Used to Treat Osteoporosis

The bisphosphonates are used to treat osteoporosis in postmenopausal women, Paget s disease of the bone, and postoperative treatment after total hip replacement (etidronate). 

Calcium, phosphorus and vitamin D are needed for formation of bones and teeth. Supplements containing calcium, fluoride and vitamin D are commonly used to treat osteoporosis, and some American physicians recommend Turns as an inexpensive source of calcium. Calcium is needed also for formation of milk, maintaining correct heart rhythm, and conversion of fibrinogen into fibrin to form blood clots. Calcium salts are sometimes administered to promote blood clotting. 

Alendronate (4-amino-l-hydroxybutane-l,l-biphosphonic acid) is a biphosphonate drug used to treat osteoporosis and Paget s disease. U.S. 4,621,077 to Istituto Gentili describes the preparation of the API. Estimate the cost of production of the API by the method of Example 3. 

Drugs currently used to treat osteoporosis are classified into those that inhibit osteoclastic bone resorption (including bisphos-phonates, denosumab, and selective estrogen receptor modulators) and those that stimulate bone formation by osteoblasts (parathyroid hormone and derivatives, such as teriparatide). Strontium ranelate may have a dual effect. Other drugs being tested in clinical trials include inhibitors of cathepsin K (an osteoclastic enzyme critical for bone resorption) and of sclerostin (a negative modulator of the Wnt pathway) [21],... 

Bisphosphonates are the best therapeutic choice for patients with glucocorticoid-induced osteoporosis. Bisphosphonates generally produce greater BMD increases than do other agents used to treat osteoporosis. They increase spine (4.3%) and femoral neck (2.1%) BMD, but to a lesser extent than in bisphosphonate users who do not take glucocorticoids. They also likely reduce the risk of vertebral fractures by approximately 50%. ... 

CCRIS 7129 Keoxifene LY-139481 Raloxifene Raloxifene Raloxifenum. Antiosteoporotic antiesiro-genic. Used to treat osteoporosis. Crystals mp = 146147° km = 290 nm (c 34000 EtOH). EliU/ly 4 Co. 

Many of the enzymes in the sterol biosynthesis pathway have selective-inhibitors (Fig. 3). These include some extremely important classes of drugs such as Statins , used to treat high cholesterol, bisphosphonates, used to treat osteoporosis, allylamines (e.g., terbinafine) and azoles used to treat fungal infections, and morpholines which are used as fungicidal agrochemicals. 

In Japan, osteoporosis is currently treated with active form of vitamin D3 (Orimo et al., 1994 Schacht, 1999), estrogen (Lufkin et ah, 1992 Weinstein et al., 2003), calcitonin (Body, 2002 Kopaliani, 2005), ipriflavone (Nakamura et al., 1992), vitamin K2 (Sakamoto et al., 2005 Steven et al., 2005), bisphosphonate (Hamdy et al., 2005 Matsumoto, 2004 Perez-Lopez, 2004), and related compoimds. However, although these drugs are used to treat osteoporosis, they caimot prevent it. In addition, some of... 

Fosamax is used to treat osteoporosis, a condition characterized by decreased bone density. Under normal conditions, the rate of bone formation and the rate of bone resorption (breakdown) are carefully matched. In osteoporosis, resorption is faster than formation, so bone is nibbled away, causing bones to become fragile (they actually start to resemble honeycombs). Fosamax goes specifically to the sites of bone resorption and inhibits the activity of cells responsible for resorption. Studies have shown that normal bone is then formed on top of Fosamax, and the rate of bone formation becomes faster that the rate of its breakdown. (Trade name labels in this book are green.)... 

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