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cabergoline (Dostinex)
Tradename: Dostinex.
Indications:
- treatment of hyperprolactinemia
a) idiopathic
b) secondary to pituitary adenoma
Contraindications:
1) uncontrolled hypertension
2) hypersensitivity to ergot alkaloids
Dosage:
1) start 0.25 mg twice weekly
2) increase by 0.25 mg up no more than every 4 weeks to 1 mg twice weekly
3) titrate to serum prolactin
4) when serum prolactin maintained for 6 months, discontinue & monitor serum prolactin to determine if cabergoline still needed
Tabs: 0.5 mg.
Adverse effects:
1) common (> 10%)
a) headache (26%)
b) dizziness (17%)
c) nausea (29%)
2) less common (1-10%)
- asthenia, fatigue, syncope (1%), flu-like syndrome (1%), malaise, periorbital edema, peripheral edema, hot flashes, hypotension, palpitation, vertigo, paresthesias, acne, pruritus, breast pain (2%), dysmenorrhea, constipation, abdominal pain, dyspepsia, vomiting, dry mouth, diarrhea, flatulence, throat irritation, toothache, pain, arthralgia, visual disturbances, depression, somnolence, anorexia, anxiety, insomnia, impaired concentration, nervousness, rhinitis
3) valvular heart disease
- aortic regurgitation (RR = 7.3) [3]
Drug interactions:
1) additive effects with antihypertensive medications
2) dopamine antagonists (phenothiazines, butyrophenones, thioxanthenes, metoclopramide) antagonize therapeutic effects of cabergoline
3) cabergoline can induce psychosis in patients receiving antipsychotics
Mechanism of action:
1) dopaminergic agonist
2) 5-HT2B receptor agonist
Interactions
drug interactions
drug adverse effects (more general classes)
Related
hyperprolactinemia
General
dopaminergic receptor agonist
endocrine agent
ergot alkaloid
Properties
AGONIST-FOR: adrenergic receptor
MISC-INFO: elimination route ?
pregnancy-category B
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Schade R et al,
Dopamine agonists and the risk of cardiac-valve regurgitation.
N Engl J Med 2007 Jan 4; 356:29-38
- Zanettini R et al,
Valvular heart disease during treatment with dopamine agonists
for Parkinson's disease.
N Engl J Med 2007 Jan 4; 356:39-46
PMID: 17202454
- Roth BL.
Drugs and valvular heart disease.
N Engl J Med 2007 Jan 4; 356:6-9
PMID: 17202450
- Prescriber's Letter 14(2): 2007
Drug-induced heart valve dysfunction
Detail-Document#: 230206
(subscription needed) http://www.prescribersletter.com