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  Bromocriptine (Parlodel)
 
Author: Donna Karasic, PharmD Last modified: March 31, 2002
 

  INDICATIONS

  • Prolactinomas
  • Hypogonadism
  • Infertility (male and female)
  • Amenorrhea with or without galactorrhea
  • Acromegaly
  • Parkinson's Disease
  • Non-FDA approved uses include: neuroleptic malignant syndrome, premenstrual symptoms, Cushing's disease, chronic hepatic encephalopathy

  DOSAGE

  • Prolactinomas-1.25mg to 2.5mg/day adding additional 2.5mg as tolerated every 3-7 days until optimal response is achieved. Usual dosage ranges from 2.5mg to 15mg/day.
  • Hypogonadism-1.25mg to 2.5mg/day adding additional 2.5mg as tolerated every 3-7 days until optimal response is achieved. Usual dosage ranges from 2.5mg to 15mg/day.
  • Infertility-1.25mg to 2.5mg/day adding additional 2.5mg as tolerated every 3-7 days until optimal response is achieved. Usual dosage ranges from 2.5mg to 15mg/day.
  • Amenorrhea with or without galactorrhea- 1.25mg to 2.5mg/day adding additional 2.5mg as tolerated every 3-7 days until optimal response is achieved. Usual dosage ranges from 2.5mg to 15mg/day.
  • Acromegaly- 1.25mg-2.5mg/day for 3 days adding additional 1.25mg to 2.5mg as tolerated every 3-7 days until patient obtains optimal benefit. Usual dosage ranges from 20-30mg/day.
  • Parkinson's Disease-1.25 mg twice daily with assessments at 2-week intervals. Increase dose by 2.5 mg daily every 14 to 28 days.

  PHARMACOKINETICS

  • Onset - Prolactin level decrease: 1 wk, amenorrhea/ ovulation 6-8wks, galactorrhea subsides 8-12 wks, menses and/or pregnancy 12-24 wks.
  • Absorption from the GI tract is 28%.
  • Metabolized extensively by the liver; excreted primarily in the feces with 2.5-5% excreted in urine.
  • Elimination Half-life: initial phase 4-5 hours and terminal phase 50 hours
  • Protein binding 90-96% serum albumin

  ADVERSE EFFECTS

  • Postural / orthostatic hypotension (6%)
  • Drowsiness / tiredness (3%)
  • Nausea (18%)
  • Constipation (14%)
  • Peripheral Vasoconstriction / Vasospasm (2%)
  • Headache (<2%)

  CONTRAINDICATIONS

  • Sensitivity to Ergot Alkaloids
  • Severe Ischemic Heart Disease or Peripheral Vascular Disease
  • Pregnancy

  DRUG INTERACTIONS

  • Cyclosporin
  • Tacrolimus (FK506)
  • Amitriptyline
  • Phenothiazines
  • Erythromycin/ Clarithromycin
  • Ethanol
  • Ergot Alkaloids

  FORMS

  • 2.5mg tablets
  • 5mg capsules

  MECHANISM OF ACTION

  • Bromocriptine is an ergot derivative and a direct-acting dopamine agonist
  • Bromocriptine stimulates hypothalamic dopaminergic receptors; this results in an increase in prolactin inhibitor factor, decreasing secretion of prolactin from the anterior pituitary
  • Bromocriptine decreases growth hormone production
 
IMPORTANT POINTS/RECOMMENDATIONS
  • Take with food.
  • Additive hypotensive effects may occur in patients receiving antihypertensives; careful adjustment of antihypertensive meds may be necessary.
  • Higher dosages may result in reduced alcohol tolerance; patients should be cautioned to limit alchol intake while on this medication.
  • Blood pressure should be monitored for all patients receiving this drug especially during first few days of therapy.
  • Bromocriptine may impair ability to perform activities requiring mental alertness or physical coordination.
  • Use with caution in patients with impaired liver or renal function.
  • Use with caution in patients with history of myocardial infarction, arrhythmias.

more...

 
REFERENCES
  1. Hutchison TA & Shahan DR (Eds): ;  Bromocriptine ;  MICROMEDEX┬« Healthcare Series: MICROMEDEX, Greenwood Village, Colorado (Edition expires 3-2002)

  2. McEvoy, Gerald K. (Ed) ;  Bromocriptine Mesylate ;  American Hospital Formulary Service 2001, Bethesda, MD

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