Itraconazole による深在性真菌症の治療  [in Japanese] Treatment of systemic fungal infections with Itraconazole preparations  [in Japanese]

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    • 河野 茂 KOHNO Shigeru
    • 長崎大学大学院医歯薬学総合研究科感染免疫学講座 Department of Microbiology and Immunology, Nagasaki University Graduate School of Biomedical Science


イトラコナゾールは,non-albicans Candidaを含めたカンジダ属やアスペルギルス属に対しても強い抗真菌活性を示すトリアゾール系抗真菌薬である。日本ではカプセル薬のみしか市販されていないが,hydroxypropyl-β-cyclodextrin(HP-β-CD)に可溶化させることで内用液と注射薬がようやく日本でも開発された。内用液はカプセル薬に比べ消化管からの吸収性が改善され,注射薬は2日間のLoading dose(400 mg分2/日)により,深在性真菌症の治療に必要な高い血漿中濃度を早期に安定して維持することが可能となった。 海外では,すでにイトラコナゾールの内用液や注射薬による標的治療や経験的治療の臨床試験が実施され,優れた効果が報告されている。侵襲性アスペルギルス症に対する標的治療では,試験対象例にアムホテリシンB(AMPH)静注無効例が多く含まれていたが,イトラコナゾール静注後にカプセル薬を継続投与することにより,寛解率(寛解+部分寛解)は静注投与終了時に32%,試験終了時に48%と優れた効果を示した。また,好中球減少時の広域抗菌薬無効の持続発熱における経験的治療では,イトラコナゾール静注と内用液を継続使用することにより,AMPH静注と同程度の効果が得られ,腎毒性を含めた有害事象や治療脱落は有意に少ないと報告されている。 日本では,すでにカプセル薬が1993年から発売されており,皮膚真菌症および内臓真菌症に広く臨床応用されている。今後,内用液や注射薬の使用可能になることで,イトラコナゾールは深在性真菌症の有用な選択肢の一つになると思われる。Itraconazole is an anti-fungal agent of the triazole family that has been shown to exhibit potent activity against fungi of Candida including non-albicans Candida and Aspergillus,. Currently, only capsule form is available for clinical use. However, with the development of a technique to dissolve the drug in hydroxypropyl-β-cyclodextrin, itraconazole oral solution and injection have begun to be developed. Itraconazole oral solution is better absorbed from the digestive tract capsule form. Itraconazole injection is administered at a loading dose level (200 mg/day in two divided doses) on the first two days, to allow rapid increase and maintenance of the plasma level of the drug to the level needed for the treatment of systemic fungal infections. In foreign countries, trials of targeted therapy and empiric therapy using itraconazole oral solution and injection administration have been carried out and obtained excellent results. In regard to targeted therapy for patients with invasive aspergillosis (including many cases failure to intravenous amphotericin B (AMPH) therapy), itraconazole injection treatment followed by itraconazole capsules has obtained excellent results, with a remission (remission+partial remission) rate of 32% at the end of the injection treatment and 48% at the end of the study. In regard to empiric therapy for cases of persistent fever due to fungal infection (associated with neutropenia and failure to broad-spectrum antimicrobial agents), the efficacy of itraconazole injection and oral solution was found to be comparable to that of intravenous AMPH therapy, with, in addition, a significantly lower incidence of adverse reactions (nephrotoxicity, etc.) and dropouts. In Japan, itraconazole capsules began to be marketed in 1993, and they have been used clinically for the treatment of skin and systemic fungal infections. When itraconazole oral solution and injection become available, the drug may become one of the major alternatives for the treatment of systemic fungal infections.


  • 日本化学療法学会雜誌 = Japanese journal of chemotherapy  

    日本化学療法学会雜誌 = Japanese journal of chemotherapy 54, 1-5, 2006-10-20 


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