Alendronate(阿仑膦酸钠)
Monoisotopic: 249.016724799
Alendronate is a nitrogen-containing, second generation bisphosphonate. Bisphosphonates were first used to treat Paget’s disease in 1971. This class of medications is comprised of inorganic pyrophosphate analogues that contain non-hydrolyzable P-C-P bonds. Similar to other bisphosphonates, alendronate has a high affinity for bone mineral and is taken up during osteoclast resorption. Alendronate inhibits farnesyl pyrophosphate synthetase, one of the enzymes in the mevalonic acid pathway involved in producing isoprenoid compounds that are essential for post-translational modification of small guanosine triphosphate (GTP)-binding proteins, such as Rho, Ras and Rab. Inhibition of this process interferes with osteoclast function and survival. Alendronate is used for the treatment of osteoporosis and Paget’s disease.
- Apotex inc
- Aurobindo pharma ltd
- Austarpharma llc
- Barr laboratories inc
- Cadista pharmaceuticals inc
- Dr reddys laboratories ltd
- Genpharm ulc
- Merck and co inc
- Mylan pharmaceuticals inc
- Sandoz inc
- Sun pharma global inc
- Teva pharmaceuticals usa
- Watson laboratories
- Watson laboratories inc
- Amerisource Health Services Corp.
- Apotex Inc.
- Arrow Pharm Malta Ltd.
- A-S Medication Solutions LLC
- Aurobindo Pharma Ltd.
- Barr Pharmaceuticals
- Cipla Ltd.
- Cobalt Pharmaceuticals Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Doctor Reddys Laboratories Ltd.
- Lake Erie Medical and Surgical Supply
- Merck & Co.
- Murfreesboro Pharmaceutical Nursing Supply
- Mylan
- Northstar Rx LLC
- Nucare Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Rebel Distributors Corp.
- Southwood Pharmaceuticals
- Sun Pharmaceutical Industries Ltd.
- Teva Pharmaceutical Industries Ltd.
- UDL Laboratories
- Watson Pharmaceuticals
Synthesis Reference | Not Available |
General Reference |
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Type | small molecule |
Classes |
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Substructures |
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Indication | For the treatment and prevention of osteoporosis in women and Paget's disease of bone in both men and women. | ||||||
Pharmacodynamics | Alendronate, a second-generation bisphosphonate is the first member of a group of drugs which strengthens bone. Alendronate is used to reduce hypercalcemia in tumor-induced bone disease, to treat corticosteroid-induced osteoporosis and Paget's disease, and to prevent osteoporosis in postmenopausal women. | ||||||
Mechanism of action | The action of Alendronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Alendronate also targets farnesyl pyrophosphate (FPP) synthase. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting FPP synthase, an enzyme in the mevalonate pathway. Inhibition of this enzyme in osteoclasts prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are essential for the post-translational farnesylation and geranylgeranylation of small GTPase signalling proteins. This activity inhibits osteoclast activity and reduces bone resorption and turnover. In postmenopausal women, it reduces the elevated rate of bone turnover, leading to, on average, a net gain in bone mass. | ||||||
Absorption | Relative to an intravenous (IV) reference dose, the mean oral bioavailability of alendronate in women was 0.7% for doses ranging from 5 to 40 mg when administered after an overnight fast and two hours before a standardized breakfast. Oral bioavailability of the 10 mg tablet in men (0.59%) was similar to that in women (0.78%) when administered after an overnight fast and 2 hours before breakfast. | ||||||
Volume of distribution |
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Protein binding | 78% | ||||||
Metabolism |
There is no evidence that alendronate is metabolized in humans or animals.
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Route of elimination | Following a single IV dose of [14C]alendronate, approximately 50% of the radioactivity was excreted in the urine within 72 hours and little or no radioactivity was recovered in the feces. | ||||||
Half life | >10 years | ||||||
Clearance |
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Toxicity | Alendronate can damage the esophagus both by toxicity from the medication itself and by nonspecific irritation secondary to contact between the pill and the esophageal mucosa, similar to other cases of "pill esophagitis." | ||||||
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State | solid | ||||||||||||||||||||||||||||||||||||||||||
Experimental Properties |
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Predicted Properties |
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Drug | Interaction |
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Calcium | Formation of non-absorbable complexes |
Calcium Acetate | Calcium Salts may decrease the serum concentration of Bisphosphonate Derivatives such as alendronate. Avoid administration of oral calcium supplements within 30 minutes after alendronate. |
Calcium Chloride | Calcium salts may decrease the serum concentration of bisphosphonate derivatives. Avoid administration of oral calcium supplements within 30 minutes after alendronate/risedronate. |
Diclofenac | Increased risk of gastric toxicity |
Diflunisal | Increased risk of gastric toxicity |
Etodolac | Increased risk of gastric toxicity |
Fenoprofen | Increased risk of gastric toxicity |
Flurbiprofen | Increased risk of gastric toxicity |
Ibuprofen | Increased risk of gastric toxicity |
Indomethacin | Increased risk of gastric toxicity |
Iron Dextran | Formation of non-absorbable complexes |
Ketorolac | Increased risk of gasrtic toxicity |
Magnesium | Formation of non-absorbable complexes |
Mefenamic acid | Increased risk of gastric toxicity |
Nabumetone | Increased risk of gastric toxicity |
Naproxen | Increased risk of gastric toxicity |
Oxaprozin | Increased risk of gastric toxicity |
Oxyphenbutazone | Increased risk of gastric toxicity |
Piroxicam | Increased risk of gastric toxicity |
Tenoxicam | Increased risk of gastric toxicity |
- Take 30-60 minutes before breakfast.
- Take with a full glass of water.