Tìm theo
Alendronate
Các tên gọi khác (6 ) :
  • (4-Amino-1-hydroxybutylidene)bisphosphonic acid
  • Acide Alendronique
  • Acido Alendronico
  • Acidum Alendronicum
  • Alendronate
  • Alendronic acid
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 66376-36-1
ATC: M05BA04
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C4H13NO7P2
PTK: 249.096
Alendronate is a nitrogen-containing, second generation bisphosphonate. Bisphosphonates were first used to treat Paget’s disease in 1971. This class of medications is comprised of inorganic pyrophosphate analogues that contain non-hydrolyzable P-C-P bonds. Similar to other bisphosphonates, alendronate has a high affinity for bone mineral and is taken up during osteoclast resorption. Alendronate inhibits farnesyl pyrophosphate synthetase, one of the enzymes in the mevalonic acid pathway involved in producing isoprenoid compounds that are essential for post-translational modification of small guanosine triphosphate (GTP)-binding proteins, such as Rho, Ras and Rab. Inhibition of this process interferes with osteoclast function and survival. Alendronate is used for the treatment of osteoporosis and Paget’s disease.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C4H13NO7P2
Phân tử khối
249.096
Monoisotopic mass
249.016724799
InChI
InChI=1S/C4H13NO7P2/c5-3-1-2-4(6,13(7,8)9)14(10,11)12/h6H,1-3,5H2,(H2,7,8,9)(H2,10,11,12)
InChI Key
InChIKey=OGSPWJRAVKPPFI-UHFFFAOYSA-N
IUPAC Name
(4-amino-1-hydroxy-1-phosphonobutyl)phosphonic acid
Traditional IUPAC Name
4-amino-1-hydroxy-1-phosphonobutylphosphonic acid
SMILES
NCCCC(O)(P(O)(O)=O)P(O)(O)=O
Độ tan chảy
234 dec °C
Độ hòa tan
1mg/L
logP
-4.3
logS
-1.2
pKa (strongest acidic)
0.69
pKa (Strongest Basic)
9.91
PSA
161.31 Å2
Refractivity
47.37 m3·mol-1
Polarizability
19.4 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
8
H Bond Donor Count
6
Physiological Charge
-1
Number of Rings
0
Bioavailability
1
pKa
2.72 (at 25 °C)
Dược Lực Học : Alendronate, a second-generation bisphosphonate is the first member of a group of drugs which strengthens bone. Alendronate is used to reduce hypercalcemia in tumor-induced bone disease, to treat corticosteroid-induced osteoporosis and Paget's disease, and to prevent osteoporosis in postmenopausal women.
Cơ Chế Tác Dụng : Alendronate is a nitrogen-containing, second generation bisphosphonate. Bisphosphonates were first used to treat Paget’s disease in 1971. This class of medications is comprised of inorganic pyrophosphate analogues that contain non-hydrolyzable P-C-P bonds. Similar to other bisphosphonates, alendronate has a high affinity for bone mineral and is taken up during osteoclast resorption. Alendronate inhibits farnesyl pyrophosphate synthetase, one of the enzymes in the mevalonic acid pathway involved in producing isoprenoid compounds that are essential for post-translational modification of small guanosine triphosphate (GTP)-binding proteins, such as Rho, Ras and Rab. Inhibition of this process interferes with osteoclast function and survival. Alendronate is used for the treatment of osteoporosis and Paget’s disease. The action of Alendronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Alendronate 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 :
Relative to an intravenous (IV) reference dose, the mean oral bioavailability of alendronate in women was 0.7% for doses ranging from 5 to 40 mg when administered after an overnight fast and two hours before a standardized breakfast. Oral bioavailability of the 10 mg tablet in men (0.59%) was similar to that in women (0.78%) when administered after an overnight fast and 2 hours before breakfast.
▧ Volume of Distribution :
* 28 L
▧ Protein binding :
78%
▧ Metabolism :
There is no evidence that alendronate is metabolized in humans or animals.
▧ Route of Elimination :
Following a single IV dose of [14C]alendronate, approximately 50% of the radioactivity was excreted in the urine within 72 hours and little or no radioactivity was recovered in the feces.
▧ Half Life :
>10 years
▧ Clearance :
* <200 mL/min [A single 10 mg IV dose]
Độc Tính : Alendronate can damage the esophagus both by toxicity from the medication itself and by nonspecific irritation secondary to contact between the pill and the esophageal mucosa, similar to other cases of "pill esophagitis."
Chỉ Định : For the treatment and prevention of osteoporosis in women and Paget's disease of bone in both men and women.
Tương Tác Thuốc :
  • Calcium Formation of non-absorbable complexes
  • Calcium Acetate Calcium Salts may decrease the serum concentration of Bisphosphonate Derivatives such as alendronate. Avoid administration of oral calcium supplements within 30 minutes after alendronate.
  • Calcium Chloride Calcium salts may decrease the serum concentration of bisphosphonate derivatives. Avoid administration of oral calcium supplements within 30 minutes after alendronate/risedronate.
  • Diclofenac Increased risk of gastric toxicity
  • Diflunisal Increased risk of gastric toxicity
  • Etodolac Increased risk of gastric toxicity
  • Fenoprofen Increased risk of gastric toxicity
  • Flurbiprofen Increased risk of gastric toxicity
  • Ibuprofen Increased risk of gastric toxicity
  • Indomethacin Increased risk of gastric toxicity
  • Iron Dextran Formation of non-absorbable complexes
  • Ketorolac Increased risk of gasrtic toxicity
  • Magnesium Formation of non-absorbable complexes
  • Mefenamic acid Increased risk of gastric toxicity
  • Nabumetone Increased risk of gastric toxicity
  • Naproxen Increased risk of gastric toxicity
  • Oxaprozin Increased risk of gastric toxicity
  • Oxyphenbutazone Increased risk of gastric toxicity
  • Piroxicam Increased risk of gastric toxicity
  • Tenoxicam Increased risk of gastric toxicity
Liều Lượng & Cách Dùng : Solution - Oral - 70 mg/75 ml
Tablet - Oral - 10 mg
Tablet - Oral - 35 mg
Tablet - Oral - 40 mg
Tablet - Oral - 5 mg
Tablet - Oral - 70 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Pliva
    Sản phẩm biệt dược : Alenotop
  • Sản phẩm biệt dược : Alned
  • Công ty : Ivax
    Sản phẩm biệt dược : Arendal
  • Công ty : Gedeon Richter
    Sản phẩm biệt dược : Beenos
  • Công ty : Duncan
    Sản phẩm biệt dược : Berlex
  • Công ty :
    Sản phẩm biệt dược : Binosto
  • Công ty : Biofarma
    Sản phẩm biệt dược : Denfos
  • Công ty : Mepha
    Sản phẩm biệt dược : Densidron
  • Công ty : Farmavita
    Sản phẩm biệt dược : Dronat
  • Công ty : Perumed
    Sản phẩm biệt dược : Durost
  • Công ty : Grupo Farma
    Sản phẩm biệt dược : Fixopan
  • Công ty : Kemofarmacija
    Sản phẩm biệt dược : Forosa
  • Công ty : Aspen Pharmacare
    Sản phẩm biệt dược : Fosagen
  • Công ty : Teriak
    Sản phẩm biệt dược : Fosalen
  • Công ty : Merck
    Sản phẩm biệt dược : Fosamax
  • Công ty : Hospimedikka
    Sản phẩm biệt dược : Fosmin
  • Công ty : Actavis
    Sản phẩm biệt dược : Fostolin
  • Công ty : Saval
    Sản phẩm biệt dược : Fosval
  • Sản phẩm biệt dược : Huesobone
  • Công ty : Actavis
    Sản phẩm biệt dược : Lendrate
  • Công ty : Intipharma
    Sản phẩm biệt dược : Oseolen
  • Công ty : Polpharma
    Sản phẩm biệt dược : Ostemax
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00630
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2088
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507199
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07752
ChemSpider
http://www.chemspider.com/Chemical-Structure.2004.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=25313
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0006-0925-31
PharmGKB
http://www.pharmgkb.org/drug/PA448082
Wikipedia
http://en.wikipedia.org/wiki/Alendronate
RxList
http://www.rxlist.com/cgi/generic/alendron.htm
Drugs.com
http://www.drugs.com/cdi/alendronate.html
... loading
... loading