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Pharmacokinetic Analysis of Benzodiazepine Receptor Binding of [123I]Iomazenil in Human Brain

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Abstract

Purpose. The purpose of this study is to evaluate the central benzodiazepine (BZP) receptor binding of iomazenil (IMZ) by pharmacokinetic analysis and to establish a methodology for the diagnosis of CNS disorders with abnormalities in BZP receptor binding.

Methods. BZP receptor binding of IMZ was analyzed kinetically using plasma concentration-time profiles and dynamic single photon emission computed tomography (SPECT) data obtained after the intravenous administration of IMZ to patients with neuropsychiatric diseases. The analysis was based on a 3-compartmental model including the processes of both blood-brain barrier (BBB) transport and BZP receptor binding.

Results. Hydrolized metabolite of IMZ was detected in plasma, indicating the need for separation by HPLC. The BBB influx clearance and the receptor binding potential of IMZ in the medial temporal region was reduced in the epileptic patient.

Conclusions. Our findings suggest the possibility of detecting the epileptic focus by using our method.

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Authors and Affiliations

  1. Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113, Japan

    Kiyomi Ito

  2. Department of Radiology, University of Tokyo Hospital, Faculty of Medicine, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113, Japan

    Toshimitsu Momose, Yoshiki Kojima & Yasuhito Sasaki

  3. Department of Pharmacy, University of Tokyo Hospital, Faculty of Medicine, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo, 113, Japan

    Hajime Kotaki, Koujirou Yamamoto, Masataka Katashima & Tatsuji Iga

  4. Faculty of Pharmaceutical Sciences, Kyushu University, 3-1-1 Mai-dashi, Higashi-ku, Fukuoka, 812, Japan

    Yasufumi Sawada

Authors
  1. Kiyomi Ito
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  2. Toshimitsu Momose
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  3. Hajime Kotaki
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  4. Yoshiki Kojima
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  5. Koujirou Yamamoto
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  6. Masataka Katashima
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  7. Yasufumi Sawada
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  8. Yasuhito Sasaki
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  9. Tatsuji Iga
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Ito, K., Momose, T., Kotaki, H. et al. Pharmacokinetic Analysis of Benzodiazepine Receptor Binding of [123I]Iomazenil in Human Brain. Pharm Res 14, 999–1003 (1997). https://doi.org/10.1023/A:1012188909100

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  • DOI: https://doi.org/10.1023/A:1012188909100

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