Drug information of Estramustine
Mechanism of effect
Estradiol and nornitrogen mustard carbamate-linked combination which has antiandrogen effects (due to estradiol) and antimicrotubule effects (due to nornitrogen mustard); causes a marked decrease in plasma testosterone and an increase in estrogen levels.
Estramustine bind to tubulin and/or microtubule-associated proteins, resulting in depolymerization of microtubules and, subsequently, cellular metaphase arrest. May damage cell membrane, promote DNA breakage, interfere with DNA replication, and induce cellular apoptosis in other cell lines (e.g., glioma cells, colon cancer cells).
Absorption is Incomplete. Initially dephosphorylated in the GI tract, then hepatically oxidated and hydrolyzed to estramustine, estromustine (oxidized isomer of estramustine), estrone, and estradiol .
Excretion is in Feces (primarily) and urine (trace amounts).Time to Peak is 2-3 hours.
Drug indicationsPalliative treatment of patients with metastatic and/or progressive carcinoma of the prostate.
Usual Adult Dose for Prostate Cancer : 14 mg/kg/day orally in 3 or 4 divided doses .
Duration of Therapy : Continue therapy as long as there is a favorable patient response; some patients have been maintained on therapy for more than 3 years .
Drug contraindicationshypersensitivity to drug or its components. , Hypersensitivity to estradiol , Hypersensitivity to nitrogen mustard , active thrombophlebitis or thromboembolic disorder , Severe hepatic or cardiac disease
Side effectsnausea , Headache , insomnia , chest pain , vomiting , flushing , Diarrhea , pulmonary embolism , anxiety , anorexia , Hyperbilirubinemia , flatulence , decreased libido , Thirst , breast pain , skin rush , tiredness , Leukopenia , thrombocytopenia , gastrointestinal hemorrhage , local thrombophlebitis , Gynecomastia , increased lactate dehydrogenase , Rhinorrhea
Interactionspimecrolimus , Fingolimod , Warfarin , Trastuzumab , Calcium carbonate , Calcitriol (topical)
• Allergic reactions and angioedema, including airway involvement, have been reported.
• Elevated blood pressure or congestive heart disease may occur.
• Estrogen treatment for prostate cancer is associated with an increased risk of thrombosis or MI (including fatalities).
• Peripheral edema (new onset or exacerbation) or congestive heart disease may occur.
• Use with caution in patients where fluid accumulation may be poorly tolerated, including cardiovascular disease (HF or hypertension), migraine, seizure disorder or renal dysfunction .
• Glucose tolerance may be decreased; use with caution in patients with diabetes mellitus .
• May cause hypertension; monitor blood pressure periodically.
• Use with caution in patients with hepatic impairment (may be metabolized poorly).
• Patients with osteoblastic metastases are at risk for hypocalcemia; monitor calcium regularly.
• Use with caution in patients with renal impairment.
Points of recommendation
Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:
• if you are pregnant, planning to become pregnant, or are breast-feeding
• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement
• if you have allergies to medicines, foods, or other substances
• if you have problems with blood vessels in your brain (cerebral vascular disease) or heart (cardiovascular disease)
• if you have diabetes or heart disease.
Take estramustine on an empty stomach at least 1 hour before or 2 hours after meals.Swallow estramustine with water.Do not take antacids containing calcium, or eat or drink dairy products within 1 hour before or 2 hours after taking estramustine.
Several days to weeks may pass before you feel the full benefit of estramustine. Do not stop taking estramustine without checking with your doctor.
If you miss a dose of estramustine , skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.