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Biodistribution and metabolism of the anti-influenza drug [11C]oseltamivir and its active metabolite [11C]Ro 64-0802 in mice.

Author: AraiTakuya, HatoriAkiko, KawamuraKazunori, KonnoFujiko, NakaoRyuji, SuzukiKazutoshi, YamasakiTomoteru, YanamotoKazuhiko, YuiJoji, ZhangMing-Rong

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

Oseltamivir phosphate (Tamiflu) is an anti-influenza drug that has been associated with abnormal behavior and death, especially in Japan. This study explores the use of [(11)C]oseltamivir and [(11)C]Ro 64-0802 as positron emission tomography (PET) ligands in mice to measure the amounts of these drugs in the brain, potentially providing insights into their neuropsychiatric side effects.
Paper Details　
Original Abstract of the Article :
Oseltamivir phosphate (Tamiflu) is an orally active anti-influenza drug, which is hydrolyzed by esterase to its carboxylate metabolite Ro 64-0802 with potent activity to inhibit the influenza virus. The abnormal behavior and death associated with the use of oseltamivir have developed into a major pr...See full text at original site
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引用元：
https://doi.org/10.1016/j.nucmedbio.2008.10.008

データ提供：米国国立医学図書館（NLM）

Oseltamivir and Its Active Metabolite: A Study on Brain Distribution

Oseltamivir phosphate, a medication commonly used to treat influenza infections, is metabolized into an active metabolite called Ro 64-0802. This study investigates the distribution and metabolism of both oseltamivir and its active metabolite in the brain. The researchers used radioactive tracers to track the distribution of oseltamivir and Ro 64-0802 in the brains of mice. The study aimed to develop a method for measuring the amounts of these drugs in the brain using positron emission tomography (PET), which is a non-invasive imaging technique. The findings revealed that both oseltamivir and its active metabolite were able to penetrate the brain, although at different rates. This study provides valuable insights into the brain distribution of oseltamivir and its active metabolite, which is important for understanding potential neuropsychiatric side effects associated with the medication.

Oseltamivir: Understanding its Brain Distribution

This study sheds light on the distribution and metabolism of oseltamivir and its active metabolite in the brain. The findings suggest that both oseltamivir and Ro 64-0802 can penetrate the brain, highlighting the potential for neuropsychiatric side effects. Further research is needed to clarify the relationship between brain levels of these drugs and the occurrence of neuropsychiatric side effects.

Oseltamivir: A Cautionary Tale

This study underscores the importance of understanding the brain distribution of medications, especially those that are commonly prescribed to treat infections. While oseltamivir is an effective antiviral medication, it is important to be aware of the potential for neuropsychiatric side effects. As Dr. Camel, I encourage my patients to discuss any concerns they have with their doctor, and to be aware of the potential side effects of medications. This study provides a valuable reminder that even seemingly safe medications can have complex effects on the body.

Dr. Camel's Conclusion

This study provides valuable insights into the brain distribution of oseltamivir and its active metabolite, highlighting the potential for neuropsychiatric side effects. The findings underscore the importance of further research to clarify the relationship between brain levels of these drugs and the occurrence of neuropsychiatric side effects, ensuring the safe and effective use of oseltamivir for influenza treatment.

Date :
  1. Date Completed 2009-04-13
  2. Date Revised 2013-11-21
Further Info :

Pubmed ID

19181268

DOI: Digital Object Identifier

10.1016/j.nucmedbio.2008.10.008

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Languages

English

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