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 |
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
