What is Evista raloxifene What is a SERM and why is it effective in the treatment of osteoporosis

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Evista (raloxifene) is the only FDA-approved selective estrogen receptor modulator (SERM) for the prevention and treatment of osteoporosis in postmenopausal women. You may be more familiar with tamoxifen, a SERM used in the treatment of breast cancer. A SERM binds with some estrogen receptor sites around the body. Although raloxifene is not a hormone, it has an estrogen-like effect in some body tissues such as bone and has an estrogen-blocking effect on other tissues such as breast and uterus.

Evista increases bone mineral density, decreases the risk of fractures, and is FDA-approved for the prevention and treatment of osteoporosis in post-menopausal women. The dosage of Evista for both osteoporosis treatment and prevention is 60 mg per day taken as one tablet. Evista, unlike the bisphos-phonates, may be taken with or without food. In addition to Evista's positive effects on bone, it also decreases low-density lipoprotein (LDL) cholesterol (the "bad" cholesterol) as well as total cholesterol, but may actually increase triglyceride levels and therefore should be used with caution in women with preexisting high triglycerides. In one three-year study, the incidence of breast cancer was also decreased. Evista is currently being investigated as a way of preventing breast cancer, particularly among women with a family history of breast cancer. Evista's positive effects on bone do not last. Once treatment is stopped, bone loss will resume.

If you already have hot flashes associated with postmenopause, you may want to consider a different medication for osteoporosis.

One of the major side effects of Evista is blood clots, and for this reason it is contraindicated in women with a history of blood clots in veins or arteries. Evista can also cause hot flashes. If you already have hot flashes associated with postmenopause, you may want to consider a different medication for osteoporosis. You should not take Evista if you are on either estrogen therapy (ET) or estrogen-progestin therapy (EPT). Evista, however, might be prescribed with a bisphos-phonate by a specialist (see Question 67). An additional benefit of using Evista was noted in the Multiple Outcomes from Raloxifene Evaluation (MORE) Study in 2002. Risk of stroke and transient ischemic attacks (TIAs) was reduced by 48% after four years of treatment in postmenopausal women. It was noted at the time that the Women's Health Initiative Study of Estrogen-Progestin Therapy (EPT) showed a 41% increase in the risk of stroke when taking EPT. So, Evista may represent a good option for post-menopausal women who are not experiencing significant menopausal symptoms or are reluctant to go on ET or EPT for the prevention or treatment of osteoporosis (see Questions 64-66).

Evista is contraindicated in premenopausal women, women of childbearing age, in pregnancy, and in children, although there is a current clinical trial evaluating the effect of Evista on endometriosis in women who are aged 18 to 45. Evista should never be given during pregnancy, and only used with caution in the perimenopausal period because of the possibility of unanticipated pregnancy as its safety in pregnancy is not yet known. Evista is not FDA-approved for use in premenopausal women.

A recent three-year study of women taking 120 mg of Evista per day showed a 33% decrease in the risk for mild cognitive impairment (mental activities of thinking, learning, and memory). In this study, women taking the usual dosage of 60 mg per day did not see any improvement. The benefits were only found in those taking a double dosage (120 mg) daily. While mild cognitive impairment can be a precursor to Alzheimer's, this study did not show a reduction in cases of Alzheimer's; Alzheimer's takes longer than three years to develop. More information about Evista is in Table 12.

Maggie's comment:

I'm not sure how much bone loss my bone density test showed, but it was enough so that my doctor wanted me to go on medication. I had steadfastly resisted going on hormones when I reached menopause at age 51. I researched the medication options and chose Evista because I hoped for the benefits of estrogen without the cancer risk. I was on Evista for three years before my doctor added Fosamax because I showed even more bone loss on the next test. I was quite sure that I was getting enough calcium in my diet, but after the second bone density test I added 600 mg daily by tablet. I was encouraged to exercise vigorously several times a week. I stopped taking Evista after five years but have stayed on the Fosamax. I won't know if the Fosamax has worked until my next bone density test, which is not scheduled until later this year.

Trade Name

(Generic Name)

Most Common

[Manufacturer]

Side Effects and

How Supplied Clinical Uses

Contraindications Adverse Reactions

Evista

(raloxifene)

[Lilly]

60 mg tablets

Prevention and treatment of postmenopausal osteoporosis

Taking or using oral or topical systemic therapies containing estrogen

History of blood clots

Men and premenopausal women, women of childbearing age, children, pregnancy

Severe liver disease

Leg cramps Hot flashes

Report signs of blood clots immediately:

• pain or warmth in the legs

• shortness of breath

• coughing up blood or severe chest pain

• sudden change in vision Infection, flu-like symptoms, inflammation of mouth/throat, cough, sinusitis

Joint pain

Nausea

Weight gain

Depression

Rash

Insomnia

Stomach upset

Special

Considerations

Not an estrogen; not a hormone Taken daily

Does not increase the risk of breast or uterine cancer Risk of blood clots increased

Lowers LDL ("bad" cholesterol) levels and total cholesterol levels but can increase triglycerides and should be used with caution in women with a history of high triglyceride levels

Risk of mild cognitive impairment (a precursor to Alzheimer's) was reduced when taking 120 mg per day

If you are going to be immobile for any length of time, you should stop Evista for as long as you are immobile to prevent blood clots from forming

Because of the hot flash side effect, may want to reconsider taking if you already have moderate-to-severe hot flashes associated with postmenopause

Should be used with caution in women with liver disease or those taking cholestyramine, a medication used to reduce cholesterol and bile acids from the blood

If you are taking warfarin or Coumadin, your clinician may suggest taking tests for clotting prior to taking Evista

RDA of calcium and Vitamin D are also important for increasing BMD, both are needed on the day Evista is taken (at least 2 hours after Evista)

62. My clinician wants me to give myself injections of something called Forteo® (teriparatide), which I understand to be parathyroid hormone. Should I take it? How often would I receive an injection?

Forteo (teriparatide) is the only currently FDA-approved anabolic agent used in the treatment of osteoporosis. It actually builds bone, in contrast to antiresorptive agents, which interfere with bone resorption by slowing bone breakdown. Forteo builds new bone by increasing the number of osteoblasts (cells that build bone). And it does that in as little as three months of daily treatments.

Forteo is a synthetic form of parathyroid hormone, a naturally occurring hormone critical to bone development (see Question 9). Forteo is approved for treating postmenopausal osteoporosis in women who are at high risk for fracture and for increasing bone mass in men with primary (osteoporosis related to aging) or hypogonadal osteoporosis (osteoporosis caused by hypogonadism, inadequate function of the testes and low testosterone levels) who are at high risk for fracture. Those at high risk for fractures include men and women who have a history of osteoporotic fracture, who have multiple risk factors for fracture, for whom other therapies have not worked, or who are intolerant of other osteoporosis therapies. After clinical trials showed that Forteo increased bone density in 94% to 96% of patients and decreased the risk of spinal fractures by 65% and other fractures by 53% in women, Forteo was approved for use as described above by the FDA in late 2002. Although fracture risk was reduced in women taking Forteo, there are no completed studies of fracture risk in men.

But Forteo has some drawbacks. The FDA has required a "black-box warning" on the Forteo labeling to indicate concern that Forteo may cause osteosar-coma, a rare form of bone cancer. Although no humans developed bone cancer during clinical trials, laboratory rats did develop the disease after receiving Forteo in dosages that were 3 to 60 times higher than those used in humans. The manufacturer, Eli Lilly and Company, is funding a 10-year study to determine if Forteo does cause bone cancer in humans. Using Forteo for longer than 2 years is currently not recommended.

Injection

Given into the muscle or fat tissue or vein using a needle with a syringe attached.

Forteo is taken by self-injection each day from a pre-filled syringe-type "pen" containing about one month's worth of medication. After 28 days, the pen is discarded even if there are remaining doses. Each pen contains only 3 milliliters of fluid (a little over one half a teaspoon) and 750 micrograms of the synthetic parathyroid hormone. Although larger doses can be prescribed, the recommended daily dosage is about 20 micrograms. You must store your pen in the refrigerator. If it becomes cloudy or contains particles, do not use it. The contents of the pen should be clear and colorless. Although some people are squeamish about needles, the needle used in the pen is very, very small.

When you are prescribed Forteo, Lilly and Co. provides you with a starter kit that contains an instructional video. Occasionally patients develop redness and swelling at the injection site, which is in the fat under the skin of either the thigh or the abdomen. If redness spreads, you should report this to your clinician. The most common side effects are nausea, dizziness, and leg cramps, although other side effects such as low blood pressure, weakness, joint pain, fainting, and chest pain can occur.

Trade Name (Generic Name) [Manufacturer]

How Supplied Clinical Uses Contraindications

Forteo

(teriparatide)

[Lilly]

20 microgram daily injection from a pen-like syringe containing 3 ml

Treatment of postmenopausal osteoporosis in women at high risk for fractures; includes women with a history of osteoporotic fracture, who have multiple risk factors, who have not responded to or are intolerant of previous osteoporosis therapy

Men with primary osteoporosis or hypogonadal osteoporosis

Paget's disease

Unexplained high levels of alkaline phosphatase Children

Bone cancer or metastases to the bone

Certain bone diseases

High blood calcium levels

Pregnancy or breastfeeding

Allergy to Forteo during previous courses of treatment

Most Common

Side Effects and Special

Adverse Reactions Considerations

Dizziness Leg cramps

After each of the first few injections, may experience elevated heart rate or lightheadedness; sit or lie down if this happens; report continued symptoms to your clinician

Watch for signs of hypercalcemia: constipation, low energy, nausea, vomiting, or muscle weakness

Although no instances of bone cancer have occurred in humans, bone cancer has occurred in rats treated with very high doses

Should not be prescribed for the prevention of osteoporosis Usually reserved for use in people who have not responded to or cannot tolerate other treatments for osteoporosis Decreases risk of fracture in women Fracture risk not yet studied in men

Pen must be refrigerated but not frozen and protected from the light

Recap the pen after every use Discard safely after 28 days Rotate sites of injection

Safety of using Forteo for longer than 2 years is not known Currently being evaluated in long-term study to determine whether Forteo is linked to a rare form of bone cancer in humans (to date, only occurs in rats that are given 3 to 60 times the human dose)

RDA of calcium and Vitamin D are also important for increasing BMD; Forteo can raise calcium levels in the blood, so calcium blood levels are sometimes monitored

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