Alendronate: Difference between revisions
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[[Alendronate]] (''Fosamax'') is commonly known for its use in treatment and prevention of osteoporosis in postmenopausal women and men, but is also used to treat Paget's disease (disease that results in deformed and enlarged bones).<ref>http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000018/</ref> Alendronate belongs to the class of nitrogen-containing bisphosphonates, which are inorganic pyrophosphate analogues. | [[Image:220px-Alendronate sf.png|thumb|left|200px|Structure of Alendronate]][[Alendronate]] ('''Fosamax''') is commonly known for its use in treatment and prevention of osteoporosis in postmenopausal women and men, but is also used to treat Paget's disease (disease that results in deformed and enlarged bones).<ref>http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000018/</ref> Alendronate belongs to the class of nitrogen-containing bisphosphonates, which are inorganic pyrophosphate analogues. | ||
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== History of Bisphosphonates == | == History of Bisphosphonates == | ||
Bisphosphonates were first synthesized in Germany in 1865, but were not studied biologically until 1968. In the interim time, they were used in the textile and fertilizer industries due to their apparent inhibitory effect on calcium carbonate. However, in 1968, a group in Switzerland found inorganic pyrophosphates in urine and plasma. In vitro testing of these molecules revealed that they inhibited calcium phosphate precipitation and dissolution, but were destroyed in vivo by phosphatases. These results led to the discovery of bisphosphonates, as they reacted in the prescribed manner.<ref>http://www.ncbi.nlm.nih.gov/pmc/articles/PMC138713/?tool=pmcentrez</ref> | Bisphosphonates were first synthesized in Germany in 1865, but were not studied biologically until 1968. In the interim time, they were used in the textile and fertilizer industries due to their apparent inhibitory effect on calcium carbonate. However, in 1968, a group in Switzerland found inorganic pyrophosphates in urine and plasma. In vitro testing of these molecules revealed that they inhibited calcium phosphate precipitation and dissolution, but were destroyed in vivo by phosphatases. These results led to the discovery of bisphosphonates, as they reacted in the prescribed manner.<ref>http://www.ncbi.nlm.nih.gov/pmc/articles/PMC138713/?tool=pmcentrez</ref> | ||
Sodium alendronate was first marketed in 1994 as Fosamax® by Merck pharmaceutical. In 2008, Merck lost their U.S. patent on alendronate, allowing Barr Pharmaceuticals and Teva Pharmaceuticals USA to begin marketing generic forms of sodium alendronate. Other brand names for the drug include '''Fosamax+D®''', '''Adronat''', Alendros, Arendal, and Onclast.<ref>http://www.drugbank.ca/drugs/DB00630</ref> | Sodium alendronate was first marketed in 1994 as Fosamax® by Merck pharmaceutical. In 2008, Merck lost their U.S. patent on alendronate, allowing Barr Pharmaceuticals and Teva Pharmaceuticals USA to begin marketing generic forms of sodium alendronate. Other brand names for the drug include '''Fosamax+D®''', '''Adronat''', '''Alendros''', '''Arendal''', and '''Onclast'''.<ref>http://www.drugbank.ca/drugs/DB00630</ref> | ||
== Structure and General Function == | == Structure and General Function == | ||
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Alendronate is an aminobisphosphonate with a nonhydrolyzable P-C-P. It is structurally similar to IPP, which is pictured further down the page, and thus can bind to FPPS in place of IPP. Alendronate generally affects the activity of osteoclasts in bone. Osteoclasts are responsible for breaking down bone and also for bone resorption (losing bone substance). <ref>http://www.medterms.com/script/main/art.asp?articlekey=11794</ref> When alendronate is present, bone resorption is inhibited and bone breakdown is diminished. | Alendronate is an aminobisphosphonate with a nonhydrolyzable P-C-P. It is structurally similar to IPP, which is pictured further down the page, and thus can bind to FPPS in place of IPP. Alendronate generally affects the activity of osteoclasts in bone. Osteoclasts are responsible for breaking down bone and also for bone resorption (losing bone substance). <ref>http://www.medterms.com/script/main/art.asp?articlekey=11794</ref> When alendronate is present, bone resorption is inhibited and bone breakdown is diminished. | ||
== Side | == Side Effects of Drug == | ||
Possible side | Possible side effects for Fosamax include nausea,stomach pain, constipation, diarrhea, gas, bloating or fullness in the stomach, change in ability to taste food, headache, dizziness, and swelling of the joints, hands, or legs. More serious side effects (symptoms requiring doctor involvement) include new or worsening heartburn, difficulty swallowing, pain on swallowing, chest pain, bloody vomit or vomit that looks like coffee grounds, black, tarry, or bloody stools, fever, blisters or peeling skin, rash (may be made worse by sunlight), itching, hives, swelling of eyes, face, lips, tongue, or throat, difficulty breathing, hoarseness, painful or swollen gums, loosening of the teeth, numbness or heavy feeling in the jaw, poor healing of the jaw, and eye pain.<ref>http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000018/</ref> | ||
Fosamax has also been linked to sudden subtrochanteric and diaphyseal femur fractures, osteonecrosis of the jaw, and esophageal disorders.<ref>http://fosamax.legalview.info/</ref> | Fosamax has also been linked to sudden subtrochanteric and diaphyseal femur fractures, osteonecrosis of the jaw, and esophageal disorders.<ref>http://fosamax.legalview.info/</ref> | ||
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== Additional Resources == | == Additional Resources == | ||
For Additional Resources, See [[Pharmaceutical Drugs]] | For Additional Resources, See [[Pharmaceutical Drugs]] | ||
== References == | == References == | ||
<references/> | <references/> | ||