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Retinoids

Advances in Basic Research and Therapy

  • C. E. Orfanos
  • O. Braun-Falco
  • E. M. Farber
  • Ch. Grupper
  • M. K. Polano
  • R. Schuppli

Table of contents

  1. Front Matter
    Pages N1-XX
  2. Introduction

    1. C. E. Orfanos
      Pages 1-2
  3. Pharmacology and Toxicology of Retinoids

  4. Biological Effects of Retinoids

    1. Front Matter
      Pages 71-71
    2. R. Marks, A. Finlay, S. Nicholls, S. Barton
      Pages 77-83
    3. Ch. N. Ellis, R. C. Gold, R. C. Grekin, N. A. Swanson, Th. F. Anderson, J. J. Voorhees
      Pages 93-98
    4. A. Vahlquist, G. Michaëlsson, A. Kober, I. Sjöholm, G. Palmskog, U. Pettersson
      Pages 109-116
    5. L. Rusciani, P. Massaro, P. Orlando, F. P. Spinnato, A. Venier, F. Serri
      Pages 139-143
    6. G. O. Mahrle, D. I. Wilkinson, E. M. Farber
      Pages 145-152
    7. K. Madison, Ph. S. Tong, C. L. Marcelo, J. J. Voorhees
      Pages 161-161
  5. Application of Oral Retinoids in Psoriasis

    1. Front Matter
      Pages 163-163
    2. S. Jablonska, H. Wolska, J. Dąbrowski, M. Haftek, M. Groniowska, M. Jarząbek-Chorzelska
      Pages 165-173
    3. J. C. Gatti, J. E. Cardama, M. Gabrielli, H. Cabrera
      Pages 185-191
    4. J. Lauharanta, T. Juvakoski, L. Kanerva, A. Lassus
      Pages 201-203
    5. R. Stollenwerk, H. Fischer-Hoinkes, K. Komenda, F. Schilling
      Pages 205-209
  6. Application of Oral Retinoids in Acne

    1. Front Matter
      Pages 211-211
    2. J. S. Strauss, R. J. Thomsen, L. N. Farrell, A. M. Stranieri
      Pages 237-243
    3. A. M. Kligman, J. J. Leyden, O. Mills Jr.
      Pages 245-253
    4. D. H. Jones, W. J. Cunliffe, J. H. Cove
      Pages 255-258
    5. M. Landthaler, J. Kummermehr, A. Wagner, J. Nikolowski, G. Plewig
      Pages 259-266
  7. Oral Retinoid Therapy of Miscellaneous Disorders of Skin and Oral Mucosa

About these proceedings

Introduction

With the aromatic retinoic acid analog Tigason oral and intravenous pharmacokinetic studies have been performed in 5 normal volunteers. Simultaneous fitting of single i. v. and oral data to a three-compartment model assuming first-order absorption was possible. Using Nonlin parameter estimates of the single-dose data, one is able to predict the decline in plasma levels of parent drug following cessation of a 10 days multiple dosing regimen up to 24 hours. The model is however unable to predict a phase of prolonged elimination observed beyond 24 hours. Moreover in 5 patients, who underwent chronic therapy (8-15 months), substantial plasma levels of both unchanged drug and main metabolite (corre­ sponding carboxylic acid) were observed up to 140 days after cessation of the therapy. An apparent half-life of elimination of 80-100 days can be calculated. The drug appears to be stored at some yet unknown storage site. Investigation of metabolism of Tigason in rats and humans revealed 19 different bio­ transformation products thus far, most of them appearing in the urine in low amounts (20010 of dose). A few of them (mainly the acid Ro 10-1670) after conjugation to glucuronic acid are excreted in the bile in high amounts (60-80% of dose). No drug appeared unchanged in the excreta after i. v. administration to rats. References 1. Bollag W (1971) Effects of vitamin A acid (NSC-122758) on transplantable and chemically-induced tumors. Cancer Chemother Rep 55:53-58 2.

Keywords

Hautkrankheit Retinsäure cancer skin disease therapy

Editors and affiliations

  • C. E. Orfanos
    • 1
  • O. Braun-Falco
    • 2
  • E. M. Farber
    • 3
  • Ch. Grupper
    • 4
  • M. K. Polano
    • 5
  • R. Schuppli
    • 6
  1. 1.Department of Dermatology, University Medical Center SteglitzThe Free University of BerlinBerlin 45West Germany
  2. 2.Universitäts-HautklinikMünchen 2West Germany
  3. 3.Department of DermatologyStanford University School of MedicineStanfordUSA
  4. 4.ParisFrance
  5. 5.Postdam 7, WarmondNetherlands
  6. 6.Dermatologische Universitätsklinik, Kantonsspital BaselBaselSwitzerland

Bibliographic information

  • DOI https://doi.org/10.1007/978-3-642-68023-6
  • Copyright Information Springer-Verlag Berlin Heidelberg 1981
  • Publisher Name Springer, Berlin, Heidelberg
  • eBook Packages Springer Book Archive
  • Print ISBN 978-3-642-68025-0
  • Online ISBN 978-3-642-68023-6
  • Buy this book on publisher's site