[New gestagens--advantages and disadvantages]

Area of Science:

• Pharmacology
• Endocrinology
• Synthetic chemistry

Context:

• Synthetic progestagens are widely used for therapeutic applications including hormone replacement therapy and contraception due to their high oral bioavailability.
• Various classes of progestogens exist, including progesterone derivatives, nortestosterone derivatives (13-methyl-gonanes and 13-ethyl-gonanes), spirolactone derivatives, and norpregnane derivatives.

Purpose:

• To review the different types of synthetic progestagens, their hormonal profiles, and their therapeutic applications.
• To highlight the varying efficacies and hormonal activities of different progestogen classes.

Summary:

• All progestagens exhibit antiestrogenic activity, inhibiting endometrial proliferation and reducing the risk of endometrial hyperplasia.
• Nortestosterone derivatives, except Dienogest, possess a 17-alpha-ethynyl group and may have mild androgenic properties. Some are prodrugs, rapidly converting to active forms post-administration.
• Spirolactone derivatives like Drospirenone have antimineralocorticoid and antiandrogenic effects. Progesterone derivatives and certain others (Gestodene, Desogestrel) show mild glucocorticoid activity.
• 19-norpregnane derivatives' effects are similar to progesterone derivatives.

Impact:

• The diverse hormonal profiles of synthetic progestagens enable individualized selection for optimal contraception and hormone replacement therapy in women.
• Understanding these profiles is crucial for managing potential side effects and optimizing therapeutic outcomes.