Tìm theo
Risedronate
Các tên gọi khác (7 ) :
  • Acide risédroniqe
  • Acido risedronico
  • Acidum risedronicum
  • Ridron
  • Risedronate
  • Risedronic acid
  • Risedronsäure
Thuốc giảm đau, hạ sốt, chống viêm không steroid, điều trị Gút và các bệnh xương khớp
Thuốc Gốc
Small Molecule
CAS: 105462-24-6
ATC: M05BA07
ĐG : Diversified Healthcare Services Inc. , http://www.dhscorp.com
CTHH: C7H11NO7P2
PTK: 283.1123
Risedronate is a bisphosphonate used to strengthen bone, treat or prevent osteoporosis, and treat Paget's disease of bone.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C7H11NO7P2
Phân tử khối
283.1123
Monoisotopic mass
283.001074735
InChI
InChI=1S/C7H11NO7P2/c9-7(16(10,11)12,17(13,14)15)4-6-2-1-3-8-5-6/h1-3,5,9H,4H2,(H2,10,11,12)(H2,13,14,15)
InChI Key
InChIKey=IIDJRNMFWXDHID-UHFFFAOYSA-N
IUPAC Name
[1-hydroxy-1-phosphono-2-(pyridin-3-yl)ethyl]phosphonic acid
Traditional IUPAC Name
1-hydroxy-1-phosphono-2-(pyridin-3-yl)ethylphosphonic acid
SMILES
OC(CC1=CN=CC=C1)(P(O)(O)=O)P(O)(O)=O
Độ hòa tan
1.04e+01 g/l
logP
-3.6
logS
-1.4
pKa (strongest acidic)
0.68
pKa (Strongest Basic)
4.91
PSA
148.18 Å2
Refractivity
57.12 m3·mol-1
Polarizability
21.91 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
8
H Bond Donor Count
5
Physiological Charge
-2
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Risedronate is a pyridinyl bisphosphonate that inhibits osteoclast-mediated bone resorption and modulates bone metabolism and is indicated for the treatment and prevention of osteoporosis in postmenopausal women.
Cơ Chế Tác Dụng : Risedronate is a bisphosphonate used to strengthen bone, treat or prevent osteoporosis, and treat Paget's disease of bone. The action of risedronate on bone tissue is based partly on its affinity for hydroxyapatite, which is part of the mineral matrix of bone. Risedronate 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 :
Rapid absorption (~1 hr) after an oral dose, occurs throughout the upper gastrointestinal tract
▧ Volume of Distribution :
* 13.8 L/kg
▧ Protein binding :
~24%
▧ Metabolism :
No evidence found for metabolization of risedronate in humans or mammals
▧ Route of Elimination :
Risedronate is excreted unchanged primarily via the kidney. Insignificant amounts (<0.1% of intravenous dose) of drug are excreted in the bile in rats.
▧ Half Life :
1.5 hours
▧ Clearance :
* 122 mL/min * 73 mL/min [osteopenic postmenopausal women]
Độc Tính : Side effects include abdominal pain, anxiety, back pain, belching, bladder irritation, bone disorders and pain, bronchitis, bursitis, cataracts, chest pain, colitis, constipation, depression, diarrhea, difficulty breathing, dizziness, dry eyes, eye infection, flu-like symptoms, gas, headache, high blood pressure, infection, insomnia, itching, joint disorders and pain, leg cramps, muscle pain, muscle weakness, nausea, neck pain, nerve pain, pain, pneumonia, rash, ringing in ears, sinus problems, sore throat, stomach bleeding, stuffy or runny nose, swelling, tendon problems, tumor, ulcers, urinary tract infection, vertigo, vision problems, and weakness.
Chỉ Định : For the treatment of Paget's disease of the bone (osteitis deformans), postmenopausal and glucocorticoid-induced osteoporosis
Tương Tác Thuốc :
  • Calcium Formation of non-absorbable complexes
  • Calcium Acetate Calcium Salts may decrease the serum concentration of Bisphosphonate Derivatives such as risedronate. Avoid administration of oral calcium supplements within or 30 minutes after risedronate.
  • Calcium Chloride Calcium salts may decrease the serum concentration of bisphosphonate derivatives. Avoid administration of oral calcium supplements within 30 minutes after alendronate/risedronate.
  • Iron Dextran Formation of non-absorbable complexes
  • Magnesium Formation of non-absorbable complexes
Liều Lượng & Cách Dùng : Tablet, film coated - Oral - 150 mg
Tablet, film coated - Oral - 30 mg
Tablet, film coated - Oral - 35 mg
Tablet, film coated - Oral - 5 mg
Tablet, film coated - Oral - 75 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Sanofi-Aventis
    Sản phẩm biệt dược : Actonel
  • Công ty : Warner Chilcott
    Sản phẩm biệt dược : Atelvia
  • Công ty : Takeda
    Sản phẩm biệt dược : Benet
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00884
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5245
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507526
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08233
ChemSpider
http://www.chemspider.com/Chemical-Structure.5055.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=12576
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0149-0471-01
PharmGKB
http://www.pharmgkb.org/drug/PA451255
Wikipedia
http://en.wikipedia.org/wiki/Risedronate
RxList
http://www.rxlist.com/cgi/generic/risedronate.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/act1580.shtml
Drugs.com
http://www.drugs.com/cdi/risedronate-tablets.html
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