Dienogest is used for the medical treatment of endometriosis. Compared to progestins used in contraception, dienogest has unique pharmacological properties. Which of the following best describes dienogest's pharmacological profile?
- A Dienogest is a 19-norprogestin with high progestogenic activity, antiandrogenic properties, and no glucocorticoid or mineralocorticoid activity; it achieves localized endometrial atrophy while partially suppressing estradiol ✓
- B Dienogest is a 17-alpha-hydroxyprogesterone derivative with strong androgenic and glucocorticoid activity
- C Dienogest inhibits GnRH secretion centrally, causing complete hypoestrogenism similar to GnRH agonists
- D Dienogest acts primarily by inhibiting aromatase in endometriotic implants
Explanation
Dienogest is a 19-nortestosterone-derived progestin specifically developed for endometriosis. Its pharmacological profile is unique: it has high selectivity for the progesterone receptor with strong progestogenic activity; antiandrogenic properties (important for women with androgenic side effects); no androgenic, glucocorticoid, or mineralocorticoid activity; and minimal estrogen suppression (estradiol maintained at approximately 50 pg/mL, unlike GnRH agonists which reduce it to <20 pg/mL). This partial estrogen suppression reduces bone loss risk while still providing adequate suppression of endometriotic tissue. Mechanism in endometriosis includes: decidualization and atrophy of endometriotic implants, anti-inflammatory effects (inhibiting prostaglandins, cytokines), and inhibiting angiogenesis in implants.
Reference: Shaw's Textbook of Gynaecology, 17th ed.
High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP
Written and medically reviewed by the StethoPrep medical team.