Chlorotrianisene

Chlorotrianisene (TACE), sold under the brand name Tace among others, is a synthetic, non-steroidal estrogen of the triphenylethylene group that was developed in the 1940s and introduced for medical use in the 1950s. It is used primarily in the treatment of menopausal symptoms and in the management of prostate cancer. Chlorotrianisene acts as an estrogen receptor agonist, mimicking the effects of natural estrogens in the body.

Medical Uses

Chlorotrianisene is used for the management of menopausal symptoms such as hot flashes, vaginal atrophy, and osteoporosis. It may also be used in the palliative treatment of advanced prostate cancer, taking advantage of its estrogenic effects to inhibit the production of testosterone, which can slow the progression of the disease.

Pharmacology

Mechanism of Action

Chlorotrianisene functions by binding to estrogen receptors in various tissues throughout the body, acting as an estrogen receptor agonist. This binding stimulates the transcription of estrogen-responsive genes, leading to the production of proteins that are responsible for the development and maintenance of female secondary sexual characteristics, as well as the modulation of the menstrual cycle and reproductive system.

Pharmacokinetics

The pharmacokinetics of chlorotrianisene involve its absorption, distribution, metabolism, and excretion. After oral administration, chlorotrianisene is absorbed from the gastrointestinal tract. It undergoes extensive first-pass metabolism in the liver, where it is converted into various metabolites. The drug and its metabolites are distributed throughout the body, with a high affinity for estrogen receptors. They are eventually excreted in the urine and feces.

Adverse Effects

The use of chlorotrianisene can lead to several adverse effects, including nausea, vomiting, weight gain, edema, and an increased risk of venous thromboembolism. Long-term use of chlorotrianisene and other estrogens has been associated with an increased risk of endometrial cancer, and it may also influence the risk of breast cancer.

Contraindications

Chlorotrianisene is contraindicated in individuals with a known hypersensitivity to the drug, as well as in patients with a history of estrogen-dependent tumors, undiagnosed vaginal bleeding, active thrombophlebitis, or thromboembolic disorders.

Interactions

Chlorotrianisene may interact with various medications, including blood thinners, thyroid hormone replacement therapy, and certain anticonvulsants. These interactions can alter the effectiveness of chlorotrianisene or the co-administered drug.

History

Chlorotrianisene was synthesized in the 1940s and introduced for medical use in the 1950s. It was one of the first synthetic estrogens to be developed and has been used for several decades in the management of menopausal symptoms and prostate cancer.

Society and Culture

Brand Names

Chlorotrianisene is sold under various brand names, including Tace among others. Its availability and use may vary by country and region.

See Also

• Estrogen
• Menopause
• Prostate cancer
• Estrogen receptor