药品详细
Sevelamer(磷能解)
化学结构式图
中文名
磷能解
英文名
Sevelamer
分子式
C6H12ClNO
化学名
2-(chloromethyl)oxirane; prop-2-en-1-amine
分子量
Average: 149.619
Monoisotopic: 149.060741718
Monoisotopic: 149.060741718
CAS号
152751-57-0
ATC分类
V03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
Sevelamer is a phosphate binding drug used to prevent hyperphosphataemia in patients with chronic renal failure. When taken with meals, sevelamer binds to dietary phosphate and prevents its absorption. It is marketed by Genzyme under the trade name Renagel.
生产厂家
- Genzyme corp
- Genzyme Corporation
封装厂家
- Atlantic Biologicals Corporation
- Cardinal Health
- Genzyme Inc.
- Heartland Repack Services LLC
- Murfreesboro Pharmaceutical Nursing Supply
- Pharma Pac LLC
- Physicians Total Care Inc.
- Prepak Systems Inc.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Southwood Pharmaceuticals
- Tya Pharmaceuticals
- Vangard Labs Inc.
- Warner Chilcott Co. Inc.
- Watson 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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| Substructures |
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适应症
药理
| Indication | For the control of serum phosphorus in patients with Chronic Kidney Disease (CKD) on hemodialysis. |
| Pharmacodynamics | Patients with end-stage renal disease (ESRD) retain phosphorus and can develop hyperphosphatemia. High serum phosphorus can precipitate serum calcium resulting in ectopic calcification. When the product of serum calcium and phosphorus concentrations (Ca x P) exceeds 55 mg2/dL2, there is an increased risk that ectopic calcification will occur. Hyperphosphatemia plays a role in the development of secondary hyperparathyroidism in renal insufficiency. An increase in parathyroid hormone (PTH) levels is characteristic of patients with chronic renal failure. Increased levels of PTH can lead to osteitis fibrosa, a bone disease. A decrease in serum phosphorus may decrease serum PTH levels. Treatment of hyperphosphatemia includes reduction in dietary intake of phosphate, inhibition of intestinal phosphate absorption with phosphate binders, and removal of phosphate with dialysis. Sevelamer taken with meals has been shown to decrease serum phosphorus concentrations in patients with ESRD who are on hemodialysis. In vitro studies have shown that the capsule and tablet formulations bind phosphate to a similar extent. Sevelamer treatment also results in a lowering of low-density lipoprotein (LDL) and total serum cholesterol levels. |
| Mechanism of action | Sevelamer prevents hyperphosphatemia by binding to dietary phosphate in the gut, preventing its absorption and thus decreasing serum parathyroid hormone levels. |
| Absorption | Not absorbed following oral administration, however no absorption studies have been performed in patients with renal disease. |
| Volume of distribution | Not Available |
| Protein binding | Not Available |
| Metabolism |
Not Available
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| Route of elimination | Not Available |
| Half life | Not Available |
| Clearance | Not Available |
| Toxicity | Sevelamer has been given to normal healthy volunteers in doses of up to 14 grams per day for eight days with no adverse effects. Sevelamer has been given in average doses up to 13 grams per day to hemodialysis patients. There are no reported overdosages of sevelamer in patients. Since sevelamer is not absorbed, the risk of systemic toxicity is low. |
| Affected organisms |
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| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||
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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 |
|---|---|
| Ciprofloxacin | Sevelamer decreases ciprofloxacin bioavailability |
| Cyclosporine | Sevelamer decreases the effect of cyclosporine |
| Trovafloxacin | Sevelamer may decrease the absorption of orally administered Trovafloxacin. The Sevelamer formulation contains iron that may intefere with Trovafloxacin absorption. Administer Trovafloxacin 2 hours before or 6 hours after the Sevelamer dose to minimize the interaction. |
食物相互作用
Not Available
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