The main side effects of Nandrolone class steroids (including Trenbolone) are associated with an increase in prolactin levels. Prolactin has the most negative effect on men when it rises in the brain. By binding to the progestin receptors of the pituitary gland, nandrolones increase the production of prolactin and suppress the secretion of gonadotropic hormones.
Suppressed libido, depressive mood, low self-esteem, and increased hysteric emotionality are just a few of the prolactin’s negative effects.
Prolactin is in many ways similar to estrogens, its effect is manifested by a decrease in the production of one's own testosterone, a slight increase in fat mass, and, in rare cases, gynecomastia, from which neither Tamoxifen nor Clomid helps.
For this, prolactin inhibitors are used: bromocriptine (an outdated drug with pronounced side effects) or a more modern and safer one – cabergoline.
And now, the highest quality Cabergoline is available under the Driada brand!
Mechanism of action (the boring part)
Cabergoline is a selective dopamine receptor agonist. This drug is highly specific in its actions, with a strong affinity for the dopamine D2 receptor, and a low affinity for dopamine Dl, A 1-adrenergic, A2-adrenergic, 5-HT1- serotonin, and 5-HT2-serotonin receptors. Its main clinical use is for the treatment of hyperprolactinemia, or the hypersecretion of prolactin from lactotropes in the anterior pituitary (pituitary tumor is a common cause of this disorder). It is also applied in the management of Parkinson's disease. Cabergoline effectively inhibits prolactin secretion, which it does by mimicking the actions of dopamine on the D2 receptor (dopamine normally serves as negative feedback for prolactin release). As a targeted agonist of the dopamine D2 receptor, cabergoline should not affect other pituitary hormones like growth hormone (GH), luteinizing hormone (LH), corticotrophin (ACTH), or thyroid-stimulating hormone (TSH).
In addition, interaction with other receptors was established: D3, D4, 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, α2B.
Administration:
During the cycle of progestin anabolic steroids (nandrolone, trenbolone) take 0.25 mg every 7-21 days. The optimal dose and frequency of administration is selected under the control of blood tests of the prolactin, since the effect of the drug is different and depends on the individual characteristics of the body. In clinical medicine, this drug may be taken for 6 months or longer
When used by athletes/bodybuilders to inhibit prolactin secretion (as with lactating gynecomastia), doses on the lower end of the therapeutic range are most commonly used. although athletes/bodybuilders usually find a 4-6 week course of therapy (combined with an intelligent rearrangement of the offending drugs) most appropriate.
When used medically to inhibit prolactin secretion, cabergoline is given in an initial dosage of 500mcg per week. This may be taken in one single dose or divided into 2 or more doses on separate days.
With an increase in the level of prolactin above the permissible frequency of administration increases: 0.25 mg, every 4 days. It is advisable to perform a control analysis of prolactin after two doses, followed by a correction of the scheme.
The drug is taken both with food and on an empty stomach.
EFFECTS:
Since the drug is a d-2 dopamine receptor agonist, it has a number of interesting and side effects that would not be correct to call side effects:
One of the effects caused by a decrease in prolactin concentration is a decrease in fluid retention in tissues, which leads to an increase in lean muscle mass
Reduces the subjective need for sleep
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.
The systemic use of cabergoline has been shown to increase glial cell-derived neurotrophic factor (GDNF) expression. GDNF is a small protein that potently promotes the survival of many types of neurons, instructions for making a protein found in the brain and spinal cord called brain-derived neurotrophic factor. This protein promotes the survival of nerve cells (neurons) by playing a role in the growth, maturation (differentiation), and maintenance of these cells.[1]
Also there is a list of positive sexual effects( the interesting part):
Effects on libido and sexual performance:
Antagonism with α2B receptors additionally explains the positive effect on erectile function (there is an expansion of the cavernous bodies).
Cabergoline significantly increases sexual desire both during the cycle and on PCT, enhances orgasm, and reduces recovery time between sexual acts. And in a case of combining it with Viagron you will feel like a teen
It is used off-label as a drug for the treatment of antidepressant-related impotence, as well as sexual performance anxiety.
Pharmacodynamics:
The elimination half-life of cabergoline estimated from urinary data of 12 healthy subjects ranged between 63 to 69 hours. The prolonged prolactin-lowering effect of cabergoline may be related to its slow elimination and long half-life.
After oral dosing of radioactive cabergoline to five healthy volunteers, approximately 22% and 60% of the dose was excreted within 20 days in the urine and feces, respectively. Less than 4% of the dose was excreted unchanged in the urine.
Warnings:
• Uncontrolled hypertension or known hypersensitivity to ergot derivatives.
• History of cardiac valvular disorders, as suggested by anatomical evidence of valvulopathy of any valve, determined by pre-treatment evaluation including echocardiographic demonstration of valve leaflet thickening, valve restriction, or mixed valve restriction-stenosis.
• History of pulmonary, pericardial, or retroperitoneal fibrotic disorders.
High dopaminergic activity in the mesolimbic pathway of the brain in a case of overdose may cause hallucinations and delusions, nasal congestion, and syncope.
[1] Cabergoline Decreases Alcohol Drinking and Seeking Behaviors Via Glial Cell Line-Derived Neurotrophic Factor