chlorotrianisene

Action and Spectrum

Actions and Spectrum: 

Actions: 

Chlorotrianisene binds to estrogen receptors in a variety of cells that contain estrogen receptors. The female reproductive system, the hypothalamus, the mammary gland, and the pituitary are among the target cells. Follicle-stimulating hormone (FSH) from the anterior pituitary is suppressed by estrogens, which also enhance the hepatic production of thyroid-binding globulin (TBG), sex hormone-binding globulin (SHBG), and other blood proteins. 

Spectrum: 

Strong synthetic non-steroidal estrogens like chlorotrianisene (TACE®) are used to treat menopausal symptoms, ovarian function deficits (such as underdevelopment of female sexual characteristics and some forms of infertility), and, in rare instances, prostate cancer. It can also be used to stop postpartum breast engorgement. On a variety of cells that contain estrogen receptors, chlorotrianisene (TACE®) binds to the estrogen receptor.

The female reproductive system, the hypothalamus, the mammary gland, and the pituitary are among the target cells. Follicle-stimulating hormone (FSH) from the anterior pituitary is suppressed by estrogens, which also boost the hepatic production of other serum proteins and thyroid-binding globulin (TBG), sex hormone-binding globulin (SHBG), and other serum proteins.

Drug Interaction

Adverse Reaction

Frequency not defined 

Nausea 

Pimples 

Vomiting 

Skin discoloration 

Dizziness 

Loss of appetite 

Depression 

Severe blood clot 

Lump in breast region 

Severe allergic reactions 

Changes in menstrual cycle

Black Box Warning

Black Box Warning: 

When using this drug, check liver function frequently as it may cause harm to the liver.

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Blood clotting disorders 
• Hypersensitivity 
• Breast cancer 

Cautions 

• Renal impairment 
• Gall bladder disease 
• Hepatic impairment 
• Headache 
• DM 
• Cardiovascular disorders 
• Drug interactions 
• Pregnancy  
• Breastfeeding 

Pregnancy / Lactation

Pregnancy consideration:  

Pregnancy category: X 

Breastfeeding warnings:  

No data is available regarding the excretion of drug in breast milk. 

Pregnancy category: X 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category.

Pharmacology

Pharmacology: 

A synthetic nonsteroidal estrogen called chlorotrianisene has been used orally to treat prostatic cancer, female hypogonadism, and menopausal symptoms. 

Pharmacodynamics: 

A synthetic nonsteroidal estrogen called chlorotrianisene is used by postmenopausal women to replace their natural estrogen. After menopause, when endogenous estrogen synthesis is absent, chlorotrianisene fills the void. Within 48 to 72 hours of stopping estrogen treatment, the endometrium may begin to bleed. Inversely, extended use of estrogen medication may cause the myometrium to expand and endometrial shrinkage. Because of their limited anabolic action, estrogens may contribute to fluid retention, edema, and sodium retention.

They might also lower high levels of phospholipids and blood cholesterol. Estrogens have an effect on bone health by encouraging calcium deposition and quickening epiphyseal closure following initial growth stimulation. Oestrogen is essential for the onset of menstruation in the nonovulatory or preovulatory phase of the menstrual cycle. Progesterone release must stop in the mature ovulatory phase, even though a decrease in estrogenic activity can cause menstruation at the conclusion of the cycle. The possible increased risk of puerperal thromboembolism should be carefully considered while using high estrogen dosages to avoid postpartum breast engorgement. 

Pharmacokinetics: 

Absorption 

Rapid absorption 

Distribution 

Protein-bound is 50-80% 

Metabolism 

Mostly metabolized in the liver, while there may also be some involvement in the gonads, kidneys,  and muscular tissues. It is still unclear exactly what happens to the synthetic estrogens during their metabolism. 

Adminstartion

Administration: 

Usually taken orally, chlorotrianisene dosage and schedule are established by the prescribing medical professional in accordance with the health and requirements of each patient. Chlorotrianisene is often administered orally, either with or without food. Patients should rigorously adhere to the recommended schedule and dose guidelines, and they should discuss any queries or worries they may have with their medical professional regarding the drug. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: chlorotrianisene 

Pronounced: klor-oh-tri-AN-i-seen 

Why do we use chlorotrianisene? 

Menopause symptoms, ovarian function deficits (such as underdevelopment of female sexual characteristics and certain forms of infertility), and, in rare instances, prostate cancer are treated with this medication. Another use of chlorotrianisene is to stop breast engorgement after giving birth.