Cabergoline

What it is and how it works

Mechanism of Action Cabergoline is an ergot derivative and dopamine receptor agonist with a high affinity for D2 receptors. Results of in vitro studies demonstrate that cabergoline exerts a direct inhibitory effect on the secretion of prolactin by rat pituitary lactotrophs. Cabergoline decreased serum prolactin levels in reserpinized rats. Receptor-binding studies indicate that cabergoline has low affinity for dopamine D1, α1- and α2-adrenergic, and 5-HT1- and 5-HT2-serotonin receptors.

Indications

Cabergoline tablets are an ergot derivative indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas in adults. Limitations of Use Avoid use of cabergoline tablets for the inhibition or suppression of postpartum physiologic lactation because of the risk of serious adverse reactions . Cabergoline tablets are an ergot derivative indicated for the treatment of hyperprolactinemic disorders, either idiopathic or due to pituitary adenomas in adults. Limitations of Use Avoid use of cabergoline tablets for the inhibition or suppression of postpartum physiologic lactation because of the risk of serious adverse reactions.

Dosage and administration (summary)

Before initiating cabergoline tablets evaluate for valvular heart disease, including with an echocardiogram. If valvular disease is detected, do not administer cabergoline tablets. Recommended starting dosage of cabergoline tablets is 0.25 mg orally twice weekly. Titrate cabergoline tablets to achieve normal serum prolactin levels by increasing cabergoline tablets by 0.25 mg orally twice weekly at intervals of no less than 4 weeks. Maximum recommended dosage is 1 mg orally, twice weekly. Recommended Evaluation Before Initiating Cabergoline Tablets Before initiating cabergoline tablets evaluate for valvular heart disease, including with an echocardiogram.

Contraindications

Cabergoline tablets are contraindicated in patients with: Uncontrolled hypertension. 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, or history of pericardial fibrosis .

Warnings and precautions

Cardiac Valvulopathy and Pericardial Fibrosis : Before initiating cabergoline tablets, perform a cardiovascular evaluation, including echocardiogram, to evaluate for valvular disease. During cabergoline tablets treatment, monitor for the development of valvulopathy with a cardiac echocardiogram at intervals of 6 to 12 months or as clinically indicated and monitor for chest pain and signs and symptoms of heart failure (if heart failure occurs, exclude valvular fibrosis and pericarditis).

Pregnancy

Pregnancy Risk Summary If conception occurs during cabergoline tablets therapy, discontinue cabergoline tablets if the risks to the mother or fetus outweigh the benefits to the mother. There are risks to the mother associated with the use of cabergoline tablets ( see Clinical Considerations ).

Storage and supply

Cabergoline Tablets, USP are white to off-white, oval shaped, flat face, beveled edge tablet with functional score on one side with the letters "IN" and the letter "G" on either side of the breakline, engraved with the number "118" on the opposite side and they are available in the following configuration: 0.5 mg strength, 8-count bottle, and NDC n…

Source: Cabergoline (Cabergoline) — US FDA prescribing information, 2025-07-04, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.