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The antiestrogen withdrawal response is a paradoxical improvement in breast cancer caused by discontinuation of antiestrogen ... tamoxifen and raloxifene. [1] [2 ...
Tamoxifen, sold under the brand name Nolvadex among others, is a selective estrogen receptor modulator used to prevent breast cancer in women and men. [13] It is also being studied for other types of cancer. [13]
Tamoxifen is a pure antiestrogenic trans-isomer and has differential actions at estrogen target tissues throughout the body. Tamoxifen is selectively antiestrogenic in the breast but estrogen-like in bones and endometrial cancer. [24] Tamoxifen undergo phase I metabolism in the liver by microsomal cytochrome P450 (CYP) enzymes.
[6] [15] Toremifene has been found to be effective in the treatment of breast pain and may be a more effective medication than tamoxifen for this indication. [16] It also has superior effects on bone mineral density and lipid profile , including levels of cholesterol and triglycerides , compared to tamoxifen. [ 15 ]
Medication discontinuation is the ceasing of a medication treatment for a patient by either the clinician or the patient themself. [1] [2] When initiated by the clinician, it is known as deprescribing. [3] Medication discontinuation is an important medical practice that may be motivated by a number of reasons: [4] [3] Reducing polypharmacy
Drug withdrawal, drug withdrawal syndrome, or substance withdrawal syndrome [1] is the group of symptoms that occur upon the abrupt discontinuation or decrease in the intake of pharmaceutical or recreational drugs. In order for the symptoms of withdrawal to occur, one must have first developed a form of drug dependence.
Treatment with unopposed estrogen (i.e., an estrogen alone without a progestogen) is contraindicated if the uterus is still present, due to its proliferative effect on the endometrium. The WHI also found a reduced incidence of colorectal cancer when estrogen and a progestogen were used together, and most importantly, a reduced incidence of bone ...
Endoxifen is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). [3] [4] [5] The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce endoxifen and afimoxifene (4-hydroxytamoxifen). [6]
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