Thursday, 11th March 2010

steroid-profiles

Fareston-Toremifene Citrate

Fareston-Toremifene Citrate

Fareston, which is used in the treatment of breast cancer in post-menopausal women, is a Selective Estrogen Receptor Modulator (SERM) that works by exerting estrogen antagonisitic effects in tissues such as breast tissues. The FDA-approved drug for treating breast cancer is derived from triphenylethelyne. Scientists are of the view that this drug can also be used to treat prostate cancer as well.

This drug is a nonsteroidal antiestrogen and its inactive ingredients are lactose, povidone, starch, sodium strach glycolate, colloidal silicon dioxide, and magnesium stearate. Available in the form of tablets, this drug can be taken only in an oral form. Each Fareston tablet includes 88.5 mg of toremifene citrate, which is equivalent to 60 mg of toremifene.

Action Mechanism

Toremifene binds to estrogen receptors and is a derivative of nonsteroidal triphenylethylene and has an ability to exert estrogenic and/or anti-estrogenic activities. The exertion is dependent upon duration of treatment, gender, target organ, animal species, or selected endpoint.

In general terms, the derivatives of nonsteroidal triphenylethylene are found to be predominantly antiestrogenic in humans and rats, and estrogenic in mice. The anti-tumor effect of Toremifine in breast cancer is believed to be primarily because of its distinctive ability with estrogen to bind the sites of cancer and blocking growth-stimulating estrogen effects in the tumor.

Contraindications

This FDA-approved drug is contraindicated in patients with a known hypersensitivity to the drug.

Warnings

Hypercalcemia and tumor flare have been reported in the past among patients with bone metastases during initial weeks of Fareston treatment. It has also been reported, though not medically proven, that patients suffering from breast cancer who undergone Fareston treatment developed endometrial cancer. Moreover, this drug is not recommended for pregnant women.

Precautions

Thromboembolic patients and patients suffering from preexisting endometrial hyperplasia should not be treated with doses of Fareston. Patients with bone metastases are required to be kept under strict medical attention for hypercalcemia during early treatment weeks.

Adverse Reactions

Some of the possible adverse reactions of this drug are depression, nausea, fatigue, vomiting, pulmonary embolism, thrombophlebitis, cardiac failure, myocardial, anorexia, and arthritis.

Over-dosage

High doses of Fareston when administered to rats showed signs of lethality leading to an interference with digestion and adrenal enlargement.

Dosage and Administration

The recommended dosage of this drug is 60 mg once a day, in oral form.

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