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SERMs

Selective estrogen receptor modulators (SERMs)

Selective estrogen receptor modulators (SERMs) have many of the same beneficial effects on your bones as estrogen but without some of the risks associated with the hormone.

When you reach menopause and your estrogen level decreases, your bones become less dense. Like estrogen, SERMs help build strong bones. As the name suggests, these drugs are selective in that they behave like estrogen in some parts of the body (like the bones) but not in others (like the uterus and breasts).

Tamoxifen, the first SERM developed, has been used to prevent breast cancer for many years. Raloxifene hydrochloride (Evista®) is the first SERM approved for the prevention and treatment of post-menopausal osteoporosis.

The benefits of raloxifene
Raloxifene has been shown to:

  • maintain bone density in the spine, hip and other bones
  • reduce the incidence of fractures in the spine

Side-effects
Possible side-effects include:

  • hot flashes or night sweats
  • leg cramps
  • muscle and joint aches
  • weight gain
  • vaginal dryness
  • rash

These effects may occur within the first three to six months of therapy and some of them may lessen over time.

Rare but serious side-effects include blood clots in the deep veins, called deep vein thrombosis (DVT), a risk also associated with estrogen therapy. Raloxifene should therefore be used with caution by women who are at risk for blood clots. Symptoms of DVT include:

  • swelling in the legs
  • pain or soreness
  • redness
  • sudden shortness of breath
  • chest pain that may get worse with a deep breath
  • a cough that brings up blood
  • a fast heart rate

You should not use this medication if you have a history of blood clots.

How to take raloxifene

Raloxifene may be taken with or without food at any time of the day. It is best to take the medication at the same time each day so that it becomes part of your daily routine.

If you are going to have a surgery, you should stop raloxifene at least 72 hours prior to your surgery. Similarly, you should stop it if you expect to have a prolonged period of bedrest or being immobile. You can resume taking raloxifene once you are mobile again.

What else does raloxifene do?
In addition to treating bone loss, raloxifene has a short-term impact on heart health. It has been shown to:

  • reduce levels of "bad" (or LDL) cholesterol
  • reduce levels of total cholesterol

For women who have a high risk of developing breast cancer, the drug has also been shown to lower the risk of breast cancer.

Raloxifene does not:

  • increase triglycerides
  • significantly increase levels of "good" (or HDL) cholesterol
  • stimulate the growth of the lining of the uterus, as does estrogen, and therefore, if you still have your uterus, you will not need to take additional progestins
  • lead to breakthrough bleeding
  • relieve menopausal symptoms, such as hot flashes and vaginal dryness

NOTE: raloxifene has not been tested in women who have a personal or family history of breast cancer.

Cost

Raloxifene is an expensive medication. Health coverage varies from province to province. To find out if raloxifene is covered in the province where you live, click here.

 

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Treatment

Bisphosphonates (BPs)

Selective estrogen receptor modulators (SERMs)

Hormone therapy (HT)

Calcitonin

Parathyroid hormone

Other medications

Monitoring treatment response

  • A publication of:
  • Women's College Hospital