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Common name
Femara (letrozole)
Synonyms: Letrozole, Femara
Description
Femara is indicated for the adjuvant treatment of postmenopausal women with hormone receptor positive early breast cancer.
Letrozole lowers estrogen levels in postmenopausal women, which may slow the growth of certain types of breast tumors that need estrogen to grow in the body.
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Active Ingredients:
Letrozole
Therapeutic actions:
Letrozole is a nonsteroidal competitive inhibitor of the aromatase enzyme system; it inhibits the conversion of androgens to estrogens. In adult nontumor- and tumor-bearing female animals, letrozole is as effective as ovariectomy in reducing uterine weight, elevating serum LH, and causing the regression of estrogen-dependent tumors. In contrast to ovariectomy, treatment with letrozole does not lead to an increase in serum FSH. Letrozole selectively inhibits gonadal steroidogenesis but has no significant effect on adrenal mineralocorticoid or glucocorticoid synthesis.
Letrozole inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues. Treatment of women with letrozole significantly lowers serum estrone, estradiol and estrone sulfate and has not been shown to significantly affect adrenal corticosteroid synthesis, aldosterone synthesis, or synthesis of thyroid hormones.
What is it used for?:
Letrozole is used to treat breast cancer in postmenopausal women. It is often given to women who have been taking tamoxifen (Nolvadex, Soltamox) for 5 years.
Contraindications and cautions:
Hypersensitivity to the medicine components.
Femara is contraindicated in women of premenopausal endocrine status.
Side effects:
Serious allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Less serious: hot flashes, warmth or redness in your face or chest; headache, muscle or joint pain; night sweats; weight gain; fatigue, feeling weak; nausea; or swelling in your hands, ankles, or feet.
Interactions:
Clinical interaction studies with cimetidine and warfarin indicated that the coadministration of Femara with these drugs does not result in clinically-significant drug interactions.
Coadministration of Femara and tamoxifen 20 mg daily resulted in a reduction of letrozole plasma levels by 38% on average. There is no clinical experience to date on the use of Femara in combination with other anticancer agents.
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