Adult: Doses are expressed in terms of estramustine phosphate. Recommended estramustine phosphate dose: 14 mg/kg (one 140 mg cap for each 10 kg) daily in 3 or 4 divided doses; most patients in some countries have received a dose range of 10-16 mg/kg daily. Alternative dosing recommendation: Initially, 560-840 mg daily in divided doses, may be adjusted to 140-1,400 mg daily according to response and gastrointestinal tolerance. Dosage and treatment recommendations may vary among countries and individual products (refer to specific product guidelines).
What are the brands available for Estramustine in Hong Kong?
Estracyt
Hepatic Impairment
Severe: Contraindicated.
Contraindications
Hypersensitivity to estramustine, estradiol, or nitrogen mustard. Active thrombophlebitis or thromboembolic disorders (except where tumour mass is the cause or if benefits outweigh the risks); severe CV disease, peptic ulcer. Severe hepatic impairment.
Special Precautions
Patient with history of thrombophlebitis, thrombosis, or thromboembolic disease (particularly if associated with estrogen therapy); cerebrovascular disease, CAD; conditions where fluid accumulation may be poorly tolerated (e.g. hypertension, heart failure, migraine, seizure disorder); diabetes mellitus, metabolic bone diseases associated with hypercalcaemia, osteoblastic metastases. Not indicated to be used in females. Avoid vaccination with live vaccines during treatment. Renal and mild to moderate hepatic impairment.
Adverse Reactions
Significant: Estrogenic effects (e.g. decreased testosterone level, gynaecomastia, impotence), CV effects (e.g. elevated blood pressure, heart failure); exacerbation of pre-existing or incipient peripheral oedema due to fluid retention; hepatic effects (e.g. liver enzyme and bilirubin abnormalities), decreased glucose tolerance; hypersensitivity reactions, including angioedema. Blood and lymphatic system disorders: Anaemia, leucopenia, thrombocytopenia. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, gastrointestinal disturbances. General disorders and administration site conditions: Lethargy. Nervous system disorders: Headache. Psychiatric disorders: Insomnia, loss of libido. Reproductive system and breast disorders: Breast tenderness. Respiratory, thoracic and mediastinal disorders: Dyspnoea. Potentially Fatal: Thrombosis, MI.
Patient Counseling Information
Men with female partners of childbearing potential must use effective contraception during treatment.
Monitoring Parameters
Monitor LFTs and endocrine function tests (e.g. testosterone levels) during and for 2 months after therapy; serum Ca levels, fluid status and blood pressure periodically; serum glucose (particularly in patients with diabetes). Assess for signs and symptoms of hypersensitivity reactions, endocrine adverse effects, and thromboembolic events.
Drug Interactions
May increase both the therapeutic effect and toxicity of TCAs. May decrease absorption with Ca-, Mg-, or Al-containing drugs (e.g. antacids). May increase the risk of angioedema with ACE inhibitors. Potentially Fatal: May increase the risk of serious infections with live vaccines.
Food Interaction
May decrease absorption with milk and other Ca-containing foods.
Action
Description: Mechanism of Action: Estramustine, an antimicrotubule antineoplastic agent, is an estradiol and nornitrogen mustard carbamate-linked combination. Estramustine and estromustine (its oxidised active metabolite) exert their cytotoxic effect mainly by binding to tubulin and/or microtubule-associate proteins. The binding to these proteins induces microtubule depolymerisation, leading to cellular metaphase arrest. Pharmacokinetics: Absorption: Incompletely absorbed from the gastrointestinal tract. Reduced absorption with Ca-containing foods. Bioavailability: 44-75%. Time to peak plasma concentration: 2-4 hours. Distribution: Distributed into prostatic carcinoma tissues and plasma. Metabolism: Estramustine phosphate is initially dephosphorylated in the gastrointestinal tract, then oxidated and hydrolysed in the liver to form estramustine, estromustine (the oxidised isomer of estramustine), estrone and estradiol. Excretion: Mainly via faeces; urine (<1% as conjugated estradiol and estrone). Elimination half-life: 9-23 hours (estromustine); 16.5 hours (estrone).
Chemical Structure
Estramustine Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 259331, Estramustine. https://pubchem.ncbi.nlm.nih.gov/compound/Estramustine. Accessed June 25, 2024.
Storage
Store between 2-8°C. Storage recommendations may vary among individual products or between countries (refer to specific product or local guidelines). This is a cytotoxic drug. Follow applicable procedures for receiving, handling, administration, and disposal.
L01XX11 - estramustine ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
References
Anon. Estramustine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 16/05/2024.Buckingham R (ed). Estramustine Sodium Phosphate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/05/2024.Emcyt Capsule (Pfizer Laboratories Div Pfizer Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 16/05/2024.Estracyt Capsules (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 16/05/2024.Estramustine. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 16/05/2024.Joint Formulary Committee. Estramustine Phosphate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 16/05/2024.
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