INDICATIONS     CONTRA-INDICATIONS     DOSAGE     SIDE-EFFECTS     PREGNANCY     OVERDOSE     IDENTIFICATION     PATIENT INFORMATION

Logo ESTRACYT® (Capsules)
SCHEDULING STATUS:
S4

PROPRIETARY NAME
(and dosage form):

ESTRACYT® (Capsules)

COMPOSITION:
Each capsule contains estramustine sodium phosphate monohydrate equivalent to estramustine phosphate 140 mg.

PHARMACOLOGICAL CLASSIFICATION:
A26 Cytostatic agents

PHARMACOLOGICAL ACTION:
Estramustine phosphate is a prodrug which is structurally composed of oestradiol and nitrogen mustard. Estramustine phosphate has weak oestrogenic and anti-gonadotrophic properties. Up to 75% of a dose is absorbed from the gastro-intestinal tract. Absorption is impaired by milk, milk products and other substances high in calcium. Estramustine is rapidly dephosphorylated during absorption into the peripheral circulation. Estramustine is then oxidised and hydrolysed to estromustine and low levels of oestradiol and oestrone. Estramustine and estromustine are excreted via the bile and faeces.

INDICATIONS:
Prostatic carcinoma in advanced stages.

CONTRA-INDICATIONS:
ESTRACYT®should not be used in patients with any of the following conditions:
- Known hypersensitivity to either oestradiol or to nitrogen mustard.
- Severe hepatic or cardiac disease.
- Active thrombophlebitis or thromboembolic disorders, including recent myocardial infarction.
- Pre-existing leukopenia and/or thromocytopenia.
- Peptic ulceration

WARNINGS:
Caution is recommended in patients with a history of thrombophlebitis, thrombosis or thromboembolic disorders, especially if they were associated with oestrogen therapy.
Caution should also be used in patients with cerebralvascular or coronary artery disease and peptic ulceration.

DOSAGE AND DIRECTIONS FOR USE:
The recommended daily dosage is 10 to 14 mg per kg body mass, given in 3 divided doses. Not more than a total of 9 capsules should be given daily. If there is no effect after 3 - 4 weeks, the treatment should be discontinued.
If there is improvement, the initial dosage should be maintained for at least three to four months, depending on the therapeutic response and the development of side-effects. The dosage should be adjusted if marked side-effects occur.
The capsules should be taken not less than one hour before or two hours after meals.
The capsules should be swallowed with water. Milk, milk products or calcium-containing drugs, (e.g. calcium-containing antacids) must not be used simultaneously with ESTRACYT capsules.

SIDE-EFFECTS AND SPECIAL PRECAUTIONS:
Gastro-intestinal disturbances (most commonly transient nausea, but vomiting, and diarrhoea also) sometimes occur at the beginning of therapy. In a few cases thrombocytopenia, leukopenia and elevated transminase/bilirubin have been noted but were completely reversible on reduction of dosage or temporary (1 - 2 weeks) withdrawal of the drug. Allergic skin rashes, oedema and anginal complaints have been reported. As with conventional oestradiol therapy, thromboembolic disorders, gynaecomastia, reduced libido and potency may occur.
Both oestradiol and nitrogen mustard are mutagenic, therefore males undergoing ESTRACYT treatment should take contraceptive measures.
Angioneurotic oedema (Quincke oedema, larynx oedema) can occur. Immediate discontinuation of ESTRACYT therapy is required.
Caution must be exercised when administered concomitantly with agents which cause bone marrow depression. Care is necessary when using ESTRACYT in the presence of infection.
Blood counts and liver function tests should be performed at regular intervals.
Fluid retention:
Conditions which might be influenced by fluid retention, such as epilepsy, migraine or renal dysfunction, require careful observation.
Exacerbation of pre-existing or incipient peripheral oedema or congestive heart disease has been seen in patients receiving ESTRACYT.
Glucose tolerance:
Because glucose tolerance may be decreased, diabetic patients should be carefully observed while receiving ESTRACYT.
Elevated blood pressure:
Because hypertension may occur, blood pressure should be monitored periodically.
Calcium/phosphorus metabolism:
ESTRACYT may influence the metabolism of calcium and phosphorus and should be used with caution in patients with metabolic bone diseases that are associated with hypercalcemia or patients with renal insufficiency.
Interactions:
Food like milk, milk products or drugs that contain calcium may impair the absorption of ESTRACYT and must not be taken simultaneously with ESTRACYT.
An interaction between ESTRACYT and ACE-inhibitors, possibly leading to increased risk of angioneurotic oedema cannot be excluded.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
There are no known cases of overdosage. By accidental overdosage the cytostatic component could have a damaging effect on the bone marrow, causing leukopenia or thrombocytopenia. Gynaecomastia and cardiac complaints may occur due to the oestradiol component. In the event of overdosage, the gastric contents must be removed by gastric lavage and symptomatic therapy initiated. Hematologic and hepatic parameters must be monitored for at least six weeks after overdosage with ESTRACYT.

IDENTIFICATION:
Off-white, opaque capsules with "Estracyt" printed on the cap and "KPh 750" printed on the body.

PRESENTATION:
Bottles or blister packs containing 40 and 100 capsules.

STORAGE INSTRUCTIONS:
Keep bottles tightly closed. Store below 25°C.
KEEP OUT OF REACH OF CHILDREN.

REGISTRATION NUMBER:
K/26/242

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
Pharmacia South Africa (Pty) Limited
Alphen West G
George Street
Midrand
1685

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
04 Jan 2000

New addition to this site: February 2005
Source: Pharmaceutical Industry

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