Retinoids

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

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.

• Hautkrankheit
• Retinsäure
• cancer
• skin disease
• therapy

• 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

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