Alendronate: Difference between revisions
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Alendronate 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. | Alendronate 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. | ||
== History of Bisphosphonates == | == History of Bisphosphonates == | ||
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Alendronate is an aminobisphosphonate with a nonhydrolyzable P-C-P. 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. 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 affects of Drug == | |||
Possible side affects 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> | |||
== Target Proteins and Bone == | == Target Proteins and Bone == | ||
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=== Protein-Tyrosine-Phosphatases (PTP) === | === Protein-Tyrosine-Phosphatases (PTP) === | ||
Protein-Tyrosine-Phosphatses (PTPs) are reported to have an effect on osteoclast formation and function. | Protein-Tyrosine-Phosphatses (PTPs) are reported to have an effect on osteoclast formation and function. Initial reports indicated that alendronate inhibited several types of PTPs, though specific mechanisms are not known. The data does suggest that alendronate works as an antagonist, which means that, when bound, the alendronate does not elicit a response from the protein but rather disallows the binding of an agonist which would cause a change (likely activating) in the protein.<ref>http://www.drugbank.ca/drugs/DB00630</ref><ref>http://www.ncbi.nlm.nih.gov/pubmed/8610169</ref><ref>http://www.ncbi.nlm.nih.gov/pubmed/9310349</ref> A | ||
<scene name='Sandbox_59/Ptpre/1'>PTP example</scene> is given, so the binding site can be seen. | <scene name='Sandbox_59/Ptpre/1'>PTP example</scene> is given, so the binding site can be seen. | ||
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Isopentenyl pyrophosphate (IPP) actually binds to and stabilizes the alendronate-FPPS complex, rather than competing with the inhibitor. | Isopentenyl pyrophosphate (IPP) actually binds to and stabilizes the alendronate-FPPS complex, rather than competing with the inhibitor. | ||
