Tìm theo
Pamidronate
Các tên gọi khác (5 ) :
  • Acide pamidronique
  • Acido pamidronico
  • Acidum pamidronicum
  • Pamidronic acid
  • Ribodroat
Thuốc chống ung thư và tác động vào hệ thống miễn dịch
Thuốc Gốc
Small Molecule
CAS: 40391-99-9
ATC: M05BA03
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C3H11NO7P2
PTK: 235.0695
Pamidronic acid (INN) or pamidronate disodium (USAN), marketed as pamidronate disodium pentahydrate under the brand name Aredia, is a bisphosphonate. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C3H11NO7P2
Phân tử khối
235.0695
Monoisotopic mass
235.001074735
InChI
InChI=1S/C3H11NO7P2/c4-2-1-3(5,12(6,7)8)13(9,10)11/h5H,1-2,4H2,(H2,6,7,8)(H2,9,10,11)
InChI Key
InChIKey=WRUUGTRCQOWXEG-UHFFFAOYSA-N
IUPAC Name
(3-amino-1-hydroxy-1-phosphonopropyl)phosphonic acid
Traditional IUPAC Name
3-amino-1-hydroxy-1-phosphonopropylphosphonic acid
SMILES
NCCC(O)(P(O)(O)=O)P(O)(O)=O
Độ hòa tan
1.58e+01 g/l
logP
-4.7
logS
-1.2
pKa (strongest acidic)
0.67
pKa (Strongest Basic)
9.86
PSA
161.31 Å2
Refractivity
42.62 m3·mol-1
Polarizability
17.34 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
8
H Bond Donor Count
6
Physiological Charge
-1
Number of Rings
0
Bioavailability
1
Dược Lực Học : Pamidronate is in a class of drugs called bisphosphonates. Pamidronate reduces breakdown of the bones. Pamidronate is used in the treatment of Paget's disease of bone; to reduce high levels of calcium in the blood associated with malignancy (cancer); and to reduce the breakdown of bone due to metastases of breast cancer or multiple myeloma.
Cơ Chế Tác Dụng : Pamidronic acid (INN) or pamidronate disodium (USAN), marketed as pamidronate disodium pentahydrate under the brand name Aredia, is a bisphosphonate. [Wikipedia] The mechanism of action of pamidronate is inhibition of bone resorption. Pamidronate adsorbs to calcium phosphate (hydroxyapatite) crystals in bone and may directly block dissolution of this mineral component of bone. In vitro studies also suggest that inhibition of osteoclast activity contributes to inhibition of bone resorption. Pamidronate 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.
Dược Động Học :
▧ Absorption :
Plasma concentration rises rapidly upon IV administration.
▧ Protein binding :
Approximately 54% to human serum proteins.
▧ Metabolism :
Pamidronate is not metabolized and is exclusively eliminated by renal excretion
▧ Route of Elimination :
Pamidronate is not metabolized and is exclusively eliminated by renal excretion.
▧ Half Life :
The mean ± SD elimination half-life is 28 ± 7 hours
▧ Clearance :
* 107 +/- 50 mlL/min
Độc Tính : Side effects include an allergic reaction, kidney problems, seizures, low levels of calcium, magnesium, or phosphorus in the blood
Chỉ Định : For the treatment of moderate or severe hypercalcemia associated with malignancy
Liều Lượng & Cách Dùng : Injection, powder, lyophilized, for solution - Intravenous - 30 mg/vial
Injection, powder, lyophilized, for solution - Intravenous - 60 mg/vial
Injection, solution - Intravenous - 3 mg/ml
Injection, solution - Intravenous - 6 mg/ml
Injection, solution - Intravenous - 9 mg/ml
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aminomux
  • Sản phẩm biệt dược : Aredia
  • Công ty :
    Sản phẩm biệt dược : Pamimed
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00282
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4674
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504823
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07395
ChemSpider
http://www.chemspider.com/Chemical-Structure.4512.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=12581
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0703-4075-51
PharmGKB
http://www.pharmgkb.org/drug/PA450767
Wikipedia
http://en.wikipedia.org/wiki/Pamidronate
RxList
http://www.rxlist.com/cgi/generic/aredia.htm
Drugs.com
http://www.drugs.com/cdi/pamidronate.html
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