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Cabergoline
Cabergoline (Dostinex)
Cabergoline
(cah-BER-goh-leen)
Pregnancy Category: B Dostinex (Rx)

Classification: Drug to treat hyperprolactinemia

Action/Kinetics: Synthetic ergot derivative that is a dopamine receptor agonist at D₂ receptors. Secretion of prolactin occurs through the release of dopamine from tuberofundibular neurons. Inhibits basal and metoclopramide-induced prolactin secretion. Peak plasma levels: 2-3 hr. Significant first-pass effect. Extensively metabolized in the liver and excreted in both the urine and feces. t1/2, elimination: 63-69 hr.

Uses: Treatment of hyperprolactinemia, either idiopathic or due to pituitary adenomas. Investigational: Shrink tumors in clients with microprolactinoma or macroprolactinoma. Parkinson's disease. Normalize androgen levels and improve menstrual cyclicity in polycystic ovary syndrome.

Contraindications: Uncontrolled hypertension or in pregnancy-induced hypertension (i.e., preeclampsia, eclampsia). Hypersensitivity to ergot alkaloids. Lactation. Not to be used to inhibit or suppress physiologic lactation.

Special Concerns: Use with caution in those with impaired hepatic function or with other drugs that lower BP. Safety and efficacy have not been determined in children.

Side Effects: GI: N&V;, constipation, abdominal pain, dyspepsia, dry mouth, diarrhea, flatulence, throat irritation, toothache, anorexia, weight loss or gain. CNS: Headache, dizziness, somnolence, vertigo, paresthesia, depression, nervousness, anxiety, insomnia. CV: Postural hypotension, hypotension, palpitations. GU: Breast pain, dysmenorrhea, increased libido. Body as a whole: Asthenia, fatigue, syncope, flu-like symptoms, malaise, periorbital edema, peripheral edema, hot flashes. Miscellaneous: Nasal stuffiness, abnormal vision, acne, epistaxis, pruritus.

Overdose Management: Symptoms: Nasal congestion, syncope, hallucinations. Treatment: Support BP, if necessary.

Drug Interactions: Antihypertensive drugs / Additive hypotension Butyrophenones / Effects of cabergoline Metoclopramide / &arrowdn;: Effects of cabergoline Phenothiazines / &arrowdn;: Effects of cabergoline Thioxanthenes / &arrowdn;: Effects of cabergoline

How Supplied: Tablets: 0.5 mg.

Dosage
•Tablets Hyperprolactinemia.
Adults, initial: 0.5 mg twice a week. Dose may be increased by 0.25 mg twice weekly to less than or equal to 1 mg twice a week, depending on the serum prolactin level. Do not increase dose more often than every 4 weeks.
Parkinson's disease.
Adults: 7.5 mg/day.
Improve menstrual cyclicity in polycystic ovary syndrome.
Adults: 0.5 mg/week.