|ESTRAMUSTINE PHOSPHATE SODIUM
Classifications: antineoplastic; alkylating agent; nitrogen mustard; Therapeutic:antineoplastic nitrogen mustard
Pregnancy Category: D
140 mg capsules
Conjugate of estradiol and the carbamate of nitrogen mustard. Incorporation of estramustine in tumor tissues is probably due
to the presence of estramustine-binding protein (EMBP), which is found in prostate carcinoma, glioma, melanoma, and breast
carcinoma. Binds to proteins and microtubulin resulting in microtubule changes in the cell division cycle, thus arresting
cell division in the G2/M phase of the cell cycle.
Major effectiveness reported to be in patients who have been refractory to estrogen therapy alone.
Palliative treatment of metabolic or progressive carcinoma of prostate.
Hypersensitivity to either estradiol or nitrogen mustard; active thrombophlebitis or thromboembolic disorders; pregnancy (category
History of thrombophlebitis, thromboses, or thromboembolic disorders; cerebrovascular or coronary artery disease; gallstones
or peptic ulcer; impaired liver function; metabolic bone diseases associated with hypercalcemia; diabetes mellitus; hypertension,
conditions that might be aggravated by fluid retention (e.g., epilepsy, migraine, kidney dysfunction); older adult patients.
Route & Dosage
Adult: PO 14 mg/kg/d in 34 divided doses
- Give with meals to reduce incidence of GI adverse effects. Some patients require drug withdrawal because of intolerable GI
- Store at 2°8° C (38°46° F) in tight, light-resistant containers, unless otherwise directed
Adverse Effects (≥1%)CNS:
Lethargy, emotional lability, insomnia
, headache, anxiety. CV:
CHF, peripheral edema. GI: Nausea, diarrhea
, anorexia, flatulence, vomiting, thirst, GI bleeding. Hematologic: Leukopenia
, abnormalities in liver function tests,
hypercalcemia, bone marrow depression
Hoarseness, burning sensation in throat, dyspnea
, upper respiratory discharge, pulmonary emboli
Rash, pruritus, urticaria, dry skin, easy bruising, flushing, peeling skin and fingertips, thinning hair. Special Senses:
Tearing of eyes. Urogenital:
Gynecomastia, breast tenderness, impotence. Endocrine:
Decrease in glucose tolerance. Musculoskeletal:
Milk, dairy products, calcium supplements may decrease estramustine absorption.
Readily absorbed from GI tract. Peak:
23 h. Metabolism:
Dephosphorylated in intestines to estramustine, estradiol
, and nitrogen mustard; further metabolized in liver. Elimination:
In feces via bile. Half-Life:
Assessment & Drug Effects
- Monitor weight and examine for peripheral edema. Be mindful that drug can cause CHF.
- Monitor I&O ratio and pattern to prevent dehydration and electrolyte imbalance, especially with vomiting or diarrhea.
- Observe diabetics closely because of possibility of estramustine-induced reduction in glucose tolerance. Monitor baseline
and periodic glucose tolerance tests.
- Lab tests: Perform baseline and periodic liver enzymes and bilirubin tests; repeat after drug has been discontinued for 2
Patient & Family Education
- Eat small meals at frequent intervals to reduce drug-induced nausea, eat slowly, and try cold food if food odors are offensive.
- Drink liquids 1 h before or 1 h after rather than with meals; clear liquids may be more palatable.