达泊西汀（dapoxetine）治疗男性早泄新药
达泊西汀Dapoxetine
获得在芬兰及挪威两国的上市许可，用于18～64岁男子早泄(PE)的按需治疗。本品成为首个获准用于早泄的口服处方药。本品采取的是欧盟非集中审批程序，有7个国家给予肯定意见，芬兰和瑞典是7个国家中首先给予上市许可的国家，预计其他5国将跟进，这5个国家包括奥地利、德国、西班牙、意大利和葡萄牙。本品在美国尚未获准上市。

  本品为短效的选择性5-羟色胺再吸收抑制剂(SSRI)，用于PE时仅按需治疗，不需每天服药。强生公司先后进行了5项临床研究，超过6000例PE男性及其伴侣参与了本品的临床测试，是迄今为止最大规模和最全面的有关PE治疗药物的临床研究项目。

  早泄最新治疗药物-达泊西汀在欧洲上市。最近芬兰和瑞典批准强生公司的新药达泊西汀用于治疗早泄，达泊西汀专用于治疗男性早泄，这是一种即需型的治疗药物，是一种特异的，短期起作用的选择性5-羟色胺再摄取抑制剂，只有当有需要时才服用，即在每次性交前1-3小时服用，而不是每天均需要服用。

  强生公司(Janssen-Cilag)近日宣布说，芬兰和瑞典已经批准其旗下新药达泊西汀(Priligy，dapoxetine)用于治疗早泄，适用人群为18-64岁男性。该药在欧洲7国于2008年12月进行的集中审批中获得认可，并首先获得了芬兰和瑞典的正式批文，另外5个国家的批文相信不久之后也会下达，这五个国家是：奥地利，德国，西班牙，葡萄牙和意大利。
  达泊西汀专用于治疗男性早泄，这是一种即需型的治疗药物，是一种特异的，短期起作用的选择性5-羟色胺再摄取抑制剂，只有当有需要时才服用，即在每次性交前1-3小时服用，而不是每天均需要服用。
    达泊西汀是世界上第一种被批准治疗早泄的该类型的口服药(片剂)。达泊西汀的疗效在五个随机，安慰剂对照的3期临床试验中得到肯定，这五个试验共有6000多男性及他们的伴侣参加，这是目前为止规模最大，最全面的关于早泄治疗药物的临床试验。

达泊西汀
化学名称：(S)-N,N-二甲基-3-(萘基-1-氧基)-苯丙氨基盐酸盐，
英文名称：(S)-N,N-dimethyl-3-(naphthalen-1-yloxy)-1-phenylpropan-1-amine hydrochloride　

分子式：C21H23NO.HCl

分子量：341.88

CAS号：[129938-20-1]；[119356-77-3] （沧海：这两个号都是盐酸盐的号，用这两个号都能查到正确的结构，不知道哪个才是对的）　

熔点：175-177℃

旋光：+128°±3(C=1,CH3OH)

性状：本品为淡黄色粉末、无嗅、微甜、能溶于水、醇。可制成片剂、饮料、药酒、胶囊等剂型。

达泊西汀是一种选择性5-羟色胺再吸收抑制剂(SSRI)，这类药广泛用于治疗抑郁和相关的情感障碍。　

用途：达泊西汀(dapoxetine)作为一种新型快速的SSRI，半衰期短，属于选择性5-羟色胺再吸收抑制剂(SSRI)，用于治疗男性早泄和勃起功能障碍。

用法用量：每次60-100mg

特点：服用后由肠胃吸收，直接口服约20-30分钟起效; 作用时间持续数十天; 副作用小，检测不出，有轻微头痛、恶心等症状，但很快消失。

相关研究：在随机的166位病人（平均年龄23~64岁）中，130位完成了研究。用药前平均基线IELT是1.01分钟。60毫克剂量治疗后IELT是2.94分钟，100毫克剂量是3.20分钟，安慰剂为2.05分钟，差异明显。最常见的不良反应是恶心。因不良反应而中断治疗的10位病人有9人是接受100毫克治疗。此项研究的结论是，采用达泊西汀为期两周的治疗在首次剂量时经IELT评价就能明显改善PE。　

  在所有的治疗药物类别中，已经确定SSRIs治疗PE的疗效最佳。较新的SSRIs制剂作用更迅速，半衰期更短，副作用发生率更低，显示出希望。美国FDA将可能批准一些正在研究的新型制剂，预期在不久的将来因PE使用SSRIs治疗的病人将不断增加。

达泊 西 汀
  吸收快，能快速达有效的血药浓度，达峰时间1.4一2.oh，单剂量达泊西汀30和60mg的血峰浓度分别为297和498ng·mL一’，呈剂量相关性[2，〕。分布容积为2.IL·kg一’;组织分布广，神经组织的药物浓度与血药浓度接近;绝对生物利用度为42%;蛋白结合率为9%〔’。」。其经多种途径(cy玛50，FMol)代谢，代谢产物多达40种左右，主要代谢产物为去甲基达泊西汀和达泊西汀一N氧化物。达泊西汀排泄快，单剂量的达泊西汀的血药浓度24h降至峰浓度的5%左右，其排泄分两相，初始相tl/2约为1.4h，终末相tl/2约为20h。连续用药4d达到稳态血药浓度，有轻度蓄积(约1.5倍)。达泊西汀的药动学特征显示为剂量相关性和时间不变性，同时不受多剂量的影响，其主要代谢产物也同样不受多剂量的影响〔2，〕。研究表明[’”〕，年轻人和老年人的Cma，和AUC相似，食物可降低达泊西汀的吸收速率，其Cmax减少11%(398对443ng·mL一’)，Tm。二延长3omin，但AUC不受影响。

  二期临床试验采用多中心、双盲、随机、对照和交叉试验研究评价达泊西汀60mg，10omg和安慰剂治疗PE的有效性和安全性。研究对166例(年龄18一65岁，IELT<Zmin，平均1.olmin，单一固定的异性伴侣>6个月)参试者，分为3组，在性活动前1一3h分别服用达泊西汀60，100mg和安慰剂，由性伴侣用秒表测定IELT。有130例完成试验，结果表明，所有剂量的达泊西汀与安慰剂相比，IELT明显增加(P<0.0001)。试验前平均IELT 为1.olmin，试验终点10omg，60mg和安慰剂组的IELT分别为3.20·，2.94和2.05min，且首剂有效，2个用药组与安慰剂组相比p<0.00 1。主要不良反应恶心的发生率分别为5.6%，16.1%和0.7%。在10例因不良反应退出试验中，有9例是loomg组，因而，在1期临床试验中采用达泊西汀的最大剂量是60mg。

  三期临床试验是为验证需、时服用达泊西汀对中重度PE患者的有效性和安全性。在全美121个试验点进行2个为期12周的多中心、随机、双盲、对照平衡试验，2614例中服用安慰剂(n二870)、达泊西汀3omg(n二874)和60mg(n二870)，在性活动前1一3h服药，主要终点用秒表测定IELT。完成试验的人数安慰剂组627 例，30mg组为676例和60mg组为610例。结果表明，与安慰剂相比，所有剂量的达泊西汀均显著延长IELT(尸<0001)，且首剂有效。试验前安慰剂，30mg和60!n9组的IELT 分别为(0.90土0，47)，(0.92土0.50)和(0.91土0.48)min，12周后终点分别为(1.75士2.21)，(2:78土3.48)和(3.32士3.68)min。因而，需时服用达泊西汀30 和60mg对中重度的PE患者是有效的，且具有良好的耐受性。主要不良反应为恶心和头痛。

  达泊 西 汀
  常见的不良反应为恶心、腹泻、头晕和头痛。在1期临床试验中，恶心发生率最高，在60mg组达20%，有10%的患者中断试验，头晕为6.2%，腹泻为6.8%。单剂量3omg和6omg的不良反应发生率分别为26.2%和40.5%，多剂量分别为45.2%和40.5%，腹泻、恶心和头晕的出现dl比dg常见，ds的不良反应发生率与单剂量相似，多数是轻中度的不良反应。没有发现心血管系统、肝脏和血液系统等严重不良事件。

  目前 还没有有关达泊西汀与其他药物的相互作用的报道。在达泊西汀与磷酸二醋酶抑制剂泰达那非和西地那非〔3，〕，以及乙醇〔’6〕的药动学的研究中，尽管西地那非(10Ing)使达泊西汀的AUC增加2%，但没有临床意义;而乙醇与达泊西汀间没有明显的药动学相互作用。

  男人女人是否“性福”？这往往是人们最难以启齿的问题。1998年3月31日，辉瑞公司“伟哥”的问世引领了一场全新的男女“性福”革命，所产生的影响远不仅仅是人们的性生活。现在，美国强生公司又推出了治疗男性性问题的药物“Dapoxetine”，相信它所产生的社会影响将决不亚于“伟哥”。5月24日，英国路透社等主流媒体对此进行了报道。

  ★新药物能解决“伟哥”没有解决的另一半？
  随着科学技术的飞速发展，阳痿在大名鼎鼎的“伟哥”问世之后，使得许多男性重振了往日雄风，虽然有关伟哥的副作用，现在一直是争论不休，但它依然是许多男性心中的最爱，它在重建夫妻和谐性生活方面的贡献也不能被忽视。

  与这些阳痿患者相比，早泄患者一直苦无良方治表去根，只能眼睁睁看着“性福”生活离自己远去。为了解除这部分患者的痛苦，科学家们此前也进行了大量的科研工作，但一直进展缓慢。在这种背景下，美国强生公司研制的“Dapoxetine”治疗药物横空出世，给黑暗中的患者带来一丝曙光。那么，这种药物当真能够如强生公司所说，能够解决“伟哥”没有解决的另一半？

  在这种药物还处于临床阶段，美国强生公司就开始通过媒体做起了强力推介工作。该公司在此前举行的一个新闻发布会上表示，这种药物可以延缓男性射精、以及达到高潮的时间，从而大大提高夫妻间性生活的质量。“这种药物见效非常快，在进行性生活三到四小时之前服用即可。”普瑞尔博士在接受记者采访时如是说。

  强生公司是在对2600多名患者进行长期临床观察后得出这一结论的。普瑞尔还将这一结果以报告的形式递交给美国泌尿协会。报告显示，与服用普通安慰剂的男性相比，那些每次服用30mg到50mg的男性，控制射精的次数可以达到三到四次，而服用的剂量越大，效果则会越好。

  “延长射精的时间之后，这些试验人群的性生活可以说由‘较好’升级到了‘非常好’。”美国强生公司说，“服用30mg剂量‘dapoxetine’治疗药物，有20.2％到38.％的实验者的性生活质量明显提高一倍；服用60 mg的剂量，实验者的数字则会上升到22.3%到46.5％；而如果服用的剂量达到极值，则会有高达47％的性伴侣都能享受到性满足。”与此相比，服用安慰剂而得到性满足的男性比例最高也不会超过25％。

  ★新药物有没有副作用？
  虽然Dapoxetin治疗药物疗效非凡，但是这并不意味着它就没有副作用。科研小组在经过临床观察后发现，服用它可能会引起恶心、头痛、腹泻以及头晕眼花等症状。

  研究显示，服用低剂量的试验人群中，有8.7％的人会产生恶心症状，5.9％的人会头痛；在服用高剂量的实验者中，则有20.1％的人群会感到恶心，6.8％的人会有头痛和腹泻，6.2％的人则会有头晕眼花。

  正是这些副作用的存在，使得许多实验者中途退出，其中服用高剂量人群退出的比例为10％，低剂量为4％。尽管如此，普瑞尔博士和他的同事表示，“两种剂量的副作用完全可以忍受。”
      

Dapoxetine & Premature Ejaculation Overview According to Medscape Medical News, Dapoxetine Hydrochloride (Dapoxetine) has been shown to be effective in all doses for treatment of premature ejaculation. Experts are hopeful that this promising treatment will do for PE what other hugelypopular drugs have done for erectile dysfunction. There are many products that claim to help with PE, but this is the first that is simple, quick and has been proven in scientific studies. Dapoxetine is an easy, on-demand solution for the 30-70% ofmenwhoexperience premature ejaculation and are looking for a way to last longer in bed. Dapoxetine was developed specifically for enabling men to lengthen the time before ejaculation. An imbalance in the brain chemical Serotonin has long been believed to be a factor in rapid ejaculation. Because of this, SSRIs are often used "off label" to treat men who experience severe premature ejaculation. Dapoxetine is considered a "novel SSRI", however, because unlike many similar medications that take over 2 weeks to become effective, it starts working within an hour. The drug is is also quickly metabolized by the body. This eliminates the risk oflong term side-effects often associated with other SSRIs. Dapoxetine HCL is the first orally administered drug developed specifically for the treatment of menwithprematureejaculation. Thesafety and effectiveness of Dapoxetine for the treatment of men with PE were studied infive,doubleblind,placebocontrolled, Phase III clinical trials. These trials involved over 6,000 men from 30 countries worldwide, including countries in North America, South America, Europe and Asia, and in Israel and South Africa. The results of these trials were overwhelmingly positive. It worked and it was shown to be safe. Men taking the 30mg dose increased time before ejaculation by 308%. For the 60mg dose, the increase was 369%. Participants in the study took a single dose from 30 minutes to 4 hours before intercourse. Although rare, the most common side effect was nausea, and this was more likely to occur with higher doses. Overall, the men who received Dapoxetine reported greater control over the timing fo their orgasms, and increased overall satisfaction with the sexual experience. No doubt, their partners felt the same way. Regulatory Status of DapoxetineDapoxetine HCL has not yet been approved by the US FDA, but has been proven to be safe for premature ejaculation treatment in numerous studies worldwide. Many countries outside the US are moving ahead with regulatory submissions and approvals. Europe, as usual , is leading the charge when it comes to approving new treatments, and our European friends will probably be treatment for premature ejaculation long before it is readily available in the USA. Janssen-Cilag companies in Europe have recently submitted a Marketing Authorization Application (MAA) for Dapoxetine, as a treatment for premature ejaculation (PE) in men 18-64 years of age (December 2007). The European Marketing Authorization Application for Dapoxetine was submitted under what is referred to as the "decentralized procedure", whereby Sweden acts the Reference Member State and Austria, Finland, Germany, Italy, Portugal and Spain will act as the Concerned Member States for the application. Regulatory submissions and approvals in other regions of the world are expected to follow. Chemical Structure PriligyDapoxetine is a drug specifically developed for the on-demand treatment of PE [Premature Ejaculation] and is the first oral medication (tablet) to be approved for this condition. Dapoxetine has been extensively evaluated in five randomised, placebo-controlled Phase III clinical trials involving more than 6,000 men with PE and their partners. This is the largest and most comprehensive clinical trial programme to date for a drug therapy to treat PE. Dapoxetine is a unique, short-acting, selective serotonin reuptake inhibitor (SSRI) designed to be taken only when needed, that is 1–3 hours before sexual intercourse is anticipated, rather than every day. “Dapoxetine is an important new medication fordoctorsandpatients,"commented Professor Dr Hartmut Porst, Private Institute for Urology and Andrology,Hamburg, Germany. “The lack of a previously approved oral medication for PE has contributed to a substantial deficiency in the diagnosis and treatment of this common condition. For the first time, physicians will be able to provide men with a pharmaceutical product that has been specifically developed for PE and that is proven to be effective.” Premature Ejaculation PE is a distressing sexual dysfunction that can be present from the first sexual encounter or can develop later in life. Depending on the methodology and criteria used to evaluate the prevalence of PE in studies, the reported proportion of men affected with this condition at some point in their lives has ranged from 4–30%. Experts in PE from the International Society of Sexual Medicine (ISSM) define the condition as consisting of three major components: a short time to ejaculation, lack of ejaculatory control and negative personal impact or distress related to ejaculation. The condition is defined by the ISSM as “a male sexual dysfunction characterised by ejaculation which always or nearlyalways occurs prior to or within about one minute of vaginal penetration; and inability to delay ejaculation on all or nearly all vaginal penetrations; and negative personal consequences, such as distress, bother, frustration and/or the avoidance ofsexual intimacy”. Unlike erectile dysfunction (ED), which tends to affect older men, PE has similar prevalence across all age groups. In fact, more men are believed to experience PE thanED.Acombinationofphysiologicalandpsychologicalfactorsarebelievedtoinfluence the mechanism of ejaculation 8, 9. Men with PE appear to go through the same process of ejaculation as other men, but it happens more quicklyandwithareduced feeling of control. Research suggests serotonin plays a central role in the timing of ejaculation. Priligy™ (dapoxetine) receives first regulatory approvals for the treatment of premature ejaculation (PE)At the Netherlands Pharmacy you can pay with Visa, Mastercard, Amex or Banktransfer to a german Bank Account. At the Romania Pharmacy you can pay with Visa and Mastercard. The Delivery time at theRomania Pharmacy takes maybe 1 or 2 Days longer then the Shipping from Netherland. You will also find oline tracking facilities.