Trimegestone

Trimegestone

Chemical structure of Trimegestone

Trimegestone is a synthetic progestin of the 19-norprogesterone group, which is used in hormonal contraception and hormone replacement therapy. It is known for its high potency and selectivity for the progesterone receptor.

Pharmacology

Trimegestone acts as a potent agonist of the progesterone receptor, with minimal activity at other steroid hormone receptors. This selectivity reduces the risk of side effects associated with non-specific receptor binding. It has been shown to have a strong effect on the endometrium, making it effective in preventing endometrial hyperplasia in women receiving estrogen therapy.

Medical Uses

Trimegestone is primarily used in combination with estrogens in hormone replacement therapy for postmenopausal women. It helps to counteract the effects of estrogen on the endometrium, reducing the risk of endometrial cancer. It is also used in some oral contraceptives.

Side Effects

Common side effects of trimegestone include headache, breast tenderness, and nausea. As with other progestins, it may also cause changes in menstrual bleeding patterns.

Chemistry

Trimegestone is a derivative of 19-norprogesterone, characterized by the presence of a triple bond at the C17 position. This modification enhances its binding affinity and selectivity for the progesterone receptor.

History

Trimegestone was developed in the 1980s and has been studied extensively for its use in hormone replacement therapy. It was introduced to the market in the 1990s and has been used in various formulations since then.

Related Pages

• Progestin
• Hormone replacement therapy
• Oral contraceptive