Gestonorone acetate

A synthetic progestin used in hormone therapy

Gestonorone acetate
INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
Excretion
Legal status
CAS Number
PubChem
DrugBank
ChemSpider
KEGG

Gestonorone acetate is a synthetic progestin, a type of medication that mimics the effects of the natural hormone progesterone. It is used in various hormone therapies, particularly in the treatment of endometriosis, menstrual disorders, and as part of hormone replacement therapy (HRT) in postmenopausal women.

Pharmacology

Gestonorone acetate acts primarily as a potent agonist of the progesterone receptor. It exerts its effects by binding to these receptors in target tissues, leading to changes in gene expression that mimic the effects of natural progesterone. This action helps regulate the menstrual cycle and maintain the endometrium in a state suitable for pregnancy.

Medical uses

Gestonorone acetate is used in the management of several conditions:

• Endometriosis: It helps reduce the growth of endometrial tissue outside the uterus, alleviating pain and other symptoms associated with this condition.
• Menstrual disorders: It is used to treat dysmenorrhea and menorrhagia, helping to regulate menstrual bleeding.
• Hormone replacement therapy: In combination with estrogens, it is used in HRT to alleviate symptoms of menopause such as hot flashes and osteoporosis.

Side effects

Common side effects of gestonorone acetate include:

• Weight gain
• Mood changes
• Breast tenderness
• Nausea

Less common but more serious side effects can include thromboembolism and liver dysfunction.

Chemistry

Gestonorone acetate is a derivative of 19-norprogesterone, modified to enhance its progestogenic activity. Its chemical structure allows it to bind effectively to progesterone receptors, making it a potent progestin.

History

Gestonorone acetate was developed in the mid-20th century as part of efforts to create synthetic progestins with improved efficacy and safety profiles. It has been used in various formulations for the treatment of gynecological disorders and in hormone replacement therapy.

Related pages

• Progesterone
• Progestin
• Hormone replacement therapy
• Endometriosis

• 

  Gestonorone acetate chemical structure