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  Cabergoline (Dostinex)
 
Author: Donna Karasic, PharmD Last modified: March 31, 2002
 

  INDICATIONS

  • Hyperprolactinemia disorders- either idiopathic or because of pituitary adenomas; includes acromegaly, amenorrhea, prolactinomas, galactorrhea
  • Parkinson's Disease (non-FDA approved use)
  • Puerperal lactation inhibition (non-FDA approved use)
  • Normalization of Androgen Levels (non-FDA approved use)
  • Improve menstrual cyclicity in polycystic ovary syndrome (non-FDA approved use)

  DOSAGE

  • Hyperprolactinemia:0.25mg twice a week, increase by 0.25mg twice a week, at 4 week intervals, according to response. Max dose is 1 mg twice weekly.
  • Parkinson's Disease:0.5-1mg daily in the AM. Upward titration should be at weekly or longer intervals in 0.5 mg increments. Max dose is 10mg daily.
  • Puerperal Lactation Inhibition: 1 mg as a single oral dose (given within 24 to 27 hours of delivery)
  • Improve Menstrual Cyclicity in Polycystic Ovary Syndrome: 0.5mg/week

  PHARMACOKINETICS

  • Absorption: not affected by food; may be taken without regard to food
  • Moderately bound to protein (40-42%)
  • Extensively metabolized by the liver. Cytochrome P450 metabolism appears to be minimal; small amounts are excreted unchanged in urine
  • Elimination Half Life- 63-69 hours; slow elimination from pituitary may account for long duration of action

  ADVERSE EFFECTS

  • Dizziness (17%)
  • Headache (26%)
  • Weakness / fatigue (1-5%)
  • Abdominal pain (5%)
  • Orthostatic hypotension (4%)
  • Epistaxis (1%)
  • Sensation of suffocation
  • Nausea (appears to be dose related) (29%)
  • Adverse effects of Cabergoline may be less frequent than with Bromocriptine.

  CONTRAINDICATIONS

  • Hypersensitivity to ergot alkaloids
  • Uncontrolled hypertension

  DRUG INTERACTIONS

  • Antihypertensives
  • Dopamine Antagonists (eg phenothiazines, butyrophenones, thioxanthenes or metoclopramide)

  FORMS

  • 0.5mg tablets

  MECHANISM OF ACTION

  • Cabergoline is a long-acting dopaminergic agonist
  • The mechanism of action of cabergoline in lowering serum prolactin is similar to that of bromocriptine
  • Cabergoline stimulates hypothalamic dopaminergic receptors resulting in an increase in prolactin inhibitor factor, decreasing secretion of prolactin from the anterior pituitary
 
IMPORTANT POINTS/RECOMMENDATIONS
  • Use with caution in patients with liver, renal or cardiovascular disease
  • Use with caution in patients with psychiatric disorders
  • Avoid high initial doses (1 gm), especially with concurrent antihypertensive regimens
 
REFERENCES
  1. Hutchison TA & Shahan DR (Eds): ;  Cabergoline ;  MICROMEDEX┬« Healthcare Series: MICROMEDEX, Greenwood Village, Colorado (Edition expires 3-2002)

  2. Hebel SK, Kastrup EK (Eds) ;  Cabergoline ;  Facts and Comparisons, St. Louis, MO (updated 2002)

Copyright © 2002 The Johns Hopkins University School of Medicine. All rights reserved.