英文药名: Dostinex (Cabergoline Tablets)
中文药名: 卡麦角林片 生产厂家: Pfizer
药品简介
通用名称:卡麦角林 英文名称:Cabergoline 英文别名:Dostinex
【药理作用】卡麦角林为长效多巴胺D2-受体激动剂。它通过促进多巴胺的释放,反馈性抑制下丘脑的功能,进而降低催乳素的分泌。
【药代动力学】 吸收:口服胃肠道吸收。经历首过代谢效应。 分布:血浆蛋白结合率:约40%。 代谢:广泛代谢为无活性的代谢产物。 排泄:主要经粪便排泄。
【适应症】用于抑制生理性泌乳以及治疗高催乳素血症相关性疾病。
【用法用量】不同适应症的用法用量: 抑制生理性泌乳:成人:1mg,产后第1天一次性给药。肝损害:调整剂量。 抑制泌乳:成人:250mcg/12小时,持续2天。 高催乳素血症相关性疾病: 成人:初始剂量:500mcg/周,然后根据反应,每月加量500mcg,可每周一次给药或分2次在不同日期给药;药量超过1mg应当分次给药。 常规剂量:1mg/周,可高达:4.5mg/周。进餐时或餐后服用。
【药物过量】症状:鼻塞、晕厥或幻觉。处理:需要时,采取措施维持血压正常。
【禁忌】下列情况禁用:妊娠毒血症,有产后精神病史者,未控制的高血压,肝功能不全。对卡麦角林和麦角衍生物过敏者。
【注意事项】下列情况慎用:心血管疾病,雷诺氏综合征,肾脏或肝脏损害,消化性溃疡,胃肠道出血,精神疾病史,高血压。影响驾车和机械操作能力。长期或高剂量用药会导致精神问题、胸膜/腹膜后纤维化或心脏瓣膜纤维化。每月一次监测血清泌乳素水平直到正常。肝损害患者定期监测肝功能。
【不良反应】血压降低,头晕,眩晕,头痛,恶心,失眠,腹痛,消化不良,胃炎,虚弱,疲劳,便秘,呕吐,胸痛,热潮红,抑郁,麻刺感,腿痛性痉挛,雷诺氏综合征,伴有幻觉,错觉和意识混乱的精神异常。副作用呈剂量相关系,高剂量时发生副作用的可能性增加。
【药物相互作用】与抗高血压药合用,增加发生体位性低血压的风险。增强多巴胺的血管收缩作用。降低硝酸甘油的血管舒张作用。与选择性5-羟色胺再摄取抑制剂或三环类抗抑郁剂合用,增加发生5-羟色胺综合征的风险。 严重药物相互作用:与西布曲明合用,有发生5-羟色胺综合征的风险。
【FDA妊娠分级】B级:在动物繁殖研究中(并未进行孕妇的对照研究),未见到药物对胎儿的不良影响。或在动物繁殖性研究中发现药物有副作用,但这些副作用并未在设对照的、妊娠首3个月的妇女中得到证实(也没有在其后6个月具有危害性的证据)。
Product Information
Cabergoline - the latest in libido enhancement
Dostinex contains Cabergoline which is more potent than Bromocriptine to block the actions of prolactin and enhance dopamine levels. Approved for use in Parkinson’s disease recent trials have exposed its libido enhancing effects.
Cabergoline increases the levels of dopamine through its action of stimulating D2 receptor sites, it is officially approved to assist in the treatment of Parkinson’s disease, as well as treat states of prolactinoma (i.e. prevent breast development in men and reduce excess milk secretion in women).
However, cabergoline (brand name Dostinex has been described as being able to do everything that Viagra can’t! This is because rather than induce an erection (as Viagra can); cabergoline has been shown to improve libido, orgasm and ejaculation (which Viagra has not).
Cabergoline is from the dopaminergic family of drugs that increase the level of dopamine and also decreases the levels of the hormone prolactin. Prolactin is the hormone secreted in women after giving birth and to enhance their lactation for breast feeding. However, prolactin has recently been shown to be an inhibitor to a healthy libido, this may help explain why many women have a low sex drive after giving birth- whilst they are breast feeding. But men can also suffer from prolactinoma (high levels of prolactin) leading to a lack of sex drive- as well as developing breasts, particularly as prolactin levels tend to increase for most men with age.
Recently it has been discovered that prolactin is released immediately after an ejaculation and may be part of the reason men like to go sleep after sex with no will for further love making.
Cabergoline has been proven to significantly decrease prolactin and in so doing increase the sex drive (libido) substantially. There have been reports of enhanced and multiple orgasms as well as stronger ejaculations.
To date, bromocriptine has been the main drug of choice to reduce prolactin levels, however clinical studies have confirmed that cabergoline is much more effective in this regard. For example in 450 tested subjects over 8-weeks 77% of the subjects had their prolactin levels returned to normal using 0.5mg of cabergoline twice a week, compared to 59% of subjects using bromocriptine at 2.5mg twice a day. Furthermore, side effects were far fewer in the cabergoline group, recorded at 2% of incidences compared with 60% of those taking bromocriptine.
One fascinating trial on 60 healthy males, between the ages of 22 and 31 discovered that they needed a break of 19 minutes between love making. However, after taking cabergoline, they were able to have several orgasms within a few minutes!
Dr. Manfred Schedlowski, who was involved in this trial in Germany, said; “Cabergoline raised the libido to enable the male to orgasm again more quickly. We saw that prolactin rises after orgasm and then thought that maybe prolactin is a negative feedback system. Our subjects who took cabergoline had decreased prolactin levels and reported their orgasm was better and there was a shorter refractory period.”
Dr. Schedlowski went on to say; "We interviewed the subjects and found they were able to have multiple orgasms in very rapid succession. This is sitting very nicely with our hypothesis that orgasms and sexual drive are steered by prolactin and dopamine in the brain."
Furthermore, cabergoline had no side effects on men during the tests; this was reported in an article for the International Journal of Impotence Research. The researchers now plan to carry out trials to investigate whether cabergoline will have the same effect on women.
Another medical study by the Federico University, in Naples, Italy published in the European Journal of Endocrinology showed cabergoline to be very potent in increasing libido and sexual potency. The study examined cabergoline vs. bromocriptine (Parlodelâ) and proved that cabergoline was superior in all respects to bromicriptine.
17 males with prolactinoma were treated with cabergoline or bromocriptine for 6 months. All patients initially suffered from libido impairment, with 10 suffering from reduced sexual potency and 6 were infertile. Before treatment all patients suffered from low number of erections and had a low sperm count. After 1 month of treatment prolactin levels were significantly reduced in both groups of patients. A notable increase in the number of erections during the first 3 months was recorded and continued throughout the 6 months of treatment. However the improvements in seminal fluid parameters and sexual function were more evident and rapid in patients treated with cabergoline. A significant increase in the serum levels of testosterone and dihydrotestosterone were also recorded. At the beginning of treatment, mild side-effects were recorded in 2 patients using cabergoline compared to 5 in the bromocriptine patients.
Conclusion It is now recognised that the stimulation of dopamine can enhance sexual arousal and this has been shown to occur with drugs such as bromocriptine, deprenyl and Sinemet®. Now that prolactin is being recognised as an inhibitor of sexual function and desire, a drug such as cabergoline that enhances dopamine levels and reduces prolactin levels is being heralded as a significant libido enhancer- despite the fact that it has not yet been approved for this purpose.
Dosage: Take 0.25mg or 0.5mg no more than twice per week, unless treating a serious medical disorder whereupon the dosage may differ according to your physician's guidance, usually built up slowly to no more than 1mg twice weekly.
Side effects: Nausea, headache, dizziness and constipation.
Caution: Cabergoline can contraindicate with psychoactive and hypotensive drugs such as phenothiazines, butyrophenones, thioxanthenes and metoclopramides. Furthermore caution must be advised if taken concurrently with other dopamine (D2) enhancing drugs, such as bromocriptine, deprenyl and Sinemet®. Although often dependant on the dosages used, these should only be administered concurrently under a physician's guidance. Cabergoline’s effects can also be exaggerated when combined with other ergots, including hydergine and nicergoline, particularly those who may be sensitive to them. Cabergoline must not be used by pregnant or lactating women. |