Pharmacodynamics SGA acts primarily as a high-affinity agonist of the progesterone receptor (272% of the affinity of progesterone and 136% of that of promegestone). It does not bind significantly to the androgen receptor, estrogen receptor, or mineralocorticoid receptor. As such, SGA does not have estrogenic, androgenic, antiandrogenic, or antimineralocorticoid activity. However, SGA does have significant affinity for the glucocorticoid receptor (38% of that of dexamethasone), but in spite of its relatively high affinity for the glucocorticoid receptor, it either does not have any glucocorticoid effects or shows glucocorticoid effects only at exceptionally high doses in animals. SGA has no antiglucocorticoid activity in animals either. The ovulation-inhibiting dosage of parenteral SGA has been reported to be 0.15 mg per day, while the endometrial transformation dosage has been reported to be 0.6 mg per cycle. SGA has antigonadotropic effects and functional antiestrogenic effects via its progestogenic activity similarly to other progestogens. Pharmacokinetics SGA is only weakly active orally, and is instead given as a subcutaneous implant. The oral bioavailability of SGA has been reported to be only 10%. However, it has also been reported that the medication is more than 100-fold as potent when delivered via subcutaneous implant relative to oral administration in rats. SGA is bound to albumin. It does not bind to sex hormone-binding globulin.<unk> , the deacetylated form of SGA, is a metabolite of the medication. The biological half-life of parenteral SGA has been reported to be 24 to 72 hours. One study specifically reported a biological half-life of 26.8 hours. It has been reported that the biological half-life of SGA with oral administration is only 1 to 2 hours. In contrast to all of the preceding however, the Food and Drug Administration (FDA) label for Annovera, a one-year vaginal ring containing ethinylestradiol and SGA, lists a circulating half-life of SGA of 4.5 hours.
Segesterone acetate
Anagestone acetate
Gestonorone caproate
Ingenol mebutate
Androstanolone enanthate
Metenolone enanthate
Quingestanol acetate
Lapisteride