What are the daily medications for patients with hyperprolactinemia?

Hyperprolactinemia is a very common disease that seriously affects the physical and mental health of patients, making them very distressed. Therefore, its treatment method is of concern to patients. So what are the daily medications for patients with hyperprolactinemia?

The following are the daily medications for hyperprolactinemia.

(1) Bromocriptine therapy:

Bromocriptine is a semi-synthetic ergot alkaloid derivative and a dopamine receptor agonist. Bromocriptine promotes the production and secretion of hypothalamic PRI-IH and inhibits the production of pituitary PRI by enhancing the function of dopamine receptors. Bromocriptine also directly inhibits the growth of pituitary tumors and the secretion of pituitary PRI, GH, TSH and ACTH.

Bromocriptine therapy is suitable for various types of hyperprolactinemia and is also the first choice for the treatment of pituitary adenomas. The oral dose is 2.5-5.0 mg/d. The blood concentration of bromocriptine reaches its peak 1-3 hours after oral administration, and the inhibitory effect on prolactin secretion lasts for 14 hours. After taking 2.5 mg of bromocriptine orally once, prolactin levels in about 90% of patients decrease, and prolactin levels in 1/3 of patients decrease to normal. Vaginal medication can be used for those who cannot tolerate oral administration.

The purpose of bromocriptine treatment is to suppress galactorrhea, restore menstruation, and promote ovulation and pregnancy. The average treatment time for non-tumor hyperprolactinemia is 12 months, and the average treatment time for tumor hyperprolactinemia is 47 months. Univariate and multivariate analysis found that the treatment effect was correlated with age, gender, initial dose of bromocriptine, duration of treatment, tumor size, pregnancy during treatment, and previous radiotherapy.

After bromocriptine treatment of tumor-induced hyperprolactinemia, 80% to 90% of pituitary microadenomas shrink, and 10% to 20% permanently disappear, mostly within the first few weeks of treatment. After discontinuation of bromocriptine, the tumor recurrence rate is 35%. Although there is no evidence that bromocriptine has teratogenic effects and does not affect pregnancy outcomes, treatment should be stopped if pregnancy occurs during treatment.

After 1 year of bromocriptine treatment, 11% of women with microadenomas had permanent restoration of normal prolactin and menstrual function. After 2 years of treatment, the permanent regression rate of pituitary tumors was 22%. Although high-dose bromocriptine (10 mg/d) is more effective than low-dose, the side effect rate is high and difficult to tolerate. Bromocriptine (5-12.5 mg/d) can cause 50% of pituitary macroadenomas to shrink, of which 2/3 occur within 6 weeks before treatment and 1/3 shrink after 6 months of treatment. For details on the ovulation rate, pregnancy rate, dosage and efficacy of bromocriptine treatment, please refer to the anti-prolactin section.

(2) Cabergoline:

It is a long-acting, highly effective anti-prolactin preparation with good clinical efficacy and tolerability. Cabergoline has a high affinity for dopamine receptor D2, directly inhibits pituitary prolactin-secreting cells, and reduces prolactin secretion. The therapeutic dose range is 0.25-1.0 mg/week. Start with a small dose of 0.25 mg, twice a week, and change to 1 mg after 4 weeks, twice a week. 2-3 hours after taking the medicine, the blood drug concentration reaches its peak, and the plasma half-life is 65 hours. After treatment with cabergoline, 80% of patients' prolactin levels dropped to normal, the ovulation rate was 72%, and the galactorrhea cessation rate was 90%. The drug was gradually discontinued 6 months after the plasma prolactin level returned to normal. Clinical observations have shown that cabergoline is superior to bromocriptine in efficacy and tolerability, and is the first choice, safe and effective new generation of drugs for the treatment of hyperprolactinemia.

Cabergoline can significantly reduce the size of pituitary tumors or even completely eliminate them, and can be used to treat giant pituitary adenomas that are resistant to bromocriptine. Clinical data show that although cabergoline has no adverse effects on pregnancy, once ovulation resumes during treatment, treatment should be stopped one month before the desired pregnancy.