Letrozole-Femara

Letrozole-Femara: Effective Drug against Breast Cancer.

Letrozole (Femara) is an effective drug that is known as an aromatase enzyme inhibitor. This means that it has the capability to block the production of estrogen in the female ovary. The blockage then leads to an increased secretion of FSH from the pituitary to stimulate the ovary for follicle development needed for ovulation.

In a sense, it acts like Clomid by inducing ovulation in women who are unable to ovulate on their own.

Chemical Composition

It has a chemical formula of C17H11N5 and name of 4-[(4-cyanophenyl)-(1,2,4-triazol-1-yl)methyl]benzonitrile and molecular weight of 285.303. It has an elimination half life of 2-4 days and is available in an oral form (film coated tablet).

Its inactive ingredients are magnesium stearate, sodium starch glycolate, colloidal silicon dioxide, hydroxypropyl methylcellulose, ferric oxide, lactose monohydrate, maize starch, polyethylene glycol, titanium dioxide, talc, and microcrystalline cellulose.

Action Mechanism

Letrozole, which is a nonsteroidal competitive inhibitor of the enzyme system (aromatase), inhibits the process of conversion from androgens to estrogens. It does not cause an increase in serum FSH in adult non-tumor and tumor-bearing females. It is known to inhibit gonadal steroidogenesis in a selective manner; it also inhibits the aromatase enzyme to the heme of cytochrome P450 sub-unit of the enzyme by via competitively binding.

Benefits of Letrozole-Femara

Letrozole-Femara is advisable for extended adjuvant treatment purposes in cases of early breast carcinoma (cancer) in postmenopausal women who have already been administered with standard adjuvant tamoxifen therapy. This highly potent estrogen suppressor is also recommended as a first-line treatment option in postmenopausal females with hormone dependent advanced breast carcinoma. It offers an extended protection to patients by reducing overall recurrence 42% versus placebo (P=0.00003), 52% in node-negative patients, and 39% in node-positive patients.

It is also used by bodybuilders to effectively reduce the levels of estrogen and proves to be an excellent option for all those who are prone to side-effects of estrogen such as gynecomastia and water retention while using anabolic-androgenic steroids. Its ability offer a ripped look to the user is also one of the many factors that bodybuilders endorse it.

Letrozole-Femara promotes the growth & development of secondary sexual characteristics of women. It helps in accelerating metabolism of the body and fat burning. It is also useful in increasing the levels of HDL and triglyceride besides reducing the level of LDLD. Letrozole-Femara also increases the hepatic production of binding proteins and growth hormones and cortisol.

Recommended Dosage of Letrozole-Femara

The recommended dosage of Letrozole-Femara is 2.5 mg once on a daily basis. It can be taken with cimetidine and warfarin, without regard to meals. It needs to be taken for a minimum period of 60 days to enjoy a steady blood plasma level.

Storage Conditions

Letrozole must be kept away from heat, direct light, and moisture. It must be stored at 25°C (77°F) with excursions permitted to 15-30°C (59-86°F).

Contraindications

The usage of Letrozole-Femara is contraindicated for people with a known hypersensitivity to letrozole or excipients. It is also not recommended for women who are pregnant or breast feeding their child. Letrozole-Femara is also not advised to women in a premenopausal endocrine status.

Possible Adverse Reactions

Some of the possible adverse reactions after the administration of Letrozole-Femara are nausea, fatigue, hot flushes, vomiting, bone pain, alopecia, pulmonary embolism, increased sweating, dizziness, increase in appetite, and diarrhea.