Trimegestone

A synthetic progestin used in hormone therapy and contraception

Trimegestone
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Trimegestone is a synthetic progestin that is used in hormone replacement therapy and contraception. It is known for its high potency and selectivity for the progesterone receptor.

Pharmacology

Trimegestone is a member of the 19-norprogesterone class of progestins. It exhibits strong progestogenic activity with minimal androgenic, estrogenic, or glucocorticoid effects. This selectivity makes it a valuable component in hormone therapy, particularly for menopausal hormone therapy and oral contraceptives.

Mechanism of Action

Trimegestone works by binding to the progesterone receptor in target tissues, which leads to changes in gene expression that mimic the effects of natural progesterone. This action helps regulate the menstrual cycle, maintain pregnancy, and prepare the endometrium for potential implantation of an embryo.

Clinical Uses

Trimegestone is primarily used in combination with estrogens in hormone replacement therapy for postmenopausal women. It helps alleviate symptoms of menopause such as hot flashes, vaginal atrophy, and osteoporosis. Additionally, it is used in combined oral contraceptives to prevent ovulation and provide effective birth control.

Side Effects

Common side effects of trimegestone include nausea, headache, breast tenderness, and mood changes. As with other progestins, there is a potential risk of thromboembolism, particularly when used in combination with estrogens.

Chemistry

Trimegestone is chemically classified as a 19-norprogesterone derivative. Its structure is characterized by the presence of a 17_-acetoxy group and a 6-methyl group, which contribute to its high progestogenic activity and receptor selectivity.

Related pages

• Progestin
• Hormone replacement therapy
• Oral contraceptive
• Progesterone receptor