| Japanese |
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| Title | 中枢性ベンゾジアゼピン受容体イメージング剤123I-イオマゼニルの第1相臨床試験 |
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| Subtitle | 技術報告 |
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| Authors | 米倉義晴*, 西澤貞彦**, 田中富美子**, 石津浩一**, 岡沢秀彦**, 藤田透**, 小西淳二**, 鳥塚莞爾*** |
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| Authors(kana) | |
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| Organization | *京都大学医学部脳病態生理学講座, **放射線核医学科, ***福井医科大学 |
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| Journal | 核医学 |
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| Volume | 32 |
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| Number | 1 |
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| Page | 87-97 |
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| Year/Month | 1995/1 |
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| Article | 報告 |
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| Publisher | 日本核医学会 |
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| Abstract | 「要旨」中枢性ベンゾジアゼピン受容体 (BZR) の局所脳内分布を評価するために開発された123I-イオマゼニルの安全性および薬物体内動態の検討を目的として, 健常成人男子6例を対象に第1相臨床試験を実施した. 本剤の脳への集積は, 投与後10〜20分で11.7±1.6%と最大に達した後, 徐々に消失した. 脳内局所における分布は, 投与直後 (0〜10分) にはほぼ脳血流を反映する取り込みを示したが, 投与後2〜3時間以降では, 深部灰白質における早い洗い出しがみられ, BZRの局在を反映した脳内分布を示し, 本剤がBZR指向性の薬剤であることが示された. 脳以外の臓器への著明な集積はみられなかった. また, 本剤に起因すると考えられる自・他覚症状の変化, 理学所見の変化あるいは臨床検査値の異常変動はいずれもみられず, また本剤による吸収線量も問題になる線量とは考えられなかった. 本剤はBZRの局所脳内分布の評価に適した放射性医薬品であると考えられた. |
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| Practice | 臨床医学：一般 |
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| Keywords | 123I-iomazenil, Benzodiazepine receptor, Phase 1 study, Biodistribution, Safety evaluation |
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| English |
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| Title | Phase 1 Clinical Study of 123I-Iomazenil : A New Probe to Evaluate Central-Type Benzodiazepine Receptor with SPECT |
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| Authors | Yoshiharu YONEKURA*, Sadahiko NISHIZAWA**, Fumiko TANAKA**, Kouichi ISHIZU**, Hidehiko OKAZAWA**, Toru FUJITA**, Junji KONISHI**, Kanji TORIZUKA*** |
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| Authors(kana) | |
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| Organization | *Department of Brain Pathophysiology, School of Medicine, Kyoto University, **Department of Nuclear Medicine, School of Medicine, Kyoto University, ***Fukui Medical School |
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| Journal | The Japanese Journal of nuclear medicine |
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| Volume | 32 |
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| Number | 1 |
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| Page | 87-97 |
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| Year/Month | 1995/1 |
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| Article | Report |
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| Publisher | THE JAPANESE SOCIETY OF NUCLEAR MEDICINE |
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| Abstract | [Summary] A Phase 1 clinical study of 123I-iomazenil (IMZ), a new radiopharmaceutical developed for evaluation of central-type benzodiazepine receptor (BZR) with SPECT, was performed to examine its safety and biodistribution in six healthy volunteers. The brain uptake of 123I-IMZ reached a maximum value of 11.7+-1.6% of the injected dose at 10-20 min after i.v. administration, and then decreased slowly. The regional tracer distribution immediately after injection (0-10 min) was considered to be a reflection of the cerebral blood flow. From 2 to 3 hours post-injection, washout of the radioactivity from the deep gray matter was observed, resulting in the distribution reflecting the reported distribution of BZR. No significant accumulation was seen in any organ other than the brain. The estimated absorbed dose of 123I-IMZ calculated by the MIRD method was comparable to that of 123I-N-isopropyl-p-iodoamphetamine. Neither adverse reactions nor abnormal clinical laboratory findings due to the drug administration were observed. These results suggest that 123I-IMZ is a safe and promising agent for evaluating the function of central-type BZR. |
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| Practice | Clinical medicine |
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| Keywords | 123I-iomazenil, Benzodiazepine receptor, Phase 1 study, Biodistribution, Safety evaluation |
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