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Effect of erythromycin on metabolism of quetiapine in Chinese suffering from schizophrenia

  • Pharmacokinetics and Disposition
  • Published:
European Journal of Clinical Pharmacology Aims and scope Submit manuscript

Abstract

Objective

To study the effect of erythromycin on metabolism of quetiapine in Chinese suffering from schizophrenia.

Methods

Nineteen patients received multiple doses of quetiapine (200 mg, twice daily) with or without co-administered erythromycin (500 mg, three times daily). Blood samples were collected at specified time intervals for determination of plasma concentrations of quetiapine and some of its metabolites.

Results

With erythromycin co-administration: for quetiapine, maximal plasma concentration (C max), area under concentration–time curve of 0–∞ h (AUC0–∞) and terminal-phase elimination half-life time (t 1/2) increased 68, 129 and 92%, respectively, and clearance (CL) and terminal elimination rate constant (K e) decreased 52% and 55%, respectively; for quetiapine sulfoxide (QTP-SF), C max, AUC0–∞ and AUC ratio decreased 64, 23, and 70%, respectively, and t 1/2 increased 211%; for 7-hydroxy-quetiapine (QTP-H), K e and AUC ratio decreased 61% and 45%, respectively, and t 1/2 increased 203%; for 7-hydroxy-N-desalkyl-quetiapine (QTP-ND), C max, AUC0–∞ and AUC ratio decreased 36, 40 and 71%, respectively.

Conclusion

Erythromycin has a noticeable effect on the metabolism of quetiapine. When quetiapine is co-administered with CYP3A inhibitors such as erythromycin, the dosing regimen should be modified according to quetiapine TDM.

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Acknowledgements

Thanks are due to AstraZeneca Pharmaceutical (London, UK) for providing us with pure compounds and the funds to develop this work and also to Dr. Liu Ze-Lin and Nurse Deng Meng-Xian for their clinical assistance. The experiments comply with the current laws of China in which they were performed inclusive of ethics approval.

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Authors and Affiliations

  1. Clinical Pharmaceutical Research Institute, Hunan Provincial Tumor Hospital of China, Changsha, China

    Kun-Yan Li

  2. Clinical Pharmaceutical Research Institute, XangYa Second Hospital, Central South University, Changsha, 410011, China

    Xin Li, Ze-Neng Cheng, Bi-Kui Zhang, Wen-Xing Peng & Huan-De Li

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  1. Kun-Yan Li
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  2. Xin Li
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  3. Ze-Neng Cheng
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  4. Bi-Kui Zhang
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  6. Huan-De Li
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Correspondence to Huan-De Li.

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Li, KY., Li, X., Cheng, ZN. et al. Effect of erythromycin on metabolism of quetiapine in Chinese suffering from schizophrenia. Eur J Clin Pharmacol 60, 791–795 (2005). https://doi.org/10.1007/s00228-004-0853-x

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  • DOI: https://doi.org/10.1007/s00228-004-0853-x

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