Retinoids

Advances in Basic Research and Therapy
Softcover Nachdruck of the original 1. Auflage 1981
ISBN: 978-3-642-68025-0
Verlag: Springer

Buch, Englisch, 530 Seiten, Paperback, Format (B × H): 170 mm x 244 mm, Gewicht: 947 g

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.

Zielgruppe

Research

Autoren/Hrsg.

Orfanos, C. E.

Braun-Falco, O.

Schuppli, R.

Farber, E.M.

Grupper, C.

Polano, M. K.

Inhaltsverzeichnis

Pharmacology and Toxicology of Retinoids.- Biological Effects of Retinoids.- Application of Oral Retinoids in Psoriasis.- Application of Oral Retinoids in Acne.- Oral Retinoid Therapy of Miscellaneous Disorders of Skin and Oral Mucosa.- Clinical and Laboratory Monitoring of Oral Retinoid Therapy.- Short Clinical and Experimental Reports.- Present Status and Perspectives.