Cabergoline stimulates centrally-located dopaminergic receptors resulting in a number of pharmacologic effects. Five dopamine receptor types from two dopaminergic subfamilies have been identified. The dopaminergic D1 receptor subfamily consists of D1 and D5 subreceptors, which are associated with dyskinesias. The dopaminergic D2 receptor subfamily consists of D2, D3 and D4 subreceptors, which are associated with improvement of symptoms of movement disorders. Thus, agonist activity specific for D2 subfamily receptors, primarily D2 and D3 receptor subtypes, are the primary targets of dopaminergic antiparkinsonian agents. It is thought that postsynaptic D2 stimulation is primarily responsible for the antiparkinsonian effect of dopamine agonists, while presynaptic D2 stimulation confers neuroprotective effects. This semisynthetic ergot derivative exhibits potent agonist activity on dopamine D2– and D3-receptors. It also exhibits: agonist activity (in order of decreasing binding affinities) on 5-hydroxytryptamine (5-HT)2B, 5-HT2A, 5-HT1D, dopamine D4, 5-HT1A, dopamine D1, 5-HT1B and 5-HT2C receptors and antagonist activity on α2B, α2A, and α2C receptors. Parkinsonian Syndrome manifests when approximately 80% of dopaminergic activity in the nigrostriatal pathway of the brain is lost. As this striatum is involved in modulating the intensity of coordinated muscle activity (e.g. movement, balance, walking), loss of activity may result in dystonia (acute muscle contraction), Parkinsonism (including symptoms of bradykinesia, tremor, rigidity, and flattened affect), akathesia (inner restlessness), tardive dyskinesia (involuntary muscle movements usually associated with long-term loss of dopaminergic activity), and neuroleptic malignant syndrome, which manifests when complete blockage of nigrostriatal dopamine occurs. High dopaminergic activity in the mesolimbic pathway of the brain causes hallucinations and delusions; these side effects of dopamine agonists are manifestations seen in patients with schizophrenia who have overractivity in this area of the brain. The hallucinogenic side effects of dopamine agonists may also be due to 5-HT2A agonism. The tuberoinfundibular pathway of the brain originates in the hypothalamus and terminates in the pituitary gland. In this pathway, dopamine inhibits lactotrophs in anterior pituitary from secreting prolactin. Increased dopaminergic activity in the tuberoinfundibular pathway inhibits prolactin secretion.
Cabergoline in bodybuilding settings is a popular medication that is known to greatly help mitigate some specific side effects of anabolic steroids. That’s why Cabergoline in bodybuilding is used as an ancillary medication for steroids to help users lower the side effects.
Cabergoline is most commonly sold as brand Dostinex. But can be found as numerous other brands such as Caber, Cabaser, and numerous others. It is a drug that was discovered by accident back in the 1980s when scientists were experimenting with ergot alkaloids. Therefore, this is an ergot derived drug (fungi derived).
This is an orally active compound (coming as pills) which is known as a dopamine agonist known for reducing serum prolactin levels. In medicine, Cabergoline is prescribed to people to find off hyperprolactinemia – the condition of too high prolactin levels that are produced by the pituitary gland. So, it is used for all needs when high prolactin levels are the main problem.
With this being said, Cabergoline in bodybuilding is used by those athletes that are running specific anabolic steroids.
Those that are capable of increasing prolactin levels to an excess. Usually, such steroids include Trenbolone and Nandrolone compounds.
As mentioned, Cabergoline is used in those situations when prolactin levels should be reduced. So, it is given to patients suffering from tumors and cancers related to high prolactin levels. Can be given to hyperprolactinemia, Parkinson’s disease, Cushing’s disease, and other purposes.
The medication is a long lasting dopamine D2 receptor agonist. According to studies done, Cabergoline is inhibiting the release of prolactin in the pituitary gland of lactotroph cells. Because prolactin isn’t secreted from the pituitary gland – serum prolactin levels are reduced.
Prolactin is that hormone that is allowing female mammals to produce milk. Is also that hormone that is making a man lose interest in sex after ejaculation. This is because prolactin levels spike in both cases.
In bodybuilding settings, Cabergoline is actually having various uses. The most popular and widely used one is to add it during the use of Trenbolone or Nandrolone – the compounds that are known to offer the side effect of low sex drive (due to high prolactin levels).
When steroids like Nandrolone are offering the side effect of “Deca Dick” – erectile dysfunction or Trenbolone lowers sex drive – Cabergoline is often seen as the perfect solution.
But another use of Cabergoline in bodybuilding is to cause an adrenalinerush during an athletic event allowing individuals to “ignore” more pain and push muscles to the limits.
Other than that, Cabergoline has been linked with weight loss because using it, offers increased levels of dopamine allowing individuals to reduce their cravings for junk foods.
And lastly, Cabergoline has been associated with better sleep. Users may get more restful sleep allowing them to train longer and harder as well as to recover faster and better.
If Cabergoline is prescribed we highly recommend you to use it exactly as said by the doctor.
But if using it for the purpose of bodybuilding (lowering side effects of high prolactin levels caused by use of steroids) then the dosage is dependent on each individual’s responses as well as dosage and cycle length of steroids.
In case you don’t have Trenbolone or Nandrolone in your cycle, you may not need Cabergoline at all.
But if you have both compounds used in higher doses for longer cycles, you may need Cabergoline.You may need more than another person running only one of these 2 compounds in lower doses in shorter cycles.
Dosages are falling in the range of 0.25 mg up to 1 mg twice per week (from 0.5 mg up to 2 mg per week). It has a long half life so using it twice weekly is enough (every 3-4 days).
- Is recommended to start at a low dosage of 0.25 mg per dose (0.5 mg weekly) as it may be enough for many.
- 0.5 mg per dose (1 mg weekly) is what most people find to be the perfect dosage.
- For most people, 1 mg (2 mg weekly) is too much – only a few people may need such a high dosage.
As mentioned, it is recommended to use it with food before going to bed.