indication

For the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate

pharmacology

Estramustine is an antineoplastic agent indicated in the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate. Estramustine is a combination of estradiol with nitrogen mustard. In vivo, the nitrogen-mustard moiety becomes active and participates in alkylation of DNA or other cellular components.. This causes DNA damage in rapidly dividing cancerous cells leading to cell death and ideally, tumor shrinkage.

mechanism of action

Estramustine is a derivative of estradiol with a nitrogen mustard moiety. This gives it alkylating properties. In vivo, the nitrogen mustard component is active and can alklyate DNA and other cellular components (such as tubulin components) of rapidly dividing cells. This causes DNA strandbreaks or misscoding events. This leads to apoptosis and cell death. Also, due to the drugs estrogen component, it can bind more selectively to active estrogen receptors.

half life

20 hours

route of elimination

The metabolic urinary patterns of the estradiol moiety of estramustine phosphate and estradiol itself are very similar, although the metabolites derived from estramustine phosphate are excreted at a slower rate.

drug interactions

Calcium Acetate: Calcium salts such as calcium acetate may decrease the absorption of estramustine. Interactions can be minimized by administering estramustine on an empty stomach, at least 1 hour before or 2 hours after the dose of an oral calcium supplement. Do not coadminister estramustine with food or milk. Monitor for decreased therapeutic effects of estramustine if administered with oral calcium supplements, food or milk.

Clodronate: Clodronate may increase the levels of estramustine.

Trastuzumab: Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.