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

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

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

Biệt dược thương mại : Coly-Mycin S 3.3-3-10 mg/ml Suspension 5ml Bottle

Giá bán buôn : USD >49.17

Đơn vị tính : bottle
Biệt dược thương mại : Colistin sulfate powder

Giá bán buôn : USD >513.26

Đơn vị tính : each

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
Công ty : King Pharmaceuticals

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

Công ty : Paddock Labs

Website : http://www.paddocklabs.com

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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