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Retinoids

Advances in Basic Research and Therapy

  • Conference proceedings
  • © 1981

Overview

Editors:
  1. C. E. Orfanos

    1. Department of Dermatology, University Medical Center Steglitz, The Free University of Berlin, Berlin 45, West Germany

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  2. O. Braun-Falco

    1. Universitäts-Hautklinik, München 2, West Germany

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  3. E. M. Farber

    1. Department of Dermatology, Stanford University School of Medicine, Stanford, USA

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  4. Ch. Grupper

    1. Paris, France

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  5. M. K. Polano

    1. Postdam 7, Warmond, Netherlands

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  6. R. Schuppli

    1. Dermatologische Universitätsklinik, Kantonsspital Basel, Basel, Switzerland

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Table of contents (84 papers)

  1. Front Matter

    Pages N1-XX
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  2. Introduction

    1. Introduction

      • C. E. Orfanos
      Pages 1-2

  3. Pharmacology and Toxicology of Retinoids

    1. Front Matter

      Pages 3-3
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    2. From Vitamin A to Retinoids: Chemical and Pharmacological Aspects

      • W. Bollag
      Pages 5-11

    3. Pharmacokinetics and Metabolism of Oral Aromatic Retinoids

      • U. Paravicini
      Pages 13-20

    4. In Vivo Immunostimulating Properties of Two Retinoids: Ro 10-9359 and Ro 13-6298

      • Th. Hercend, M. Bruley-Rosset, I. Florentin, G. Mathé
      Pages 21-30

    5. Vitamin A Transport and Delivery and the Mechanism of Vitamin A Toxicity

      • DeWitt S. Goodman
      Pages 31-39

    6. Experimental Toxicology of the Aromatic Retinoid Ro 10-9359 (Etretinate)

      • K. Teelmann
      Pages 41-47

    7. Studies in Reproductive Toxicology and Mutagenicity with Ro 10-9359

      • H. Hummler, M. E. Schüpbach
      Pages 49-59

    8. Cytogenetic Studies in Patients Treated with Oral Retinoid Ro 10-9359

      • R. Happle, A. Niedworok
      Pages 61-65

    9. Chromosomal Analysis in Patients Treated with the Aromatic Retinoid Ro 10-9359

      • G. Obe, D. Tsambaos
      Pages 67-70

  4. Biological Effects of Retinoids

    1. Front Matter

      Pages 71-71
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    2. Retinoids: New Developments in Their Mechanism of Action as Related to Control of Proliferative Diseases

      • M. B. Sporn
      Pages 73-76

    3. The Effects of Retinoids on Stratum Corneum. Structure and Function

      • R. Marks, A. Finlay, S. Nicholls, S. Barton
      Pages 77-83

    4. Light and Electron Microscopic Changes of Human Epidermis Under Oral Retinoid Treatment

      • U. Schultz-Ehrenburg, C. E. Orfanos
      Pages 85-92

    5. Retinoid-Stimulated Material in Psoriatic Epidermis During Ro 10-9359 Therapy

      • Ch. N. Ellis, R. C. Gold, R. C. Grekin, N. A. Swanson, Th. F. Anderson, J. J. Voorhees
      Pages 93-98

    6. Effects of Oral Retinoid on Dermal Components in Human and Animal Skin

      • D. Tsambaos, C. E. Orfanos
      Pages 99-108

    7. Retinoid-binding Proteins and the Plasma Transport of Etretinate (Ro 10-9359) in Man

      • A. Vahlquist, G. Michaëlsson, A. Kober, I. Sjöholm, G. Palmskog, U. Pettersson
      Pages 109-116

    8. Biochemical Mechanism of Modulation of Skin Carcinogenesis by Retinoids

      • Ajit K. Verma
      Pages 117-131

    9. Mitogenic Properties of Aromatic Retinoids: in vivo and in vitro Effects on Epidermal Cells

      • J. Pohl, E. Christophers
      Pages 133-138
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Keywords

About this book

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.

Editors and Affiliations

  • Department of Dermatology, University Medical Center Steglitz, The Free University of Berlin, Berlin 45, West Germany

    C. E. Orfanos

  • Universitäts-Hautklinik, München 2, West Germany

    O. Braun-Falco

  • Department of Dermatology, Stanford University School of Medicine, Stanford, USA

    E. M. Farber

  • Paris, France

    Ch. Grupper

  • Postdam 7, Warmond, Netherlands

    M. K. Polano

  • Dermatologische Universitätsklinik, Kantonsspital Basel, Basel, Switzerland

    R. Schuppli

Bibliographic Information

  • Book Title: Retinoids

  • Book Subtitle: Advances in Basic Research and Therapy

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

  • DOI: https://doi.org/10.1007/978-3-642-68023-6

  • Publisher: Springer Berlin, Heidelberg

  • eBook Packages: Springer Book Archive

  • Copyright Information: Springer-Verlag, Berlin Heidelberg 1981

  • Softcover ISBN: 978-3-642-68025-0Published: 10 December 2011

  • eBook ISBN: 978-3-642-68023-6Published: 06 December 2012

  • Edition Number: 1

  • Number of Pages: XX, 530

  • Topics: Dermatology

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