Osteoporosis (cont.)
Medications that prevent bone loss and breakdown
Currently, the most effective medications for
osteoporosis that are approved by the FDA are anti-resorptive
agents, which prevent bone breakdown. The bone is a living dynamic structure; it
is constantly being removed (resorbed) and rebuilt. This process is an essential
part of maintaining the normal calcium level in the blood and serves to repair
tiny cracks in the bones that occur with normal daily activity. Osteoporosis
results over time when the rate of bone resorption exceeds that of bone rebuilding. Anti-resorptive
medications inhibit bone removal (resorption), thus tipping the balance in favor
of bone rebuilding and increasing bone density. Menopausal estrogen hormone therapy is
one example of an anti-resorptive agent. Others include alendronate
(Fosamax),
risedronate (Actonel), raloxifene (Evista), ibandronate (Boniva), calcitonin
(Calcimar), and the recently approved zoledronate (Reclast).
Bisphosphates
Bisphosphonates decrease the risk of hip fracture, wrist
fracture, and spine fracture in postmenopausal women
osteoporosis.
To reduce side effects and to enhance absorption of the
medicine, all bisphosphonates taken by mouth (orally) should be taken in the morning, on an empty
stomach, thirty minutes before breakfast, and with at least 8 ounces (240 ml) of
water (not juice). Taking the pill sitting or standing minimizes the chances of
the pill being lodged in the esophagus. Patients should also remain upright for
at least 30 minutes after taking the pill to avoid reflux of the pill into the esophagus. Newer intravenous bisphosphonates, such as ibandronate (Boniva) and zoledronate (Reclast) avoid these potential gastrointestinal problems.
Food, calcium, iron supplements, vitamins with minerals, or antacids containing calcium, magnesium,
or aluminum can reduce the absorption of oral bisphosphonates, thereby resulting in
loss of effectiveness. Therefore, oral bisphosphonates should be taken with plain
water only in the morning before breakfast. Also, no food or drink should be
taken for at least 30 minutes afterwards.
Alendronate (Fosamax)
Alendronate (Fosamax) is a biphosphonate
anti-resorptive medication. Alendronate is approved for the prevention and
treatment of postmenopausal osteoporosis as well as for osteoporosis that is
caused by cortisone-related medications (glucocorticoid-induced osteoporosis).
Alendronate has been shown to increase bone density and reduce fractures in
the spine, hips, and arms. Alendronate is taken by mouth once-a-week to
prevent and treat postmenopausal osteoporosis. Alendronate is the first
osteoporosis medication also approved for increasing bone density in men with
osteoporosis, either in a daily or a weekly dose schedule.
Alendronate is generally well tolerated with few side
effects. One side effect of alendronate is irritation of the esophagus (the
food pipe connecting the mouth to the
stomach). Inflammation of the esophagus (esophagitis) and ulcers of the
esophagus have been reported infrequently with alendronate use. For more, please
read the Fosamax drug
information article.
Risedronate (Actonel)
Risedronate
(Actonel) is another bisphosphonate anti-resorptive medication. Like
alendronate, this drug it is approved for the prevention and treatment of
postmenopausal osteoporosis as well as for osteoporosis that is caused by
cortisone-related medications (glucocorticoid-induced osteoporosis). Risedronate
is chemically different from alendronate and has less likelihood of causing
esophagus irritation. Risedronate is also more potent in preventing the
resorption of bone than alendronate. For more,
please read the Actonel drug information article.
Ibandronate (Boniva)
Ibandronate (Boniva) is an oral bisphosphonate for prevention and treatment of postmenopausal
osteoporosis. It is available in both daily and monthly oral formulas as well as intravenously every three months.
For more, please read the
Boniva drug information article.
Zoledronate (Reclast)
Zoledronate (Reclast) is a unique yearly intravenous bisphosphonate anti-resorptive medication. This formulation seems to have very good bone strengthening ability by increasing bone density as well as significant fracture prevention both for spinal bone and bones away from the spine. Its convenience as given only once a year are obvious. As with all bisphosphonates, patients taking zoledronate (Reclast) must be loaded with adequate calcium and vitamin D prior to and after taking the medication for optimal results. Generally patients are given acetaminophen the day of the infusion and for several days afterward to prevent occasional minor muscle and joint aching. The infusion lasts approximately 20-30 minutes.
Selective estrogen receptor modulators (SERMs)
Raloxifene (Evista)
Raloxifene (Evista) belongs to a class of drugs called selective
estrogen receptor modulators (SERMs). SERMs work like estrogen in some tissues
but as an anti-estrogen in other tissues. The SERMs are developed to reap the
benefits of estrogen while avoiding the potential side effects of estrogen.
Thus, raloxifene can act like estrogen on bone, but as an anti-estrogen on the
lining of the uterus.
The first SERM to reach the market was tamoxifen, which
blocks the stimulative effect of estrogen on breast tissue. Tamoxifen has
proven valuable in women who have had
cancer in one breast in preventing
cancer in the second breast. Raloxifene is the second SERM to be approved by
the FDA. Raloxifene has been approved for the prevention and treatment of
osteoporosis in postmenopausal women. In a three year study involving some 600
postmenopausal women, raloxifene was found to increase bone density and lower
LDL cholesterol,
while having no stimulative effect on the uterine lining (which means that it is
unlikely to cause uterine cancer).
Because of its anti-estrogen effects, the
most common side effects with raloxifene are hot flashes . Conversely, because of
its estrogenic effects, raloxifene increases the risk of blood clots, including
deep vein thrombosis (DVT) and pulmonary embolism (blood clots in the lung).
The greatest increase in risk occurs during the first 4 months of use.
Patients taking raloxifene should avoid prolonged periods of immobility during
travel, when blood clots are more prone to occur. The risk of deep vein
thrombosis with raloxifene is
probably comparable to that of estrogen, about 2 to 3 times higher than the
usual low occurrence rate. Raloxifene decreases the risk of spine fractures in
postmenopausal women with osteoporosis, but the benefit in decreasing hip
fracture risk is not yet known. (The only agents that are definitely proven to
decrease hip fracture risk are bisphosphonates.) For more, please read the
Evista drug information
article.
Calcitonin (Calcimar, Miacalcin)
Calcitonin (Calcimar,
Miacalcin) is a hormone that has been approved by the FDA in the United States
for treating osteoporosis. Calcitonins come from several animal species, but
salmon calcitonin is the one most widely used. Calcitonin can be administered as
a shot under the skin (subcutaneously) or into the muscle (intramuscularly), or
inhaled nasally (intranasally). Intranasal calcitonin is the most convenient of
the three methods.
Calcitonin has been shown to prevent bone loss in
postmenopausal women. In women with established osteoporosis, calcitonin has
been shown to increase bone density and strength in the spine only.
Calcitonin
is not as effective in increasing bone density and strengthening bone as
estrogen and the other anti-resorptive agents. In addition, it is not as
effective in reducing spine fracture risk, and has not been proven effective in
reducing hip fracture risk. Therefore, calcitonin is not the first choice of
treatment in women with established osteoporosis. Nevertheless, calcitonin is a
helpful alternative osteoporosis treatment for patients who cannot tolerate
other medications.
Common side effects of either injected or nasal spray
calcitonin are nausea and flushing. Patients using Miacalcin Nasal Spray can
develop nasal irritations, a runny nose, or nosebleeds. Injectable calcitonin
can cause local skin redness at the site of injection, skin rash, and flushing.
For more, please read the
Calcitonin drug information article.
Teriparatide (Forteo)
Teriparatide (Forteo) is a synthetic version of the human
hormone, parathyroid hormone, which helps to regulate calcium metabolism. It promotes the growth of
new bone, while the other osteoporosis medications improve bone density by
inhibiting bone resorption. Teriparatide (Forteo) is self-injected into the
skin. Because long-term safety is not yet established, it is only FDA-approved
for 24 months of use. It reduces spine fractures in women with known
osteoporosis, but reduction of hip fracture risk is currently unproven. For
more, please read the Forteo
drug information article.
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