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
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
Images
Patient Handout
Formulary
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Adding plans allows you to:
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- Compare formulary status to other drugs in the same class.
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