药品详细
Risedronate(利塞膦酸钠)
化学结构式图
中文名
利塞膦酸钠
英文名
Risedronate
分子式
C7H11NO7P2
化学名
[1-hydroxy-1-phosphono-2-(pyridin-3-yl)ethyl]phosphonic acid
分子量
Average: 283.1123
Monoisotopic: 283.001074735
Monoisotopic: 283.001074735
CAS号
105462-24-6
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
Risedronate is a bisphosphonate used to strengthen bone, treat or prevent osteoporosis, and treat Paget’s disease of bone.
生产厂家
- Procter & Gamble
- Teva pharmaceuticals usa
- Warner chilcott co llc
封装厂家
- Diversified Healthcare Services Inc.
- Lake Erie Medical and Surgical Supply
- Murfreesboro Pharmaceutical Nursing Supply
- Norwich Pharmaceuticals Inc.
- Physicians Total Care Inc.
- Procter & Gamble
- Resource Optimization and Innovation LLC
- Stat Rx Usa
- Warner Chilcott Co. Inc.
- WC Pharmaceuticals
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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适应症
药理
| Indication | For the treatment of Paget's disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis | ||||||
| Pharmacodynamics | Risedronate is a pyridinyl bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism and is indicated for the treatment and prevention of osteoporosis in postmenopausal women. | ||||||
| Mechanism of action | The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate 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 | Rapid absorption (~1 hr) after an oral dose, occurs throughout the upper gastrointestinal tract | ||||||
| Volume of distribution |
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| Protein binding | ~24% | ||||||
| Metabolism |
No evidence found for metabolization of risedronate in humans or mammals
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| Route of elimination | Risedronate is excreted unchanged primarily via the kidney. Insignificant amounts (<0.1% of intravenous dose) of drug are excreted in the bile in rats. | ||||||
| Half life | 1.5 hours | ||||||
| Clearance |
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| Toxicity | Side effects include abdominal pain, anxiety, back pain, belching, bladder irritation, bone disorders and pain, bronchitis, bursitis, cataracts, chest pain, colitis, constipation, depression, diarrhea, difficulty breathing, dizziness, dry eyes, eye infection, flu-like symptoms, gas, headache, high blood pressure, infection, insomnia, itching, joint disorders and pain, leg cramps, muscle pain, muscle weakness, nausea, neck pain, nerve pain, pain, pneumonia, rash, ringing in ears, sinus problems, sore throat, stomach bleeding, stuffy or runny nose, swelling, tendon problems, tumor, ulcers, urinary tract infection, vertigo, vision problems, and weakness. | ||||||
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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 |
|---|---|
| Calcium | Formation of non-absorbable complexes |
| Calcium Acetate | Calcium Salts may decrease the serum concentration of Bisphosphonate Derivatives such as risedronate. Avoid administration of oral calcium supplements within or 30 minutes after risedronate. |
| Calcium Chloride | Calcium salts may decrease the serum concentration of bisphosphonate derivatives. Avoid administration of oral calcium supplements within 30 minutes after alendronate/risedronate. |
| Iron Dextran | Formation of non-absorbable complexes |
| Magnesium | Formation of non-absorbable complexes |
食物相互作用
Not Available
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