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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.
[11] [7] Peak levels of tamoxifen after a single 40 mg oral dose were 65 ng/mL and steady state levels at 20 mg/day were 310 ng/mL. [5] Levels of tamoxifen show clear dose dependency across a dosage range of 1 to 20 mg/day. [5] [93] Endoxifen levels are approximately 5 to 10 times higher than afimoxifene levels, with large interindividual ...
Antiestrogens include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestrant, [6] [7] aromatase inhibitors (AIs) like anastrozole, and antigonadotropins including androgens/anabolic steroids, progestogens, and GnRH analogues.
Estrogen deprivation therapy, also known as endocrine therapy, is a form of hormone therapy that is used in the treatment of breast cancer.Modalities include antiestrogens or estrogen blockers such as selective estrogen receptor modulators (SERMs) like tamoxifen, selective estrogen receptor degraders like fulvestrant, and aromatase inhibitors like anastrozole and ovariectomy.
The side effects of toremifene are similar to those of tamoxifen. [5] The most common side effect is hot flashes. [5] Other side effects include sweating, nausea, vomiting, dizziness, vaginal discharge, and vaginal bleeding. [5] [7] In women with bone metastases, hypercalcemia may occur. [5] Toremifene has a small risk of thromboembolic events. [5]
Notes: Prevention of breast symptoms—specifically gynecomastia and breast pain—induced by 150 mg/day bicalutamide monotherapy with tamoxifen in 282 men with prostate cancer. Bicalutamide and tamoxifen were initiated at the same time (0 months). Estradiol levels were in the range of about 22 to 47 pg/mL in the treated group. [1] Sources: [2] [1]
The four testosterone esters are as follows; . 30 mg testosterone propionate [1]; 60 mg testosterone phenylpropionate [1]; 60 mg testosterone isocaproate [1]; 100 mg testosterone decanoate [1]
As such, it can cause side effects such as gynecomastia and fluid retention. [1] The co-administration of an antiestrogen such as an aromatase inhibitor like anastrozole or a selective estrogen receptor modulator like tamoxifen can reduce or prevent such estrogenic side effects. [1] Metandienone has no progestogenic activity. [1]