Tìm theo
Dacarbazine
Các tên gọi khác (22 ) :
  • 4-(3,3-Dimethyl-1-triazeno)imidazole-5-carboxamide
  • 4-(5)-(3,3-Dimethyl-1-triazeno)imidazole-5(4)-carboxamide
  • 4-(Dimethyltriazeno)imidazole-5-carboxamide
  • 5-(3,3-Dimethyl-1-triazeno)imidazole-4-carboxamide
  • 5-(3,3-Dimethyltriazeno)imidazole-4-carboxamide
  • 5-(Dimethyltriazeno)imidazole-4-carboxamide
  • Biocarbazine
  • Dacarbazin
  • Dacarbazina
  • Dacarbazine
  • Dacarbazinum
  • DIC
  • DTCI
  • Dtic-dome (tn)
  • DTIE
  • HSDB 3219
  • ICDMT
  • Imidazole Carboxamide
  • Imidazole-4-carboxamide, 5-(3,3-dimethyl-1-triazeno)-
  • NCI-C04717
  • NSC 45388
  • NSC-45388
Thuốc điều trị ung thư
Thuốc Gốc
Small Molecule
CAS: 4342-03-4
ATC: L01AX04
ĐG : APP Pharmaceuticals , http://www.apppharma.com
CTHH: C6H10N6O
PTK: 182.1832
An antineoplastic agent. It has significant activity against melanomas. (from Martindale, The Extra Pharmacopoeia, 31st ed, p564). Dacarbazine with Oblimersen is in clinical trials for the treatment of malignant melanoma.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H10N6O
Phân tử khối
182.1832
Monoisotopic mass
182.091608972
InChI
InChI=1S/C6H10N6O/c1-12(2)11-10-6-4(5(7)13)8-3-9-6/h3H,1-2H3,(H2,7,13)(H,8,9)
InChI Key
InChIKey=FDKXTQMXEQVLRF-UHFFFAOYSA-N
IUPAC Name
5-(dimethyltriaz-1-en-1-yl)-1H-imidazole-4-carboxamide
Traditional IUPAC Name
dacarbazine
SMILES
CN(C)N=NC1=C(N=CN1)C(N)=O
Độ tan chảy
205 °C
Độ hòa tan
4220 mg/L
logP
-0.24
logS
-2.1
pKa (strongest acidic)
5.89
pKa (Strongest Basic)
1.72
PSA
99.73 Å2
Refractivity
49.71 m3·mol-1
Polarizability
17.78 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
5
H Bond Donor Count
2
Physiological Charge
-1
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Dacarbazine is a synthetic analog of naturally occurring purine precursor 5-amino-1H-imidazole-4-carboxamide (AIC). After intravenous administration of dacarbazine, the volume of distribution exceeds total body water content suggesting localization in some body tissue, probably the liver. Its disappearance from the plasma is biphasic with initial half-life of 19 minutes and a terminal half-life of 5 hours. 1 In a patient with renal and hepatic dysfunctions, the half-lives were lengthened to 55 minutes and 7.2 hours. 1 The average cumulative excretion of unchanged DTIC in the urine is 40% of the injected dose in 6 hours. 1 DTIC is subject to renal tubular secretion rather than glomerular filtration. At therapeutic concentrations dacarbazine is not appreciably bound to human plasma protein.
Cơ Chế Tác Dụng : An antineoplastic agent. It has significant activity against melanomas. (from Martindale, The Extra Pharmacopoeia, 31st ed, p564). Dacarbazine with Oblimersen is in clinical trials for the treatment of malignant melanoma. The mechanism of action is not known, but appears to exert cytotoxic effects via its action as an alkylating agent. Other theories include DNA synthesis inhibition by its action as a purine analog, and interaction with SH groups. Dacarbazine is not cell cycle-phase specific.
Dược Động Học :
▧ Absorption :
Erratic, slow and incomplete
▧ Protein binding :
Less than 5%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Dacarbazine is subject to renal tubular secretion rather than glomerular filtration. In man, dacarbazine is extensively degraded. Besides unchanged dacarbazine, 5-aminoimidazole -4 carboxamide (AIC) is a major metabolite of dacarbazine excreted in the urine.
▧ Half Life :
5 hours
Độc Tính : LD50=350mg/kg (orally in mice)
Chỉ Định : For the treatment of metastatic malignant melanoma. In addition, dacarbazine is also indicated for Hodgkin's disease as a secondary-line therapy when used in combination with other antineoplastic agents.
Tương Tác Thuốc :
  • Bendamustine Increases toxicity through pharmacodynamic synergism. Additive myelosuppression.
  • Thiabendazole The strong CYP1A2 inhibitor, Thiabendazole, may increase the effects and toxicity of Dacarbazine by decreasing Dacarbazine metabolism and clearance. Monitor for changes in the therapeutic and adverse effects of Dacarbazine if Thiabendazole is initiated, discontinued or dose changed.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00851
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00288
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0703-5075-01
PharmGKB
http://www.pharmgkb.org/drug/PA449197
Wikipedia
http://en.wikipedia.org/wiki/Dacarbazine
RxList
http://www.rxlist.com/cgi/generic2/dacarbazine.htm
Drugs.com
http://www.drugs.com/cdi/dacarbazine.html
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