estramustine (Rx)

Brand and Other Names:Emcyt
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

capsule

  • 140mg

Prostate Carcinoma

Palliative treatment of metastatic and/or progressive prostate carcinoma

14 mg/kg divided q6-8hr PO  

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

Prostate Carcinoma

Palliative treatment of metastatic and/or progressive prostate carcinoma

14 mg/kg PO divided q6-8hr  

Treat for 30-90 days to determine benefits of continued therapy; continue treatment as long as favorable response lasts

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Interactions

Interaction Checker

and estramustine

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     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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             activity indicator 

            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)

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                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

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                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

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                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.

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                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

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                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                Emcyt oral
                -
                140 mg capsule

                Copyright © 2010 First DataBank, Inc.

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                Patient Handout

                Patient Education
                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, either 1 hour before or 2 hours after a meal, usually 3-4 times a day or as directed by your doctor.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 (e.g., 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 persist or worsen, 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 any of these unlikely but serious side effects occur: mental/mood changes (e.g., depression), swelling of hands/feet, worsening of seizures, signs of worsening diabetes control (e.g., increased thirst and urination).This medication may rarely cause serious problems such as heart attacks, stroke, and blood clots. Seek immediate medical attention 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 (e.g., double vision, loss of vision), pain/redness/swelling of legs, shortness of breath, coughing up blood, sudden dizziness/fainting.Tell your doctor right away if any of these rare but very serious side effects occur: easy bruising/bleeding, stomach/abdominal pain, persistent nausea/vomiting, dark urine, yellowing eyes/skin.This medication can lower the body's ability to fight an infection. Notify your doctor promptly if you develop any signs of an infection such as fever, chills, or persistent sore throat.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention 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 (e.g., 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: history of stroke or other blood clots (e.g., in the legs, eyes, lungs), bone disease (e.g., bone metastases, high calcium levels), high cholesterol or triglyceride (blood fat) levels, depression, diabetes, severe headaches (e.g., migraine), heart disease (e.g., 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: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.This drug should not be used with the following medications because very serious interactions may occur: aromatase inhibitors (e.g., anastrozole, exemestane), troleandomycin, tranexamic acid.If you are currently using any of these medications listed above, tell your doctor or pharmacist before starting this medication.Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: corticosteroids (e.g., prednisolone), ospemifene, tamoxifen, medication for low thyroid (hypothyroidism).Certain drugs can affect the estrogen levels in your system. Drugs that may cause this effect include: azole antifungals (e.g., itraconazole, ketoconazole), many antibiotics (e.g., cephalosporins, chloramphenicol, macrolides, penicillins, tetracyclines, sulfas), aprepitant, bexarotene, bosentan, dapsone, griseofulvin, certain HIV protease inhibitors (e.g., nelfinavir, ritonavir), modafinil, nevirapine, rifamycins (e.g., rifampin), many seizure medications (e.g., barbiturates, carbamazepine, phenytoin, primidone, topiramate), St John's wort.This document does not contain all possible interactions. Before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

                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.Laboratory tests (e.g., blood pressure, liver function tests, calcium levels) should be performed periodically to monitor your progress or check for side effects. 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 between 36-46 degrees F (2-8 degrees C) 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 medicines 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 for more details about how to safely discard your product.

                Information last revised August 2021. Copyright(c) 2021 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.

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                Formulary

                FormularyPatient Discounts

                Adding plans allows you to compare formulary status to other drugs in the same class.

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                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.