Conventional medications for hyperprolactinemia

Hyperprolactinemia (HPRL) is a common reproductive endocrine disease in women, with clinical manifestations mainly including menstrual disorders, infertility, galactorrhea, tumor compression symptoms and sexual function changes. Drug therapy is the main treatment for HPRL, so how to use drugs correctly is crucial to the treatment of HPRL.

Dopamine receptor agonists are the first choice for the treatment of hyperprolactinemia and pituitary prolactinoma. Commonly used therapeutic drugs include the following:

1. Bromocriptine mesylate

① Principle of action: It is a polypeptide ergot alkaloid that selectively stimulates dopamine receptors, can effectively reduce prolactin levels, and can also inhibit the proliferation of prolactinoma cells, thereby shrinking the tumor.

② Usage: To reduce the adverse reactions of patients, a small dose is generally used at the beginning, initially 1.25 mg/d orally, and 1.25 mg/d is increased every 3-7 days until it reaches an effective dose of 5.0-7.5 mg/d. Individual sensitivity to bromocriptine is closely related to the efficacy, and the therapeutic effect is not necessarily positively correlated with the dose of bromocriptine. After taking bromocriptine for 1 month continuously, the blood prolactin level should be rechecked to help guide the adjustment of the drug dosage.

③Adverse reactions: mainly nausea, vomiting, headache, dizziness, constipation, fatigue, drowsiness and orthostatic hypotension. The symptoms will disappear on their own after a few days of medication.

2. Alpha-dihydroergocryptine mesylate

① Principle of action: It is a highly selective dopamine D2 receptor agonist and α-adrenergic antagonist.

②Usage: The efficacy is equivalent to that of bromocriptine. The initial dose is 5 mg/bid. Increase the dose after 1-2 weeks. Pay attention to monitor the serum prolactin level while using it. Adjust to the optimal dose (20-40 mg/d) for maintenance based on the changes in the blood prolactin level.

③Adverse reactions: Occasionally, there are nausea, vomiting, constipation, dizziness, orthostatic hypotension, headache and tachycardia. The discomfort symptoms usually appear in the early stage of medication, are transient, and disappear immediately. The drug is well tolerated for long-term use.

3. Cabergoline

① Mechanism of action: Cabergoline has a high affinity for dopamine D2 receptors and a long duration of efficacy. It directly inhibits prolactin secretion from the pituitary gland. Compared with bromocriptine, it has higher D2 specificity, longer duration of effect, and a lower tendency to cause vomiting.

②Usage: The usual dose is 0.5-2.0 mg, 1-2 times a week.

③Adverse reactions: The side effects are fewer than those of bromocriptine, and symptoms such as nausea and vomiting rarely occur.

4. Quinagolide

① Principle of action: It is a selective dopamine D2 receptor stimulant that has a strong inhibitory effect on the secretion of the anterior pituitary hormone prolactin, but does not reduce the normal levels of other pituitary hormones.

②Usage: 25μg per day for 3 consecutive days, then increase by 25μg every 3 days until the best effect is achieved. The usual maintenance dose is 75-150μg.

④Adverse reactions: nausea, vomiting, headache, drowsiness and fatigue, etc. These adverse reactions often occur at the beginning of medication or in a short period of time after increasing the dosage.

5. Vitamin B6

① Principle of action: Vitamin B6 acts as a coenzyme in the conversion of hypothalamic L-dopa into dopamine, promoting the production of dopamine, increasing the central inhibition of PRL, and reducing PRL secretion.

②Usage: 20-30mg/tid, oral.