Brand name: Estracyt
Active ingredient (generic name): Estramustine Phosphate
Manufacturer: Pharmacia
Importer: Behestan Darou
Pharmacotherapeutic group: Anti- neoplasm
Pharmaceutical form: 140 mg Capsules
Pharmacodynamic:
Estracyt is a chemical compound of oestradiol and nitrogen mustard and it has a dual mode of action. The intact molecule acts as an anti-miotic agent; after hydrolysis of the carbamate ester, the metabolites act to bridge the released oestrogens and exert an anti-gonadotrophic effect. The low level of clinical side effects may be due to the fact that estramustine binds to a protein present in the tumour tissue, so resulting in accumulation of the drug at the target site. Estracyt also has weak oestrogenic and anti-gonadotrophic properties.
Pharmacokinetic:
Estramustine phosphate sodium is rapidly dephosphorylated in the intestine and prostate to estramustine and estromustine, which accumulate in the prostatic tissue. The plasma half-lives of these metabolites are 10 - 20 hours. Estramustine and estromustine are further metabolized before excretion.
Therapeutic indication:
It is prescribed in Carcinoma of the prostate, especially in cases unresponsive to or relapsing after, treatment by conventional oestrogens or by orchidectomy.
Estracyt is effective in patients who have not previously received drug therapy, as well as in those who have shown no response to conventional hormone treatment.
Dosage and administration:
The capsules should be taken not less than 1 hour before or 2 hours after meals. The capsules should not be taken with milk or milk products. Standard starting dosage is 4-8 capsules a day in divided doses with later adjustment according to response and gastrointestinal tolerance.
Contraindications:
Use in patients with peptic ulceration, or those with severe liver dysfunction or myocardial insufficiency and in patients hypersensitive to oestradiol or nitrogen mustard is prohibited.
Adverse reaction:
The most common adverse reactions include gynaecomastia and impotence, nausea/vomiting and fluid retention/edema, anemia, leucopenia, thrombocytopenia, confusion and depression, headache,nausea and vomiting, diarrhea (particularly during the first two weeks of treatment), fluid retention.
Pharmacokinetic interactions:
Milk, milk products or drugs containing calcium may impair the absorption of Estracyt and should not be taken simultaneously with Estracyt.
An interaction between Estracyt and ACE-inhibitors, possibly leading to an increased risk of angioneurotic oedema cannot be excluded.
Special warnings:
Use with caution in patients with moderate to severe bone marrow depression, thrombophlebitis, thrombosis, thromboembolic disorders, cardiovascular disease, coronary artery disease and congestive heart failure.
Caution should also be exercised in patients with diabetes, hypertension, epilepsy, hepatic and renal impairment and diseases associated with hypercalcaemia. Blood counts, liver function tests and serum calcium in hypercalcaemia should be performed at regular intervals. Patients with prostate cancer and osteoblastic metastases are at risk of hypocalcaemia and should have calcium levels closely monitored.
Pregnancy and lactation:
Estracyt is divided in group X since it is known that both estradiol and nitrogen mustard are mutagenic and therefore males undergoing treatment with Estracyt should employ contraceptive methods.
Storage temperature:
Estracyt should be kept in room temperature (15-25 C)
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