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ORGANIZATION OF CLASS

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Some of the drugs for osteoporosis have been covered elsewhere, but many of these drugs do not fit into other categories, so this chapter was created to pull this information together in one place.

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Osteoporosis is the term used for a set of diseases characterized by the loss of bone mass. It is the most common of the metabolic bone diseases and is an important cause of morbidity in the elderly.

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Pharmacological therapy is targeted toward both prevention of bone loss and treatment of established osteoporosis (increasing bone mass and reducing fractures).

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Remember that bone is constantly forming and resorbing. The rates of the remodeling vary between people, between different bones, and at different ages. Diet and exercise play a major role in maintenance of bone mass. Intake of calcium and vitamin D are critical and supplements have been used for the treatment of osteoporosis. Calcium is not well absorbed from the gut and vitamin D improves absorption. Vitamin D levels are now being tested and daily recommended intake has been increasing.

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Calcium supplementation has been shown to reduce bone loss in postmenopausal women, but not to increase bone density once lost. Calcium supplements are available in a variety of salts.

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BISPHOSPHONATES

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  • ALENDRONATE

  • ibandronate

  • risedronate

  • zoledronate

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The bisphosphonates inhibit osteoclastic activity and decrease bone turnover and resorption. They have been shown to reduce the incidence of fractures.

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These agents have been shown to improve bone mass in established osteoporosis. They are not well absorbed from the GI tract, and absorption is decreased even more by the presence of food. They bind to bone, thus having a lasting effect from a single dose. This is the basis of the once weekly or once yearly dosing now available. The half-life of alendronate in bone has been measured to be at least 10 years.

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DENOSUMAB

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Denosumab, a monoclonal antibody (but you knew that, right?), is a RANK ligand inhibitor. RANK is “receptor activator of nuclear factor-κB.” Denosumab prevents the interaction of the ligand with the receptor on cells of osteoclastic lineage. Remember that osteoclasts break down bone and activation of the RANK receptor stimulates osteoclasts. Thus blocking this receptor will inhibit bone resorption.

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PARATHYROID HORMONE

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Teriparatide, recombinant parathyroid hormone, is effective in reducing the incidence of new fractures in patients with osteoporosis.

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Parathyroid hormone was reviewed in Chapter 38. Unlike other treatments for osteoporosis, teriparatide stimulates the formation of new bone and increases bone mass. It must be given by injection.

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SELECTIVE ESTROGEN RECEPTOR MODULATORS

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These compounds were introduced in Chapter 37. The selective estrogen receptor modulators have different degrees of estrogen agonist or antagonist activity in different tissues.

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