Dosing & Uses
Dosage Forms & Strengths
capsule
- 140mg
Prostate Carcinoma
Palliative treatment of metastatic and/or progressive prostate carcinoma
Treat for 30-90 days to determine benefits of continued therapy; continue treatment as long as favorable response lasts
Administration
Take 1 hr before or 2 hr after meals
Avoid calcium-rich foods
Not recommended
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (3)
- deferiprone
deferiprone, estramustine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.
- palifermin
palifermin increases toxicity of estramustine by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hrbefore, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b, estramustine. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.
Monitor Closely (12)
- acalabrutinib
acalabrutinib, estramustine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects.
- calcium acetate
calcium acetate decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- calcium carbonate
calcium carbonate decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- calcium chloride
calcium chloride decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- calcium citrate
calcium citrate decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- calcium gluconate
calcium gluconate decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- food
food decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Esp. calcium rich foods; Patients should take estramustine with water at least 1h before or 2h after meals.
- hydroxyurea
estramustine, hydroxyurea. Other (see comment). Use Caution/Monitor. Comment: Combination may increase risk of myelosuppression.
- ofatumumab SC
ofatumumab SC, estramustine. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.
- siponimod
siponimod and estramustine both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- trastuzumab
trastuzumab, estramustine. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- trastuzumab deruxtecan
trastuzumab deruxtecan, estramustine. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
Minor (0)
Adverse Effects
>10%
Edema
Dyspnea
Nausea
Diarrhea
Breast tenderness and enlargement
1-10%
Lethargy
Insomnia
Cerebrovascular accident
Myocardial infarction
Thrombophlebitis
Pulmonary embolism
Congestive heart failure
Easy bruising
Anorexia
Vomiting
Pruritus
Dry skin
Impotence
Leg cramps
Leukopenia
Decreased testosterone
Abnormality of hepatic enzymes and/or bilirubin
Warnings
Contraindications
Hypersensitivity to estradiol or nitrogen mustard
Active thrombophlebitis or thromboembolic disorder, except when tumor mass is cause of thromboembolic phenomenon and benefits of therapy outweigh risk
Cautions
Increased risk of thrombosis, including fatal and non-fatal MI
Liver dysfunction, metabolic bone disease associated with hypercalcemia, renal insufficiency
History of thromoboembolic phenomenon especially associated with estrogen therapy
Decreased glucose tolerance-monitor diabetics
Risk of HTN-monitor BP periodically
May cause fluid retention with exacerbation of CHF, peripheral edema, or conditions influenced by fluid retention, such as epilepsy, migraine, renal dysfunction
May cause gynecomastia and impotence
Allergic reactions, including angioedema of airway has been reported
Avoid becoming pregnant
Pregnancy & Lactation
Pregnancy Category: X
Lactation: not intended for use in women
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Has the effects of estradiol and nitrogen mustard combination. It may inhibit tubulin function by binding to microtubule proteins. Antitumor effects may result from estrogenic effect. Plasma testosterone levels decrease while estrogen levels increase
Pharmacokinetics
Absorption: 75% (PO)
Metabolism: Liver
Metabolite: estramustine, estradiol, estrone
Half-life elimination: 15-24hr
Excretion: Feces (2.9-4.8%)
Time to peak serum: 2-3 hr
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Formulary
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