Estramustine

Estramustine Uses, Dosage, Side Effects, Food Interaction and all others data.

A nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.

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.

Trade Name Estramustine
Availability Prescription only
Generic Estramustine
Estramustine Other Names Estramustina, Estramustine, Estramustinum
Related Drugs estradiol, Premarin, Xtandi, Casodex, Zytiga, Lynparza
Weight 140mg
Type Oral capsule
Formula C23H31Cl2NO3
Weight Average: 440.403
Monoisotopic: 439.168099277
Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Estramustine
Estramustine

Uses

Estramustine is an antineoplastic agent used for the management of metastatic and/or progressive prostate cancer in palliative setting.

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

Estramustine is also used to associated treatment for these conditions: Metastatic Hormone Refractory Prostate Cancer

How Estramustine works

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.

Food Interaction

  • Avoid milk and dairy products.
  • Take on an empty stomach.

[Moderate] ADJUST DOSING INTERVAL: Food and milk may significantly decrease serum concentrations of estramustine.

The mechanism of the interaction is not known.



MANAGEMENT: It is recommended that estramustine be taken at least 1 hour before or 2 hours after meals, and that it not be coadministered with milk, or calcium containing products.

Estramustine Hypertension interaction

[Major] The risk of myocardial infarction and strokes, including those associated with estrogen use, may be increased in patients with hypertension.

Moreover, estramustine may elevate blood pressure and worsen the hypertension, thus compounding the risk.

Therapy with estramustine should be administered cautiously in patients with preexisting hypertension.

Patients should be monitored for changes in cardiovascular status, and their antihypertensive regimen adjusted as necessary.

Half Life

20 hours

Elimination Route

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.

Innovators Monograph

You find simplified version here Estramustine

*** Taking medicines without doctor's advice can cause long-term problems.
Share