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Action/Kinetics:
Water-soluble drug that combines estradiol and mechlorethamine (a nitrogen mustard). Estradiol facilitates uptake into cells containing the estrogen receptor while the nitrogen mustard acts as an alkylating agent. Chronic estramustine administration results in plasma levels and effects of estradiol similar to those of conventional estradiol therapy. Well absorbed from the GI tract and dephosphorylated before reaching the general circulation. Metabolites include estromustine, estrone, and estradiol.
t
1/2: 20 hr. Major route of excretion is in the feces.
Uses:
Palliative treatment of metastatic and/or progressive prostatic carcinoma.
Contraindications:
Active thrombophlebitis or thromboembolic disease unless the tumor mass is causing the thromboembolic disorder. Allergy to nitrogen mustard or estrogen.
Special Concerns:
Use with caution in presence of cerebrovascular disease, CAD, diabetes, hypertension, CHF, impaired liver or kidney function, and metabolic bone diseases associated with hypercalcemia.
Additional Side Effects:
CV:
MI, CVA thrombosis, CHF, increased BP, thrombophlebitis, leg cramps, edema.
Respiratory:
Pulmonary embolism dyspnea, upper respiratory discharge, hoarseness.
GI: Flatulence, burning sensation of throat, thirst.
CNS: Emotional lability, insomnia, anxiety, lethargy, headache.
Dermatologic: Easy bruising, flushing, peeling of skin or fingertips.
Miscellaneous: Chest pain, tearing of eyes, leg cramps, breast tenderness or enlargement, decreased glucose tolerance.
Laboratory Test Alterations:
Bilirubin, AST, LDH.
Glucose tolerance. Abnormal hematologic tests for leukopenia and thrombocytopenia.
Overdose Management:
Symptoms: Extensions of the side effects.
Treatment: Gastric lavage; treat symptoms. Monitor blood counts and liver profiles for at least 6 weeks.
Drug Interactions:
Drugs or food containing calcium may
estramustine absorption.
How Supplied:
Capsule: 140 mg
Dosage
?Capsules
14 mg/kg/day in three to four divided doses (range: 10-16 mg/kg/day) or 600 mg (base)/m
2 daily in three divided doses. One 140-mg capsule is taken for each 10 kg or 22 lb of body weight. Treat for 30-90 days before assessing beneficial effects; continue therapy as long as the drug is effective. Some clients have taken doses from 10 to 16 mg/kg/day for more than 3 years.
