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药品详细

Pamidronate(帕米膦酸二钠)

化学结构式图
中文名
帕米膦酸二钠
英文名
Pamidronate
分子式
C3H11NO7P2
化学名
(3-amino-1-hydroxy-1-phosphonopropyl)phosphonic acid
分子量
Average: 235.0695
Monoisotopic: 235.001074735
CAS号
40391-99-9
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

Pamidronic acid (INN) or pamidronate disodium (USAN), marketed as pamidronate disodium pentahydrate under the brand name Aredia, is a bisphosphonate. [Wikipedia]

生产厂家
  • Aesgen inc
  • Akorn strides llc
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Cipla ltd
  • Generamedix inc
  • Hospira inc
  • Mn pharmaceuticals
  • Novartis pharmaceuticals corp
  • Pharmaforce inc
  • Pliva lachema as
  • Sun pharma global inc
  • Teva parenteral medicines inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Zarychanski R, Elphee E, Walton P, Johnston J: Osteonecrosis of the jaw associated with pamidronate therapy. Am J Hematol. 2006 Jan;81(1):73-5. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Bisphosphonates
Substructures
  • Hydroxy Compounds
  • Carboxylic Acids and Derivatives
  • Phosphonic Acids and Derivatives
  • Aliphatic and Aryl Amines
  • Phosphinic Acids and Derivatives
  • Bisphosphonates
适应症
药理
Indication For the treatment of moderate or severe hypercalcemia associated with malignancy
Pharmacodynamics 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.
Mechanism of action 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.
Absorption Plasma concentration rises rapidly upon IV administration.
Volume of distribution Not Available
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
Toxicity Side effects include an allergic reaction, kidney problems, seizures, low levels of calcium, magnesium, or phosphorus in the blood
Affected organisms
  • Humans and other mammals
Pathways
Pathway Name SMPDB ID
Smp00117 Pamidronate Pathway SMP00117
理化性质
Properties
State solid
Experimental Properties
Property Value Source
logP -4.7 Not Available
Predicted Properties
Property Value Source
water solubility 1.58e+01 g/l ALOGPS
logP -1.4 ALOGPS
logP -4.5 ChemAxon
logS -1.2 ALOGPS
pKa (strongest acidic) 0.67 ChemAxon
pKa (strongest basic) 9.86 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 8 ChemAxon
hydrogen donor count 6 ChemAxon
polar surface area 161.31 ChemAxon
rotatable bond count 4 ChemAxon
refractivity 42.62 ChemAxon
polarizability 17.34 ChemAxon
药物相互作用
食物相互作用
Not Available

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