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

No Results

     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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                Formulary

                FormularyPatient Discounts

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                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.
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                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the 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.