Segesterone acetate

Nestorone.svg

Segesterone acetate is a progestin of the 19-norprogesterone group which is used as a hormonal contraceptive. It is also known by its developmental code name Nestorone. Segesterone acetate is notable for its high potency and selectivity for the progesterone receptor.

Chemical Structure and Properties

Segesterone acetate is a synthetic steroid and a derivative of progesterone. Its chemical structure is characterized by the presence of an acetate group at the 17α position. This modification enhances its potency and duration of action compared to natural progesterone.

Mechanism of Action

As a progestin, segesterone acetate works primarily by binding to the progesterone receptor in target tissues. This binding inhibits ovulation by suppressing the secretion of gonadotropins from the pituitary gland. Additionally, it induces changes in the endometrium that make it less suitable for implantation and thickens the cervical mucus to prevent sperm penetration.

Clinical Uses

Segesterone acetate is used in combination with an estrogen in various forms of hormonal contraception, including vaginal rings and transdermal patches. It is particularly valued for its minimal androgenic and estrogenic side effects, making it suitable for a wide range of users.

Pharmacokinetics

Segesterone acetate is administered via non-oral routes such as vaginal rings or transdermal patches to avoid first-pass metabolism in the liver. This allows for more consistent and controlled release of the hormone into the bloodstream.

Side Effects

Common side effects of segesterone acetate include headache, nausea, breast tenderness, and irregular menstrual bleeding. Serious but rare side effects may include thromboembolism and hypertension.

Research and Development

Segesterone acetate has been the subject of extensive research for its potential use in male contraception and as a treatment for various gynecological disorders such as endometriosis and menorrhagia.

See Also

• Progestin
• Hormonal contraception
• Progesterone receptor
• Vaginal ring
• Transdermal patch