Tìm theo
Ibandronate
Các tên gọi khác (2) :
  • Bondronat
  • Ibandronic Acid
bone density conservation agents, antihypocalcemic agents, antiresorptives, bisphosphonates
Thuốc Gốc
Small Molecule
CAS: 114084-78-5
ATC: M05BA06
ĐG : Diversified Healthcare Services Inc. , http://www.dhscorp.com
CTHH: C9H23NO7P2
PTK: 319.2289
Ibandronate is a nitrogen-containing bisphosphonate in the same class as alendronate and risedronate. Ibandronate inhibits osteoclast-mediated bone resorption. All of the bisphosphonates prevent the breakdown of bone by bone cells called osteoclasts. In persons who are at high risk for osteoporosis, bisphosphonates not only result in increased amounts of bone and bone strength, they also reduce the risk of hip fractures and other bone fractures.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C9H23NO7P2
Phân tử khối
319.2289
Monoisotopic mass
319.094975119
InChI
InChI=1S/C9H23NO7P2/c1-3-4-5-7-10(2)8-6-9(11,18(12,13)14)19(15,16)17/h11H,3-8H2,1-2H3,(H2,12,13,14)(H2,15,16,17)
InChI Key
InChIKey=MPBVHIBUJCELCL-UHFFFAOYSA-N
IUPAC Name
{1-hydroxy-3-[methyl(pentyl)amino]-1-phosphonopropyl}phosphonic acid
Traditional IUPAC Name
1-hydroxy-3-[methyl(pentyl)amino]-1-phosphonopropylphosphonic acid
SMILES
CCCCCN(C)CCC(O)(P(O)(O)=O)P(O)(O)=O
Độ hòa tan
Freely soluble
logP
-2.1
logS
-1.4
pKa (strongest acidic)
0.66
pKa (Strongest Basic)
9.93
PSA
138.53 Å2
Refractivity
71.16 m3·mol-1
Polarizability
29.51 Å3
Rotatable Bond Count
9
H Bond Acceptor Count
8
H Bond Donor Count
5
Physiological Charge
-1
Number of Rings
0
Bioavailability
1
Rule of Five
true
Dược Lực Học : Ibandronate is a nitrogen-containing bisphosphonate in the same class as alendronate and risedronate. Ibandronate inhibits osteoclast-mediated bone resorption. All of the bisphosphonates prevent the breakdown of bone by bone cells called osteoclasts. In persons who are at high risk for osteoporosis, bisphosphonates not only result in increased amounts of bone and bone strength, they also reduce the risk of hip fractures and other bone fractures.
Cơ Chế Tác Dụng : Ibandronate is a nitrogen-containing bisphosphonate in the same class as alendronate and risedronate. Ibandronate inhibits osteoclast-mediated bone resorption. All of the bisphosphonates prevent the breakdown of bone by bone cells called osteoclasts. In persons who are at high risk for osteoporosis, bisphosphonates not only result in increased amounts of bone and bone strength, they also reduce the risk of hip fractures and other bone fractures. The action of ibandronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Nitrogen-containing bisphosphonates (such as pamidronate, alendronate, risedronate, ibandronate and zoledronate) appear to act as analogues of isoprenoid diphosphate lipids, thereby inhibiting farnesyl pyrophosphate (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 :
Poorly absorbed (mean bioavailability following a 2.5 mg oral dose is about 0.6% compared to intravenous dosing). Absorption is impaired by any kind of food or drink other than plain water.
▧ Volume of Distribution :
* 90 L
▧ Protein binding :
90.9 to 99.5% over an ibandronate concentration range of 2 to 10 ng/mL
▧ Metabolism :
No evidence of ibandronate being metabolized in humans.
▧ Route of Elimination :
Ibandronate is eliminated by renal excretion. Unabsorbed ibandronate is eliminated unchanged in the feces.
▧ Half Life :
10-60 hours
▧ Clearance :
* 84 to 160 mL/min [IV administration]
Độc Tính : LD50 = 811 mg/kg (rat, oral), side effects include bronchitis, pneumonia and urinary tract infections.
Chỉ Định : For the treatment and prevention of osteoporosis in postmenopausal women.
Tương Tác Thuốc :
  • Aluminium Formation of non absorbable complexes
  • Calcium Formation of non-absorbable complexes
  • Calcium Acetate Calcium Salts may decrease the serum concentration of Bisphosphonate Derivatives such as ibandronate. Avoid administration of oral calcium supplements within 60 minutes after oral ibandronate.
  • Calcium Chloride Calcium salts may decrease the serum concentration of bisphosphonate derivatives. Avoid administration of oral calcium supplements within 60 minutes after oral ibandronate.
  • Iron Formation of non absorbable complexes
  • Iron Dextran Formation of non-absorbable complexes
  • Magnesium Formation of non-absorbable complexes
  • Magnesium oxide Formation of non absorbable complexes
  • Sucralfate Formation of non absorbable complexes
Liều Lượng & Cách Dùng : Injection - Intravenous - 1 mg/ml
Tablet, film coated - Oral - 150 mg
Tablet, film coated - Oral - 2.5 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : ADRONiL
  • Công ty : Roche
    Sản phẩm biệt dược : Bondronat
  • Sản phẩm biệt dược : Boniva
  • Công ty :
    Sản phẩm biệt dược : Bonviva
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00710
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60852
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508134
ChemSpider
http://www.chemspider.com/Chemical-Structure.54839.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=12577
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0004-0185-23
PharmGKB
http://www.pharmgkb.org/drug/PA10270
Wikipedia
http://en.wikipedia.org/wiki/Ibandronate
RxList
http://www.rxlist.com/cgi/generic3/boniva.htm
Drugs.com
http://www.drugs.com/cdi/ibandronate.html
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