Cabergoline

Indications
Oral
Inhibition of physiological lactation
Adult: 1 mg as a single dose on the 1st day postpartum.
Hepatic impairment: Dosage adjustments may be needed.
Oral
Suppression of lactation
Adult: 250 mcg every 12 hr for 2 days.
Hepatic impairment: Dosage adjustments may be needed.
Oral
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.
Hepatic impairment: Dosage adjustments may be needed.
Oral
As monotherapy 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.
Oral
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.
Contraindications
Hypersensitivity to ergot derivatives. Uncontrolled hypertension.
Warnings / 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.
Adverse Reactions
Decrease in BP, dizziness, vertigo, headache, nausea, sleeplessness, abdominal pain, dyspepsia, gastritis, weakness, fatigue, constipation, vomiting, breast pain, hot flushes, depression, tingling, leg cramps, Raynaud's syndrome, psychosis with hallucinations, delusions and confusion.
Potentially Fatal: Risk of serotinin syndrome with sibutramine; avoid combination.
Overdose Reactions
Symptoms may include nasal congestion, syncope or hallucinations. Measures to support BP should be taken if necessary.
Drug 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.
See Below for More cabergoline Drug Interactions
Mechanism of Actions
Cabergoline is a long-acting dopamine D2-agonist. It inhibits prolactin secretion through hypothalamic inhibitory control exerted through the release of dopamine.
Absorption: Absorbed from the GI tract. Undergoes 1st pass effect.
Distribution: Plasma protein binding: about 40%.
Metabolism: Extensively metabolised to inactive metabolites.
Excretion: Mainly via faeces.
Administration
Should be taken with food.
Storage Conditions
Oral: Store at 20-25°C.
ATC Classification
G02CB03 - cabergoline ; Belongs to the class of prolactine inhibitors. Used to suppress lactation.
N04BC06 - cabergoline ; Belongs to the class of dopamine agonist. Used in the management of Parkinson's disease.
Storage
Oral: Store at 20-25°C.
Available As
  • Cabergoline 0.25 mg
  • Cabergoline 0.5 mg
  • Cabergoline 1 mg
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