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Chlorambucil

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Intraocular Inflammation

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Abstract

Chlorambucil (Leukeran) is an alkylating agent that has been available since 1952. Alkylating agents substitute an alkyl group for hydrogen ions in organic compounds. Alkylation of DNA results in binding of DNA strands so they cannot “unzip” and replicate. Cell death is induced in rapidly proliferating tissue such as the bone marrow. Chlorambucil is readily and reliably absorbed orally with availability of 56–105 %. Bioavailability increases from 50 to 75 % when taken on a full stomach. The half-life in the serum is 1.5 h, and it is metabolized in the liver to phenyl acetic acid mustard which also has cytotoxicity. Hydrolysis of both chlorambucil and phenyl acetic acid mustard to inactive compounds results in elimination of less than 1 % of both in the urine. Chlorambucil has a very slow onset of action (~4 weeks for full activity) making acute toxicity unlikely.

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Author information

Authors and Affiliations

  1. Ophthalmology, University of Illinois at Chicago, 48 S Greenleaf, Gurnee, IL, 60031, USA

    Howard H. Tessler MD (Professor Emeritus)

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  1. Howard H. Tessler MD
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Correspondence to Howard H. Tessler MD .

Editor information

Editors and Affiliations

  1. Centre of Ophthalmology, University of Tuebingen, Tuebingen, Germany

    Manfred Zierhut

  2. Biomedical Research Centre, Institute of Ophthalmology, Moorfields Eyes Hospital, Department of Medical Retina, UCL, London, United Kingdom

    Carlos Pavesio

  3. School of Medicine, Department of Ophthalmology, Hokkaido University Graduate, Sapporo, Hokkaido, Japan

    Shigeaki Ohno

  4. University of Belo Horizonte, Belo Horizonte, Brazil

    Fernando Orefice

  5. USC Eye Institute, University of Southern California, Los Angeles, California, USA

    Narsing A. Rao

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© 2016 Springer-Verlag Berlin Heidelberg

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Tessler, H.H. (2016). Chlorambucil. In: Zierhut, M., Pavesio, C., Ohno, S., Orefice, F., Rao, N. (eds) Intraocular Inflammation. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-540-75387-2_23

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  • DOI: https://doi.org/10.1007/978-3-540-75387-2_23

  • Publisher Name: Springer, Berlin, Heidelberg

  • Print ISBN: 978-3-540-75385-8

  • Online ISBN: 978-3-540-75387-2

  • eBook Packages: MedicineMedicine (R0)

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