Gestrinone

Overview of the drug Gestrinone

Gestrinone
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Gestrinone is a synthetic steroid with both progestogen and antiprogestogen 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 a gonadotropin-releasing hormone (GnRH) antagonist, which leads to a decrease in the production of estrogen and progesterone by the ovaries. This reduction in hormone levels helps to alleviate the symptoms of endometriosis by reducing the growth of endometrial tissue.

Mechanism of Action

Gestrinone binds to progesterone receptors and androgen receptors, exerting its effects by modulating the activity of these receptors. It also has weak androgenic activity, which contributes to its therapeutic effects in endometriosis.

Clinical Use

Gestrinone is administered orally and is typically prescribed for women who have not responded to other treatments for endometriosis. The usual dosage is 2.5 mg taken twice a week. Treatment duration is generally limited to six months due to potential side effects.

Side Effects

Common side effects of gestrinone include weight gain, acne, oily skin, and changes in menstrual bleeding patterns. Due to its androgenic activity, some women may experience hirsutism or deepening of the voice.

Contraindications

Gestrinone is contraindicated in women who are pregnant or breastfeeding, as well as in those with severe liver dysfunction or a history of thromboembolic disorders.

Related pages

• Endometriosis
• Progestogen
• Antiprogestogen
• Androgen

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  Gestrinone