Tìm theo
Allopurinol
Các tên gọi khác (16 ) :
  • 1,5-Dihydro-4H-pyrazolo(3,4-D)pyrimidin-4-one
  • 1,5-Dihydro-4H-pyrazolo(3,4-D)pyrimidine-4-one
  • 1H-Pyrazolo(3,4-D)pyrimidin-4-ol
  • 4-HPP
  • 4-Hydroxy-1H-pyrazolo(3,4-D)pyrimidine
  • 4-Hydroxy-3,4-pyrazolopyrimidine
  • 4-Hydroxypyrazolo(3,4-D)pyrimidine
  • 4-Hydroxypyrazolopyrimidine
  • 4-Hydroxypyrazolyl(3,4-D)pyrimidine
  • 4'-Hydroxypyrazolol(3,4-D)pyrimidine
  • 4H-Pyrazolo(3,4-D)pyrimidin-4-one
  • AL-100
  • Allopurinol
  • Allopurinolum
  • Alopurinol
  • Zyloprim (tn)
Thuốc Gốc
Small Molecule
CAS: 315-30-0
ATC: M04AA01
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C5H4N4O
PTK: 136.1115
A xanthine oxidase inhibitor that decreases uric acid production. It also acts as an antimetabolite on some simpler organisms. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C5H4N4O
Phân tử khối
136.1115
Monoisotopic mass
136.03851077
InChI
InChI=1S/C5H4N4O/c10-5-3-1-8-9-4(3)6-2-7-5/h1-2H,(H2,6,7,8,9,10)
InChI Key
InChIKey=OFCNXPDARWKPPY-UHFFFAOYSA-N
IUPAC Name
1H,2H,4H-pyrazolo[3,4-d]pyrimidin-4-one
Traditional IUPAC Name
allopurinol
SMILES
O=C1N=CN=C2NNC=C12
Độ tan chảy
350 °C
Độ hòa tan
569 mg/L (at 25 °C)
logP
-0.55
logS
-2.38
pKa (strongest acidic)
7.83
pKa (Strongest Basic)
2.57
PSA
65.85 Å2
Refractivity
54.24 m3·mol-1
Polarizability
11.67 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Dược Lực Học : Allopurinol, a structural analog of the natural purine base hypoxanthine, is used to prevent gout and renal calculi due to either uric acid or calcium oxalate and to treat uric acid nephropathy, hyperuricemia, and some solid tumors.
Cơ Chế Tác Dụng : A xanthine oxidase inhibitor that decreases uric acid production. It also acts as an antimetabolite on some simpler organisms. [PubChem] Allopurinol and its active metabolite, oxypurinol, inhibits the enzyme xanthine oxidase, blocking the conversion of the oxypurines hypoxanthine and xanthine to uric acid. Elevated concentrations of oxypurine and oxypurine inhibition of xanthine oxidase through negative feedback results in a decrease in the concentrations of uric acid in the serum and urine. Allopurinol also facilitates the incorporation of hypoxanthine and xanthine into DNA and RNA, leading to a feedback inhibition of de novo purin synthesis and a decrease in serum uric acid concentrations as a result of an increase in nucleotide concentration.
Dược Động Học :
▧ Absorption :
Approximately 80-90% absorbed from the gastrointestinal tract.
▧ Protein binding :
Allopurinol and oxypurinol are not bound to plasma proteins
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Approximately 20% of the ingested allopurinol is excreted in the feces.
▧ Half Life :
1-3 hours
Độc Tính : LD50=214 mg/kg (in mice)
Chỉ Định : For the treatment of hyperuricemia associated with primary or secondary gout. Also indicated for the treatment of primary or secondary uric acid nephropathy, with or without the symptoms of gout, as well as chemotherapy-induced hyperuricemia and recurrent renal calculi.
Tương Tác Thuốc :
  • Acenocoumarol Allopurinol may increase the anticoagulant effect of acenocoumarol.
  • Anisindione Allopurinol may increase the anticoagulant effect of anisindione.
  • Azathioprine Allopurinol may increase the effect of thiopurine, azathioprine.
  • Cyclosporine Allopurinol increases the effect and toxicity of cyclosporine
  • Dicoumarol Allopurinol may increase the anticoagulant effect of dicumarol.
  • Mercaptopurine Allopurinol may increase the effect of thiopurine, mercaptopurine.
  • Trandolapril The ACE inhibitor, Trandolapril, may increase the risk of hypersensitivity reactions to Allopurinol.
  • Warfarin Allopurinol may increase the anticoagulant effect of warfarin. Monitor for changes in prothrombin times and therapeutic effects of warfarin if allopurinol is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Tanabe
    Sản phẩm biệt dược : Adenock
  • Công ty :
    Sản phẩm biệt dược : Allohexal
  • Công ty :
    Sản phẩm biệt dược : Alloril
  • Công ty :
    Sản phẩm biệt dược : Aloprim
  • Công ty :
    Sản phẩm biệt dược : Aluron
  • Công ty :
    Sản phẩm biệt dược : Milurit
  • Công ty :
    Sản phẩm biệt dược : Progout
  • Công ty : Wellcome
    Sản phẩm biệt dược : Zyloprim
  • Công ty :
    Sản phẩm biệt dược : Zyloric
  • Công ty :
    Sản phẩm biệt dược : Zyrik
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00437
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2094
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508516
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00224
ChemSpider
http://www.chemspider.com/Chemical-Structure.2010.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50241255
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/55111-729-01
PharmGKB
http://www.pharmgkb.org/drug/PA448320
Wikipedia
http://en.wikipedia.org/wiki/Allopurinol
RxList
http://www.rxlist.com/cgi/generic/allopur.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/zyl1508.shtml
Drugs.com
http://www.drugs.com/allopurinol.html
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