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Bromocriptine-prolactin inhibition


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Post by CYPHON on Thu Jul 13, 2017 5:39 am

A Prolactin blocker.

This semi-synthetic derivative of the ergo group is a dopamine receptor agonist and a Prolactin inhibitor.

Its first major anti-aging use is the enhancement of Dopamine, (a key brain neurotransmitter that undergoes an age-related decline). Past the age of 40 it is estimated that �on-average� the healthy person undergoes a Dopamine decline of approximately 13% per decade, (Dean, Fowkes & Morgenthaler). Accordingly, some neurologists have stated that; �if we all live long enough we shall all become senile.� This is due to the fact that abnormally low levels of Dopamine (after 70% to 80% loss) are diagnosed as Parkinson�s disease, hence protection and enhancement of the Dopamine producing neurons is a key strategy for anti-aging medicine. Not surprisingly then, Bromocriptine is sometimes used in conjunction with other drugs, (such as Deprenyl and Sinemet) in the management of Parkinson�s disease, but anti-aging medicine also considers its preventative properties.

Its second major anti-aging use is the inhibition of Prolactin, this hormone is one of the few that actually appears to increase with age. Prolactin is produced by the pituitary gland and its release is inhibited by Bromocriptine.

Prolactin has been described as a �fat synthesis hormone.� This is because one of its primary functions is to trigger lactation, (milk production) and weight gain in pregnancy. In women, Bromocriptine has been used to help restore ovulation, but it also helps to reduce serum Prolactin levels in men, (although the precise role of Prolactin in men is unclear). A further possible need to control age-related Prolactin levels, is offered by some researchers who believe that Prolactin is an immune system suppressant.

Bromocriptine also effects the most famous of all pituitary hormones- Growth Hormone (GH). Bromocriptine increases growth hormone secretion in individuals with normal growth hormone concentrations, but paradoxically suppresses GH secretion in some patients with acromegaly,(a condition of excessive-production of GH). Studies indicate that Bromocriptine does not affect the release of any other anterior pituitary hormones.

An interesting clinical study administered a component of tobacco called DMBA to rats, at a level where it is known to be very effective in producing breast cancer. However, rats that had been pretreated with Bromocriptine completely avoided any cancer development. Bromocriptine therefore appears to also offer itself as a very potent free radical quencher.

One of the most recent studies indicates that Bromocriptine may be a candidate for the treatment of Type-II diabetes. This is because Bromocriptine has been shown to suppress lipogenesis and improve glucose tolerance and insulin resistance.

One animal study suggested that a further action of Bromocriptine is to alter CNS (central nervous system) regulating metabolism, and as such, has another important use in helping to prevent weight gain, (this would be in addition to its improvement of diabetic conditions).

Bromocriptine is a very potent substance and it must not be used by pregnant or lactating women, (unless under the guidance of a physician). Side effects include nausea, dizziness, lowering of blood pressure, hypotension and confusion. The first three are relatively common, especially when undertaking initial use. It is also known to increase fertility, and thus �extra care� and contraception is advised where necessary.

It does contraindicate with psychoactive and hypotensive drugs and other Dopamine enhancing drugs, such as Deprenyl and Sinemet etc. Although often dependant on the dosages used, these should only be administered concurrently under a physician�s guidance. Its effects can also be exaggerated when combined with other ergots, including Hydergine and Nicergoline.

Overall, there is little need to exceed a dosage in excess of 1.25mg or 2.5mg daily for most people, unless treating a serious medical disorder (and therefore only under a physician�s guidance). Bromocriptine has a wide and diverse range of clinically applications, it could be considered to only be an anti-aging medicine for the serious longevist.

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Post by CYPHON on Thu Jul 13, 2017 6:15 am

by Lyle McDonald - Bromocriptine is a dopamine agonist drug (meaning it acts like dopamine in the brain), primarily activating the dopamine D2 receptors. It's main use is for the treatment of high prolactin, Parkinson's disease, and acromegaly; it was also used by bodybuilders in the 80's for it's GH releasing properties. However, it's metabolic effects are far greater than that.

In genetically obese rats, bromocriptine normalizes metabolism and there are many good reasons to think it will do the same in humans. Bromocriptine has use during dieting (to minimize the negative adaptations), muscle gain when very lean, and may be beneficial post-steroid cycle. It may also be useful for diabetes treatment and may have pro-sexual effects.

Bromocriptine has a half-life of roughly 12-14 hours, and dosing is 2.5-5 mg/day taken in the morning.

For additional information, read Lyle McDonald's ebook, Bromocriptine: An Old Drug With New Uses

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Post by CYPHON on Thu Jul 13, 2017 7:03 am

By aurthor rea:

Prolactin Control

*In opposition to what we normally see with all of the other pituitary hormones, the hypothalamus predominantly suppresses prolactin release from the pituitary gland. In other words, there is usually a hypothalamic "Stop that" order set against the lactotroph, and prolactin is released only when the order is released or ended.

A note of interest is that if the pituitary stalk is severed, prolactin release increases, while secretion of all the other pituitary hormones decreases dramatically due to loss of hypothalamic releasing hormones. But this is an unlikely scenario for most athletes and should obviously be avoided nonetheless.

The neurotransmitter Dopamine appears to act as the top dog prolactin-inhibiting factor. Dopamine is secreted into portal blood by the hypothalamic neurons. Next it binds to receptors on lactotrophs, and inhibits both the synthesis and release of prolactin. So chemicals and drugs that interfere with dopamine release or receptor binding also increase the release of prolactin. These are called antagonists. Drugs and chemicals that either increase, act as, or potentate dopamine are agonists.

Of course there are other chemicals in the body's Action/Reaction Factor closet that positively regulate prolactin. The major ones are GnRH, TRH (thyroid Releasing Hormone) and VIP (Vasoactive Intestinal Polypeptide). By the way, hyper-stimulation of the nipples may have a stimulatory effect upon prolactin release as well. But that is one we will leave alone.

So, Why Do Non-Cross Dressing Men Produce Prolactin?

*As a man ages his body begins to decrease the amount of androgens that it synthesizes. In fact many studies have shown that an average 40-year-old male produces about half of the testosterone that he did when he was 18. So, he possesses a lower rate of muscle anabolism yet a higher rate of fat anabolism.

Many researches have claimed that this is due to normal physiological changes that occur as we progress through the years. In truth this is bullshit and supposition based upon average sedimentary individuals. I monitor the physiological indicators of athletes for a living. I can say conclusively that almost any otherwise healthy male that remains in peak condition and eats a proper diet will retain a superior androgen production profile. So this is more so a matter of choice than pre-programmed physiological events. With that said let's get on with the "why" of prolactin.

Estrogen is a primary promoter of prolactin release. Of course there are other factors to consider (which we will discuss in a moment) that may trigger excessive prolactin secretion, but the normal trend toward increased prolactin release is due to increased estrogen synthesis.

More Action/Reaction

The clinical term for excessive release of prolactin is hyperprolactinemia. It is actually a relatively common disorder in humans, especially those who utilize AAS. There are many causes that initiate the condition including prolactin-secreting tumors and therapy with certain drugs.

Males that experience hyperprolactinemia commonly develop hypogonadism (the shut down of the HPTA) with decreased sperm production, decreased sex-drive and impotence. Those affected normally show breast enlargement (gynecomastia), but very rarely actually lactate.

The gyno can initially manifest itself as an increase in fatty tissue under the lower pectorals and a puffy appearance to the areola and nipple prior to formation of the painful benign (usually) tumors.

A simple blood test for serum prolactin levels is commonly employed to evaluate the degree of potential feminization a male can or is experiencing. The lab results are quite simple to read, though a trained professional should interpret the results.

Normal Levels:

Adult: <20 ng/ml (Male/Female)
Newborn: 100 to 300 (falls below 20 after 6 weeks)
First Trimester: <80 ng/ml
Second trimester: <160 ng/ml
Third Trimester: <400 ng/ml

*References Bakerman (1984) ABCs of Lab Data, p. 342

Anti-Prolactin Drugs

An older drug called Parlodel (bromocriptine) is enjoying new popularity for multiple uses. Though commonly prescribed for the treatment of pituitary tumors resulting in heavy prolactin secretion the drug has found itself in a newer position as a sexual stimulant. This is simply explained since the drug is a dopamine agonist with profound stimulatory effects upon the brains D-2 receptors.

The sexual side of this drugs effects coupled with the antiprolactin value is reason enough to include it in this article. Additional consideration for all athletes has been the drug's pro-GH and pro-Leptin values due to a respectable up-regulation in production of both seen in patients who have been treated with bromocriptine.

The result is leaner more muscular individuals that are obviously hornier as well. Some who have used bromocriptine suffered from nasal and sinus congestion as well as nausea and a decrease in blood pressure. Due to the 12 hour half-life for bromocriptine 2.5mg in the morning is highly effective though some have had need to progress to 2.5mg 2-3 times daily after the first two weeks of administration.

*The drug Dostinex (cabergoline) is another dopamine agonist drug employed for treatment of medical conditions that occur from an over production of prolactin and some menstrual problems. (The correct term for an anti-prolactin is antihyperprolactinemic by the way)

Over all, the sexual and anti-prolactin effects of cabergoline are similar to bromocriptine. Many who have suffered from the nausea, sinus and nasal congestion side effects of bromocriptine, report none with administration of this drug. Cabergoline has a rather long half-life and as such as little as 0.25mg once weekly has been notably effective. Some have had to increase their dosage up to 0.50mg twice weekly to maintain the result value.

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Post by Body2see on Thu Jul 13, 2017 7:48 am

Excellent post.

I don't think many people realize how significan high prolactin levels are in identifying gyno symptoms. If your levels test high, you should get on either Dos or Bromo immediately. Normal levels can be acheived quickly and quite easily.

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Post by user643598 on Thu Jul 13, 2017 8:47 am

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Post by BrotherIron on Thu Jul 13, 2017 9:29 am

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