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
Contraindicated (0)
Serious - Use Alternative (3)
- deferiprone
deferiprone, estramustine. Either increases toxicity of the other by pharmacodynamic synergism. Avoid or Use Alternate Drug. Avoid use of deferiprone with other drugs known to be associated with neutropenia or agranulocytosis; if an alternative is not possible, monitor absolute neutrophil count more frequently.
- palifermin
palifermin increases toxicity of estramustine by Other (see comment). Avoid or Use Alternate Drug. Comment: Palifermin should not be administered within 24 hrbefore, during infusion of, or within 24 hr after administration of antineoplastic agents. Coadministration of palifermin within 24 hr of chemotherapy resulted in increased severity and duration of oral mucositis.
- ropeginterferon alfa 2b
ropeginterferon alfa 2b, estramustine. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.
Monitor Closely (12)
- acalabrutinib
acalabrutinib, estramustine. Either increases toxicity of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration may increase risk of myelosuppressive effects.
- calcium acetate
calcium acetate decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- calcium carbonate
calcium carbonate decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- calcium chloride
calcium chloride decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- calcium citrate
calcium citrate decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- calcium gluconate
calcium gluconate decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Patients should take estramustine with water at least 1h before or 2h after meals.
- food
food decreases levels of estramustine by inhibition of GI absorption. Applies only to oral form of both agents. Use Caution/Monitor. Esp. calcium rich foods; Patients should take estramustine with water at least 1h before or 2h after meals.
- hydroxyurea
estramustine, hydroxyurea. Other (see comment). Use Caution/Monitor. Comment: Combination may increase risk of myelosuppression.
- ofatumumab SC
ofatumumab SC, estramustine. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.
- siponimod
siponimod and estramustine both increase immunosuppressive effects; risk of infection. Use Caution/Monitor. Caution if coadministered because of additive immunosuppressive effects during such therapy and in the weeks following administration. When switching from drugs with prolonged immune effects, consider the half-life and mode of action of these drugs to avoid unintended additive immunosuppressive effects.
- trastuzumab
trastuzumab, estramustine. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
- trastuzumab deruxtecan
trastuzumab deruxtecan, estramustine. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .
Minor (0)
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
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Emcyt oral - | 140 mg capsule |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
estramustine oral
ESTRAMUSTINE PHOSPHATE - ORAL
(ess-TRAM-you-steen FOSS fate)
COMMON BRAND NAME(S): Emcyt
USES: This medication is used to treat some types of prostate cancer. In the body, estramustine breaks down into estrogens (estrone, estradiol) and a type of cancer drug (estromustine). This medication is thought to work by increasing estrogens, which interfere with prostate cancer, and by slowing/stopping the growth of cancer cells.
HOW TO USE: Take this medication by mouth on an empty stomach (1 hour before or 2 hours after a meal) as directed by your doctor, usually 3 to 4 times a day.Take this medication with a full glass of water (8 ounces or 240 milliliters) unless your doctor directs you otherwise.Take this medication regularly in order to get the most benefit from it. Remember to take it at the same times each day as directed. The dosage is based on your medical condition, weight, and response to therapy.Take this medication 3 hours before or after taking any products containing magnesium, aluminum, or calcium. Some examples include quinapril, didanosine, vitamins/minerals, and antacids. Dairy products (such as milk, yogurt), calcium-enriched juice, sucralfate, bismuth subsalicylate, iron, and zinc are also included. These products bind with estramustine, preventing its full absorption.Do not increase your dose or take this medication more often than prescribed. Your condition will not improve any faster, and the risk of serious side effects may be increased.Since this drug can be absorbed through the skin and lungs, women who are pregnant or who may become pregnant should not handle this medication or breathe the dust from the capsules.
SIDE EFFECTS: Nausea, vomiting, loss of appetite, flushing, dry skin, headache, leg cramps, decreased sexual interest/ability, and male breast tenderness/enlargement may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptlyRemember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.This medication may raise your blood pressure. Check your blood pressure regularly and tell your doctor if the results are high.Tell your doctor right away if you have any serious side effects, including: mental/mood changes (such as depression), swelling of hands/feet, worsening of seizures, increased thirst/urination, nausea/vomiting that doesn't stop, easy bruising/bleeding, stomach/abdominal pain, dark urine, yellowing eyes/skin.This medication may rarely cause serious problems such as heart attacks, stroke, and blood clots. Get medical help right away if you experience any of the following symptoms: chest/jaw/left arm pain, sudden severe headache, weakness on one side of the body, confusion, trouble speaking, sudden vision changes (such as double vision, loss of vision), pain/redness/swelling of legs, shortness of breath, coughing up blood, sudden dizziness/fainting.This medication can lower the body's ability to fight an infection. Tell your doctor promptly if you develop any signs of an infection such as sore throat that doesn't go away, fever, or chills.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking estramustine, tell your doctor or pharmacist if you are allergic to it; or to estradiol or other estrogens; or to nitrogen mustard (such as mechlorethamine); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: blood clots (such as in the legs, eyes, lungs), bone disease (such as bone metastases, high calcium levels), high cholesterol or triglyceride (blood fat) levels, depression, diabetes, severe headaches (such as migraine), heart disease (such as angina, heart attack, heart failure), high blood pressure, kidney disease, liver disease, seizure, long periods of sitting or lying down (for example, due to being bedridden), stroke, thyroid problems.Do not smoke cigarettes or use tobacco. Estrogens combined with smoking further increase your risk for stroke, blood clots, high blood pressure, and heart attacks.If you will be having surgery or will be confined to a chair or bed for a long time (such as on a long plane flight), notify your doctor beforehand. Special precautions may need to be taken in these circumstances while you are taking this drug because of the increased risk for blood clots.If you have diabetes, estramustine may affect your blood sugar. Check your blood sugar regularly as directed and share the results with your doctor.If you are nearsighted or wear contact lenses, you may develop vision problems or trouble wearing your contact lenses. Contact your eye doctor if these problems occur.This medication may cause blotchy, dark areas on your face and skin (melasma). Sunlight may worsen this effect. Limit your time in the sun. Avoid tanning booths and sunlamps. Use sunscreen and wear protective clothing when outdoors.This medication may affect the production of sperm. Use a reliable form of birth control while on this medication. Consult your doctor.This medication is not usually used in women. It is unlikely to be used during pregnancy or breast-feeding. Consult your doctor if you have any questions about this medication.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug are: aromatase inhibitors (such as anastrozole, exemestane), corticosteroids (such as prednisolone), ospemifene, tamoxifen, troleandomycin, tranexamic acid, medication for low thyroid (hypothyroidism).Certain drugs can affect the estrogen levels in your system. Drugs that may cause this effect include: azole antifungals (such as itraconazole, ketoconazole), many antibiotics (such as cephalosporins, chloramphenicol, macrolides, penicillins, tetracyclines, sulfas), aprepitant, bexarotene, bosentan, dapsone, griseofulvin, certain HIV protease inhibitors (such as nelfinavir), modafinil, nevirapine, rifamycins (such as rifampin), ritonavir, many seizure medications (such as barbiturates, carbamazepine, phenytoin, primidone, topiramate), St John's wort.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab tests (such as blood pressure, liver function, calcium levels) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store the U.S. product in the refrigerator away from light and moisture. Do not store in the bathroom.Store the Canadian product between 36-77 degrees F (2-25 degrees C) away from light and moisture. Do not store in the bathroom.Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised December 2022. Copyright(c) 2023 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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