Anastrozole is a prescription tablet used to treat breast cancer in women who have been through menopause. Each tablet contains 1 mg of the active ingredient. Anastrozole belongs to a group of medicines called non-steroidal aromatase inhibitors. It lowers the amount of oestrogen (also spelled estrogen), a female hormone that many breast cancers need in order to grow. Doctors use it after surgery for early hormone receptor-positive breast cancer, as a first treatment for breast cancer that has spread, and for advanced breast cancer that has grown after tamoxifen treatment. It is usually taken once a day for several years.
Anastrozole is a hormone-lowering medicine for breast cancer in women past menopause. Many breast cancers are "hormone receptor-positive". This means the cancer cells carry docking points (receptors) for oestrogen, and oestrogen helps them grow. After menopause, the ovaries stop making oestrogen. The body still makes a small amount in other tissues, using an enzyme called aromatase. Anastrozole blocks this enzyme, so oestrogen levels fall sharply. With less oestrogen, hormone-sensitive cancer cells can slow down or stop growing.
Most women who take Anastrozole have already had surgery, radiotherapy or sometimes chemotherapy. In this setting it is an add-on (adjuvant) treatment that helps stop the cancer from coming back. It is also used as a first treatment for breast cancer that has spread to nearby tissue or to other parts of the body, and for advanced breast cancer that has grown after tamoxifen. Women whose cancer is oestrogen receptor-negative rarely respond to it.
Anastrozole comes as a small film-coated tablet taken by mouth once a day, with or without food. It stays in the body for a long time, with an average half-life of about 50 hours, so one tablet a day keeps oestrogen levels low around the clock. Treatment for early breast cancer often lasts 5 years, and sometimes longer if your specialist advises it.
The US label says Anastrozole does not work in women with breast cancer who have not yet gone through menopause, because their ovaries are still the main source of oestrogen. NHS says it is mainly prescribed after menopause, but a specialist may also use it to treat breast cancer in younger women before menopause, or in men. If your specialist has prescribed it for you in one of these situations, keep taking it as directed and ask them any questions you have. Tell your doctor if you are still having periods or are not sure whether you have been through menopause.
Because lower oestrogen affects the whole body, Anastrozole needs regular medical follow-up. It can thin the bones and raise cholesterol, and in women who already have heart disease it has been linked to more heart problems than tamoxifen. Your doctor will usually check your bone density and cholesterol during treatment. Do not stop taking it without talking to your doctor first, unless you have signs of a serious skin or liver reaction (see Side Effects).
Anastrozole is approved for the following uses in women who have been through menopause:
Other uses: NHS and MedlinePlus note that specialists sometimes prescribe Anastrozole to lower the chance of breast cancer in women past menopause who have a medium or high risk, for example because of their family history. This is not one of the uses listed on the US label. NHS also says it can be used to treat breast cancer in men and in younger women before menopause.
Common Side Effects (Usually Mild and may lessen with continued use)
Many of these feel like menopause symptoms, and NHS guidance says they usually improve during the first months of treatment.
Serious Side Effects (Seek Urgent Medical Attention)
Many breast cancers use oestrogen as a growth signal. The cancer cells have receptors, which work like locks, and oestrogen acts like the key that switches on their growth.
After menopause, the ovaries no longer make oestrogen. The body still makes some, though. An enzyme called aromatase (an enzyme is a protein that speeds up a chemical change in the body) turns hormones called androgens, mainly androstenedione and testosterone, into the oestrogens oestrone and oestradiol. This happens in tissues around the body and in the cancer tissue itself.
Anastrozole is a selective, non-steroidal aromatase inhibitor. "Inhibitor" means it blocks the enzyme. "Selective" means it targets aromatase without switching off the other hormone-making steps in the adrenal glands, so levels of cortisol and aldosterone stay normal. "Non-steroidal" means its chemical structure is not built like a steroid hormone.
With aromatase blocked, much less oestrogen is made, and hormone-sensitive cancer cells lose their main growth signal. In studies, the usual daily dose lowered oestradiol by about 70% within 24 hours and by about 80% after 14 days. Oestrogen stayed low for up to 6 days after the last dose.
Anastrozole is absorbed well from the gut. With daily use, blood levels settle at a steady level after about 7 days. The liver breaks down about 85% of it, and only about 10% leaves the body unchanged in the urine. Its main breakdown product (triazole) has no effect of its own.
In women who have not reached menopause, the ovaries make most of the oestrogen, and aromatase in other tissues is only a small source. That is why Anastrozole is not expected to lower oestrogen in these women.
Anastrozole can harm an unborn baby, based on animal studies and the way it works, and it should not be used during pregnancy. If you are able to become pregnant, the US label advises a pregnancy test before starting, and effective birth control during treatment and for at least 3 weeks after the last dose. Some women find their periods come back while taking it; if this happens, use reliable contraception and tell your doctor. Tell your doctor straight away if you become pregnant or think you might be.
Do not breastfeed while taking Anastrozole and for at least 2 weeks after the last dose. It is not known if it passes into breast milk, and it affects hormones that may affect how a baby develops.
There is no evidence that drinking alcohol causes problems with Anastrozole. Some people get hot flushes or redness of the skin when they drink alcohol, and cutting down may help.
Anastrozole can make some people feel very tired or dizzy. If this happens, do not drive, ride a bike or use tools or machines until you feel better.
Only about 10% of Anastrozole leaves the body through the kidneys, and the US label says no dose change is needed for kidney problems. Tell your doctor before starting if you have severe kidney disease.
No dose change is recommended for mild to moderate liver problems. Anastrozole has not been studied in severe liver disease, so tell your doctor if you have serious liver problems. Rarely, it can cause liver inflammation.
Anastrozole is not meant for children. In studies in teenage boys with breast enlargement (gynaecomastia) and young girls with a rare condition called McCune-Albright syndrome who had started puberty too early (precocious puberty), it did not show a benefit.
Age does not change how the body handles Anastrozole, and no dose change is needed for older women. In the main early breast cancer study, the extra benefit over tamoxifen appeared smaller in women aged 65 and over than in younger women, so your doctor will consider your age when choosing treatment.
Do not take Anastrozole if you have ever had an allergic reaction to it or to any of its ingredients. Some brands contain lactose, so tell your doctor if you cannot have lactose. Swelling of the face, lips, tongue or throat, trouble breathing, hives or itching need emergency help.
Always tell your doctor or pharmacist about every medicine, vitamin, herbal remedy and supplement you take.
Get emergency help or contact your doctor straight away if you have:
Therapeutic Class
Anticancer (hormonal therapy for breast cancer)
Action Class
Non-steroidal aromatase inhibitor
Chemical Class
Triazole derivative
Habit Forming
No
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