Adult: Initially, 560-840 mg daily in divided doses, adjusted to 140-1,400 mg daily according to response and GI tolerance. Assess for possible benefits of continued therapy after 30-90 days. Continue treatment as long as favourable response is maintained.
Active thrombophlebitis or thromboembolic disorders (except when the actual tumour mass is the cause of phenomenon); peptic ulcer, severe CV disease. Severe hepatic impairment. Pregnancy and lactation. Admin of live vaccines.
Patient w/ history of thrombophlebitis or thromboembolic disorders esp if associated w/ estrogen therapy, CV/cerebrovascular/coronary artery disease, DM, HTN, epilepsy, migraine, metabolic bone disease associated w/ hypercalcaemia. May exacerbate pre-existing or incipient peripheral oedema or congestive heart disease. Hepatic and renal impairment.
Oestrogenic effects (e.g. gynaecomastia, impotence, fluid retention, CV effects); GI disturbance, nausea, vomiting, hepatic dysfunction, loss of libido, leucopenia, thrombocytopenia. Potentially Fatal: Embolism, MI, CHF, angioedema.
Monitor BP, LFT, and Ca levels.
May increase therapeutic activity and toxicity of TCAs. Decreased absorption w/ drugs containing Ca, Mg or Al (e.g. antacids). Increased risk of angioedema w/ ACE inhibitors. Potentially Fatal: Admin of live vaccines during treatment may result in serious infections due to immunosuppression.
Milk, milk products and Ca-containing foods may impair absorption.
May affect endocrine and liver function tests.
Description: Estramustine is a complex of 17-β-estradiol and nitrogen mustard (normustine) linked by a carbamate ester. Estramustine and its oxidised isomer, estromustine, exert their cytotoxic effect by binding to tubulin and/or microtubule-associated proteins, thus inducing depolymerisation of microtubules, resulting in cellular metaphase arrest. Upon hydrolysis, estradiol is released causing a weak antiandrogen effect. Pharmacokinetics: Absorption: Incompletely (approx 75%) absorbed from the GI tract. Reduced absorption w/ food. Bioavailability: 44-75%. Time to peak plasma concentration: 2-4 hr. Distribution: Accumulates in the prostatic carcinoma tissues and plasma. Metabolism: Initially dephosphorylated in the GI tract. Hydrolysed and oxidised in the liver into estromustine, estradiol, and estrone. Excretion: Mainly via faeces; urine (<1% as estradiol and estrone). Plasma half-life: 10-20 hr.
L01XX11 - estramustine ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
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