Tìm theo
Colistin
Các tên gọi khác (5 ) :
  • Colistin
  • Colistina
  • Colistine
  • Colistinum
  • Polymyxin E
Thuốc trị ký sinh trùng, chống nhiễm khuẩn
Thuốc Gốc
Small Molecule
CAS: 1264-72-8
ATC: J01XB01, A07AA10
ĐG : Paddock Labs , http://www.paddocklabs.com
CTHH: C52H98N16O13
PTK: 1155.4339
Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C) which act as detergents on cell membranes. Colistin is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C52H98N16O13
Phân tử khối
1155.4339
Monoisotopic mass
1154.749927302
InChI
InChI=1S/C52H98N16O13/c1-9-29(6)11-10-12-40(71)59-32(13-19-53)47(76)68-42(31(8)70)52(81)64-35(16-22-56)44(73)63-37-18-24-58-51(80)41(30(7)69)67-48(77)36(17-23-57)61-43(72)33(14-20-54)62-49(78)38(25-27(2)3)66-50(79)39(26-28(4)5)65-45(74)34(15-21-55)60-46(37)75/h27-39,41-42,69-70H,9-26,53-57H2,1-8H3,(H,58,80)(H,59,71)(H,60,75)(H,61,72)(H,62,78)(H,63,73)(H,64,81)(H,65,74)(H,66,79)(H,67,77)(H,68,76)/t29?,30-,31-,32+,33+,34+,35+,36+,37+,38+,39-,41+,42+/m1/s1
InChI Key
InChIKey=YKQOSKADJPQZHB-QNPLFGSASA-N
IUPAC Name
N-[(1S)-3-amino-1-{[(1S,2R)-1-{[(1S)-3-amino-1-{[(3S,6S,9S,12S,15R,18S,21S)-6,9,18-tris(2-aminoethyl)-3-[(1R)-1-hydroxyethyl]-12,15-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptaazacyclotricosan-21-yl]carbamoyl}propyl]carbamoyl}-2-hydroxypropyl]carbamoyl}propyl]-5-methylheptanamide
Traditional IUPAC Name
colistin
SMILES
[H][C@]1(NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC(=O)[C@H](CCNC1=O)NC(=O)[C@H](CCN)NC(=O)[C@@H](NC(=O)[C@H](CCN)NC(=O)CCCC(C)CC)[C@@H](C)O)[C@@H](C)O
Độ tan chảy
200-220 °C
Độ hòa tan
5.64E+005 mg/L
logP
-2.4
logS
-3.7
pKa (strongest acidic)
11.6
pKa (Strongest Basic)
10.23
PSA
490.66 Å2
Refractivity
297.67 m3·mol-1
Polarizability
125.93 Å3
Rotatable Bond Count
28
H Bond Acceptor Count
18
H Bond Donor Count
18
Physiological Charge
5
Number of Rings
1
Bioavailability
0
Dược Lực Học : Colistin is a polymyxin antibiotic agent. Polymyxins are cationic polypeptides that disrupt the bacterial cell membrane through a detergentlike mechanism. With the development of less toxic agents, such as extended-spectrum penicillins and cephalosporins, parenteral polymyxin use was largely abandoned, except for the treatment of multidrug-resistant pulmonary infections in patients with cystic fibrosis. More recently, however, the emergence of multidrug-resistant gram-negative bacteria, such as Pseudomonas aeruginosa and Acinetobacter baumannii, and the lack of new antimicrobial agents have led to the revived use of the polymyxins.
Cơ Chế Tác Dụng : Cyclic polypeptide antibiotic from Bacillus colistinus. It is composed of Polymyxins E1 and E2 (or Colistins A, B, and C) which act as detergents on cell membranes. Colistin is less toxic than Polymyxin B, but otherwise similar; the methanesulfonate is used orally. [PubChem] Colistin is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistin is polycationic and has both hydrophobic and lipophilic moieties. It interacts with the bacterial cytoplasmic membrane, changing its permeability. This effect is bactericidal. There is also evidence that polymyxins enter the cell and precipitate cytoplasmic components, primarily ribosomes.
Dược Động Học :
▧ Absorption :
Very poor absorption from gastrointestinal tract.
▧ Metabolism :
As 80% of the dose can be recovered unchanged in the urine, and there is no biliary excretion, it can be assumed that the remaining drug is inactivated in the tissues, however the mechanism is unknown.
▧ Half Life :
5 hours
Độc Tính : Oral LD50 in rats is 5450 mg/kg. Overdosage with colistimethate can cause neuromuscular blockade characterized by paresthesia, lethargy, confusion, dizziness, ataxia, nystagmus, disorders of speech and apnea. Respiratory muscle paralysis may lead to apnea, respiratory arrest and death.
Chỉ Định : For the treatment of acute or chronic infections due to sensitive strains of certain gram-negative bacilli, particularly Pseudomonas aeruginosa.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Catalysis
    Sản phẩm biệt dược : Alfacolin
  • Công ty : Nova Argentia
    Sản phẩm biệt dược : Alficetin
  • Công ty : Pari Pharma
    Sản phẩm biệt dược : ColiFin
  • Công ty : Quimifar
    Sản phẩm biệt dược : Colimicina
  • Công ty : Sanofi Aventis
    Sản phẩm biệt dược : Colimycine
  • Công ty : Rafa
    Sản phẩm biệt dược : Coliracin
  • Công ty : Atlantic Lab
    Sản phẩm biệt dược : Colistate
  • Công ty : SteriMax
    Sản phẩm biệt dược : Colistimethate
  • Công ty : Forest
    Sản phẩm biệt dược : Colomycin
  • Sản phẩm biệt dược : Coly-Mycin
  • Công ty : CNP
    Sản phẩm biệt dược : Diarönt mono
  • Công ty : Profile Pharma
    Sản phẩm biệt dược : Promixin
  • Công ty : Allertec
    Sản phẩm biệt dược : Tadim
  • Công ty : Wallace
    Sản phẩm biệt dược : Walamycin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00803
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5311054
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505467
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C13768
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02138
ChemSpider
http://www.chemspider.com/Chemical-Structure.4470591.html
PharmGKB
http://www.pharmgkb.org/drug/PA164760862
Wikipedia
http://en.wikipedia.org/wiki/Colistin
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