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The corpus cavernosum after treatment with dutasteride or finasteride： a histomorphometric study in a benign prostatic hyperplasia rodent model

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Asian Journal of Andrology 2018年第5期20卷 505-510页

作者： Marcello H A Da Silva Waldemar S Costa Francisco J B Sampaio Diogo B De Souza Urogenital Research Unit Rio de Janeiro State University Rio de Janeiro RJ 20551-030 Brazil

Erectile dysfunction is a common side effect of finasteride and dutasteride treatments. The objective of this study was to investigate the structural changes in the penis using a benign prostatic hyperplasia （BPH） rodent model treated with dutasteride or finasteride. Sixty male rats were divided into the following groups： C, untreated control rats; C ＋ D, control rats receiving dutasteride; C ＋ F, control rats receiving finasteride; H, untreated spontaneously hypertensive rats （SHRs）; H ＋ D, SHRs treated with dutasteride; and H ＋ F, SHRs treated with finasteride. Treatments were performed for 40 days, and penises were collected immediately thereafter. The organs were analyzed using histomorphometric methods to determine the cross-sectional penile area, as well as the surface density （Sv） of smooth muscle fibers, connective tissue, elastic system fibers, and sinusoidal spaces of the corpus cavernosum. The results were compared using a one-way ANOVA with Bonferroni＇s posttest. Groups C ＋ D and C ＋ F had a significantly smaller penile cross-sectional area, but more elastic system fiber Sv compared to Group C. Group C ＋ D showed less smooth muscle Sv, and Group H showed more connective tissue but a smaller sinusoidal space Sv in the corpus cavernosum compared to Group C. Groups H ＋ D and H ＋ F had less smooth muscle Sv than Group H. Group H ＋ D also had more connective tissue and elastic system fiber Sv than Group H. Both dutasteride and finasteride promoted penile modifications in the control rat penis, although this affect was ~reater in Group H animals. In this rodent model, dutasteride was the drug that most affected the corpus cavernosum.

关键词： animal models benign prostatic hyperplasia dutasteride erectile dysfunction finasteride penis

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The intriguing role of fibroblasts and c-Jun in the chemopreventive and therapeutic effect of finasteride on xenograft models of prostate cancer

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Asian Journal of Andrology 2016年第6期18卷 913-919页

作者： Yi-Nong Niu Kai Wang Song Jin Dong-Dong Fan Ming-Shuai Wang Nian-Zeng Xing Shu-Jie Xia Department of Urology Beijing Chao-Yang Hospital Capital Medical University Beijing China Weifang Hospital of Traditional Chinese Medicine Weifang China Department of Urology Shanghai First Hospital Jiao Tong University Shanghai China

In a large clinical trial, finasteride reduced the rate of low-grade prostate cancer （PCa） while increasing the incidence of high-grade cancer. Whether finasteride promotes the development of high-grade tumors remains controversial. We demonstrated the role of fibroblasts and c-Jun in chemopreventive and therapeutic effect of finasteride on xenograft models of PCa. LNCaP （PC3） cells or recombinants of cancer cells and fibroblasts were implanted in male athymic nude mice treated with finasteride. Tumor growth, cell proliferation, apoptosis, p-Akt, and p-ERKI/2 were evaluated. In LNCaP （PC3） mono-grafted models, finasteride did not change the tumor growth. In recombinant-grafted models, fibroblasts and c-Jun promoted tumor growth; finasteride induced proliferation of LNCaP cells and repressed PC3 cell apoptosis. When c-Jun was knocked out, flbroblasts and/or finasteride did not promote the tumor growth. finasteride inhibited p-Akt and p-ERKI/2 in mono-culture cancer cells while stimulating the same signaling molecules in the presence of fibroblasts. Reduced p-Akt and p-ERKI/2 were noted in the presence of c-Jun-I- fibroblasts. Fibroblasts and c-Jun promote PCa growth; finasteride further stimulates tumor growth with promoted proliferation, repressed apoptosis, and up-regulated pro-proliferative molecular pathway in the presence of fibroblasts and c-Jun. Stromal-epithelial interactions play critical roles in finasteride＇s therapeutic effects on PCa. Our findings have preliminary implications in using finasteride as a chemopreventive or therapeutic agent for PCa patients.

关键词： chemoprevention c-Jun fibroblasts finasteride mouse model prostate cancer

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A Stability Indicating UPLC Method for finasteride and Its Related Impurities

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American Journal of Analytical Chemistry 2012年第11期3卷 737-745页

作者： Y. Koti Reddy G. V. Subba Reddy K. N. Jaya Veera Kishore Kumar Hotha Bioanalytical Department Integrated Product Development Dr. Reddy’s Laboratories Ltd Bachupally India Department of Chemistry JNTUA College of Engineering Pulivendula India JNT University Anantapur India Sri Krishna Chaitanya College of Pharmacy Madanapalle India

The objective of the present research work is to develop a gradient, reversed-phase liquid chromatographic (RP-UPLC) method for the determination of finasteride in pharmaceutical bulk drugs for assay and its related impurities. The chromatographic separation was achieved on a Waters ACQUITY UPLC BEH Phenyl Column (150 mm × 2.1 mm, 1.7 μm), The gradient LC method employs solutions A and B as mobile phase. The solution A Contains 2.5 mM ortho phosphoric acid (Buffer) and solution B contains a mixture of acetonitrile and water in the ratio of (90:10 v/v). The flow rate was 0.22 ml/min and the detection wavelength was 210 nm. In the developed UPLC method, the resolution between finasteride and its potential impurities, namely Imp-1, Imp-2, Imp-3 and Imp-4 was found to be greater than 2.0. The drug was subjected to stress conditions of hydrolysis, oxidation, photolysis and thermal degradation. Considerable degradation was found to occur in alkaline medium and oxidative stress conditions. Degradation product formed during oxidative hydrolysis was found to be Imp-1. The stress samples were assayed against a qualified reference standard and the mass balance was found close to 99.5%. The developed RP-UPLC method was validated with respect to linearity, accuracy, precision and robustness. The limit of quantification of Imp-1, Imp-2, Imp-3 and Imp-4 were 0.06, 0.06, 0.05 and 0.036% (of analyte concentration, i.e. 0.5 mg/ml) with 1μl injection volume. The developed method was found to be linear in the range of 2.5 - 15 μg/mL with correlation coefficient of 0.999 for assay procedures and found to be linear in the range of 0.05 - 3 μg/mL with correlation coefficient of 0.999 for related impurities.

关键词： RP-UPLC Forced Degradation Validation finasteride Method Development

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Controlled clinical trial for evaluation of hair growth with low dose cyclical nutrition therapy in men and women without the use of finasteride

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Plastic and Aesthetic Research 2017年第9期4卷 161-173页

作者： Rajendrasingh Jalamsingh Rajput Department of Hair Transplant&Trichology Dr Rajesh Rajput Hair Restore ClinicMumbai 400050India.

Aim: To evaluate possible results with the stimulation use of minoxidil and the strengthening of hair roots with nutritional cyclical supplements, resulting in increased hair regrowth, without the use of anti androgens and enzyme blockers. Methods: This prospective controlled clinical trial compares the current acknowledged form of treatment for hair loss within two controlled groups for both men and women against the use of cyclical nutritional therapy and minoxidil 2%. One hundred patients in each of the 4 groups, a total of 400 patients, were followed for 1 year. The progress was evaluated every 2 months with computerised measurements of hair density, hair calibre, global photography and uniquely designed self-assessment scores. Results: The use of nutritional supplements showed consistent improvements in both treatment groups of men and women against the controlled groups with a correction of hair fall and minimum 18% increased density within 2 months with further improvement to a maximum of 156% over 1 year. Conclusion: Hair loss occurs when weak, sensitive, follicles are affected by multiple causes. Hair regrowth can be achieved consistently and safely by strengthening the hair roots and promoting hair growth without necessarily depending on the use of anti androgens.

关键词： Androgenic alopecia finasteride minoxidil cyclical vitamin hair nutrition trichoscopy hair growth hair loss side effects cyclical therapy

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finasteride治疗前列腺增生的尿流动力学估价

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国际泌尿系统杂志 1993年第2期 87-88页

作者：王仁顺

69例前列腺增生病人用finasteride进行治疗,采用双盲法对照进行研究,将病人分为三组,分别服用finasteride 5mg/日,10mg/日和安慰剂共3个月,检查结果显示:血浆双氢睾酮在服药5mg/日下降61.4%,10mg/日组下降72.4%,对照组无变化,LH、T、FS... 详细信息

69例前列腺增生病人用finasteride进行治疗,采用双盲法对照进行研究,将病人分为三组,分别服用finasteride 5mg/日,10mg/日和安慰剂共3个月,检查结果显示:血浆双氢睾酮在服药5mg/日下降61.4%,10mg/日组下降72.4%,对照组无变化,LH、T、FSH无明显变化,PSA于5mg/日组下降20.5%,10mg/日组下降19.9%,对照组下降6.2%,3个月治疗后服药组前列腺体积虽有缩小,但与对照组比较相差不显著,症状记分三组均有明显降

关键词：前列腺男生殖器最大尿流率 finasteride

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Sub-chronic effects of a Phthirusa pyrifolia aqueous extract on reproductive function and comparative hormone levels in male rats

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Asian Pacific Journal of Tropical Biomedicine 2016年第3期6卷 202-210页

作者： Romero Marcos Pedrosa Brandao-Costa Vivianne Ferreira Araujo Elizabeth Neves Maria Tereza Santos Correia Ana Lucia Figueiredo Porto Maria das Gracas Carneiro-da-Cunha Department of Biochemistry Center of Biological Sciences Federal University of Pernambuco Keizo Asami Laboratory of Imunopathology LIKA/UFPE Department of Anatomy Federal University of Pernambuco Department of Animal Morphology and Physiology Federal Rural University of Pernambuco Keizo Asami Laboratory of Imunopathology LIKA/UFPE

Objective: To explore the effects of aqueous extract from Phthirusa pyrifolia leaves(67 mg/kg body weight for 12 days) on the reproductive function of male Wistar rats through oral administration.Methods: Animals(n = 30), aged 13 weeks and weighing(378.5 ± 5.0) g, were housed in a vivarium under controlled environmental conditions [photoperiod of 12 h light/dark,temperature of(23 ± 1)C] and were fed standard rations ad libitum. The experiment ran for 12 days, wherein animals were divided into three groups: negative control(n = 6)received water, positive control(n = 12) with finasteride at a concentration of 1.0 mg/kg;and a test group(n = 12) submitted to aqueous extract. At the end of the experiment, the animals were sacrificed and submitted to analyses.Results: The morphological results of the testes showed that the aqueous extract induced significant changes in the diameter and cross-sectional area of the seminiferous tubules as well as the thickness of the seminiferous epithelium. Furthermore, the extract was able to abruptly decrease testosterone concentrations by about 81.88% in the treated group when compared with the negative control,(47.0 ± 4.8) ng/d L and(255.0 ± 2.0) ng/d L,respectively, and 76.8%,(211.0 ± 8.7) ng/d L, when compared with finasteride. However,the extract causes neither liver damage nor impairment of renal function.Conclusions: These results suggest that the high amounts of flavonoids shown to be in the extract may be responsible for its hepato-protective effects and suggest a possible decrease in the libido and reproduction of rats.

关键词： Reproductive function Phytochemical Testosterone finasteride Phthirusa pyrifolia

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5α-还原酶抑制剂finasteride

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国外医药（合成药．生化药．制剂分册） 1994年第1期15卷 23-26页

作者：周瑞海

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前列腺增生治疗药——finasteride

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国外新药介绍 2000年第1期 15-18页

作者：朱晓红

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Diane 35及其与finasteride合用治疗多毛症的比较

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国际妇产科学杂志 2001年第1期28卷 54-55页

作者：周凌仁

多毛症主要见于卵巢雄激素产生过度(如多囊卵巢综合征,PCOS)或者周围组织对正常血循环的雄激素高度敏感(如特发性多毛症,IH)。醋酸环丙氯地孕酮(CPA)用于减少多毛症妇女的毛发生长,降低雄激素水平,通过和雄激素受体结合而抑制睾酮或二... 详细信息

多毛症主要见于卵巢雄激素产生过度(如多囊卵巢综合征,PCOS)或者周围组织对正常血循环的雄激素高度敏感(如特发性多毛症,IH)。醋酸环丙氯地孕酮(CPA)用于减少多毛症妇女的毛发生长,降低雄激素水平,通过和雄激素受体结合而抑制睾酮或二氢雄烯酮(DHT)。Diane 35含2mgCPA和35μg炔雌醇,用于雄激素过多症。finasteride是一种重氮类固醇,新的抗雄激素药物,竞争性抑制2型5α还原

关键词：多毛症 CPA finasteride Diane 35

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前列腺增生治疗药—finasteride

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国外新药介绍 1999年第4期 1-2页

作者：郭丽仪

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