Cabergoline
Indications
Cabergoline is used for:
Hyperprolactinemia, prolactinomas, parkinson's disease, uterine fibroids, acromegaly, cushing's disease, pituitary adenomas, lactation suppression
Adult Dose
Oral
Inhibition of physiological lactation
Adult: 1 mg as a single dose on the 1st day postpartum.
Suppression of lactation
Adult: 250 mcg every 12 hr for 2 days.
Hyperprolactinaemia-associated disorders
Adult: Initially, 500 mcg/wk then increased at mthly intervals by 500 mcg/wk according to response. Wkly dose may be admin on a single occasion or in 2 divided doses on separate days; doses >1 mg should be given as divided doses. Usual dose: 1 mg (up to 4.5 mg)/wk.
As monotherapy in Parkinson's disease; Adjunct to levodopa treatment in Parkinson's disease
Adult: Initially, 0.5 mg daily in monotherapy and 1 mg daily as adjunct, may increase in increments of 0.5-1 mg at 7- or 14-day intervals. Max: 3 mg daily.
Elderly: Start with lower doses.
Hepatic impairment: Dosage adjustments may be needed.
Child Dose
Renal Dose
Administration
Should be taken with food.
Contra Indications
Hypersensitivity to ergot derivatives. Uncontrolled hypertension.
Precautions
CV disease, Raynaud's syndrome, renal or hepatic impairment, peptic ulcer, GI bleeding, history of psychosis, hypertension. May affect ability to drive or operate machinery. Pregnancy, lactation. Prolonged use and/or usage of high doses may lead to psychiatric disorders, pleural/retroperitoneal fibrosis or cardiac valvular fibrosis. Monitor serum prolactin level mthly until normalisation. Monitor hepatic function regularly in patients with hepatic impairment.
Lactation: excretion in milk unknown; use with caution
Pregnancy-Lactation
Interactions
Increased risk of orthostatic hypotension when used with antihypertensives. May increase vasoconstriction effect of dopamine. May reduce vasodilation effect of nitroglycerin. Concurrent use with SSRIs or TCAs may increase the risk of serotonin syndrome.
Potentially Fatal: Risk of serotonin syndrome with sibutramine.
Adverse Effects
Side effects of Cabergoline :
>10%
Nausea (27%),Headache (26%),Dizziness (15%),Constipation (10%)
1-10%
Asthenia (9%),Fatigue (7%),Abdominal pain (5%),Somnolence (5%),Postural hypotension (4%),Depression (3%),Dyspepsia (2%),Nervousness (2%),Abnormal vision (1%),Breast pain (1%),Dysmenorrhea (1%),Hot flashes (1%),Paresthesia (1%)
Potentially Fatal: Risk of serotinin syndrome with sibutramine; avoid combination.
Mechanism of Action
Cabergoline is a long-acting dopamine D2-agonist. It inhibits prolactin secretion through hypothalamic inhibitory control exerted through the release of dopamine.