GnRH Analogues

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GnRH Analogues

Use

• suppression of ovarian steroid secretion
• reduction in size of prostate in Benign Prostatic Hyperplasia

Mechanism of Action

• (initially stimulates release of FSH/LH)
• after 2 weeks down regulates this response
• decreases pituitary stimulation of male and female gonads → medical orchidectomy/ovariectomy

Adverse effects

• Menopausal
  • hot flushes
  • increased sweating
  • vaginal dryness
  • decreased bone density
  • headaches
• skin reactions
• asthma
• amenorrhoea (70%)
• 2-4% reversible bone loss over 6 months (3%)

Drugs in class

• goserelin (Zoladex)
  • injected every 28 days
• leuprorelin
  • injected every 28 days
• buserelin
  • nasal spray TDS
• nafarelin
  • nasal spray BD
• triptorelin
  • injection every 28 days

Pharmacokinetics

• peptides so parenteral administration
• cleared by hepatic and renal excretion
• plasma half-life 80 mins to 4-5 hours

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