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D1 dopamine receptor antagonist
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Bromocriptine mesylate (Bromo for short). It is an ergot derivative with D2 dopamine receptor agonist and D1 dopamine receptor antagonist activities. In medicine, it is a versatile drug with many uses thanks to its dopamine increasing effects. In bodybuilding, it's used for its ability to inhibit prolactin, and during calorie restricted dieting.
Bromocriptine was first used in the 1970's for treatment of Parkinson's, and to suppress HGH when high dosages were used. Since the late 80's its been used off label for cocaine withdrawal; in addition, in 2009, it was approved by the FDA for treatment of type 2 diabetes for its effect at improving glycemic control. Many of its uses involve how bromo is related to dopamine increasing effects.
How it Works
Bromocriptine mesylate is a dopamine agonist. It activates dopamine receptors in the absence of that receptor's physiological ligand, the neurotransmitter dopamine. Essentially, it will forcefully increase dopamine in the body.
Understanding Dopamine
Dopamine is a hormone and neurotransmitter, which plays an important role in the human brain and body. With the brain, dopamine functions as a neurotransmitter: a chemical released by nerve cells to send signals to other nerve cells. When a person is addicted to drugs, dopamine levels will be increased.
Parkinson's disease involves a dysfunction of the dopamine system, which will result in tremors and motion impairment. There is also evidence that schizophrenia involves altered levels of dopamine activity. Furthermore, ADHD and restless legs syndrome are believed to be associated with decreased dopamine activity.
Bodybuilding
There are a couple ways Bromocriptine is used in bodybuilding.
Prolactin inhibition: Whenever a progestin based compound is used (trenbolone and nandrolone decanoate), prolactin levels will rise. Using bromocriptine to bring down prolactin levels will keep prolactin based gynecomastia away and also keep libido strong.
Calorie restricted dieting: When a bodybuilder cuts calories, leptin levels will drop and the body will respond by holding onto nutrient stores. It is believed that bromocriptine will help normalize the slowing metabolism during this time, and it will help maintain normal leptin stimulation. This phenomenon is connected to its dopamine effects.
Prolactin
Prolactin is a hormone protein that plays the role of enabling females mammals to produce milk. It is not fully understood why males have prolactin, but we do know that it provides sexual gratification after ejaculation. After ejaculation, the male loses interest in sex, this is called the sexual refractory period, where prolactin levels go up. Therefore, lower prolactin levels should decrease the refractory period. In general, high prolactin levels can cause impotence and loss of interest in sex (low libido).
Side Effects
There is no shortage of possible side effects with Bromo, and many bodybuilders have avoided this drug for that reason.
Nausea is one of the most common side effects and is usually the first thing noticed. Guys will feel terrible when using bromocriptine, sick like they want to throw up. Low blood pressure, dizziness and confusion can also occur. There are a host of less likely sides including: anxiety, dry mouth, fatigue, headache, and lethargy.
Dosage
The normal starting dose in bodybuilding is 2.5 to 5mg, either split during the day or everyday. If side effects become too great then cutting the dose in half can be effective.
Bromocriptine vs. Cabergoline vs. Pramipexole and Half Life
Bromo was very popular in the bodybuilding world until recently, and there are several reasons why it lost popularity. The side effects tend to be higher versus other dopamine drugs like cabergoline and pramipexole. Also, the half life is only 12 hours vs. cabergoline which has a 3-4 days half life. This means you must take it at least everyday, while cabergoline can be taken once every 3 days.
Sandoz is a division of the Novartis Group and a global leader in generic pharmaceuticals and biosimilars. The division was established in 2003,
when Novartis united all of its generics businesses under the name Sandoz – a single global brand with a long history.
Since then, Sandoz has grown into a leading global generics business with annual sales in excess of USD 10 billion.
The Sandoz brand is a seal of quality, and healthcare professionals around the world trust it as a symbol of high-quality,
affordable medications. It can trace its origins to a small chemical company that came into being in Basel, Switzerland, in 1886. Kern & Sandoz, as the company was initially called, focused on the production of dyes. However, within a decade it produced its first pharmaceutical substance, antipyrine, a fever-controlling agent.
By 1917, the company had established its first pharmaceutical department and, in 1929,
Calcium Sandoz was introduced, laying the foundation for modern calcium therapy.
Calcium Sandoz went on to establish itself as one of the company’s best known products and is still well represented in today’s Sandoz portfolio.
Sandoz’ globally leading anti-infectives and biosimilars businesses can trace their origins back to the work done at Biochemie in the 1940s and 1950
In 1939, Kern & Sandoz became Sandoz Ltd., a name it operated under for nearly sixty years. Meanwhile, across the border in 1946 post-war Austria, a company called Biochemie was founded in order to produce and supply scarce, urgently needed penicillin for the nation’s populace. It would be two researchers from Biochemie who in 1951 discovered acid-resistant penicillin, which meant that for the first time, penicillin could be administered orally. The discovery drove the further development and rapid growth of the company. In 1963, Sandoz acquired Biochemie GmbH, representing the beginning of large-scale production of antibiotics and substances developed on the basis of biotechnology. The Sandoz portfolio today continues to be spearheaded by its leading global positions in biosimilars and generic antibiotics respectively.
Sandoz currently is the world’s second largest producer of antibiotics.
Over the course of the 20th century, the Sandoz brand grew consistently and came to enjoy international recognition. In 1996, the merger of Sandoz and Ciba-Geigy led to the creation of Novartis. The Sandoz brand became dormant for a few years, but did not lose its name recognition, and in 2003, when Novartis united its global generics businesses under a single global brand, the name Sandoz was reestablished.
From its roots in 19th century Basel, the Sandoz brand has been transformed into a global leader in generic pharmaceuticals and biosimilars. Today, as a division of the Novartis Group, we offer approximately 1,000 molecules covering a broad range of therapeutic areas. In 2015, our products reached more than 500 million patients and we aspire to reach one billion.
