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.
Suy gan
Severe: Contraindicated.
Chống chỉ định
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.
Thận trọng
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.
Tác dụng không mong muốn
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.
Chỉ số theo dõi
Monitor BP, LFT, and Ca levels.
Tương tác
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.
Tương tác với thức ăn
Milk, milk products and Ca-containing foods may impair absorption.
Ảnh hưởng đến kết quả xét nghiệm
May affect endocrine and liver function tests.
Tác dụng
Description: Mechanism of Action: 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.
Tài liệu tham khảo
Anon. Estramustine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 12/07/2016.Buckingham R (ed). Estramustine Sodium Phosphate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com/. Accessed 12/07/2016.Emcyt Capsule (Pharmacia and Upjohn Company). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 12/07/2016.Joint Formulary Committee. Estramustine Phosphate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/07/2016.McEvoy GK, Snow EK, Miller J et al (eds). Estramustine Phosphate Sodium. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com/mc/ahfs/current/. Accessed 12/07/2016.