Estramustine

Indications
 Oral
Advanced prostatic carcinoma
Adult: 560-840 mg daily in divided doses, adjusted to between 140 mg and 1.4 g daily according to response and GI tolerance. Should be treated for at least 30-90 days before assessing the benefits of the treatment.
Contraindications
 Active thrombophloebitis or thromboembolic disorders. Hypersensitivity.
Warnings / Precautions
 Diabetes mellitus, CHF, epilepsy, hypertension, migraine, hepatic impairment. Increased risk of thrombosis and myocardial infarction. May exacerbate fluid retention. May affect the metabolism of calcium and phosphorus. Monitor hepatic function and bilirubin level regularly and for at least 2 mth after treatment withdrawal. Pregnancy.
Adverse Reactions
 Gynaecomastia, fluid retention and CV effects, GI disturbances, hepatic dysfunction, loss of libido, hypersensitivity reactions and occasionally leucopaenia and thrombocytopaenia.
Lab Interactions
 Certain endocrine and liver function tests may be affected. May depress testosterone levels.
Food Interactions
 Milk, dairy products or calcium-containing foods may impair oral absorption. To be taken at least 1 hr before or 2 hrs after meals.
Mechanism of Actions
 Estramustine is a combination of oestradiol and normustine which readily dephosphorylates during absorption to give estramustine, oestrone analog, oestradiol and oestrone. The oestrodiols released facilitate the uptake of the alkylating agent into the prostate cancer cells which inhibits microtubule assembly. Its effects are weaker than most alkylating agents and oestradiols.
ATC Classification
 L01XX11 - estramustine ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
Available As
  • Estramustine 140 mg

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