Tìm theo
Clofazimine
Các tên gọi khác (6 ) :
  • Clofazimin
  • Clofazimina
  • Clofazimine
  • Clofaziminum
  • Lamprene
  • Riminophenazine
anti inflammatory agents non steroidal, leprostatic agents, coloring agents, antimycobacterials, dyes
Thuốc Gốc
Small Molecule
CAS: 2030-63-9
ATC: J04BA01
ĐG : Ciba Geigy Ltd. , http://cibasc.com
CTHH: C27H22Cl2N4
PTK: 473.396
A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C27H22Cl2N4
Phân tử khối
473.396
Monoisotopic mass
472.122152138
InChI
InChI=1S/C27H22Cl2N4/c1-17(2)30-24-16-27-25(15-23(24)31-20-11-7-18(28)8-12-20)32-22-5-3-4-6-26(22)33(27)21-13-9-19(29)10-14-21/h3-17,31H,1-2H3/b30-24+
InChI Key
InChIKey=WDQPAMHFFCXSNU-BGABXYSRSA-N
IUPAC Name
N,5-bis(4-chlorophenyl)-3-[(propan-2-yl)imino]-3,5-dihydrophenazin-2-amine
Traditional IUPAC Name
clofazimine
SMILES
CC(C)N=C1C=C2N(C3=CC=C(Cl)C=C3)C3=C(C=CC=C3)N=C2C=C1NC1=CC=C(Cl)C=C1
Độ tan chảy
210-212 °C
Độ hòa tan
0.225 mg/L (virtually insoluble)
logP
7.66
logS
-5.5
pKa (strongest acidic)
16.15
pKa (Strongest Basic)
9.29
PSA
39.99 Å2
Refractivity
142.55 m3·mol-1
Polarizability
51.52 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
5
Bioavailability
1
pKa
8.51
Dược Lực Học : Clofazimine exerts a slow bactericidal effect on Mycobacterium leprae (Hansen's bacillus). Clofazimine inhibits mycobacterial growth and binds preferentially to mycobacterial DNA. Clofazimine also exerts antiinflammatory properties in controlling erythema nodosum leprosum reactions. Clofazimine is highly lipophilic and tends to be deposited predominantly in fatty tissue and in cells of the reticuloendothelial system. It is taken up by macrophages throughout the body. Measurement of the minimum inhibitory concentration (MIC) of clofazimine against leprosy bacilli in vitro is not yet feasible. In the mouse footpad system, the multiplication of M.leprae is inhibited by introducing 0.0001%- 0.001% clofazimine in the diet. Although bacterial killing may begin shortly after starting the drug, it cannot be measured in biopsy tissues taken from patients for mouse footpad studies until approximately 50 days after the start of therapy.
Cơ Chế Tác Dụng : A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619) Appears to preferentially bind to mycobacterial DNA leading to disruption of the cell cycle and eventually kills the bacterium. It may also bind to bacterial potassium transporters, thereby inhibiting their function. Lysophospholipids have been found to mediate the activity of this drug.
Dược Động Học :
▧ Absorption :
Absorption varies from 45 to 62% following oral administration in leprosy patients. Bioavailability is approximately 70%. Food increases bioavailability and rate of absorption.
▧ Metabolism :
Hepatic. Three metabolites have been identified - two conjugated and one unconjugated, however, it is not yet known whether these metabolites are pharmacologically active. Metabolite I is formed by hydrolytic dehalogenation of clofazimine, metabolite II presumably is formed by a hydrolytic deamination reaction followed by glucuronidation, and metabolite III appears to be a hydrated clofazimine glucuronide.
▧ Half Life :
10 days following a single dose, 70 days after long-term, high-dose therapy.
Độc Tính : Oral, rabbit: LD50 = 3.3 g/kg; Oral, mouse: LD50 = > 4 g/kg. Severe abdominal symptoms have necessitated exploratory laparotomies in some patients on clofazimine therapy. Rare reports have included splenic infarction, bowel obstruction, and gastrointestinal bleeding. Deaths have been reported, following severe abdominal symptoms.
Chỉ Định : For the treatment of lepromatous leprosy, including dapsone-resistant lepromatous leprosy and lepromatous leprosy complicated by erythema nodosum leprosum.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Clofazimine powder
    Giá bán buôn : USD >187.2
    Đơn vị tính : g
Nhà Sản Xuất
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Clofozine
  • Công ty : Abbott
    Sản phẩm biệt dược : Hansepran
  • Công ty : Pond's Chemical
    Sản phẩm biệt dược : Lamcoin
  • Công ty : Novartis
    Sản phẩm biệt dược : Lampren
  • Công ty : Novartis
    Sản phẩm biệt dược : Lamprène
  • Công ty : Novartis
    Sản phẩm biệt dược : Lamprene
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00845
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06915
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00278
PharmGKB
http://www.pharmgkb.org/drug/PA164748759
Wikipedia
http://en.wikipedia.org/wiki/Clofazimine
RxList
http://www.rxlist.com/cgi/generic3/clofazimine.htm
Drugs.com
http://www.drugs.com/cons/clofazimine.html
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