Cabergoline Powder CAS 81409-90-7

Cabergoline powder, also known as Dostinex (R), is a white to off white powdery substance. The melting point is between 102 and 104 ℃. It is also a dopamine receptor agonist with strong, long-lasting, and selective characteristics. It has a high affinity for D2 dopamine receptors and works by stimulating D2 dopamine receptors, thereby inhibiting the secretion of prolactin by the anterior pituitary gland and reducing prolactin levels in the blood. It is mainly used to treat disorders related to hyperprolactinemia, as well as to manage symptoms of Parkinson's syndrome. It can be used as a monotherapy for early symptom management or as an adjuvant medication for levodopa treatment in late stages of the disease.

It is insoluble in water, soluble in ethanol or chloroform, and has hygroscopicity. It should be stored at 2-8 ℃ to avoid contact with strong oxidants, strong bases, strong reducing agents, and strong acids that may cause it to deteriorate.

Cabergoline is a derivative of ergot alkaloids, which acts as a long-acting dopamine receptor agonist. Its core mechanism of action is to selectively excite dopamine D2 receptors, inhibit prolactin secretion in the anterior pituitary gland, and have a weak excitatory effect on D1 receptors.

Human medical field: multi-target therapy from endocrine to nervous system

 

1. Hyperprolactinemia and related diseases
Core indications:
Cabergoline powder is the preferred drug for treating hyperprolactinemia, especially for patients with pituitary prolactinoma. It significantly reduces serum prolactin levels by continuously stimulating D2 receptors, inhibiting prolactin secretion for up to two weeks. Clinical data shows that treatment can restore normal prolactin levels in 83% of patients and restore ovulation cycles in 72%, which is much better than the traditional drug bromocriptine (52% and 58%). For patients with prolactinoma, cabergoline not only controls hormone secretion but also reduces tumor volume and pressure on surrounding tissues.

 

Symptom relief and reproductive function recovery:
Hyperprolactinemia often leads to menstrual disorders, amenorrhea, galactorrhea, and infertility in women, while men experience decreased libido, breast development, and infertility. By reducing prolactin levels, it is possible to effectively alleviate symptoms such as breast tenderness and galactorrhea, and restore menstrual cycle and reproductive function. For example, in the study conducted at the First Hospital of Shijiazhuang City, the decrease in serum prolactin levels of patients treated with cabergoline at 1, 3, and 6 months after treatment was significantly higher than that of patients treated with bromocriptine, and the success rate of pregnancy was higher.

 

Long term health management:
Long term hyperprolactinemia may inhibit hormone secretion and lead to osteoporosis. Adjusting hormone levels can help prevent osteoporosis and improve long-term prognosis for patients. During the treatment period, regular monitoring of prolactin levels and changes in pituitary adenomas is required, usually with imaging examinations conducted every 2-3 years. Asymptomatic patients may have extended follow-up intervals.

 

2. Parkinson's disease and movement disorders
Single drug therapy and combination therapy:
Used for the treatment of Parkinson's Disease, it can be used as a monotherapy or in combination with levodopa. It enhances the dopaminergic effect of the central nervous system, reduces the dosage and fluctuation of levodopa (such as the "end of dose phenomenon" and "on/off" state). Research has shown that combined treatment with levodopa can significantly reduce the demand for levodopa by 18%, prolong the "on" state time, and improve patients' daily living ability and exercise scores.

Early intervention and advanced treatment:
Some neurologists use it for early treatment of Parkinson's disease to delay the use of levodopa;

 

Others use it as an alternative when levodopa becomes ineffective or intolerant. Its long-lasting properties (half-life of about 6 hours) and low-dose requirements (usually twice a week) improve patient compliance, making it particularly suitable for elderly patients.
Improvement of motor symptoms:
It can alleviate the core symptoms of Parkinson's disease, such as tremors, stiffness, and bradykinesia. It enhances the function of the nigrostriatal pathway and improves motor control by stimulating dopamine receptors. Clinical observations have shown that patients' exercise flexibility is significantly improved after medication, and their daily living abilities (such as dressing and eating) are improved.

 

3. Adjuvant treatment of breast cancer
Potential mechanism of action:
The activation of cabergoline on dopamine receptor may inhibit the growth of some breast cancer cells and promote their apoptosis. Although the evidence is not sufficient at present, the experimental application shows that it has a certain effect on some hormone receptor positive breast cancer patients, which may play a role by regulating prolactin related signal pathways.
Current clinical application status:
In the treatment of breast cancer, it is still in the exploratory stage, and the indications should be strictly controlled. Usually used for adjuvant therapy, it needs to be combined with other therapies (such as surgery, chemotherapy) under the guidance of professional physicians, and closely monitored for efficacy and adverse reactions.

 

4. Other potential uses
Return of milk and lactation inhibition
Can be used for milk return, but not recommended for routine use to inhibit physiological lactation. It reduces milk production by inhibiting prolactin secretion, but attention should be paid to dosage control (usually no more than 1mg per dose) to avoid excessive inhibition leading to breast atrophy or hormonal imbalance.
Mental and neural regulation
Some studies suggest that it may have an adjuvant therapeutic effect on mental and neurological disorders such as neurasthenia and anxiety disorders, but its mechanism is still unclear and needs further verification. At present, clinical applications are still mainly focused on endocrine and neurological diseases.

Animal Medicine: Reproductive Management and Termination of Pregnancy

 

1.  Dog breeding management
Inducing/synchronizing estrus:
Can be used for inducing and synchronizing estrus in dogs, promoting follicular development and ovulation by regulating the hypothalamic pituitary gonadal axis function. The typical usage is oral administration of 5 μ g/kg once a day for 4-25 days, which can significantly improve the estrus rate and facilitate centralized breeding.
Pseudopregnancy therapy:
For False Pregnancy dogs, inhibiting prolactin secretion can alleviate breast swelling, lactation, and behavioral abnormalities such as nesting and protecting offspring. The usage is oral administration of 5 μ g/kg once a day for 5-10 consecutive days. For severe symptoms, subcutaneous injection can be administered in combination with other medications.

 

2. Termination of pregnancy and abortion
Dog and cat abortion
Can be used as an abortion drug for dogs or cats, by inhibiting corpus luteum function and promoting embryonic arrest. After 30 days of mating, oral administration of 5 μ g/kg, once every 24 hours, combined with clopidogrel (5 μ g/kg, subcutaneous injection, once every 48 hours) can improve the success rate of miscarriage.
Postpartum lactation suppression
Postpartum use of cabergoline powder can inhibit breast secretion, but close monitoring of blood pressure changes is necessary to avoid the risk of hypotension. It is recommended to take medication at least 4 hours after delivery and after stable vital signs. The dosage should be adjusted according to individual needs.

What side effects?

1.Common side-effects

2.Less common side effects

• Respiratory reactions: Symptoms such as nasal congestion and difficulty breathing may occur.
• Cardiovascular system response:Orthostatic hypotension, syncope, lower limb vascular spasm, arrhythmia, worsening angina pectoris, etc. These    symptoms usually gradually disappear after discontinuing the medication.
• Skin reactions: Long term use of cabergoline may lead to skin reticular green spots and peritoneal fibrosis.
• Other reactions: erythematous limb pain, dry mouth, dizziness, chest tightness, shortness of breath, pulmonary congestion, heart valve disease  (such as shortness of breath, chest tightness, pulmonary congestion, etc.), etc. Heart valve disease is usually caused by high concentrations of  drugs in the plasma, and long-term use of higher doses of cabergoline may increase the risk of patients developing heart valve disease.   

3.Side effects of special populations

• Elderly people: Clinical observations have found that elderly people are prone to adverse reactions in the central nervous system, which should be taken seriously.
• Pregnant women: Although extensive long-term research has not found an increase in fetal teratogenicity caused by cabergoline, the medication  should generally be discontinued once pregnancy is confirmed. However, in pregnant women undergoing treatment for pituitary prolactinoma,medication can still be continued to prevent tumor enlargement during pregnancy.

4.Precautions

 

5.Toxicity

Fibrotic diseases such as pleural effusion, pulmonary fibrosis, and retroperitoneal fibrosis may occur. Patients with a history of pulmonary, pericardial, or retroperitoneal fibrosis should use caution.

Risk of fibrotic diseases:

Animal reproductive studies have revealed some evidence of maternal toxicity and loss of embryos and fetuses after implantation, but developmental abnormalities have not been consistently observed. However, it is contraindicated for pregnant and lactating women as it may have adverse effects on the fetus and infant.

Embryotoxicity:

Dopamine antagonists such as metoclopramide or phenothiazine can reduce their effectiveness and should be avoided for simultaneous use. In addition, it also has the effect of lowering blood pressure. If used together with other antihypertensive drugs, it may lead to an additive effect of lowering blood pressure.

Drug interactions:

1. Market demand growth

Parkinson's treatment needs

With the advancement of diagnostic technology for prolactinoma, the demand for drugs that can effectively control prolactin levels will continue to increase. As an effective drug for treating prolactinoma, its market demand will also grow accordingly.

Treatment needs for prolactinoma

Parkinson's disease is a chronic neurodegenerative disease for which there is currently no cure. It can improve the motor function and quality of life of Parkinson's disease patients by stimulating dopamine receptors, so its market prospects are broad.

Other indications and requirements

In addition to prolactinoma and Parkinson's disease, it is also being studied for the treatment of other diseases such as infertility and breast lesions. These new indications will further expand the market space.

2.Technological progress drives development

3. Policy support and market promotion

(1).Policy support

Governments around the world are continuously increasing their investment in healthcare and providing policy support for the research and promotion of innovative drugs. This will help innovative drugs such as cabergoline powder enter the market faster and be widely applied.

(2).Market promotion

Pharmaceutical companies will promote their products through various channels, including academic conferences, professional journals, and online advertising. This will increase its visibility and recognition, further expanding its market share.

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