Estramustine

Estramustine (emcyt), a combination of estradiol coupled to normustine (nornitrogen mustard) by a carbamate link, has weaker estrogenic and antineoplastic activity than estradiol and other alky-lating agents, respectively. While the combination was intended to enhance the uptake of the alky-lating agent into estradiol-sensitive prostate cancer cells, estramustine does not appear to function as an alkylating agent. Rather, estramustine binds to ^-tubulin and microtubule-associated proteins, causing microtubule disassembly and antimitotic actions. Estramustine is used for the treatment of metastatic or progressive prostate cancer at a usual initial dose of 10-16 mg/kg daily in 3 or 4 divided doses. Following oral administration, at least 75% of a dose of estramustine is absorbed from the GI tract and rapidly dephosphorylated. Estramustine is found in the body mainly as its oxidized 17-keto analog isomer, estromustine; both forms accumulate in the prostate. Some hydrolysis of the carbamate linkage occurs in the liver, releasing estradiol, estrone, and the normustine group. Estramustine and estromustine have plasma t1/2 of 10-20 hours, respectively, and are excreted with their metabolites, mainly in the feces. In addition to myelosuppression, estramustine also possesses estrogenic side effects (gynecomastia, impotence, and elevated risk of thrombosis, and fluid retention) and is associated with hypercalcemia, acute attacks of porphyria, impaired glucose tolerance, and hypersensitivity reactions including angioedema.

Blood Pressure Health

Blood Pressure Health

Your heart pumps blood throughout your body using a network of tubing called arteries and capillaries which return the blood back to your heart via your veins. Blood pressure is the force of the blood pushing against the walls of your arteries as your heart beats.Learn more...

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