Colistin

Colistin (Polymyxin E) is an orally active polypeptide antibiotic and has excellent activity against various Gram-negative rod-shaped bacteria, including multidrug-resistant Pseudomonas aeruginosa, Acinetobacter baumannii and Klebsiella pneumoniae. Colistin (Polymyxin E) is associated with nephrotoxicity and can be used for the research of infections caused by Gram-negative bacilli[1][2].

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> Bacterial

Colistin (Polymyxin E) (16 mg/kg/day, i.p.) shows the enrichment of cell cycle arrest genes and suggests that injury or cellular stress caused by colistin is acting through p53 to inhibit cell cycle progression. Colistin (Polymyxin E) (16 mg/kg/day, i.p.) has elevated blood urea nitrogen (BUN), creatinine, and pathologic evidence of acute tubular necrosis and apoptosis[1]. Animal Model: C57/BL6 mice[1] Dosage: 16 mg/kg/day Administration: 16 mg/kg/day, i.p. Result: Detected apoptosis, necrosis PCNA staining in mice.

[1]. Silpak Biswas, et al. Colistin: an update on the antibiotic of the 21st century. Expert Rev Anti Infect Ther. 2012 Aug;10(8):917-34.

[2]. Jian Li, et al. Pharmacokinetics of colistin methanesulphonate and colistin in rats following an intravenous dose of colistin methanesulphonate.

[3]. Michael T Eadon, et al. Cell cycle arrest in a model of colistin nephrotoxicity. Physiol Genomics. 2013 Oct 1;45(19):877-88.

MOLECULAR FORMULA :

C45-H85-N13-O10

MOLECULAR WEIGHT :

968.43

WISWESSER LINE NOTATION :

T-24-MV DMV GMV JMV MMV PMV SMV VMVTJ CYQ1 F2MV4Y2&1 I1Y1&1 L2Z O1Y1&1 R2Z U2Z A&2Z

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD - Lethal dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

>2 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

236 mg/kg

TOXIC EFFECTS :

Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - muscle contraction or spasticity

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

115 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

8800 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - cat

DOSE/DURATION :

250 mg/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity) Behavioral - ataxia Gastrointestinal - nausea or vomiting

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rabbit

DOSE/DURATION :

100 mg/kg

TOXIC EFFECTS :

Peripheral Nerve and Sensation - flaccid paralysis with appropriate anesthesia Behavioral - convulsions or effect on seizure threshold Behavioral - ataxia

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - cat

DOSE/DURATION :

1500 mg/kg/30D-I

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity) Gastrointestinal - changes in structure or function of salivary glands Nutritional and Gross Metabolic - weight loss or decreased weight gain

MUTATION DATA

TYPE OF TEST :

Cytogenetic analysis

TEST SYSTEM :

Human Lymphocyte

DOSE/DURATION :

142 units/ml

REFERENCE :

TCMUD8 Teratogenesis, Carcinogenesis, and Mutagenesis. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 3,515,1983 *** REVIEWS *** TOXICOLOGY REVIEW MMWOAU Muenchener Medicinische Wochenschrift. (Munich, Fed. Rep. Ger.) V.33-115, 1886-1973. Volume(issue)/page/year: 115,1661,1973 TOXICOLOGY REVIEW AJMEAZ American Journal of Medicine. (Technical Pub., 875 Third Ave., New York, NY 10022) V.1- 1946- Volume(issue)/page/year: 38,409,1965 TOXICOLOGY REVIEW CRTXB2 CRC Critical Reviews in Toxicology. (CRC Press, Inc., 2000 Corporate Blvd., NW, Boca Raton, FL 33431) V.1- 1971- Volume(issue)/page/year: 2,159,1973 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5828 No. of Facilities: 143 (estimated) No. of Industries: 1 No. of Occupations: 5 No. of Employees: 1941 (estimated) No. of Female Employees: 1403 (estimated)