Gestrinone

Synthetic steroid with antiestrogenic and antiprogestogenic properties

Chemical structure of Gestrinone

Gestrinone is a synthetic steroid with both antiprogestogen and antigonadotropin properties. It is primarily used in the treatment of endometriosis, a condition where tissue similar to the lining inside the uterus grows outside the uterus, causing pain and potentially leading to infertility.

Pharmacology

Gestrinone acts as an antagonist of the progesterone receptor and has weak androgenic and anabolic effects. It also exhibits antigonadotropic activity, which leads to a reduction in the production of gonadotropins and subsequently decreases the levels of estrogen and progesterone in the body. This hormonal modulation is beneficial in the management of endometriosis, as it helps to reduce the growth and activity of endometrial tissue.

Mechanism of Action

Gestrinone binds to the progesterone receptor, inhibiting the effects of progesterone. This inhibition leads to a decrease in the proliferation of endometrial tissue. Additionally, by reducing gonadotropin secretion, gestrinone lowers estrogen levels, which further contributes to the suppression of endometrial growth. The androgenic activity of gestrinone may also play a role in its therapeutic effects, although this is not fully understood.

Clinical Use

Gestrinone is administered orally and is typically prescribed for the treatment of endometriosis. The usual dosage regimen involves taking the medication twice a week. The treatment duration and specific dosage may vary based on the severity of the condition and the patient's response to therapy.

Side Effects

Common side effects of gestrinone include acne, weight gain, hirsutism, and voice deepening. These effects are primarily due to its androgenic properties. Other potential side effects include menstrual irregularities, hot flashes, and mood changes.

Contraindications

Gestrinone is contraindicated in patients with known hypersensitivity to the drug, as well as in those with severe liver dysfunction, pregnancy, and breastfeeding. It is also not recommended for use in patients with a history of thromboembolic disorders.

Related Pages

• Endometriosis
• Progesterone receptor
• Antiprogestogen
• Androgen