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Bisphosphonates are either administered orally or intravenously. They reduce bone resorption. [31] Mechanism of action: Bisphosphonate binds to the mineral component of the bone and inhibits enzymes (i.e. farnesyl-pyrophosphate synthase) responsible for bone formation, osteoclast recruitment and osteoclast function. [29] [31]
Bisphosphonates, when administered intravenously for the treatment of cancer, have been associated with osteonecrosis of the jaw (ONJ), with the mandible twice as frequently affected as the maxilla and most cases occurring following high-dose intravenous administration used for some cancer patients. Phossy jaw has been described since Victorian ...
In patients with bisphosphonates-associated ONJ, the response to surgical treatment is usually poor. [37] Conservative debridement of necrotic bone, pain control, infection management, use of antimicrobial oral rinses, and withdrawal of bisphosphonates are preferable to aggressive surgical measures for treating this form of ONJ. [38]
Nitrogen containing bisphosphonates are the current most used drugs in the class because of their potency. [15] Studies have showed that nitrogen on bisphosphonates forms hydrogen bond with threonine (Thr201) and the carbonyl part of Lysine (Lys200) on target enzyme, therefore enhancing the binding of the complex. Altering the position of ...
Etidronic acid is a bisphosphonate used to strengthen bone, treat osteoporosis, and treat Paget's disease of bone.. Bisphosphonates primarily reduce osteoclastic activity, which prevents bone resorption, and thus moves the bone resorption/formation equilibrium toward the formation side and hence makes bone stronger on the long run.
Ibandronic acid is a bisphosphonate medication used in the prevention and treatment of osteoporosis and metastasis-associated skeletal fractures in people with cancer. [4] It may also be used to treat hypercalcemia (elevated blood calcium levels). It is typically formulated as its sodium salt ibandronate sodium. [medical citation needed]
The Agency recommended that doctors who prescribe bisphosphonate-containing medicines should be aware that atypical fractures may occur rarely in the femur, especially after long-term use, and that doctors who are prescribing these medicines for the prevention or treatment of osteoporosis should regularly review the need for continued treatment ...
In the early 2000s, a link between bisphosphonate use and impaired bone physiology was noted. [3] [4] The strong inhibition of osteoclast function precipitated by bisphosphonate therapy can lead to inhibition of normal bone turnover, leading to impaired wound healing following trauma (such as dental surgery) or even spontaneous non-healing bone exposure.