Letrozole

What is Letrozole?

• Letrozole (Femara) is an aromatase inhibitor which effectively blocks estrogen synthesis in postmenopausal women and is used as therapy of estrogen receptor positive breast cancer, usually after resection and after failure of tamoxifen.

Letrozole

Letrozole2DACS

What are the uses of this medicine?

Letrozole (Femara) is used for:

• Early-stage, hormone receptor–positive (HR+) breast cancer that has been treated.
• Early-stage breast cancer that has been treated with tamoxifen citrate for at least 5 years.
• Breast cancer that is locally advanced or has metastasized (spread to other parts of the body) and is HR+. It is used as the first treatment.
• Breast cancer that is locally advanced or has metastasized and it is not known whether the cancer is HR+ or hormone receptor negative (HR-). It is used as the first treatment.
• Breast cancer that has gotten worse after antiestrogen therapy. It is used as the second treatment.

How does this medicine work?

• Letrozole (let' roe zole) is a nonsteroidal aromatase inhibitor that is widely used as therapy of breast cancer, usually after surgical resection.
• Aromatase is the enzyme responsible for the conversion of testosterone to estrone (E1) and of androstenedione to estradiol (E2).
• Highest levels of aromatase are found in the ovary and placenta, which are the major sources of estrogen in premenopausal women.
• However, aromatase is also found in other tissues, such as liver, kidney, adrenals, brain, muscle and subcutaneous fat where it is also active in producing estrogens, although at low levels.
• These tissues are the major source of estrogen in postmenopausal women.
• Inhibitors of aromatase were developed to block the synthesis of estrogen in the peripheral tissues and, thus, as antiestrogen therapy of breast cancer in postmenopausal women.
• Letrozole is a nonsteroidal, specific aromatase inhibitor which has little or no effect on adrenal glucocorticoid or mineralocorticoid synthesis.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• with Pregnancy
• with Known hypersensitivity to the active substance, or to any of the excipients

What drug interactions can this medicine cause?

Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following:

• medications that contain estrogen such as hormone replacement therapy (HRT) and hormonal contraceptives (birth control pills, patches, rings, and injections); raloxifene (Evista); and tamoxifen (Nolvadex)

Is this medicine FDA approved?

• Letrozole was approved for use in postmenopausal women with estrogen receptor positive breast cancer in the United States in 1997.

How should this medicine be used?

Recommended dosage:

• The recommended dose of Femara is one 2.5 mg tablet administered once a day, without regard to meals.
• Patients with cirrhosis or severe hepatic impairment: 2.5 mg every other day.

Administration:

• Letrozole comes as a tablet to take by mouth once a day with or without food.
• Take letrozole at around the same time every day.
• You may need to take letrozole for several years or longer.
• Continue to take letrozole even if you feel well.
• Do not stop taking letrozole without talking to your doctor.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 2.5 mg tablets

This medicine is available in fallowing brand namesː

• Femara

What side effects can this medication cause?

The most common side effects of this medicine include:

• hot flashes
• arthralgia
• flushing
• asthenia
• edema
• arthralgia
• headache
• dizziness
• hypercholesterolemia
• sweating increased
• bone pain
• musculoskeletal

• Uncommon, but potentially severe side effects include decrease in bone mineral density, increases in serum cholesterol levels and embryo-fetal toxicity.

What special precautions should I follow?

• Letrozole has been associated with a low rate of serum enzyme elevations during therapy and rare instances of clinically apparent liver injury.
• Decreases in bone mineral density may occur. Consider bone mineral density monitoring.
• Increases in total cholesterol may occur. Consider cholesterol monitoring.
• Fatigue, dizziness, and somnolence may occur. Exercise caution when operating machinery.
• Femara can cause fetal harm when administered to pregnant women. Obtain a pregnancy test in females of reproductive potential. Advise females of reproductive potential to use effective contraception.
• Advise women not to breastfeed during Femara treatment and for at least 3 weeks after the last dose.
• Advise females and males of reproductive potential of the potential for reduced fertility from Femara.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• reduced motor activity
• ataxia
• dyspnea
• depressed blood pressure
• arrhythmia

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.

Can this medicine be used in pregnancy?

• Based on postmarketing reports, findings from animal studies and the mechanism of action, Femara can cause fetal harm and is contraindicated for use in pregnant women.

Can this medicine be used in children?

• The safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• LETROZOLE

Inactive ingredients:

• SILICON DIOXIDE
• FERRIC OXIDE YELLOW
• HYPROMELLOSES
• LACTOSE MONOHYDRATE
• MAGNESIUM STEARATE
• STARCH, CORN
• CELLULOSE, MICROCRYSTALLINE
• POLYETHYLENE GLYCOL
• SODIUM STARCH GLYCOLATE TYPE A POTATO
• TALC
• TITANIUM DIOXIDE

Who manufactures and distributes this medicine?

Distributed by:

• Novartis Pharmaceuticals Corporation
• East Hanover, New Jersey

What should I know about storage and disposal of this medication?

• Store at 20°C to 25°C (68°F to 77°F); excursions are permitted between 15°C and 30°C (59°F and 86°F).

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• Dailymed label info on Letrozole
• FDA Letrozole