Emcyt (Estramustine Sodium Phosphate)

EMCYT®

Pharmacia & Upjohn

Estramustine Sodium Phosphate

Antineoplastic

Action And Clinical Pharmacology: Estramustine has a dual mode of action. The intact molecule acts as an antimitotic agent and after hydrolysis of the carbamate ester bridge the released estrogens exert an antigonadotrophic effect. The low level of clinically manifested side effects may be due to the fact that estramustine binds to a protein present in the tumor tissue, which results in an accumulation of the drug at the target site.

Indications And Clinical Uses: The treatment of metastatic prostatic carcinoma (stage D) in patients whose disease is refractory to hormonal therapy. Estramustine may produce either a stabilization or regression of the disease process and improvement in ability to function.

Contra-Indications: In patients with any of the following conditions: known hypersensitivity to either estradiol or to nitrogen mustard, severe hepatic or cardiac disease or active thrombophlebitis or thromboembolic disorders.

Manufacturers’ Warnings In Clinical States: Caution: Estramustine is a potent drug and should be prescribed only by physicians experienced with cancer chemotherapeutic drugs (see Precautions). Blood counts, as well as renal and hepatic function tests, should be performed regularly. Discontinue the drug if abnormal renal or hepatic function is seen. Capsules should not be opened.

Estramustine should be used with caution in patients with a history of thrombophlebitis, thrombosis or thromboembolic disorders, especially if associated with estrogen therapy. Caution should also be used in patients with cerebral vascular or coronary artery disease.

Angioneurotic edema has been reported in few cases during estramustine therapy, with or without concomitant medication.

Glucose Tolerance: Because glucose tolerance may be decreased, diabetic patients should be carefully observed while receiving the drug.

Elevated Blood Pressure: Because hypertension may occur, blood pressure should be monitored periodically.

Precautions: Estramustine should be administered by individuals experienced in the use of antineoplastic therapy. Professional staff administering estramustine should exercise particular care to prevent spillage and contact with the drug. Should skin contact occur, the area should be vigorously washed with soap and cold water and material used for cleansing disposed of by incineration.

Exacerbation of pre-existing or incipient peripheral edema or congestive heart disease has been seen in some patients receiving estramustine therapy. Other conditions which might be influenced by fluid retention, such as epilepsy, migraine, or renal dysfunction, require careful observation.

Estramustine may be poorly metabolized in patients with impaired liver function and should be administered with caution in such patients.

Because estramustine may influence the metabolism of calcium and phosphorus, it should be used with caution in patients with metabolic bone diseases that are associated with hypercalcemia or in patients with renal insufficiency.

Although testing by the Ames method failed to demonstrate mutagenicity for estramustine, it is known that both estradiol and nitrogen mustard are mutagenic. Patients should therefore be advised to use contraceptive measures during therapy with estramustine.

Laboratory Tests: Certain endocrine and liver function tests may be affected by estrogen-containing drugs. Abnormalities of hepatic enzymes and of bilirubin have occurred in patients receiving estramustine, but have seldom been severe enough to require cessation of therapy. Such tests should be done at appropriate intervals during therapy and repeated 2 months after the drug has been withdrawn.

Food/Drug Interactions : Food like milk, milk products or drugs which contain calcium or other polyvalent ions may impair the absorption of estramustine and must not be taken simultaneously with estramustine.

Angioneurotic edema has been reported in few cases when estramustine was administered concomitantly with ACE-inhibitors.

Adverse Reactions: Gastrointestinal disturbances (most commonly transient nausea, but occasionally vomiting, and rarely diarrhea) sometimes occur at the beginning of therapy. In a few cases thrombocytopenia, leukopenia and elevated transaminases/bilirubin have been noted but were completely reversible on reduction of dosage or temporary (1 to 2 weeks) withdrawal of the drug. A few cases of allergic skin rashes, edema and anginal complaints have been reported. A few cases of angioneurotic edema have been reported during estramustine therapy, with or without concomitant medication. As when after conventional estradiol therapy, thromboembolic disorders, gynecomastia, reduced libido and potency may occur.

Symptoms And Treatment Of Overdose: Symptoms and Treatment: There has been no experience, to date, with overdoses of estramustine. In the event of overdosage, treatment should be symptomatic and supportive. Gastric lavage should be performed and measures taken to encourage diuresis. Hematologic and hepatic parameters should be monitored for at least 6 weeks after overdosage of estramustine.

Dosage And Administration: The recommended dose of estramustine is 14 mg/kg of body weight/day (i.e., one 140 mg capsule for each 10 kg), given in 3 or 4 divided doses. Most patients have been treated at a dose range of 10 to 16 mg/kg/day.

Treatment for at least 30 days is recommended before assessing the benefits of therapy and may be continued as long as a favorable response lasts. Some patients have been maintained on therapy for more than 2 years at doses ranging from 10 to 16 mg/kg of body weight/day.

The capsules should be taken at not less than 1 hour before or 2 hours after meals.

The capsules should be swallowed with a glass of water. Milk, milk products or calcium containing drugs (such as calcium-containing antacids) must not be used simultaneously with estramustine capsules.

Availability And Storage: Each white, opaque, hard gelatin capsule contains: estramustine sodium phosphate 140 mg. Nonmedicinal ingredients: gelatin capsule, isopropanol, magnesium stearate, silica and sodium laurylsulfate. Bisulfite-, gluten-, lactose- and tartrazine-free. Bottles of 100. Store at 2 to 25°C.

EMCYT® Pharmacia & Upjohn Estramustine Sodium Phosphate Antineoplastic

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