Search results for "Antiandrogen"
showing 8 items of 28 documents
Topical canrenoic acid. Quantification of the antiandrogenic activity in the hamster flank organ
1991
: The topical antiandrogenic activity of potassium canrenoate (CAK), compared with that of spironolactone (SP), was assayed in vivo in female golden Syrian hamsters whose flank organs were stimulated by subcutaneous administration of testosterone propionate. Sebaceous glands and hair were measured by a computerized image analyzer. Pigmented spots, sebaceous gland areas, and the diameter of hairs of the treated flank organs were smaller in the groups that received CAK (1·6 mg/day) and SP (0·4 mg/day). The authors' results showed that CAK may act as a topical antiandrogen on the hamster flank organ when applied in concentrations four times greater than the minimal active dosage of SP. Potassi…
Evaluation of anti-androgenic activity of di-(2-ethylhexyl)phthalate
2005
International audience; DEHP is a widely used platiciser in the manufacture of PVC-based materials. It is known to disrupt the reproductive tract development in male rats. We have performed the Hershberger assay with DEHP on an immature castrated rat model to check if DEHP antagonise the testosterone propionate androgenic effect on the accessory sex organs development. DEHP significantly decreased the BC/LA muscles, the prostate, and the seminal vesicles relative weights from 100, 200, and 400 mg/kg bw/day, respectively. DEHP increased the liver relative weight from 100 mg/kg bw/day. A study was also performed on MDA-MB453 cell line stably transfected with pMMTVneo-Luc with DEHP and its maj…
REDUCTION OF NILUTAMIDE BY NO SYNTHASES : IMPLICATIONS FOR THE ADVERSE EFFECTS OF THIS NITROAROMATIC ANTIANDROGEN DRUG
2003
Nitric oxide synthases (NOSs) are flavohemeproteins that catalyze the oxidation of l-arginine to l-citrulline with formation of the widespread signal molecule NO. Beside their fundamental role in NO biosynthesis, these enzymes are also involved in the formation of reactive oxygen species and in the interactions with some xenobiotic compounds. Nilutamide is a nonsteroidal antiandrogen that behaves as a competitive antagonist of the androgen receptors and is proposed in the treatment of metastatic prostatic carcinoma. However, therapeutic effects of nilutamide are overshadowed by the occurrence of several adverse reactions mediated by toxic mechanism(s), which remain(s) poorly investigated. H…
Abnormal peripubertal development of the rat mammary gland following exposure in utero and during lactation to a mixture of genistein and the food co…
2011
The impact of early exposure to endocrine disruptor mixtures on mammary gland development is poorly known. Here, we identify the effects of a conception to weaning exposure of rats to the phytoestrogen genistein (G) and/or the antiandrogen vinclozolin (V) at 1 mg/kg-d, alone or in association. Using several approaches, we found that G- and GV-exposed rats displayed significantly greater epithelial branching and proliferation, wider terminal end buds than controls at PND35, as well as ductal hyperplasia and periductal fibrosis. Focal branching defects were present in V-exposed rats. An increased ER and AR expression was observed in G- and CV- as compared to V-exposed rats at PND35. Surprisin…
Serum miRNAs in women affected by hyperandrogenic polycystic ovary syndrome: the potential role of miR-155 as a biomarker for monitoring the estropro…
2018
MicroRNAs can be used as very efficient circulating biomarkers. The role of microRNAs in polycystic ovary syndrome (PCOS) and the effects of antiandrogen therapy on microRNA expression is still not fully understood. A panel of serum microRNAs were retrotranscribed via looped reverse primer transcription specific for each miRNA and quantified via probe specific RT-PCR in 16 Caucasian hyperandrogenic PCOS women selected according to the Rotterdam criteria and in a subset of seven patients after four months of sequential reverse antiandrogenic therapy. All women recruited underwent an oral glucose tolerance test (OGTT) and a baseline total cholesterol, high density lipoproteins cholesterol, tr…
Long-term outcome of antiandrogen monotherapy in advanced prostate carcinoma: 12-year results of a phase II study
2003
OBJECTIVE To present the long-term outcome of patients with locally advanced or metastatic prostate carcinoma treated by first-line antiandrogen monotherapy. PATIENTS AND METHODS From 1983 to 1990, 41 patients with advanced prostate carcinoma were treated with flutamide monotherapy until progression or the appearance of toxicity. Twenty-five patients (61%) had T3-T4N0M0 and 16 (39%) T2–4N0–3M1 prostate carcinoma. Consensus criteria were adopted to evaluate the response. Plasma testosterone and sexual function were recorded for the first 3 years. RESULTS Flutamide was administered for up to 147 months; seven patients (17%) interrupted the treatment because of toxicity. There was an objective…
A comparison of the relative efficacy of antiandrogens for the treatment of acne in hyperandrogenic women
2002
Summary objectives To compare the relative effectiveness of two newer antiandrogens (flutamide and finasteride) with cyproterone acetate (CPA), at both low and high doses in the treatment of moderate to severe acne in hyperandrogenic women. subjects and design Forty-eight hyperandrogenic women were prospectively randomized to the following treatments for 1 year: CPA 2 mg with 35 µg ethinylestradiol; CPA 50 mg with 25 µg ethinylestradiol (reverse sequential regimen); flutamide 250 mg daily; and finasteride 5 mg daily. Assessment of Cook scores was the primary end-point of the trial. Blood for androgens was obtained at baseline in these women and 30 ovulatory age-matched controls. results Ser…
Long-term outcome of antiandrogen monotherapy in advanced prostate carcinoma. Twelve-year’s results of a phase II study.
2003
OBJECTIVE: To present the long-term outcome of patients with locally advanced or metastatic prostate carcinoma treated by first-line antiandrogen monotherapy. PATIENTS AND METHODS: From 1983 to 1990, 41 patients with advanced prostate carcinoma were treated with flutamide monotherapy until progression or the appearance of toxicity. Twenty-five patients (61%) had T3-T4N0M0 and 16 (39%) T2-4N0-3M1 prostate carcinoma. Consensus criteria were adopted to evaluate the response. Plasma testosterone and sexual function were recorded for the first 3 years. RESULTS: Flutamide was administered for up to 147 months; seven patients (17%) interrupted the treatment because of toxicity. There was an object…