Health and Prostate

Drug Nomenclature

Pharmacopoeias. In British.

British Pharmacopoeia 2008 (Estramustine Sodium Phosphate). A white or almost white powder. Freely soluble in water and in methyl alcohol; very slightly soluble in dehydrated alcohol and in chloroform. A 0.5% solution in water has a pH of 8.5 to 10.0. Protect from light.

Adverse Effects, Treatment, and Precautions

Oestrogenic adverse effects are fairly common, and may include gynaecomastia, fluid retention, and cardiovascular effects. Gastrointestinal disturbances, hepatic dysfunction, loss of libido, hypersensitivity reactions, and occasionally leucopenia and thrombocytopenia may occur. Estramustine is contra-indicated in patients with peptic ulceration and severe hepatic or cardiovascular disease. Diabetes mellitus may be exacerbated, and the drug should be given with care to patients with disorders such as congestive heart failure, epilepsy, hypertension, migraine, and renal impairment which may be adversely affected by additional fluid retention. Care is also required in patients with conditions predisposing to hypercalcaemia, and serum calcium should be monitored in hypercalcaemic patients.

Porphyria. Estramustine has been associated with acute attacks of porphyria and is considered unsafe in porphyric patients.

Interactions

Estramustine sodium phosphate should not be given with milk products or products high in calcium, which may interfere with its absorption. Hypersensitivity reactions including angioedema have occurred rarely in patients given estramustine who were also receiving an ACE inhibitor.

Pharmacokinetics

Up to 75% of a dose of estramustine sodium phosphate is absorbed from the gastrointestinal tract and rapidly dephosphorylated. Estramustine is found in the body mainly as its oxidised isomer estromustine; both forms accumulate in the prostate. Some hydrolysis of the carbamate linkage occurs in the liver, releasing estradiol, estrone, and the normustine group. Estramustine and estromustine have plasma half-lives of 10 to 20 hours, and are excreted with their metabolites mainly in the faeces.

Uses and Administration

Estramustine is a combination of estradiol and normustine and has weaker oestrogenic activity than estradiol and weaker antineoplastic activity than most other alky fating agents. Estramustine phosphate is given orally as the disodium salt. Doses are calculated in terms of estramustine phosphate; 108 mg of estramustine sodium phosphate is equivalent to about 100 mg of estramustine phosphate. Estramustine phosphate with meglumine has been given by intravenous injection.

Estramustine sodium phosphate is licensed for use in the treatment of advanced prostatic carcinoma. An estramustine phosphate dose of about 14 mg/kg daily in divided doses is used. The usual initial dose is 560 to 840 mg daily, which may be adjusted to between 140 mg and 1.4 g daily according to the response and gastrointestinal tolerance. It should be given not less than 1 hour before or 2 hours after meals.

Preparations

British Pharmacopoeia 2008: Estramustine Phosphate Capsules.

Proprietary Preparations

Argentina: Amsupros †; Estracyt;

Austria; Estracyt;

Belgium: Estracyt;

Canada: Emcyt;

Chile: Estracyt;

Czech Republic: Estracyt;

Denmark: Estracyt;

Finland: Estracyt;

France: Estracyt;

Germany; cellmustin; Estracyt; Medactin; Multosin; Prostamustin †;

Greece: Estracyt;

Hong Kong; Estracyt;

Hungary: Estracyt;

India: X-Trant;

Ireland: Estracyt;

Israel: Estracyt;

Italy: Estracyt;

Japan: Estracyt;

Malaysia: Estracyt †;

Mexico: Emcyt;

The Netherlands: Estracyt;

Norway: Estracyt;

Poland: Estracyt;

Portugal: Estracyt;

Russia: Estracyt;

South Africa: Estracyt;

Singapore: Estracyt;

Spain: Estracyt;

Sweden: Estracyt;

Switzerland: Estracyt;

Turkey: Estracyt;

United Kingdom (UK): Estracyt;

United States of America (USA): Emcyt;

Venezuela: Estracyt.

ESTRAMUSTINE

(ess-tra-MUSS-teen)

Other Names for this Medication: Emcyt, Estracit(Brand Names)

Appearance

White capsules containing 140mg Estramustine.

Why this Medication is Used

Estramustine is used to treat prostate cancer.

How do you take this Medication

Estramustine capsules are swallowed with a full glass of water, on an empty stomach (I hour before or 2 hours after eating). DO NOT open capsules. Calcium containing products (such as milk, dairy products, or antacids containing calcium) should not be taken at the same time as Estramustine.

Precautions

• Estramustine should not be used if you are trying to father a child. It is important to discuss with your doctor the possibility that this medication may cause sterility, if you plan to have children in the future. It is also important to discuss birth control methods with your doctor (Note: birth control pills alone are not recommended as the birth control method).

• Tell your doctor if you are taking any other medications. Drugs containing calcium should NOT be taken at the same time as Estramustine. Medications for high blood pressure, called ACE inhibitors (such as the medications Captopril, Enalapril, or Lisinopril) may also cause problems if taken with Estramustine.

• Tell your doctor if you have asthma, epilepsy, migraine, mental depression, blood clots, stroke, kidney disease, chickenpox, shingles, diabetes, gallbladder disease, jaundice, or stomach ulcer. Any of these conditions could affect therapy with this medication.

• If you smoke, your doctor may advise you to quit while taking Estramustine. Smoking may interact dangerously with this medication, harming your blood vessels.

• This medication may have to be taken for several months to be effective.

• Store capsules in a cool place between temperatures of 2 to 25°C (may be kept in the fridge, but do not freeze), and protected from light. Keep out of the reach of children.

For more information on this medication, please call your doctor, pharmacist or nurse.