Pharmacokinetics of Droloxifene and Its Metabolites in Breast Cancer Patients

Pharmacokinetics and metabolism of droloxifene, a new antiestrogenic drug, have been investigated by single- and multiple-dose studies in postmenopausal patients with advanced breast cancer. Short terminal elimination half-life, low accumulation, and improved drug tolerability are the most striking features of this safe and effective new antiestrogen. Bioequivalence of film-coated tablet, tablet, and standard solution of droloxifene has been shown. The concentrations of droloxifene and its metabolites have been determined by a highly selective HPLC method.

Hypophysäre/Ovarielle Wirkstoffe

Unruptured tubal pregnancy: local low-dose therapy with methotrexate under transvaginal ultrasonographic guidance.

Thirty patients with unruptured ectopic pregnancy (4-10 weeks' gestation) were treated locally with methotrexate (MTX) under sonographic guidance. The transvaginal puncture was performed under analgesic sedation using an automatic puncturing device. Local MTX therapy was successful in 25 patients (83.3%). Eighteen of these patients had received a single MTX instillation with a total dose of 10 mg, 7 patients had received a second instillation with 10 mg because of plateauing hCG levels after the first instillation. In 5 patients MTX therapy was unsuccessful. Surgical intervention was necessary within 4 h to 15 days after MTX treatment, due to severe tubal bleeding (n = 1) or the development…

The Effects of Chlorotrianisene (Tace) on Kinetics of 3H-testosterone Metabolism in Patients with Carcinoma of the Prostate

Summary— Alterations in the metabolism of testosterone and plasma levels of testosterone, luteinising hormone (LH), follicle stimulating hormone (FSH), prolactin and oestradiol were studied in 6 patients with newly diagnosed prostatic carcinoma before and during treatment with chlorotrianisene at a daily dosage of 48 mg for 14 days. Parameters of plasma kinetics were determined according to the single injection technique and the 2-compartment model, and the plasma hormones by radioimmunoassay. Chlorotrianisene altered neither plasma levels of testosterone, gonadotrophins, prolactin and oestradiol, nor metabolic clearance rate, production rate and other kinetic parameters of testosterone. Th…

Radioimmunoassay of Plasma and Urinary Norepinephrine

Various analytical methods, such as fluorimetry, radioenzymic assay and in particular liquid chromatography are used for the analysis of norepinephrine (NA) in body fluids and tissue homogenates. These procedures, however, often lack sensitivity, are expensive and/or time consuming. Basing on our previous reports on the radioimmunoassay of chemically modified serotonin1, 5-hydroxy-3-indole acetic acid2 and normetanephrine (NMN)3, a sensitive radioimmunoassay of the N-acetyl,3-methoxy analogue of urinary and plasma norepinephrine was developed.

Einfluß von Steroidhormonen auf das Wachstum exokriner Pankreascarcinome. In vivo- und in vitro-Untersuchungen

In jungerer Zeit wurde in der Literatur uber eine mogliche Bedeutung von Steroidhormonen (SH) fur das Wachstum ductaler menschlicher Pankreascarcinome (PaCa) mehrfach berichtet (1, 2, 3). Auch die Steroidhormonkonzentration i.S. von Pankreascarcinomtragern scheint verandert zu sein (4). Um weitere Information uber den moglichen Einflus von Steroidhormonen auf das Wachstum von Pankreascarcinomen zu bekommen, wurden in dieser Arbeit folgende Fragen untersucht: 1. Lassen sich Steroidhormon-Receptoren in normalem Pankreas, in Gewebe von Pankreascarcinomen sowie in Gewebe transplantierter Pankreascarcinome auf der Nacktmaus nachweisen? 2. Lassen sich unterschiedliche Steroidhormon-Konzentratione…