| Identification | Back Directory | [Name]
COLISTIN METHANESULFONATE SODIUM SALT | [CAS]
8068-28-8 | [Synonyms]
w1929
Promixi
colimycinm
colistinat
colymycinm
Coly-mycin M (TN)
colistinsulfomethat
colistinsulfomethate
sodiumcolistimethate
coly-mycininjectable
ColistimethaleSodium
coly-mycinmparenteral
colistrimethatesodium
Colistimethate sodium CRS
Colistin Methanesulfonate
ColistiMethate SodiuM, USP
colistinsulfomethatesodium
COLISTINSULPHOMETHATESODIUM
sodiumcolistinmethanesulfonate
Colistimethate Sodium (200 mg)
Colistimethate Sodium (1147009)
sodiumcolistinemethanesulfonate
colistinmethanesulfonicacid,sod
COLISTIN METHANESULFONATE SODIUM
COLISTIN SODIUM METHANESULFONATE
COLIMYCIN SODIUM METHANESULFONATE
COLISTIN METHANESULFATE SODIUM USP
POLYMYXIN E SODIUM METHANESULFONATE
pentasodiumcolistinmethanesulfonate
COLISTIN METHANESULFONATE SODIUM SALT
Colistin, methyl sulfate, sodium salt
colistinmethanesulfonicacid,sodiumsalt
Methanesulfonic acid derivative of Polymyxin E
E1 Colistimethate sodium for peak identification
Sodium Colistin Methanesulfonate (Technical Grade)
Colistimethate sodium for peak identification (Y0001888)
3a,6-Dimethyl-3a,4,7,7a-tetrahydro-2-benzofuran-1,3-dione
COLISTIN SODIUM METHANESULFONATE FROM BA CILLUS COLISTINUS
(METHANESULFONIC ACID DERIVATIVE OF POLYMYXIN E) SODIUM SALT
Colimycin sodium methanesulfonate, Methanesulfonic acid derivative of Polymyxin E, Polymyxin E sodium methanesulfonate
Colistimethate sodiumQ: What is
Colistimethate sodium Q: What is the CAS Number of
Colistimethate sodium Q: What is the storage condition of
Colistimethate sodium Q: What are the applications of
Colistimethate sodium
colistimethatesodiumispreparedfromcolistinbytheactionofformaldehydeandsodiumhydrogensulfitetoformamixtureofditopentabis-sulfomethylatedprimaryaminederivatives,mainlypolymyxinse1ande2.
Semi-syntheticproductderivedfromafermentationproduct
pentasodium [[4-[[2-hydroxy-1-[[1-[[19-(1-hydroxyethyl)-7,10-diisobutyl-2,5,8,11,14,17,20-heptaketo-4,13,16-tris[2-(sulfonatomethylamino)ethyl]-3,6,9,12,15,18,21-heptazacyclotricos-1-yl]carbamoyl]-3-(sulfonatomethylamino)propyl]carbamoyl]propyl]amino]-4-keto-3-(6-methyloctanoylamino)butyl]amino]methanesulfonate
pentasodium [[4-[[3-hydroxy-1-[[1-[[19-(1-hydroxyethyl)-7,10-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-4,13,16-tris[2-(sulfonatomethylamino)ethyl]-3,6,9,12,15,18,21-heptazacyclotricos-1-yl]amino]-1-oxo-4-(sulfonatomethylamino)butan-2-yl]amino]-1-oxobutan-2-yl]amino]-3-(6-methyloctanoylamino)-4-oxobutyl]amino]methanesulfonate
pentasodium [[4-[[3-hydroxy-1-[[1-[[19-(1-hydroxyethyl)-7,10-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-4,13,16-tris[2-(sulfonatomethylamino)ethyl]-3,6,9,12,15,18,21-heptazacyclotricos-1-yl]amino]-1-oxo-4-(sulfonatomethylamino)butan-2-yl]amino]-1-oxo-butan-2-yl]amino]-3-(6-methyloctanoylamino)-4-oxo-butyl]amino]methanesulfonate | [EINECS(EC#)]
232-516-9 | [Molecular Formula]
C58H115N16Na5O28S5 | [MDL Number]
MFCD00130824 | [MOL File]
8068-28-8.mol | [Molecular Weight]
1759.9 |
| Chemical Properties | Back Directory | [Appearance]
White or almost white, hygroscopic powder. | [Melting point ]
>228°C (dec.) | [storage temp. ]
2-8°C
| [solubility ]
H2O: soluble10mg/mL | [form ]
powder | [color ]
white to faintly beige | [PH]
6-8 (10mg/mL in H2O) | [Water Solubility ]
Freely soluble in water | [Merck ]
13,2503 | [CAS DataBase Reference]
8068-28-8 | [EPA Substance Registry System]
Colistimethate sodium (8068-28-8) |
| Hazard Information | Back Directory | [Chemical Properties]
White or almost white, hygroscopic powder. | [Uses]
antibacterial | [Definition]
ChEBI: A mixture where R = H or Me. Colistin in which each of the primary amino groups is converted to the corresponding aminomethanesulfonic acid sodium salt, commonly by the action of formaldehyde followed by sodium bisulfite. A polymyxin antibiotic derivative,
it is used in the treatment of severe infections, particularly of multidrug-resistant Gram-negative bacteria such as Pseudomonas aeruginosa and Acinetobacter baumannii. | [Brand name]
Coly-Mycin (Monarch). | [General Description]
Two forms of colistins, colistin sulfate and colistin methanesulfonate sodium (Colistin sodium methanesulfonate)(CMS-Na), are commercially available. CMS-Na is administered intravenously, and CMS, the free base of CMS-Na consisting of CMS A and CMS B, is hydrolyzed in vivo to form active colistin A and colistin B6 . Colistin first became available for clinical use in 1959 and has been used worldwide for several decades[5]. | [Biological Activity]
colistin methanesulfonate is an inactive prodrug of colistin (also known as polymyxin e), which is an antibiotic with effect against most gram-negative bacteria, but also causes nephro- and neurotoxicity [1]. colistin is produced by certain strains of the bacteria paenibacillus polymyxa, and belongs to the class of polypeptide antibiotics known as polymyxins.in vitro: studying the time-kill kinetics of colistin methanesulfonate against a type culture of pseudomonas aeruginosa found that 8.0 or 32 mg/l colistin methanesulfonate began killing at approximately 90 or 30 min, and the mean auc0-240 values were 186.3±6.0 and 90.4±4.1, respectively [2]. besides, by investigation among mucoid and nonmucoid strains of pseudomonas aeruginosa isolated from patients with cystic fibrosis, colistin methanesulfonate was found to require a concentration of 16 times the mic to achieve complete killing within 24 h [3]. | [Pharmacokinetics]
Colistin is administered intravenously as the non-active prodrug, colistin methanesulfonate sodium (CMS). Colistin methanesulfonate sodium (Colistin sodium methanesulfonate) is eliminated mainly by renal clearance. If CMS is cleared rapidly by the kidney, less CMS is converted to colistin resulted in low colistin that could lead to ineffective antibacterial therapy. In patients with normal renal function (1–2 MIU of CMS), approximately 30–60% of a dose of CMS is converted to colistin. The renal clearance of CMS is much more efficient than the conversion of CMS to colistin. Therefore, to achieve a targeted concentration of >2 mg/L, patients must receive four to five times the amount of CMS. There was wide variability of colistin Cmax values (0.6–8.7 mg/L) in plasma among single-dose studies receiving 2–3 MIU of CMS in critically ill patients with preserved renal function. Almost none of the ICU patients achieved a colistin concentration of more than 2 mg/L in the Plachouras et al. and Mohamed et al. studies[4].
| [storage]
4°C, protect from light | [References]
[1] nation r l, li j. colistin in the 21st century.[j]. current opinion in infectious diseases, 2009, 22(6): 535-543.
[2] bergen p j, li j, rayner c r, et al. colistin methanesulfonate is an inactive prodrug of colistin against pseudomonas aeruginosa.[j]. antimicrobial agents and chemotherapy, 2006, 50(6): 1953-1958.
[3] li j, turnidge j d, milne r w, et al. in vitro pharmacodynamic properties of colistin and colistin methanesulfonate against pseudomonas aeruginosaisolates from patients with cystic fibrosis[j]. antimicrobial agents and chemotherapy, 2001, 45(3): 781-785. |
| Safety Data | Back Directory | [RIDADR ]
3249 | [WGK Germany ]
2
| [RTECS ]
GH1650000
| [F ]
3 | [TSCA ]
Yes | [HazardClass ]
6.1(b) | [PackingGroup ]
III | [HS Code ]
2941906000 | [Safety Profile]
Human poison by intramuscular route. Experimental poison by intramuscular, intraperitoneal, subcutaneous, and intravenous routes. Mildly toxic by ingestion. An experimental teratogen. Human systemic effects by intramuscular route: convulsions or effect on seizure threshold, change in motor activity, change in lrldney tubules, and urine volume decrease or anuria. Experimental reproductive effects. Used as an antibiotic. When heated to decomposition it emits very toxic fumes of NOx, SOx, and NazO | [Toxicity]
LD50 i.v. in mice: >550 mg/kg (Barnett) |
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