Cabergoline 0.5mg is a dopamine agonist used to lower elevated prolactin levels and support the treatment of hyperprolactinemia and certain prolactin producing pituitary conditions. Each pack contains 8 tablets.
Format8 Tablets
Concentration0.5mg
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Cabergoline is a potent, long acting ergot derived dopamine receptor agonist used primarily for the treatment of disorders associated with abnormally elevated prolactin levels. It demonstrates high affinity for dopamine D2 receptors, which play a central role in regulating prolactin secretion from the anterior pituitary gland.
Under normal physiological conditions, dopamine produced by the hypothalamus acts as the primary inhibitory regulator of prolactin secretion. Cabergoline mimics this dopaminergic activity by stimulating D2 receptors on pituitary lactotroph cells, directly suppressing the release of prolactin and lowering circulating serum prolactin concentrations.
Cabergoline is indicated for the treatment of hyperprolactinemic disorders, including cases that are idiopathic or associated with prolactin secreting pituitary adenomas. Excess prolactin can interfere with normal reproductive hormone signaling and may be associated with menstrual disturbances, galactorrhea, reduced fertility and other endocrine symptoms depending on the patient.
Its relatively prolonged pharmacological activity allows cabergoline to maintain prolactin suppression for an extended period compared with shorter acting dopamine agonists. Clinical studies included in current prescribing information demonstrate that cabergoline can normalize serum prolactin and, in patients with hyperprolactinemic amenorrhea, may contribute to restoration of menstruation and resolution of galactorrhea.
Each tablet contains 0.5mg of cabergoline, with this product supplied as a pack of 8 oral tablets. Cabergoline 0.5mg products are also listed within Health Canada’s Drug Product Database.
Cabergoline has important cardiovascular and neurological safety considerations. Current prescribing information recommends evaluation for valvular heart disease before treatment and ongoing monitoring where appropriate because cabergoline has been associated with cardiac valvopathy and fibrotic disorders. Orthostatic hypotension can also occur, particularly when combined with other medications that lower blood pressure.
Dopamine agonists can additionally produce changes in impulse control in some patients, including increased gambling, spending or sexual urges. Commonly reported adverse effects include nausea, headache and dizziness. Cabergoline should therefore be used under the supervision of a qualified healthcare professional, with treatment and monitoring based on serum prolactin levels and the underlying medical condition.
Cabergoline is a prescription dopamine receptor agonist belonging to the ergot derived medication class. It has high affinity for dopamine D2 receptors and is primarily used to reduce excessive prolactin secretion from the pituitary gland. Each tablet contains 0.5mg of cabergoline, with 8 tablets supplied per package for 4mg total.
Cabergoline is approved for the treatment of hyperprolactinemic disorders in adults, including elevated prolactin levels that are idiopathic or caused by pituitary adenomas such as prolactinomas. By lowering prolactin concentrations, treatment can address endocrine and reproductive effects associated with excessive prolactin secretion.
Cabergoline acts primarily as an agonist at dopamine D2 receptors. Activation of D2 receptors on pituitary lactotroph cells directly inhibits prolactin secretion, producing a sustained reduction in circulating prolactin concentrations. Its long elimination half-life allows the prolactin lowering effect to persist substantially longer than the plasma exposure of many shorter acting dopamine agonists.
Cabergoline has an elimination half-life of approximately 63 to 69 hours, which contributes to prolonged dopamine receptor activity and sustained suppression of prolactin. It is extensively metabolized, while its long pharmacokinetic profile allows therapeutic effects to continue for several days after administration.
Cabergoline has important cardiovascular and fibrotic safety considerations. Current prescribing information recommends evaluation for valvular heart disease, including echocardiography, before treatment and periodic monitoring during therapy. Cabergoline is contraindicated in patients with certain valvular, pericardial, pulmonary, pleural, or retroperitoneal fibrotic disorders and uncontrolled hypertension. It can also cause orthostatic hypotension and, in some patients, impulse control or compulsive behaviors.
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