Estramustine Phosphate Capsules BP 140 mg

Estramustine Phosphate Capsules BP 140 mg is used in palliative therapy of metastatic or progressive prostate cancer. Estramustine appears to act as a relatively weak alkylating agent and imparts a weak estrogenic activity. The estrogenic portion of the molecule acts as a carrier to facilitate selective uptake of the drug into estrogen receptor-positive cells. Because of the selective steroidal uptake, the alkylating effect of the nitrogen mustard is enhanced in these cells. Estramustine phosphate is readily dephosphorylated during absorption, and the major metabolites in plasma are estramustine, the estrone analog, estradiol, and estrone.

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Dose in Prostate Cancer
Adults

14 mg/kg/day (range, 10 to 16 mg/kg/day) in 3 to 4 divided doses for 30 to 90 days before assessing for continuation of therapy. Continue therapy as long as response is favorable.

General Advice

Administer  with water 1 h or more before or 2 h after meals.

Cardiovascular

Hypertension; CHF; edema; increased risk of cerebrovascular accident; MI, thrombosis.

CNS

Lethargy; emotional lability; insomnia.

Dermatologic

Rash; pruritus; dry skin; easy bruising.

Endocrine

Decreased glucose tolerance; breast tenderness or enlargement.

GI

Nausea; vomiting; diarrhea; anorexia; flatulence; elevated LFTs.

Genitourinary

Decreased glucose tolerance; gonadal suppression; breast tenderness; breast enlargement.

Hematologic

Leukopenia and thrombocytopenia have been reported in a small number of patients.

Musculoskeletal

Leg cramps.

Respiratory

Dyspnea.