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01.12.2014 | Research article | Ausgabe 1/2014 Open Access

The Journal of Headache and Pain 1/2014

Theory-based analysis of clinical efficacy of triptans using receptor occupancy

The Journal of Headache and Pain > Ausgabe 1/2014
Kentaro Tokuoka, Risa Takayanagi, Yuji Suzuki, Masayuki Watanabe, Yasuhisa Kitagawa, Yasuhiko Yamada
Wichtige Hinweise

Electronic supplementary material

The online version of this article (doi:10.​1186/​1129-2377-15-85) contains supplementary material, which is available to authorized users.

Competing interests

The authors declare that they have no competing interests.

Authors’ contributions

KT conceptualized and designed the study, acquired and analysis the data, and drafted the manuscript. RT conceptualized and designed the study, acquired and analysis the data, and drafted the manuscript. YS conceptualized and designed the study. MW conceptualized and designed the study. YK critically revised the manuscript. YY conceptualized and designed the study and critically revised the manuscript. All authors read and approved the final manuscript.



Triptans, serotonin 5-HT1B/1D receptor agonists, exert their action by targeting serotonin 5-HT1B/1D receptors, are used for treatment of migraine attack. Presently, 5 different triptans, namely sumatriptan, zolmitriptan, eletriptan, rizatriptan, and naratriptan, are marketed in Japan. In the present study, we retrospectively analyzed the relationships of clinical efficacy (headache relief) in Japanese and 5-HT1B/1D receptor occupancy (Φ1B and Φ1D). Receptor occupancies were calculated from both the pharmacokinetic and pharmacodynamic data of triptans.


To evaluate the total amount of exposure to drug, we calculated the area under the plasma concentration-time curve (AUCcp) and the areas under the time curves for Ф1B and Ф1D (AUCФ1B and AUCФ1D). Moreover, parameters expressing drug transfer and binding rates (A cp , A Ф 1B , A Ф 1D ) were calculated.


Our calculations showed that Фmax1B and Фmax1D were relatively high at 32.0-89.4% and 68.4-96.2%, respectively, suggesting that it is likely that a high occupancy is necessary to attain the clinical effect. In addition, the relationships between therapeutic effect and AUCcp, AUCΦ1B, AUCΦ1D, and A cp  · AUCcp differed with each drug and administered form, whereas a significant relationship was found between the therapeutic effect and A Φ 1B  · AUCΦ1B or A Φ 1D  · AUCΦ1D that was not affected by the drug and the form of administration.


These results suggest that receptor occupancy can be used as a parameter for a common index to evaluate the therapeutic effect. We considered that the present findings provide useful information to support the proper use of triptans.
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