An important therapeutic option for prevention of PONV is 5-hydroxytryptaminetype 3 (5-HT3) receptor antagonists. Nonetheless, therapeutic failure sometimes occurs. Metabolism bythe cytochrome P450 (CYP) system differs among the 5-HT3 receptor antagonists, and provides a rationalexplanation for decreased therapeutic efficacy in some patients. Four of the 5-HT3 receptor antagonistagents (dolasetron, ondansetron, palonosetron, and tropisetron) are metabolized in various degrees viaCYP2D6, an isoform subject to marked genetic polymorphism. In patients with duplicate CYP2D6 alleles,degradation into inactive metabolites occurs rapidly with these four 5-HT3 receptor antagonists, resultingin decreased efficacy for preventing PONV. Granisetron is the only agent in this class that is not metabolizedvia CYP2D6. Instead, granisetron is metabolized via the CYP3A4 isoform, which is not subject to significantgenetic polymorphism. CYP2D6 genotype screening prior to PONV treatment may allow for modification ofantiemetic dosing. An alternative is to use a 5-HT3 agent that is metabolized independently of the CYP2D6isoform, such as granisetron, that would obviate the need for genotyping and may lead to improved prophylaxisof PONV.
Keywords: Genotype, Cytochrome P-450 Enzyme System - metabolism, Cytochrome P-450 CYP2D6 - metabolism, Postoperative Nausea and Vomiting - prevention & control, Serotonin 5-HT3 Receptor Antagonists, Serotonin Antagonists - therapeutic use
626 31
Editorial
01 June 2023 : Editorial
Editorial: Infectious Disease Surveillance Using Artificial Intelligence (AI) and its Role in Epidemic and Pandemic PreparednessDOI: 10.12659/MSM.941209
Med Sci Monit 2023; 29:e941209
In Press
08 Jun 2023 : Clinical Research
Risk Factors for New Vertebral Compression Fracture After Percutaneous Vertebral Augmentation: A Retrospect...Med Sci Monit In Press; DOI: 10.12659/MSM.940134
08 Jun 2023 : Clinical Research
A Nomogram for Identifying HR+/Her2- Breast Cancer Patients with Positive Sentinel Lymph Nodes and Omitted ...Med Sci Monit In Press; DOI: 10.12659/MSM.940124
08 Jun 2023 : Clinical Research
Burden of COVID-19 on Mental Health of Resident Doctors in PolandMed Sci Monit In Press; DOI: 10.12659/MSM.940208
08 Jun 2023 : Clinical Research
Risk Prediction for Rapidly Progressive Interstitial Lung Disease in Anti-MDA5-Positive Dermatomyositis: Th...Med Sci Monit In Press; DOI: 10.12659/MSM.940251
Most Viewed Current Articles
13 Nov 2021 : Clinical Research
Acceptance of COVID-19 Vaccination and Its Associated Factors Among Cancer Patients Attending the Oncology ...DOI :10.12659/MSM.932788
Med Sci Monit 2021; 27:e932788
30 Dec 2021 : Clinical Research
Retrospective Study of Outcomes and Hospitalization Rates of Patients in Italy with a Confirmed Diagnosis o...DOI :10.12659/MSM.935379
Med Sci Monit 2021; 27:e935379
08 Mar 2022 : Review article
A Review of the Potential Roles of Antioxidant and Anti-Inflammatory Pharmacological Approaches for the Man...DOI :10.12659/MSM.936292
Med Sci Monit 2022; 28:e936292
01 Jan 2022 : Editorial
Editorial: Current Status of Oral Antiviral Drug Treatments for SARS-CoV-2 Infection in Non-Hospitalized Pa...DOI :10.12659/MSM.935952
Med Sci Monit 2022; 28:e935952