Keywords:Bisphosphonates, Calcium balance, Bone homeostasis
Bisphosphonates are chemical-related to pyrophosphate. The oxygen atom in pyrophosphate is substituted by a carbon atom in these compounds, resulting in a P-C-P bond. They are potent antiresorptive medicines because they have a strong inhibitory effect on osteoclasts. It lowers fracture risk by reducing bone turnover, increasing bone mineral density, and decreasing fracture risk in the lumbar spine and hip. Bisphosphonates are strongly attracted to bone surfaces, where they accumulate, primarily at remodeling sites. They are rarely associated with systemic side effects due to their selectivity in action. Irritation of the upper gastrointestinal tract is the most common side effect. A strong third-generation bisphosphonate, zoledronate, is currently approved to treat postmenopausal-induced osteoporosis. This review mainly focuses on the mechanism of action, therapeutic uses, and its adverse effects.
Lambrinoudaki I, Christodoulakos G, Botsis D. Bisphosphonates. Ann N Y Acad Sci. 2006;1092:397-402.
McClung MR. Bisphosphonates. Endocrinol Metab Clin North Am. 2003;32(1):253-71.
Ebetino FH, Hogan A-ML, Sun S, Tsoumpra MK, Duan X, Triffitt JT. The relationship between the chemistry and biological activity of the bisphosphonates. Bone. 2011;49(1):20-33.
Cremers S, Papapoulos S. Pharmacology of bisphosphonates. Bone. 2011;49(1):42-9.
Ralston SH. Bisphosphonates in the management of Paget’s disease. Bone. 2020;138:115465.
Coleman RE. Bisphosphonates for the prevention of bone metastases. Semin Oncol. 2002;29(6-21):43-9.
Chapurlat R, Legrand MA. Bisphosphonates for the treatment of fibrous dysplasia of bone. Bone. 2021;143:115784.
Fleisch HA. Bisphosphonates: preclinical aspects and use in osteoporosis. Ann Med. 1997;29(1):55-62.
Fleisch H. New bisphosphonates in osteoporosis. Osteoporos Int J Establ Result Coop Eur Found Osteoporos Natl Osteoporos Found USA. 1993;3(2):S15-22.
Coleman RE. Bisphosphonates in breast cancer. Ann Oncol Off J Eur Soc Med Oncol. 2005;16(5):687-95.
Papapetrou PD. Bisphosphonate-associated adverse events. Horm Athens Greece. 2009;8(2):96-110.
Shannon J, Shannon J, Modelevsky S, Grippo AA. Bisphosphonates and osteonecrosis of the jaw. J Am Geriatr Soc. 2011;59(12):2350-5.
Miller PD. The kidney and bisphosphonates. Bone. 2011;49(1):77-81.