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Dostinex~Cabergoline

heavyiron

Chemistry Experiment
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by Anthony Roberts -- Dostinex (Cabergoline) is a dopamine agonist. Dopamine is a chemical, found in the brain, which transmits nerve impulses and is involved in the formation of epinephrine. More likely than not, this is why the Life-Extentionistas are very big on this drug. Dopamine is also released by the hypothalamus, and hormone can inhibit the release of prolactin from the anterior lobe of the pituitary, so given all the bad things that we have already seen to be a result of excess. If you use anabolic steroids, Dostinex will help you reduce the chance of any of these prolactin related side-effects. It has actually been shown in numerous studies to have a very high success rate in lowering prolactin and prolactin related conditions and side-effects (1) (2).In fact, for management of hyperprolactinemia and it???s symptoms (got milk?), Dostinex is the preferred treatment in terms of effectiveness as well as having very few undesirable side effects (3). It does this very well for both men and women, it should be noted???almost identically actually (4)

Since it lowers prolactin very efficiently, Dostinex will even get rid sexual dysfunction caused by excess prolactin (5) (which is (anecdotally at least) highly correlative with the use of certain steroids like the Nandrolones and Trenbolones (Deca and Tren). This is great news for everyone who loves Tren and Deca, because those two steroids are really great additions to almost any cycle- but many people avoid using them because of the possibility of them causing impotence (often called ???deca dick???).

Using Dostinex will allow you to include steroids like Tren and Deca in any cycle- and even combine them in the same cycle- without worrying about sexual dysfunction. In fact???even if you aren???t experiencing any sort of sexual dysfunction, Dostinex will shorten the time you need to recover and gain an erection between orgasms, and can significantly enhance all parameters of sexual drive and function (6). In other words, if you???re not worried about sexual issues and you take Dostinex anyway???it???ll still help you out in bed. And from what I have heard, it???s well worth the money for that effect.

Of course you can actually use Dostinex safely for an extended amount of time (many studies go on for months if not years, and its efficacy and safety are well documented), but women need to be more careful than men, and certainly need to discontinue using it if they???re pregnant or trying to conceive. SO Dostinex can help you, the average steroid user, by combating gyno-like effects, as well as galactorrhea, and sexual dysfunction. Sounds great, right? Of course it is???but since Dostinex is a dopamine agonist, which means it???s good for a whole lot more.

You see Dopamine is what???s called a monoamine, which is naturally produced in the body by modifying an amino acid.

dopamine.gif

Dopamine
And it???s this structure which makes it very interesting to us. Dostinex as you already know is what???s known as a dopamine ???agonist???- or substance that triggers a response in a specific body tissue or group of cells by binding to specific receptor on or inside the cells, as if it were actually the bodily substance that usually binds to that receptor. Probably the one that most people are familiar with, with regards to agonists is ephedrine, which is an andrenergic agonist. This is why ephedrine makes you feel ???wired??????it ???feels??? like adrenaline to your body. Cabergoline is a dopamine agonist???which makes it ???feel??? like dopamine to your body.

dostinex.gif

Dostinex

So what does that mean? Well, in the brain, dopamine helps control the flow of information from other areas of the brain. So a dopamine agonist will help you process information more quickly, and possibly improve your memory also. Some athletes use Dostinex because it helps them learn new motor skills more quickly and thus they can learn new techniques or plays at a faster rate than their competition; needless to say this gives the athletes using Dostinex a huge advantage over their competition. This ability to work on your bodies information pathways and nervous system are doubtless why it???s been successfully been used to fight Parkinsons disease (7)(8).

But does this actually work in real athletes? Well, actually, that???s why I started reading about Dostinex. See, I have the fortune of being able to basically call some of the most famous strength coaches in the world whenever I want. And, recently the last time I spoke to one about training and anabolic steroids, I asked him about different training programs for a person on steroids- and his answer said that it depends on whether that person was taking a nootropics or not. And as you may remember, Dostinex is a nootropic. It was that conversation that made me really take a closer look at Dostinex. And of course, that strength coach told me that his athletes have used nootropics with great success. The down side of knowing internationally renowned strength coaches is that their sense of humor is usually a little off, and if you have the fortune of being able to pick their brains on training, you also invariably have the misfortune of ending up on their group e-mail list which gets you a whole host of bizarre forwarded e-mails???


In fact, when you don???t have enough dopamine, you may even have difficulty concentrating???low dopamine levels have also been cited as a possible underlying cause for Attention deficit disorder (ADD) and Attention deficit/ Hyperactivity disorder (ADHD). In fact, many several medications used to treat ADD and ADHD will also serve to stimulate dopaminergic, and this could be one of their possible mechanisms of action.

Dopamine is also what???s called a ???pleasure chemical??????it???s usually released by your body when you experience a rewarding experience such as eating your favorite food, having sex, winning the lottery???.whatever. Interestingly, since this ???happy??? effect is felt when you are satiated from food, it???s highly possible that Dopamine agonists will cause you to feel ???full??? more often and decrease desire for food without the discomfort that dieting usually brings. Dopamine is released when you eat a nice big meal???so???a dopamine agonist like Dostinex may make you not want to eat as much, and help you feel full even if you don???t eat enough. Dostinex, therefore, may be of great interest to precontest bodybuilders and other dieters, who want to avoid some of the discomfort and anxiety that calorie restriction can bring.

Certain recreational drugs also have a lot to do with their effects on dopamine. Cocaine is what is known as a dopamine transporter blocker; what this means is that it competitively inhibits dopamine uptake to increase the amount of time released dopamine is active in your body. This makes you feel good, while the dopamine is floating around your body. Methamphetamine is another illicit (illegal) recreational drug that acts on dopamine as well. It actually serves to competitively inhibit dopamine uptake as well as increasing dopamine flow through a dopamine transporter pathway. That???s how those drugs make you ???feel good.??? Dostinex is, of course, neither physically nor mentally addictive, but since it is a dopamine agonist, its users often experience an enhanced positive sense of well being. So besides helping with all of the things discussed earlier, Cabergoline will also just make you feel damn good.

So now that I told you about it, I???ll tell you how much Dostinex do you need to start experiencing these effects???or basically, how I???m going to use it, now that I did all this research on it!

From the reading I???ve done, you only need about half a milligram (1/2mg) a week to experience all of the anti-prolactin, prosexual, antidepressant, and cognitive effects of Dostinex, but that???s on the very low end of the effectiveness scale. This stuff has an extremely long active life in the body, so once a week dosing is fine???but if it were me, and I were taking this stuff, I???d probably be using about .25mgs-.5mgs twice a week.
It should be taken before bed-time, because it may actually help you sleep a bit better, (9), Can be taken with or without food and not alter the pharmacokinetics (how it functions in your body) (10), and (incidentally) according to the literature is a much more efficient drug thanBromocriptine (11).

I think once people find out about this drug, it???s going to find it???s way into quite a few bodybuilders??? cycles alongside Tren, Deca, or both???and athletes are going to take advantage of it???s uses for skill acquisition and motor co-ordination help???and all the other stuff???the prosexual properties and general ???feel good??? properties of Dostinex make it a great choice for anyone interested in ???err???feeling good and having better sex???which I suspect is basically everyone, not just bodybuilders and athletes. I guess I should have paid more attention to this stuff when it started appearing on those Life-Extension club pricelists a decade ago???but at least I figured it out now???.even if I happen to be a bit late on this one.

Cabergoline is the chemical name of active ingredient in Dostinex.
Dostinex is a registered trademark of Pfizer Inc. in the United States and/or other countries.


References

1. J Clin Psychiatry. 2004 Feb;65(2):187-90
2. Pituitary. 2005;8(1):39-42
3. Treat Endocrinol. 2003;2(1):23-32. Review.
4. Eur J Endocrinol. 2003 Mar;148(3):325-31
5. J Clin Endocrinol Metab. 2004 Feb;89(2):621-5.
6. J Endocrinol. 2003 Dec;179(3):357-65
7. CNS Drugs. 2004;18(11):733-46. Erratum in: CNS Drugs. 2005;19(7):633.
8. J Neural Transm. 2004 Jun;111(6):725-32. Epub 2004 Mar 19.
9. Neurol Sci. 2003 Oct;24(3):170-1.
10. Biopharm Drug Dispos. 1996 Jul;17(5):443-55.
11. Eur J Endocrinol. 1998 Mar;138(3):286-93
 
Cabergoline- the latest in libido enhancement

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 and proved that cabergoline was superior in all respects to bromocriptine.

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.
 
Six Months of Treatment with Cabergoline Restores Sexual Potency in Hyperprolactinemic Males: An Open Longitudinal Study Monitoring Nocturnal Penile Tumescence

Michele De Rosa, Stefano Zarrilli, Giovanni Vitale, Carolina Di Somma, Francesco Orio, Libuse Tauchmanova’, Gaetano Lombardi and Annamaria Colao

Department of Molecular and Clinical Endocrinology and Oncology, Federico II University of Naples, 80131 Naples, Italy
[SIZE=-1]Address all correspondence and requests for reprints to: Annamaria Colao, M.D., Ph.D., Department of Molecular and Clinical Endocrinology and Oncology, Federico II University of Naples, via S. Pansini 5, 80131 Naples, Italy. E-mail: colao@unina.it .[/SIZE]

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Abstract



This open longitudinal study investigated the prevalence of depressed sexual potency by monitoring erectile dysfunction using nocturnal penile tumescence (NPT) in 51 consecutive men with hyperprolactinemia (41 macroprolactinomas and 10 microprolactinomas) and evaluated potential reversibility of sexual failure after 6 months of treatment with cabergoline. Fifty-one healthy men served as controls.
Compared with controls, the patients with either micro- or macroprolactinoma had low testosterone levels with severe alterations of erectile function. Testosterone deficiency was present in 73.2% of macro- and 50% of microprolactinomas; reduced libido and sexual potency were referred by 53.6% of macroprolactinomas, 50% of microprolactinomas, and none of controls. Fewer than three erectile events per night by NPT were found in 96.7% of patients and 13.7% of controls (P < 0.0001). After 6 months of cabergoline treatment, prolactin levels normalized in 74.5% of patients: 73.2% of macroprolactinomas and 80% of microprolactinomas. Testosterone levels normalized in 68.6% of patients, whereas NPT normalized in 60.6% of patients who had normalized prolactin levels and in 7.7% of patients who did not. In conclusion, at study entry, 50% of the patients complained of sexual disturbances, 96.7% of whom had an impairment of erectile events per night compared with 13.7% of controls. Six months of treatment with cabergoline normalized testosterone levels in most cases, thus restoring and maintaining during treatment the capability of normal sexual activity in hyperprolactinemic males.

full study;
http://jcem.endojournals.org/cgi/content/full/89/2/621
 
Sex and Cabergoline

By David Jay Brown

Cabergoline is a fairly new pharmaceutical that has enormous potential to aid male stamina. Perhaps the most remarkable aspect of carbergoline is that it has been found to substantially raise a man’s chances of sustaining multiple orgasms during sex. Some men on cabergoline are able to have numerous multiple orgasms in rapid succession.

Cabergoline, which is marketed under the trade name of Dostinex, is used to treat Parkinson's disease, to prevent women producing milk when they want to stop breast feeding, and to lower prolactin levels in patients with a pituitary tumor. It is also sometimes used to help men with sexual dysfunction.

It is cabergoline’s capacity to lower prolactin levels that makes it such a sexual wonder drug for men. Prolactin is a single-chain protein hormone, closely related to growth hormone, that stimulates the secretion of milk of women. The hormone also has the effect of reducing a man’s desire for more sex by preventing new erections. Cabergoline has been found to to minimize the effects of the hormone prolactin, which is produced by men at the point of orgasm. As a result, some subjects who tried the drug found that they were able to have multiple orgasms in rapid succession.

In one study, 60 subjects, all healthy males, between the ages of 22 and 31, normally needed a break of 19 minutes between lovemaking sessions. However, after taking Cabergoline, they were able to have several orgasms within a few minutes. Medical psychologist Manfred Schedlowski, who was involved in the trials at Essen in Germany, said the drug raised the libido to enable the male to orgasm again more quickly.

Schedlowski said, "We saw that prolactin rises after orgasm and then thought maybe prolactin is a negative feedback system. Subjects who took this drug had decreased prolactin levels, and reported their orgasm was better and there was a shorter refractory period. We interviewed these 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."

Cabergoline was reported to have no side effects on men during the tests, according to a paper that was published in the International Journal of Impotence Research. However, there may be a drawback. There’s evidence that the release of prolactin in the brain, which surges during orgasm, promotes the growth of new neurons in the brain--a process called neurogenesis. Researchers at the University of Cal-gary discovered that the release of prolactin spurs the growth of new brain cells in the front regions of the brain involved in smell. So Cabergoline may allow men to have multiple orgasms at the expense of
less brain growth. Sounds like a tough call to me.

Researchers are carrying out trials to investigate whether Cabergoline will have similar effects on women. Some anecdotal reports suggest that the drug has the potential to enhance the intensity of orgasms in both men and women.
 
J Endocrinol. 2003 Dec;179(3):357-65.

Effects of acute prolactin manipulation on sexual drive and function in males.

Krüger TH, Haake P, Haverkamp J, Krämer M, Exton MS, Saller B, Leygraf N, Hartmann U, Schedlowski M.
Department of Medical Psychology, University of Essen, Hufelandstrasse 55, 45122 Essen, Germany. tillmann.krueger@web.de

Abstract

The neuroendocrine response to sexual activity in humans is characterized by a pronounced orgasm-dependent increase of plasma levels of prolactin. In contrast to the well-known inhibitory effects of chronic hyperprolactinemia on sexual drive and function, the impact of acute prolactin alterations on human sexual physiology is unknown. Therefore, this study was designed to investigate the effects of acute manipulation of plasma prolactin on sexual behavior. Ten healthy males participated in a single-blind, placebo-controlled, balanced cross-over design. Prolactin levels were pharmacologically increased to high levels (protirelin, 50 micro g i.v.) or reduced to low physiological concentrations (cabergoline, 0.5 mg p.o.). Sexual arousal and orgasm were then induced by an erotic film and masturbation. In addition to continuous neuroendocrine and cardiovascular recordings, the quality and intensity of the acute sexual drive, arousal, orgasm and refractory period were assessed by extensive psychometric measures. Administration of cabergoline decreased prolactin levels and significantly enhanced all parameters of sexual drive (P<0.05), function (P<0.01) and positive perception of the refractory period (P<0.01). Administration of protirelin increased prolactin concentrations and produced small, but not significant reductions of sexual parameters. The sexual effects observed from cabergoline were completely abrogated by coadministration of protirelin. Although different pharmacological sites of action of prolactin-altering drugs have to be considered, these data demonstrate that acute changes in prolactin plasma levels may be one factor modulating sexual drive and function. Therefore, besides a neuroendocrine reproductive reflex, a post-orgasmic prolactin increase may represent one factor modulating central nervous system centers controlling sexual drive and behavior. These findings may offer a new pharmacological approach for the treatment of sexual disorders.


PMID: 14656205 [PubMed - indexed for MEDLINE]

Full study

http://joe.endocrinology-journals.org/cgi/reprint/179/3/357
 
Int J Impot Res. 2007 Jan-Feb;19(1):104-7. Epub 2006 May 18.

Cabergoline treatment in men with psychogenic erectile dysfunction: a randomized, double-blind, placebo-controlled study.

Nickel M, Moleda D, Loew T, Rother W, Pedrosa Gil F.
Clinic for Psychosomatic, Inntalklinik, Simbach/Inn, Germany. m.nickel@inntalklinik.de

Abstract

The effectiveness of cabergoline in 50 men with psychogenic erectile dysfunction was investigated in a 4-month, randomized, placebo-controlled, double-blind study with validated psychological tests, and prolactin, follicle-stimulating hormone, luteinizing hormone and testosterone serum levels. Cabergoline treatment was well-tolerated and resulted in normalization of hormone levels in most cases. In the cabergoline-treated group, significant interactions between prolactin and testosterone serum concentrations were observed. Erectile function improved significantly. Sexual desire, orgasmic function, and the patient's and his partner's sexual satisfaction were also enhanced. Cabergoline may be an effective and safe alternative agent for men with psychogenic ED.


PMID: 16728967 [PubMed - indexed for MEDLINE]
 
Eur J Endocrinol. 1998 Mar;138(3):286-93.

Cabergoline treatment rapidly improves gonadal function in hyperprolactinemic males: a comparison with bromocriptine.

De Rosa M, Colao A, Di Sarno A, Ferone D, Landi ML, Zarrilli S, Paesano L, Merola B, Lombardi G.
Department of Endocrinology and Molecular and Clinical Oncology, Federico II University, Naples, Italy.

Abstract

This study evaluated the effects of chronic treatment with cabergoline (CAB), a new, potent and long-lasting ergoline-derived dopamine agonist, on seminal fluid parameters and sexual and gonadal function in hyperprolactinemic males in comparison with the effect of bromocriptine (BRC) treatment. Seventeen males with macroprolactinoma were treated with CAB at a dose of 0.5-1.5 mg/week (n = 7), or BRC at a dose of 5-15 mg/day (n = 10) for 6 months. Baseline prolactin (PRL) was 925.7 +/- 522.6 microg/l in the CAB-treated group and 1059.4 +/- 297.6 microg/l in the BRC-treated group. All the patients suffered from libido impairment, ten from reduced sexual potency, and six had infertility. In five patients provocative bilateral galactorrhea was found. Seminal fluid analysis, functional seminal tests and penis rigidity and tumescence, measured by nocturnal penile tumescence (NPT) using Rigiscan equipment, were assessed before and after 1, 3 and 6 months of CAB or BRC treatment. Hormone profiles were assessed before and after 15, 30, 60, 90 and 180 days of both treatments. Before treatment, all patients had a low sperm count with oligoasthenospermia, reduced motility and rapid progression with an abnormal morphology and decreased viability, and a low number of erections. After 1 month, serum PRL levels were significantly reduced in both groups of patients (20.6 +/- 6.6 microg/l during CAB and 256.3 +/- 115.1 microg/l during BRC treatment) and were normalized after 6 months in all patients (CAB: 7.9 +/- 2.2 microg/l; BRC: 16.7 +/- 1.8 microg/l). After 6 months, a significant increase of number, total motility, rapid progression and normal morphology was recorded in patients treated with both CAB and BRC. An increase in the number of erections during the first 3 months of both treatments was noted by NPT. However, the improvements in seminal fluid parameters and sexual function were more evident and rapid in patients treated with CAB. The number of erections was normalized after 6 months of treatment in all patients submitted to CAB treatment, and in all patients but one treated by BRC. In addition, a significant increase of serum testosterone (from 3.7 +/- 0.3 to 5.3 +/- 0.2 microg/l) and dihydrotestosterone (from 0.4 +/- 0.1 to 1.1 +/- 0.1 nmol/l) was recorded. At the beginning of treatment, mild side-effects were recorded in two patients after CAB and mild-to-moderate side-effects in five patients after BRC administration. The treatment with CAB normalized PRL levels, improving gonadal and sexual function and fertility in males with prolactinoma, earlier than did BRC treatment, providing good tolerability and excellent patient compliance to medical treatment.


PMID: 9539303 [PubMed - indexed for MEDLINE]

Full study
Cabergoline treatment rapidly improves gonadal function in hyperprolactinemic males: a comparison with bromocriptine -- De Rosa et al. 138 (3): 286 -- European Journal of Endocrinology
 
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