The extract of Celtis choseniana Nakai alleviates testosterone-induced benign prostatic hyperplasia through inhibiting 5α reductase type 2 and the Akt/NF-κB/AR pathway / 中国天然药物

Benign prostatic hyperplasia (BPH) is a chronic male disease characterized by the enlarged prostate. Celtis chosenianaNakai (C. choseniana) is medicinally used to alleviate pain, gastric disease, and lung abscess. In this study, the effect of C. choseniana extract on BPH was investigated using testosterone-induced rats. Sprague Dawley rats were divided into five groups: control, BPH (testosterone 5 mg·kg-1), Fina (finasteride 2 mg·kg-1), and C. choseniana (50 and 100 mg·kg-1). After four weeks of TP treatment with finasteride or C. choseniana, prostate weights and DHT levels were measured. In addition, the prostates were histopathologically examined and measured for protein kinase B (Akt)/nuclear factor-κB (NF-κB)/AR signaling, proliferation, apoptosis, and autophagy. Prostate weight and epithelial thickness were reduced in the C. choseniana groups compared with that in the BPH group. The extract of C. choseniana acted as a 5α reductase inhibitor, reducing DHT levels in the prostate. Furthermore, the extract of C. choseniana blocked the activation of p-Akt, nuclear NF-κB activation and reduced the expression of AR and PSA compared with BPH. Moreover, the expression of Bax, PARP-1, and p53 increased, while the expression of bcl-2 decreased. The present study demonstrated that C. choseniana extract alleviated testosterone-induced BPH by suppressing 5α reductase and Akt/NF-κB activation, reducing AR signaling and inducing apoptosis and autophagy in the prostate. These results suggested that C. choseniana probably contain potential herbal agents to alleviate BPH.

Post-finasteride syndrome

Abstract Finasteride is a 5α-reductase enzyme inhibitor that has been approved for the treatment of male androgenic alopecia since 1997. Over time, it has been considered a safe and well-tolerated drug with rare and reversible side effects. Recently there have been reports of adverse drug-related reactions that persisted for at least three months after discontinuation of this drug, and the term post-finasteride syndrome arose. It includes persistent sexual, neuropsychiatric, and physical symptoms. Studies to date cannot refute or confirm this syndrome as a nosological entity. If it actually exists, it seems to occur in susceptible people, even if exposed to small doses and for short periods, and symptoms may persist for long periods. Based on currently available data, the use of 5α-reductase inhibitors in patients with a history of depression, sexual dysfunction, or infertility should be carefully and individually assessed.

Efectos adversos de finasteride: mitos y realidades. una revisión actualizada / Finasteride adverse effects: an update

Finasteride is a 5-α reductase inhibitor that is widely used in the management of benign prostate hyperplasia and male pattern hair loss. It is well known that these agents improve the quality of life in men suffering from these conditions. However, they are associated with some transient and even permanent adverse effects. The aim of this article is to clarify the controversies about the safety of finasteride by analyzing the evidence available in the literature.

Finasteride: mitos y verdades / Finasteride: myths and truths

La alopecia androgénica consiste en un patrón específico de caída de pelo. Es más común en el sexo masculino. Antes de la caída total del pelo, ocurre una transformación del pelo grueso, pigmentado y terminal en vellos pequeños, hipopigmentados y finos, fenómeno dado por aumento en la afinidad de los receptores del pelo a andrógenos. La dihidrotestosterona es un andrógeno con una afinidad 5 veces mayor por los receptores en el pelo del cuero cabelludo. La enzima 5 a-reductasa cataliza la transformación de testosterona a dihidrotestosterona. El finasteride es un bloqueador selectivo de la 5 a -reductasa tipo 2 utilizado como tratamiento para la alopecia de patrón andrógeno. Existen numerosas controversias respecto a la eficacia y a los efectos no deseados que pudiera causar el finasteride; éste artículo pretende dilucidar aquellos más relevantes.

Androgenetic alopecia is characterized by progressive, patterned hair loss from the scalp. The transition of terminal hair into vellus hairs is characteristic, and attributed to an increased affinity of hair androgen receptors to circulating androgens. It is considered to be a genetically, hereditary condition. Among androgens, dihydrotestosterone (DHT) has approximately five fold greater affinity for the androgen receptor compared to testosterone. DHT is a result of peripheral conversion of testosterone, a reaction catalyzed by the enzyme 5 a-reductase. Finasteride, a type 2-selective inhibitor of 5 a -reductase, was first used to treat benign prostate hyperplasia and later to treat androgenetic alopecia, with good outcomes. Many controversies arise related to the efficacy and safety of finasteride; the objective of this article is to elucidate the most relevant information.

Tratamento hormonal do hirsutismo baseado em evidências / Evidence-based hormonal treatment of hirsutism

A revisão de estudos baseados em evidências mostra o melhor tratamento hormonal para o hirsutismo. Inicialmente, resumiu-se a fisiologia do pelo, caracterizou-se o hirsutismo, suas variantes e suas causas. Revelou-se que o tratamento hormonal do hirsutismo deve ser complementado pelo tratamento cosmético e não deve ser indicado para mulheres grávidas ou que desejam engravidar. A primeira opção é o contraceptivo hormonal oral, seguro para contracepção e eficaz para tratamento do hirsutismo. Após tempo estipulado, não ocorrendo resposta satisfatória, associar acetato de ciproterona ou espironolactona. A finasterida é indicada para hirsutismo idiopático e a flutamida, devido aos efeitos colaterais, ainda não é opção segura

An evidence-based review shows the best hormonal treatment of hirsutism. This paper summarized the physiology of the hair, characterized the hirsutism, its variants and etiologies. The study revealed that hormonal treatment of hirsutism has to be complemented by esthetic treatment, and it is not recommended for pregnant women or for those who want to get pregnant. The first option is hormonal oral contraceptive, which is safe for contraception and effective for treatment of hirsutism. After a established period of treatment, if good results do not occur, the association of cyproterone or spironolactone is recomended. Finasteride is the treatment of idiopathic hirsutism, and flutamide is not a safe option due to its side effects

Laboratory diagnosis of late-onset male hypogonadism andropause / Diagnóstico laboratorial do hipogonadismo masculino tardio (andropausa)

OBJECTIVES: To evaluate which factors influence the laboratorial diagnosis of late-onset male hypogonadism (LOH). METHODS: Total testosterone (TT), SHBG and albumin were measured in 216 men aged 52-84 years. The laboratorial definition of LOH was two values of calculated free testosterone (cFT) <6.5 ng/dl, according to Vermeulen's formula. RESULTS: At the first blood test, cFT was <6.5 ng/dl in 27 percent of the men. Laboratorial LOH (confirmed by two tests) was present in 19 percent, but TT levels were low in only 4.1 percent. Age influenced TT (p=0.0051) as well as BMI; 23.5 percent of patients > 70 years and 38.9 percent of the obese men who had TT within the reference range were, in fact, hypogonadal. CONCLUSION: Especially in obese men and in those > 70 years old, SHBG dosage is important to calculate FT levels and diagnose hypogonadism.

OBJETIVOS: Avaliar os fatores que influenciam o diagnóstico laboratorial do hipogonadismo masculino tardio. MÉTODOS: Avaliamos 216 homens entre 52 e 84 anos. O diagnóstico laboratorial foi definido como dois valores de testosterona livre calculada (TLC) <6,5 ng/dl, segundo a fórmula de Vermeulen, a partir das dosagens de testosterona total (TT), SHBG e albumina. RESULTADOS: Na primeira dosagem, a TLC foi <6.5 ng/dl em 27 por cento da amostra. Hipogonadismo laboratorial (confirmado por duas dosagens) esteve presente em 19 por cento, no entanto a TT foi baixa em apenas 4.1 por cento dos homens. A idade influenciou a TT (p=0.0051) bem como o IMC; 23,5 por cento dos homens > 70 anos e 38,9 por cento dos obesos com TT dentro dos níveis de referência eram, na verdade, hipogonádicos. CONCLUSÃO: Especialmente em homens obesos e nos > 70 anos a dosagem de SHBG é importante para calcular TL e diagnosticar o hipogonadismo.

Finasteride-associated male infertility

A finasterida é um potente e específico inibidor da enzima 5a-redutase em homens. Estudos clínicos demonstraram que finasterida 1mg/dia diminui a progressão da queda e aumenta o crescimento do cabelo em homens que sofrem de queda de cabelo hereditária. Por sua influência no metabolismo dos andrógenos existe uma preocupação a respeito do seu uso, principalmente em pacientes em idade fértil. Neste trabalho são descritos 3 casos de pacientes jovens, que apresentaram piora do espermograma durante o uso continuado de finasterida 1mg revertida após a suspensão do mesmo. Dois deles tinham varicocele unilateral e o terceiro era obeso. Aparentemente o tratamento com finasterida promoveu alteração significativa na qualidade seminal. Pode-se especular que talvez a finasterida por si só não traga alteração para a espermatogênese como reportado por Overstreet et al. (1999), mas que em pacientes de risco com possíveis causas de infertilidade associadas, possa ocorrer a amplificação da influência deletéria da finasterida. Estudos futuros devem ser realizados para esclarecer a influência da finasterida nestes pacientes.