Alendronate
Alendronate sodium
CAS: 129318-43-0
Molecular Formula: C4H13NNaO7P2
Alendronate - Names and Identifiers
| Name | Alendronate sodium |
| Synonyms | MK-217 Fosamax ALENDRONATE SODIUM ALENDRONATE Alendronate sodium Alendronic acid, sodiuM salt tetrasodium 4-amino-1,1-diphosphonatobutan-1-ol tetrasodium 4-amino-1,1-diphosphonato-butan-1-ol Sodium 4-amino-1-hydroxy-1-phosphonobutane-1-phosphonate 4-AMINO-1-HYDROXY-1-PHOSPHONOBUTYL PHOSPHONIC ACID, MONOSODIUM sodium hydrogen (4-amino-1-hydroxy-1-phosphonobutyl)phosphonate (4-Amino-1-hydroxybutylidene) bisphosphonic acid monosodium salt |
| CAS | 129318-43-0 |
| EINECS | 603-329-3 |
| InChI | InChI=1/C4H13NO7P2.Na/c5-3-1-2-4(6,13(7,8)9)14(10,11)12;/h6H,1-3,5H2,(H2,7,8,9)(H2,10,11,12);/q;+1/p-1 |
Alendronate - Physico-chemical Properties
| Molecular Formula | C4H13NNaO7P2 |
| Molar Mass | 272.09 |
| Melting Point | 119 °C |
| Storage Condition | 2-8°C |
Alendronate - Risk and Safety
| Hazard Class | IRRITANT |
Alendronate - Reference
| Reference Show more | 1. [IF=6.953] Hao Wu et al."Low molecular weight heparin modified bone targeting liposomes for orthotopic osteosarcoma and breast cancer bone metastatic tumors."Int J Biol Macromol. 2020 Dec;164:2583 |
Alendronate - Reference Information
| osteoporosis drug | alendronate sodium is the most widely used anti-osteoporosis drug in the world. it was listed in the United States in 1993 and can significantly increase bone density of patients and reduce fracture risk. it is the first-line treatment drug for osteoporosis. Alendronate sodium is an aminodiphosphonate bone resorption inhibitor. It has a strong affinity with intraosseous hydroxyapatite and can enter the bone matrix hydroxyapatite crystals. When osteoclasts dissolve the crystals, the drug is released, It can inhibit the activity of osteoclasts, and indirectly inhibit bone resorption through osteoblasts. It has the characteristics of strong anti-bone resorption activity and no bone mineralization inhibition. It is clinically used to treat osteoporosis in postmenopausal women to prevent hip and spinal fractures. Special attention should be paid to all patients with osteoporosis who should take calcium and vitamin D supplements if they cannot get free calcium and vitamin D from food. Alendronate sodium tablets, like all other aminodiphosphonates, may also cause local irritation to the upper gastrointestinal mucosa, so they should be used with caution for active upper gastrointestinal diseases, such as dysphagia, esophageal disease, Patients with gastritis, 12-finger inflammation or ulcers. Osteoporosis is a disease that leads to an increased risk of fracture. Its main manifestations are reduced bone density, deterioration of bone microstructure, and changes in the number and types of proteins in the bone. The main hazard of osteoporosis is to increase the risk of fracture in patients. Fracture occurs when normal people are not easy to fracture. This kind of fracture is also called fragility fracture. Common parts include spine, ribs, buttocks, wrists, etc. It is the main cause of disability or death in patients with osteoporosis. Statistics show that the incidence of osteoporosis is on the rise worldwide. There are more than 0.2 billion osteoporosis patients in the world, and there are about 70 million osteoporosis patients in my country. Osteoporosis has become an important disease that endangers human health, especially the health of middle-aged and elderly women. Bisphosphonate is a general term for a class of prescription drugs for the treatment of osteoporosis, including etidronate sodium, alendronate sodium, risedronate sodium, zoledronic acid, etc., their chemical structure and pharmacological effects are similar. Alendronate sodium, the trade name Fosamax, is the most widely used anti-osteoporosis drug in the world. This product is the third-generation aminodiphosphonate bone resorption inhibitor, which has a strong affinity with hydroxyapatite in the bone, and exerts an anti-bone resorption effect by inhibiting the activity of osteoclasts. Its anti-bone resorption effect is 1000 times stronger than etidronate sodium, and there is no inhibition of bone mineralization. Mainly used for osteoporosis in postmenopausal women, it can increase the bone mass of the spine, vertebral body distortion, shortened height, and fracture incidence (including hip bone, spine, carpal bone). |
| Synthetic route | Using γ-aminobutyric acid (gamma-aminobutyric acid,GABA), phosphorous acid, and phosphorus trichloride as raw materials, using diphenyl ether as a solvent to prepare alendric acid, and then alkalization to obtain its monosodium salt. The synthesis route is shown in the following figure: Figure 1 shows the synthesis route of alendronate sodium |
| adverse reactions | well tolerated after taking the medicine, a few patients can see gastrointestinal reactions, such as nausea, abdominal distension, abdominal pain, occasionally headache, skeletal muscle pain, rare rash and erythema. (2016-01-22) |
| contraindications | 1. esophageal motility disorders, such as esophageal retardation and esophageal stenosis, are prohibited. 2. Severe renal insufficiency is disabled. 3. Patients with osteomalacia are contraindicated. 4. Those who are allergic to this product and other diphosphates and have obvious hypocalcemia are contraindicated. 5. Pregnant, lactating women and children are prohibited. |
| precautions | 1. take 200ml of warm boiled water at least 30 minutes before breakfast, and eat at least 30 minutes after medication. 2. Taking orange juice and coffee at the same time will significantly affect the absorption of this product. 3. milk, dairy products and beverages containing more calcium should not be drunk within 30 minutes before and after taking this product. Bedrest immediately after taking the drug may cause esophageal irritation or ulcerative esophagitis. 4. Patients with gastrointestinal dysfunction, gastritis, esophageal discomfort, duodenitis and ulcer disease should be used with caution. 5. Use with caution in patients with mild and moderate renal dysfunction. 6. Before starting to use this product, calcium metabolism and mineral metabolism disorders, vitamin D deficiency and hypocalcemia must be corrected. Calcium supplements, antacids and some oral drugs are likely to hinder the absorption of this product. Therefore, after taking this product, you should postpone taking other drugs for at least half an hour. 7. If food intake is insufficient, all patients with osteoporosis should be supplemented with calcium and vitamin D. |
| drug interaction | 1. antacids and laxatives often contain calcium or other metal ions such as magnesium and iron, which will affect the absorption of this drug. 2. The combination with aminoglycosides can induce hypocalcemia. |
Last Update：2024-04-10 22:29:15
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