头发维基百科——非那雄胺

好头发翻译小组 · 发表于 2015-10-15 10:46:10

本帖最后由好头发翻译小组于 2015-10-23 10:48 编辑

地址：https://en.wikipedia.org/wiki/Finasteride

1.Finasteride
非那雄胺

Finasteride (INN, USAN, BAN) (brand names Proscar, and Propecia by Merck, among other generic names; former developmental code name MK-906) is a drug used for the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB).[1][2] It is a type IIand type III 5α-reductase inhibitor;[3] 5α-reductase, an enzyme, converts testosterone to dihydrotestosterone(DHT).[2]
非那雄胺片（它包括由默克公司生产的保列治和保法止，还有一些其它的品牌名称，保列治和保法止的发展代号为 MK-906）是一种治疗良性前列腺增生以及恶性前列腺增生的药物。它也是一种II型和III型5α还原酶抑制剂，5α还原酶是一种促进睾酮转化为双氢睾酮（DTH）的酶。(译者注：DTH是杀死毛囊，使毛囊退化从而导致脱发的元凶！)

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好头发翻译小组 · 发表于 2015-10-15 10:47:25

2.Medical uses
2.医疗上的用途

Benign prostatic hyperplasia
良性前列腺增生

Physicians use finasteride for the treatment of BPH, informally known as an enlarged prostate. Finasteride may improve the symptoms associated with BPH such as difficulty urinating, getting up during the night to urinate, hesitation at the start of urination, and decreased urinary flow. It provides less symptomatic relief than alpha-1 blockers such as tamsulosin and symptomatic relief is slower in onset (six months or more of treatment with finasteride may be required to determine the therapeutic results of treatment). Symptomatic benefits are mainly seen in those with prostate volume > 40 cm2. In long-term studies finasteride but not alpha-1 inhibitors reduce the risk of acute urinary retention (-57% at 4 years) and the need for surgery (-54% at 4 years). If the drug is discontinued, any therapeutic benefits reverse within about 6–8 months.[4][5][6]
医生使用非那雄胺治疗前列腺增生症，俗称前列腺肥大。非那雄胺可改善前列腺增生的相关症状，这些症状包括：排尿困难，夜间起床排尿，没有尿意，以及尿量很小等等。这种药物与α-1受体阻滞剂如坦索罗相比见效并没有那么明显，并且见效也没有那么快（一般的话至少需要连续服用非那雄胺六个月以上才能看到效果）。只有当前列腺增生达到40 cm2以上时使用这种药物效果才会比较明显。在长期的研究中非那雄胺而不是α抑制剂降低急性尿潴留的风险（在4年的研究中降低了57%）和做手术的需要（在4年研究中降低了54%）。如果停止使用非那雄胺的话，那么在6-8个月前列腺症状将会复发。

好头发翻译小组 · 发表于 2015-10-15 10:47:58

3.Male pattern baldness
3.男性脱发

Finasteride is used to treat male pattern hair loss(androgenetic alopecia) in men only.[7] Treatment provides about 30% improvement in hair loss after six months of treatment, and effectiveness only persists as long as the drug is taken.[8]
非那雄胺也用来治疗男性脱发（雄性激素脱发）。使用这种药物六个月以后会使脱发恢复30%左右，而且这种效果只能通过持续用药来维持。

好头发翻译小组 · 发表于 2015-10-15 10:48:36

4.Off-label uses
4.其它的用途

Finasteride is sometimes used in hormone replacement therapy for male-to-female transsexuals in combination with a form of estrogen due to itsantiandrogen properties. However, little clinical research of finasteride use for this purpose has been conducted and evidence of efficacy is limited.[9]
非那雄胺有时用于激素紊乱治疗，例如可以治疗那些由于体内雌激素分泌过多导致偏女性化的男性。然而，非那雄胺在这方面的应用研究还很少，它的效果也很有限。

好头发翻译小组 · 发表于 2015-10-15 10:48:55

5.Contraindications
5.禁忌

Finasteride is not approved for use in women, especially due to risks of birth defects in afetus. It is classified in the FDA pregnancy category X.[7]
女性禁止使用这种药，它会增加胎儿畸形的风险。它被美国食品药品管理局列为怀孕应当禁止接触的药物。

好头发翻译小组 · 发表于 2015-10-15 10:50:13

本帖最后由好头发翻译小组于 2015-10-15 11:02 编辑

5.Adverse effects
5.副作用

Adverse effects from finasteride are rare.[4] The FDA has added a warning to 5α-reductase inhibitors concerning an increased risk of high-grade prostate cancer, as the treatment of BPH lowers PSA, which could mask the development of prostate cancer.[10][11]
非那雄胺片的副作用并不多。美国食品药品管理局已经发出了一个警告，称5α还原酶抑制剂会增加前列腺癌发病率，因为治疗前列腺会降低前列腺特异性抗原，这恰好掩饰了前列腺癌的发展。

Although overall incidence of male breast cancer in clinical trials for finasteride 5 mg was not increased, there are post-marketing reports of breast cancer in association with its use. Available evidence does not provide clarity as to whether there is a causative relationship between finasteride and these cancers.[7][12]
尽管临床实验表明服用5mg非那雄胺后男性乳腺癌总体的发病率并没有增加，但是在使用这种药物之后有发生乳腺癌的报道。现在没有很明确的证据证明使用非那雄胺和发生这种癌症之间有联系。

The effect of finasteride on sexual function is controversial. There are case reports of persistent diminished libido or erectile dysfunction after stopping the drug and the FDA has updated the label to inform healthcare professionals of these reports.[8][13] A 2010 review found moderate quality evidence that finasteride increased the risk of sexual dysfunction, but not of discontinuing treatment due to sexual side effects.[14]
非那雄胺片对性功能的影响是有争议的。有病例报告称停止使用菲娜性能之后会发生持续性性欲减弱，以及勃起困难，美国食品药品管理局已经将这些病例通知给了一些专业的保健人员了。在2010年一份调查报告中发现使用非那雄胺会增加性功能障碍的发病率，但是这种情况是因为在使用过程中有副作用的前提下还在坚持服药所导致的。

A 2015 meta analysis found none of the clinical trials had adequate safety reporting and did not provide sufficient information to establish the safety profile for finasteride's treatment of hairloss. The study concluded the existing clinical trials of finasteride for hair loss provide very limited information on toxicity, are of poor quality, and seem to be systematically biased toward under detection of adverse events. Moreover, the trials submitted to the FDA for approval for hair loss excluded most men who would normally be prescribed finasteride for androgenic alopecia.[15][16]
Meta在2015临床试验分析中发现现在既没有足够的安全报告也没有建立有关非那雄胺在治疗脱发在安全性方面足够的信息。研究发现：现在的临床试验基本不能说明非那雄胺在治疗脱发所带来的病毒性，这些临床实验本身也有很多缺陷，并且它似乎是偏向不良事件检测系统下所得出的结果。此外，在向食品药品管理局提交有关允许使用这种药治疗脱发的案例中缺少了很大一部分那些诊断为雄性激素脱发后会自然选择非那雄胺来治疗这样的群体。

When finasteride was originally approved for hair loss in 1997, the FDA approval review reported that it appears well tolerated, with the most common side effects being related to sexual function.[17] In many people these side effects resolve if the medication is stopped and occasionally resolve even if the medication is continued.[17] They additionally state "the sexual functioning questionnaire seems to have given a sensitive reflection of the disturbance on sexual functioning".[17]
当非那雄胺这种药在1997年被批准用来治疗脱发时，食品药品管理局审查报告表示：这种要具有良好的耐受性，有关它最常见的副作用是性功能障碍。如果停止用药或者持续用药一段时间，很多人的这种副作用就会消失。他们还提出，性功能调查问卷似乎对那些性功能障碍的人来说是一个很敏感的话题。

6.Mechanism of action
作用机理

Finasteride is a 5α-reductase inhibitor, specifically the type II and III isoenzymes.[3][18] By inhibiting 5α-reductase, finasteride prevents conversion of testosterone to dihydrotestosterone (DHT) by the type II and III isoenzymes, resulting in a decrease in serum DHT levels by about 65–70% and in prostate DHT levels by up to 85–90%,[3][19] where expression of the type II isoenzyme dominates. Unlike triple inhibitors of all three isoenzymes of 5α-reductase like dutasteride which can reduce DHT levels in the entire body by more than 99%,[3]finasteride does not completely suppress DHT production because it lacks significant inhibitory effects on the 5α-reductase type I isoenzyme, with 100-fold less affinity for I as compared to II.[7] In addition to blocking the type II and III isoenzymes, finasteride competitively inhibits the 5β-reductase type II isoenzyme,[20] though this is not believed to affect androgen metabolism.
非那雄胺是一种5α还原酶抑制剂，特别是针对II型和III型同工酶。通过抑制5α还原酶的产生，非那雄胺抑制了睾酮在II型与III型同工酶作用下向双氢睾酮（DHT）转化的过程，最终使得血液中的双氢睾酮浓度下降65%到70%同时使得前泪腺中的双氢睾酮含量下降多大85%到90%，在这些器官中原本含有大量的II型同工酶。与抑制所有三个同工酶的度他雄胺不同，非那雄胺不能使得体内的DHT含量减少高达99%。主要原因在于非那雄胺缺乏对I型同工5α还原酶抑制剂，因此对于I型同工酶的抑制效应显著若于对II型同工酶的抑制作用，使得其并不能像度他雄胺一样完全抑制DHT的产生。而为了抑制II型和III型同工5α还原酶的产生，度他雄胺完全阻断了II型同工5α还原酶的产生，尽管这种物质不被认为影响着雄激素的代谢。

By blocking DHT production, finasteride reduces androgen activity in the scalp. In the prostate, inhibition of 5α-reductase reduces prostate volume, which improves BPH and reduces risk of prostate cancer. Inhibition of 5α-reductase also reduces epididymal weight, and decreases motility and normal morphology of spermatozoa in the epididymis.[21]
通过抑制DHT的产生，非那雄胺减少雄激素在头皮上的活性。在前列腺中，5α还原酶减少改善了前列腺增生同时降低了患前列腺癌的风险。同时5α还原酶的减少降低了附睾的重点，减少了附睾中正常形态的精子及其活力。

DHT helps activate the GABAA receptor, which functions to tamp down signaling among neurons; because finasteride prevents the formation of DHT, it may contribute to a reduction of GABAAactivity. Reduced GABAA has been implicated in depression, anxiety, and sexual dysfunction.[22][23][24]
DHT有助于激活GABA受体，这一效应抑制神经元之间的信号传递。由于非那雄胺对于DHT的抑制作用使得GABA活性降低，而GABA的降低对于抑郁、焦虑和性功能障碍产生有着一定的影响。

好头发翻译小组 · 发表于 2015-10-15 10:51:13

7.Physical and chemical properties
理化性质

Finasteride is a 4-azasteroid analogue of testosterone and is lipophilic.[25]
非那雄胺是睾酮的4-氮杂甾族类似物，具有亲脂性。

Drug trade names include Propecia and Proscar, the former marketed for male pattern baldness (MPB) and the latter for benign prostatic hyperplasia (BPH), both are products of Merck & Co. There is 1 mg of finasteride in Propecia and 5 mg in Proscar. Merck's patent on finasteride for the treatment of BPH expired on June 19, 2006.[26] Merck was awarded a separate patent for the use of finasteride to treat MPB. This patent expired in November 2013.[27]
药物品名包括保法止和保列治，前者用于治疗雄性脱发，后者用于前列腺增生的前期治疗，这两种产品都由默克公司生产。保法止含1毫克非那雄胺而保列治含5毫克。默克公司在非那雄胺可治疗雄性脱发上的专利于2006年6月19日到期，而同时默克公司被授予一个独立的专利于非那雄胺对男性脱发的治疗，这一专利在2013年11月到期。

好头发翻译小组 · 发表于 2015-10-15 10:52:10

8.History
药物历史

In 1974, Julianne Imperato-McGinley of Cornell Medical College in New York attended a conference on birth defects. She reported on a group of intersex children in the Caribbean who appeared sexually ambiguous at birth, and were initially raised as girls, but then grew external male genitalia and other masculine characteristic after onset of puberty. Her research group found these children shared a genetic mutation, causing deficiency of the 5α-reductase enzyme and male hormone dihydrotestosterone (DHT), which was found to have been the etiology behind abnormalities in male sexual development. Upon maturation, these individuals were observed to have smaller prostates which were underdeveloped, and were also observed to lack incidence of male pattern baldness.[28][29]
1974年，康奈尔医学院的朱莉安娜在纽约参加一个主题为“先天缺陷”的会议。她讲到一群出生于加勒比海的雌雄同体的孩子，他们在出生时候性别并不确定。最初这些孩子被认为是女性，但是随着年龄增长，这些孩子长出了男性的生殖器并有男性的青春期特征。她的研究小组发现,这些孩子有一个共同基因突变，导致5α还原酶和双氢睾酮（DHT）的缺乏，这被认为是这些孩子发育异常的原因。待到这些孩子成熟后,这些人被观察到前列腺较小切发育不正常，同时这些人中很少见到患有男性脱发的人。

In 1975, copies of Imperato-McGinley's presentation were seen by P. Roy Vagelos, who was then serving as Merck's basic-research chief. He was intrigued by the notion that decreased levels of DHT led to the development of smaller prostates. Dr. Vagelos then sought to create a drug which could mimic the condition found in these children to treat older men who were suffering from benign prostatic hyperplasia.[30]
1975年，朱莉安娜的演讲稿件被罗伊瓦格洛斯看到，此人后来成为默克公司首席研究员。他对于体内DHT水平的减少使得前列腺较小这一研究很感兴趣。因此瓦格洛斯博士希望制造一种药物，通过参照这群雌雄同体孩子的症状，缓减许多老年男性前列腺增生的痛苦。

In 1992, finasteride (5 mg) was approved by the U.S. Food and Drug Administration (FDA) for treatment of BPH, which Merck marketed under the brand name Proscar.
1992年，5毫克的非那雄胺被美国药品和药物管理局允许用于治疗前列腺增生，默克公司以保列治为名销售该产品。

In 1997, Merck was successful in obtaining FDA approval for a second indication of finasteride (1 mg) for treatment of MPB, which was marketed under the brand name Propecia.
1997年，默克公司成功获得美国药品和药物管理局的允许使用1毫克的非那雄胺治疗男性脱发，该公司以保法止为名销售该产品。

好头发翻译小组 · 发表于 2015-10-15 10:54:46

9.Society and culture
文化与社会影响

In 2005, the World Anti-Doping Agency banned finasteride because a laboratory in Germany discovered the drug could be used to mask steroid abuse.[31] It was removed from the list effective January 1, 2009, after improvements in testing methods made the ban unnecessary.[32]Notable athletes who used finasteride for hair loss and were banned from international competition include skeleton racer Zach Lund, bobsledder Sebastien Gattuso, footballer Romárioand ice hockey goaltender José Théodore.[32][33]

In 2012, an advocacy group called the Post-Finasteride Syndrome Foundation was formed; the group "coined the phrase 'post finasteride syndrome' which they say is characterised by sexual, neurological, hormonal and psychological side effects that can persist in men who have taken finasteride for hair loss or an enlarged prostate".[34][35]

2005，世界反兴奋剂机构禁止非那雄胺，因为德国的一个实验室发现这种药物可以用来掩盖类固醇的滥用。非那雄胺在2009年1月1日被从这份禁用名单上删除，因为后来有了更先进的测试类固醇滥用方法，使得非那雄胺的禁止不再有必要。有许多著名运动员因使用非那雄胺治疗兔哦啊发而被国际大赛禁赛，包括赛车手Zach Lund，雪橇运动员Sebastien Gattuso, 橄榄球运动员Romário，冰球守门员José Théodore。

2012年，非那雄胺后综合征基金会成立，这一基金会提出“非那雄胺后综合征”，这是因为长期服用非那雄胺的治疗男性脱发或前列腺增生的副作用，影响到患者的性，神经，内分泌和心理。

好头发翻译小组 · 发表于 2015-10-15 10:55:07

10.Research
后续研究

Finasteride has been clinically tested for baldness in women; the results were no better than placebo.[36]

非那雄胺也在临床上治疗女性脱发，结果显示其在女性脱发治疗上与安慰剂无异。