Hyperprolactinemic disorders, either idiopathic or due to pituitary tumors.
Long-acting dopamine agonist and prolactin inhibitor
Cabergoline is a dopamine receptor agonist. The secretion of prolactin by the anterior pituitary is mainly under hypothalamic inhibitory control, likely exerted through release of dopamine by tuberoinfundibular neurons. Cabergoline is a long acting 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 5HT1, 5HT2 serotonin receptors.
Prevention of lactation BY MOUTH Adult: 1 mg, to be taken as a single dose on the first day postpartum Suppression of established lactation BY MOUTH Adult: 250 micrograms every 12 hours for 2 days Hyperprolactinaemic disorders BY MOUTH Adult: Initially 500 micrograms once weekly, dose may be taken as a single dose or as 2 divided doses on separate days, then increased in steps of 500 micrograms every month until optimal therapeutic response reached, increase dose following monthly monitoring of serum prolactin levels; usual dose 0.25-2 mg once weekly, usually 1 mg weekly; reduce initial dose and increase more gradually if patient intolerant, doses over 1 mg weekly to be given as divided dose; maximum 4.5 mg per week Alone or as adjunct to co-beneldopa or co-careldopa in Parkinson’s disease where dopamine-receptor agonists other than ergot derivative not appropriate BY MOUTH Adult: Initially 1 mg daily, then increased in steps of 0.5-1 mg every 7-14 days, concurrent dose of levodopa may be decreased gradually while dose of cabergoline is increased; maximum 3 mg per day
Medicines to lower blood pressure Medicines used to treat mental illness (e.g. antipsychotic medicines like
chlorpromazine, haloperidol) Medicines for nausea and vomiting (e.g. domperidone, Medicines for severe migraine headaches (e.g. pergolide, metoclopramide, bromocriptine, lisuride, ergotamine, dihydroergotamine, ergometrine or methysergide)
Avoid in pre-eclampsia . cardiac valvulopathy (exclude before treatment) . history of pericardial fibrotic disorders . history of puerperal psychosis . history of pulmonary fibrotic disorders . history of retroperitoneal fibrotic disorders Acute porphyrias. cardiovascular disease . history of peptic ulcer (particularly in acromegalic patients) . history of serious mental disorders (especially psychotic disorders) . Raynaud’s syndrome
Common or very common Abdominal pain . angina . breast pain . confusion . constipation . depression . dyspepsia . epigastric pain . gastritis . hallucinations . headache . nausea . syncope Rare Digital vasospasm . epistaxis . hot flushes . muscle weakness . palpitation . paraesthesia . transient hemianopia . vomiting Frequency not known Allergic skin reactions . alopecia . cardiac valvulopathy . constrictive pericarditis . drowsiness . dyskinesia . erythromelalgia . hypersexuality . hypotension . increased libido . leg cramps . pathological gambling . pericardial effusion . peripheral oedema . pleural effusion . pleural fibrosis . pleuritis . pulmonary fibrosis . retroperitoneal fibrosis
PREGNANCY Discontinue if pregnancy occurs during treatment (specialist advice needed). BREAST FEEDING Suppresses lactation; avoid breastfeeding if lactation prevention fails.
Overdosage might be expected to produce nasal congestion, syncope or hallucinations. Measures to support blood pressure should be taken if necessary.
Store in a cool and dry place protected from light. Keep away from the reach of children.