药品详细
Clodronate(氯膦酸二钠)
化学结构式图
中文名
氯膦酸二钠
英文名
Clodronate
分子式
CH4Cl2O6P2
化学名
[dichloro(phosphono)methyl]phosphonic acid
分子量
Average: 244.892
Monoisotopic: 243.886016298
Monoisotopic: 243.886016298
CAS号
10596-23-3
ATC分类
M05B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
A diphosphonate which affects calcium metabolism. It inhibits bone resorption and soft tissue calcification. [PubChem]
生产厂家
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | For the management of hypercalcemia of malignancy and as an adjunct in the management of osteolysis resulting from bone metastases of malignant tumors. |
| Pharmacodynamics | Clodronate is a first generation (non-nitrogenous) bisphosphonate in the same family as etidronate and tiludronate. Clodronate affects calcium metabolism and inhibits bone resorption and soft tissue calcification. Of the clodronate that is resorbed (from oral preparation) or infused (for intravenous drugs), about 50% is excreted unchanged by the kidney. The remainder has a very high affinity for bone tissue, and is rapidly absorbed onto the bone surface. Clodronate has been shown to prevent or delay skeletal-related events and decrease bone pain as well as normalize calcium levels in the presence of hypercalcemia. |
| Mechanism of action | The bisphosphonate group binds strongly to the bone mineral, hydroxyapatite. This explains the specific pharmacological action of these compounds on mineralized tissues, especially bone. The exact mechanism of action of clodronate is not known, however it is known that it does not inhibit protein isoprenylation but can be metabolized intracellularly to a β-γ-methylene (AppCp-type) analog of ATP (AppCCl2p), which is cytotoxic to macrophages in vitro. Inhibition of the ADP/ATP translocase by the metabolite AppCCl2p is a likely route by which clodronate causes osteoclast apoptosis and inhibits bone resorption. Recently, the slime mold Dictyostelium discoideum was shown to take up bisphosphonates by pinocytosis. In these cells, clodronate, but not other pharmacologically active bisphosphonates, was incorporated into adenine nucleotides, which could potentially explain why this bisphosphonate sometimes seems to act differently than the other bisphosphonates. Clodronate, like all biphosphonates, also binds protein-tyrosine-phosphatase. |
| Absorption | After oral administration, absorption is estimated at 1–3% of the ingested dose because of the low uptake from the gastrointestinal tract. |
| Volume of distribution | Not Available |
| Protein binding | 2%-36% |
| Metabolism |
Clodronate is not metabolized in humans.
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| Route of elimination | Not Available |
| Half life | Approximately 13 hours. |
| Clearance | Not Available |
| Toxicity | Decreases in serum calcium following substantial overdosage may be expected in some patients. Signs and symptoms of hypocalcemia also may occur in some of these patients. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | |||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Aluminium | Formation of non-absorbable complexes |
| Calcium | Formation of non-absorbable complexes |
| Calcium Acetate | Calcium Salts may decrease the serum concentration of Bisphosphonate Derivatives such as clodronate. Avoid administration of oral calcium supplements within 2 hours before or after tiludronate/clodronate/etidronate. |
| Calcium Chloride | Calcium salts may decrease the serum concentration of bisphosphonate derivatives. Avoid administration of oral calcium supplements within 2 hours before or after tiludronate/clodronate/etidronate. |
| Dihydroxyaluminium | Formation of non-absorbable complexes |
| Estramustine | Clodronate may increase the levels of estramustine. |
| Iron | Formation of non-absorbable complexes |
| Iron Dextran | Formation of non-absorbable complexes |
| Magnesium | Formation of non-absorbable complexes |
| Magnesium oxide | Formation of non-absorbable complexes |
| Sucralfate | Formation of non-absorbable complexes |
食物相互作用
- Food decreases absorption. Take on an empty stomach.
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