Tìm theo
Sevelamer
Các tên gọi khác (5 ) :
  • Renagel
  • Sevelamer
  • Sévélamer
  • Sevelamero
  • Sevelamerum
Thuốc Gốc
Small Molecule
CAS: 152751-57-0
ATC: V03AE02
ĐG : Atlantic Biologicals Corporation , http://www.atlanticbiologicals.com
CTHH: C6H12ClNO
PTK: 149.619
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H12ClNO
Phân tử khối
149.619
Monoisotopic mass
149.060741718
InChI
InChI=1S/C3H5ClO.C3H7N/c4-1-3-2-5-3;1-2-3-4/h3H,1-2H2;2H,1,3-4H2
InChI Key
InChIKey=ZNSIZMQNQCNRBW-UHFFFAOYSA-N
IUPAC Name
2-(chloromethyl)oxirane; prop-2-en-1-amine
Traditional IUPAC Name
allylamine; epichlorohydrin
SMILES
NCC=C.ClCC1CO1
Độ hòa tan
Insoluble
logP
0.559
pKa (Strongest Basic)
-4.2
PSA
12.53 Å2
Refractivity
20.06 m3·mol-1
Polarizability
8.38 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
1
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. Sevelamer prevents hyperphosphatemia by binding to dietary phosphate in the gut, preventing its absorption and thus decreasing serum parathyroid hormone levels.
Dược Động Học :
▧ Absorption :
Not absorbed following oral administration, however no absorption studies have been performed in patients with renal disease.
Độc Tính : 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.
Chỉ Định : For the control of serum phosphorus in patients with Chronic Kidney Disease (CKD) on hemodialysis.
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Renagel 400 mg tablet
    Giá bán buôn : USD >1.66
    Đơn vị tính : tablet
  • Biệt dược thương mại : Renvela 800 mg tablet
    Giá bán buôn : USD >2.17
    Đơn vị tính : tablet
  • Biệt dược thương mại : Renagel 800 mg tablet
    Giá bán buôn : USD >2.41
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Sản phẩm biệt dược : Phosblock
  • Công ty : Sanofi
    Sản phẩm biệt dược : Renagel
  • Công ty : Sanofi
    Sản phẩm biệt dược : Renvela
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00658
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3085017
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505951
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01983
ChemSpider
http://www.chemspider.com/Chemical-Structure.2341997.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/58468-0021-3
PharmGKB
http://www.pharmgkb.org/drug/PA164781197
Wikipedia
http://en.wikipedia.org/wiki/Sevelamer
RxList
http://www.rxlist.com/cgi/generic2/sevel.htm
Drugs.com
http://www.drugs.com/cdi/sevelamer.html
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