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Basic Sciences & Clinical Skills (NUCOG 1) » Notes
Pharmacology - GnRH & Anti-androgens
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GnRH ANALOGUES

  • GnRH is a decapeptide which is released in short pulses from the hypothalamus, stimulating pituitary FSH / LH production
  • Continuous administration causes down-regulation of pituitary receptors, inhibiting FSH / LH production and therefore ovarian / testicular activity and inducing a menopausal state in women
  • Associated with risk of osteoporosis with long-term use therefore use restricted to 6 months


Clinical use

  • Pituitary desensitization prior to induction of ovulation with gonadotrophins.
  • Used to treat endometriosis, fibroids and prepare the endometrium prior to hysteroscopic surgery
  • Administered by intramuscular / sub dermal injection and as nasal spray
  • Contraindicated in osteoporosis, pregnancy, breastfeeding


ANTI-ANDROGENS

Clinical use

  • Treatment of androgenic symptoms in women with polycystic ovary syndrome (PCOS) especially hirsutism
  • Anti-androgens may emasculate a male fetus therefore women must be informed of this risk and use effective contraception while on treatment

Cyproterone acetate

  • Progestogenic anti-androgen
  • Used in combination with ethinyloestradiol as a combined oral contraceptive to treat acne and hirsutism especially in women with Polycystic Ovary Syndrome (PCOS)
  • Inhibits spermatogenesis (but is not a male contraceptive) & libido and reduces sebum production


Spironolactone

  • Aldosterone antagonist with anti-androgenic effects
  • Used to treat hirsutism in women with PCOS


Finasteride

  • 5-alpha reductase inhibitor
  • Prevents the conversion of testosterone to the active metabolite dihydrotestosterone


Flutamide

  • Androgen antagonist
  • Used to treat hirsutism in PCOS


Cimetidine

  • Displaces testosterone from its receptor
  • Used to treat hirsutism in PCOS
     
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