Estramustine Phosphate Sodium
Pronouncation: (ESS-truh-muss-TEEN)Class: Nitrogen mustard
Trade Names:
Emcyt
- Capsules for oral use 140 mg estramustine phosphate.
Pharmacology
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Estramustine appears to act as a relatively weak alkylating agent and imparts a weak estrogenic activity. The estrogenic portion of the molecule acts as a carrier to facilitate selective uptake of the drug into estrogen receptor-positive cells. Because of the selective steroidal uptake, the alkylating effect of the nitrogen mustard is enhanced in these cells. Estramustine phosphate is readily dephosphorylated during absorption, and the major metabolites in plasma are estramustine, the estrone analog, estradiol, and estrone. Terminal half-life of estramustine phosphate is approximately 20 h and mainly excreted in the stool.
Pharmacokinetics
Metabolism
Readily dephosphorylated during absorption; major metabolites in plasma are estramustine, the estrone analog, estradiol, and estrone.
Elimination
The t 1/2 is approximately 20 h. Majority excreted in the feces.
Special Populations
Hepatic Function ImpairmentMay be poorly metabolized in these patients.
Indications and Usage
Palliative therapy of metastatic or progressive prostate cancer.
Unlabeled Uses
Metastatic renal cell carcinoma.
Contraindications
Hypersensitivity to estradiol or nitrogen mustard; active thrombophlebitis or thromboembolic disorders, except where the actual tumor mass is the cause of the thromboembolic phenomenon and the benefits of therapy outweigh the risks.
Dosage and Administration
Prostate CancerAdults
PO 14ߙmg/kg/day (range, 10 to 16ߙmg/kg/day) in 3 to 4 divided doses for 30ߙto 90ߙdays before assessing for continuation of therapy. Continue therapy as long as response is favorable.
General Advice
Administer PO with water 1 h or more before or 2 h after meals.
Storage/Stability
Refrigerate. Capsules may be stored at room temperature for 24 to 48 h without affecting potency. Protect from light.
Drug Interactions
FoodMilk, milk products, and calcium-rich foods or antacids may impair the absorption of estramustine.
Laboratory Test Interactions
Abnormalities of hepatic enzymes and of bilirubin have occurred but have seldom required cessation of therapy. Perform such tests at appropriate intervals during therapy and repeat after the drug has been withdrawn for 2 mo.
Adverse Reactions
Cardiovascular
Hypertension; CHF; edema; increased risk of cerebrovascular accident; MI, thrombosis.
CNS
Lethargy; emotional lability; insomnia.
Dermatologic
Rash; pruritus; dry skin; easy bruising.
Endocrine
Decreased glucose tolerance; breast tenderness or enlargement.
GI
Nausea; vomiting; diarrhea; anorexia; flatulence; elevated LFTs.
Genitourinary
Decreased glucose tolerance; gonadal suppression; breast tenderness; breast enlargement.
Hematologic
Leukopenia and thrombocytopenia have been reported in a small number of patients.
Musculoskeletal
Leg cramps.
Respiratory
Dyspnea.
Precautions
Children
Safety and efficacy not established.
Hepatic Function
Estramustine may be poorly metabolized in patients with impaired liver function.
Mutagenesis
Both estradiol and nitrogen mustard are mutagenic. Advise use of contraceptive measures.
Thrombosis
The risk of thrombosis including nonfatal MI, increases in men receiving estrogens for prostate cancer. Use with caution in patients with a history of thrombophlebitis, thrombosis, or thromboembolic disorders, especially if associated with estrogen therapy. Use with caution in patients with cerebral vascular or coronary artery disease.
Glucose tolerance
Tolerance to glucose may be decreased. Monitor blood sugar in diabetic patient when therapy is started. Report significant changes to health care provider.
Elevated BP
BP elevation may occur. Monitor BP periodically while on estramustine.
Fluid retention
Exacerbation of preexisting or incipient peripheral edema or CHD may occur.
Calcium/Phosphorus metabolism
Calcium/phosphorus metabolism may be influenced. Use with caution in patients with metabolic bone disease associated with hypercalcemia or in patients with renal function impairment.
Patient Information
- Use contraceptive measures during therapy because of the possibility of mutagenic effects.
- Milk, milk products, and calcium-rich foods or antacids may impair the absorption of estramustine.
- Take with water at least 1 h before or 2 h after meals.
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