Tìm theo
Etidronic acid
Các tên gọi khác (28 ) :
  • (1-Hydroxyethylene)diphosphonic acid
  • (1-Hydroxyethylidene)bis(phosphonic acid)
  • (1-Hydroxyethylidene)bisphosphonic acid
  • (1-Hydroxyethylidene)diphosphonic acid
  • (Hydroxyethylidene)diphosphonic acid
  • 1-Hydroxy-1,1-diphosphonoethane
  • 1-hydroxyethane 1,1-diphosphonic acid
  • 1-Hydroxyethane-1,1-bisphosphonic acid
  • 1-Hydroxyethane-1,1-diphosphonate
  • 1-Hydroxyethane-1,1-diphosphonic acid
  • 1-Hydroxyethanediphosphonic acid
  • 1-Hydroxyethylidene-1,1-bisphosphonate
  • 1-Hydroxyethylidene-1,1-diphosphonic acid
  • 1,1,1-Ethanetriol diphosphonate
  • Acetodiphosphonic acid
  • Acide etidronique
  • Acido etidronico
  • Acidum etidronicum
  • EHDP
  • Ethane-1-hydroxy-1,1-bisphosphonic acid
  • Ethane-1-hydroxy-1,1-diphosphonate
  • Ethane-1-hydroxy-1,1-diphosphonic acid
  • Etidronate
  • Etidronsaeure
  • Etidronsäure
  • HEDP
  • Hydroxyethanediphosphonic acid
  • Oxyethylidenediphosphonic acid
bone density conservation agents, antihypocalcemic agents, bisphosphonates
Thuốc Gốc
Small Molecule
CAS: 7414-83-7
ATC: M05BA01, M05BB01
ĐG : Genpharm LP
CTHH: C2H8O7P2
PTK: 206.0282
A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C2H8O7P2
Phân tử khối
206.0282
Monoisotopic mass
205.974525634
InChI
InChI=1S/C2H8O7P2/c1-2(3,10(4,5)6)11(7,8)9/h3H,1H3,(H2,4,5,6)(H2,7,8,9)
InChI Key
InChIKey=DBVJJBKOTRCVKF-UHFFFAOYSA-N
IUPAC Name
(1-hydroxy-1-phosphonoethyl)phosphonic acid
Traditional IUPAC Name
1-hydroxy-1-phosphonoethylphosphonic acid
SMILES
CC(O)(P(O)(O)=O)P(O)(O)=O
Độ hòa tan
1.15e+01 g/l
logP
-3.8
logS
-1.2
pKa (strongest acidic)
0.7
pKa (Strongest Basic)
-5.1
PSA
135.29 Å2
Refractivity
34.51 m3·mol-1
Polarizability
13.97 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
7
H Bond Donor Count
5
Physiological Charge
-2
Number of Rings
0
Bioavailability
1
Rule of Five
true
Dược Lực Học : Etidronic acid is a first generation (non-nitrogenous) bisphosphonate in the same family as clodronate and tiludronate. Etidronic acid affects calcium metabolism and inhibits bone resorption and soft tissue calcification. Of the etidronic acid that is resorbed (from oral preparation) or infused (for intravenous drugs), about 50% is excreted unchanged by the kidney. The remainder has a very high affinity for bone tissue, and is rapidly absorbed onto the bone surface. Etidronic acid has been shown to prevent or delay skeletal-related events and decrease bone pain as well as normalize calcium levels in the presence of hypercalcemia.
Cơ Chế Tác Dụng : A diphosphonate which affects calcium metabolism. It inhibits ectopic calcification and slows down bone resorption and bone turnover. [PubChem] Bisphosphonates, when attached to bone tissue, are absorbed by osteoclasts, the bone cells that breaks down bone tissue. Although the mechanism of action of non-nitrogenous bisphosphonates has not been fully elucidated, available data suggest that they bind strongly to hydroxyapatite crystals in the bone matrix, preferentially at the sites of increased bone turnover and inhibit the formation and dissolution of the crystals. Other actions may include direct inhibition of mature osteoclast function, promotion of osteoclast apoptosis, and interference with osteoblast-mediated osteoclast activation. Etidronic acid does not interfere with bone mineralization. In malignancy-related hypercalcemia, etidronic acid decreases serum calcium by inhibiting tumour-induced bone resorption and reducing calcium flow from the resorbing bone into the blood. Etidronic acid also reduces morbidity of osteolytic bone metastases by inhibiting tumour-induced bone resorption. Etidronic acid may promote osteoclast apoptosis by competing with adenosine triphosphate (ATP) in the cellular energy metabolism. The osteoclast initiates apoptosis and dies, leading to an overall decrease in the breakdown of bone.
Dược Động Học :
▧ Absorption :
The amount of drug absorbed after an oral dose is approximately 3%.
▧ Metabolism :
Not metabolized.
▧ Route of Elimination :
Etidronate disodium is not metabolized. Within 24 hours, approximately half the absorbed dose is excreted in urine; the remainder is distributed to bone compartments from which it is slowly eliminated. Unabsorbed drug is excreted intact in the feces.
▧ Half Life :
In normal subjects, plasma half-life of etidronic acid, based on non-compartmental pharmacokinetics is 1 to 6 hours.
Độc Tính : Clinical experience with acute etidronic acid overdosage is extremely limited. Decreases in serum calcium following substantial overdosage may be expected in some patients. Signs and symptoms of hypocalcemia also may occur in some of these patients. Some patients may develop vomiting. In one event, an 18-year-old female who ingested an estimated single dose of 4800 to 6000 mg (67 to 100 mg/kg) of etidronate was reported to be mildly hypocalcemic (7 .5 2 mg/ dl) and experienced paresthesia of the fingers.
Chỉ Định : For the treatment of symptomatic Paget's disease of bone and in the prevention and treatment of heterotopic ossification following total hip replacement or due to spinal cord injury.
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 etidronic acid (etidronate). Avoid administration of oral calcium supplements within 2 hours before or after tiludronate/clodronate/etidronate.
  • Calcium Chloride Calcium salts may decrease the serum concentration of bisphosphonate derivatives. Avoid administration of oral calcium supplements within 2 hours before or after tiludronate/clodronate/etidronate.
  • 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 : Tablet - Oral - 200 mg
Tablet - Oral - 400 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Procter & Gamble
    Sản phẩm biệt dược : Didronel
  • Công ty : Gentili
    Sản phẩm biệt dược : Etidron
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01077
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3305
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507694
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07736
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00314
ChemSpider
http://www.chemspider.com/Chemical-Structure.3189.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50115102
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-3286-91
PharmGKB
http://www.pharmgkb.org/drug/PA449548
Wikipedia
http://en.wikipedia.org/wiki/Etidronic_acid
RxList
http://www.rxlist.com/cgi/generic/didronel.htm
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