Medicine & USMLE

Progestins

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Reproductive Pharm
  1. Leuprolide
  2. Anastrozole
  3. Estrogens
  4. Clomiphene
  5. Progestins
  6. Mifepristone
  7. Copper IUDs
  8. Danazol
  9. Terbutaline, Ritodrine
  10. Minoxidil
  11. Androgens (Testosterone, Methyltestosterone)
  12. Flutamide
  13. PDE-5 Inhibitors (Sildenafil, Vardenafil, Tadalafil)
  14. Finasteride

Summary

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Key Points

  • Progestins
    • Medications
      • Levonorgestrel
        • Found in OCPs and IUDs
      • Medroxyprogesterone
        • Found in OCPs or depot injections
      • Norethindrone
        • Found in OCPs
      • Etonogestrel
        • found in vaginal rings and implants
      • Megestrol
    • Mechanism
      • Synthetic progesterone agonists
        • Binds progesterone receptors on the uterus and hypothalamus
    • Indications
      • Contraception
        • Anovulation
          • in oral contraceptives/patch/depot injections
          • Synthetic progestins act on the hypothalamus to induce negative feedback→ decreased GnRH → decreased LH/FSH → decreased LH surge → no ovulation
        • Thickens cervical mucus
          • in IUDs/progestin-only pills
          • Limits the sperm access to ova
        • Thinning of uterine lining
          • All progesterones therefore impair embryo implantation
          • This is a minor effect in comparison to the above
      • Reduces growth of endometrial tissue
      • Used in the treatment of endometrial hyperplasia/cancer and endometriosis
        • Increases endometrial vascularity and shedding for menses
        • Counteracts endometrial growth/hyperplasia induced by estrogens in combined OCPs
      • Progestin challenge for abnormal uterine bleeding
        • presence of withdrawal bleeding excludes anatomic defects (i.e. Asherman syndrome) and chronic anovulation without estrogen
    • Adverse Effects
      • PE/DVT and other hypercoagulable events seen in combined progestin/estrogen OCPs
        • Due to estrogen, not progesterone in formulation; Used alone, progestins have NOT been associated with thromboembolic events.
      • Decreased bone density (osteoporosis)