OCT1 mediates hepatic uptake of sumatriptan and loss-of-function OCT1 polymorphisms affect sumatriptan pharmacokinetics.

Author: Abu AbedM, BrockmöllerJ, Dos Santos PereiraJ N, FaltracoF, KnochT, KuronD, MatthaeiJ, PrukopT, TzvetkovM V

Paper Details 
Original Abstract of the Article :
The low bioavailability of the anti-migraine drug sumatriptan is partially caused by first-pass hepatic metabolism. In this study, we analyzed the impact of the hepatic organic cation transporter OCT1 on sumatriptan cellular uptake, and of OCT1 polymorphisms on sumatriptan pharmacokinetics. OCT1 tra...See full text at original site
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引用元:
https://doi.org/10.1002/cpt.317

データ提供:米国国立医学図書館(NLM)

Unlocking the Secrets of Sumatriptan's Absorption: The Role of OCT1

The field of [pharmacokinetics] focuses on how drugs are absorbed, distributed, metabolized, and eliminated by the body. This study sheds light on the role of the hepatic organic cation transporter OCT1 in sumatriptan's absorption, a crucial element in the effectiveness of this anti-migraine drug. Researchers explored the impact of various OCT1 polymorphisms, genetic variations affecting OCT1's function, on sumatriptan's pharmacokinetics. They found that OCT1 plays a significant role in transporting sumatriptan to the liver, and that certain OCT1 polymorphisms can significantly alter its absorption and bioavailability.

OCT1 Polymorphisms: A Tale of Two Transporters

This research reveals the intricate interplay between genetic variations and drug absorption. The authors found that individuals with OCT1 deficiency had significantly higher plasma concentrations of sumatriptan compared to those with fully active OCT1. This observation suggests that OCT1 polymorphisms can influence the effectiveness of sumatriptan in individuals, highlighting the importance of personalized medicine approaches in treating migraines.

Migraine Management: A Personalized Approach

This research underscores the need for personalized medicine in migraine management. Understanding the individual differences in OCT1 function can help tailor treatment strategies for patients with migraines, optimizing the effectiveness of medications like sumatriptan. This research encourages us to move beyond a one-size-fits-all approach to healthcare and embrace the power of personalized interventions.

Dr. Camel's Conclusion

This research is a testament to the intricate network of factors that govern drug absorption and effectiveness. It's like navigating a vast desert landscape where even a subtle change in the terrain, such as a genetic variation, can significantly alter the journey of a drug. Understanding these individual differences is crucial to ensure that the right drug reaches the right destination at the right time, leading to more effective migraine management.

Date :
  1. Date Completed 2017-05-23
  2. Date Revised 2018-06-29
Further Info :

Pubmed ID

26659468

DOI: Digital Object Identifier

10.1002/cpt.317

SNS
PICO Info
in preparation
Languages

English

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