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Encyclopedia > Colistin
Colistin
Systematic (IUPAC) name
 ?
Identifiers
CAS number 1264-72-8
ATC code J01XB01 A07AA10
PubChem 5311054
DrugBank APRD00886
Chemical data
Formula C52H98N16O13 
Mol. mass 2797.3193 g/mol
Pharmacokinetic data
Bioavailability 0%
Metabolism  ?
Half life 5 hours
Excretion  ?
Therapeutic considerations
Pregnancy cat.

C Image File history File links No higher resolution available. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... A division of the Anatomical Therapeutic Chemical Classification System A Alimentary tract and metabolism A07A Intestinal anti-infectives A07AA Antibiotics A07AA01 Neomycin A07AA02 Nystatin A07AA03 Natamycin A07AA04 Streptomycin A07AA05 Polymyxin B A07AA06 Paromomycin A07AA07 Amphotericin B A07AA08 Kanamycin A07AA09 Vancomycin A07AA10 Colistin A07AA11 Rifaximin A07AA51 Neomycin, combinations A07AA54 Streptomycin, combinations... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... A chemical formula is a concise way of expressing information about the atoms that constitute a particular chemical compound. ... For other uses, see Carbon (disambiguation). ... This article is about the chemistry of hydrogen. ... General Name, symbol, number nitrogen, N, 7 Chemical series nonmetals Group, period, block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, symbol, number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, period, block 16, 2, p Appearance colorless (gas) pale blue (liquid) Standard atomic weight 15. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The biological half-life of a substance is the time required for half of that substance to be removed from an organism by either a physical or a chemical process. ... The kidneys are important excretory organs in vertebrates. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ...

Legal status

PoM (UK), not available in US The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ...

Routes topical, PO, IV

Colistin (polymyxin E) is a polymyxin antibiotic produced by certain strains of Bacillus polymyxa var. colistinus. Colistin is a mixture of cyclic polypeptides colistin A and B. Colistin is effective against Gram-negative bacilli, except Proteus and Burkholderia cepacia. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body. ... Polymyxins are cationic detergent antibiotics, with a general structure of a cyclic peptide with a long hydrophobic tail. ... Staphylococcus aureus - Antibiotics test plate. ... alpha amanitin bacitracin cyclosporine Cyclic peptides (or cyclic proteins) are polypeptide chains whose amino and carboxy termini are themselves linked together with a peptide bond, forming a circular chain. ... Bacteria that are Gram-negative are not stained dark blue or violet by Gram staining, in contrast to Gram-positive bacteria. ... In biology, Proteus is a genus of Gram-negative Proteobacteria, which includes pathogens responsible for many human urinary tract infections. ... Burkholderia cepacia complex or simply Burkholderia cepacia is a group of catalase-producing, non-lactose-fermenting Gram-negative bacteria composed of at least seven different species, including Burkholderia multivorans, Burkholderia vietnamiensis, Burkholderia stabilis, and Burkholderia ambifaria. ...

Contents

Administration and posology

Forms

There are two forms of colistin available commercially: colistin sulfate and colistimethate sodium (colistin methanesulphonate sodium, colistin sulfomethate sodium). Colistin sulfate is cationic, colistimethate sodium is anionic; colistin sulphate is stable, but colistimethate sodium is readily hydrolysed to a variety of methanesulfonated derivatives. Colistin sulfate and colistimethate sodium are eliminated from the body by different routes. With respect to Pseudomonas aeruginosa, colistimethate is the inactive prodrug of colistin. The two drugs are not interchangeable. In chemistry, a cationic species is one that contains a full positive charge. ... In chemistry, an anionic species is one that contains a full negative charge. ... Binomial name Pseudomonas aeruginosa (Schroeter 1872) Migula 1900 Synonyms Bacterium aeruginosum Schroeter 1872 Bacterium aeruginosum Cohn 1872 Micrococcus pyocyaneus Zopf 1884 Bacillus aeruginosus (Schroeter 1872) Trevisan 1885 Bacillus pyocyaneus (Zopf 1884) Flügge 1886 Pseudomonas pyocyanea (Zopf 1884) Migula 1895 Bacterium pyocyaneum (Zopf 1884) Lehmann and Neumann 1896 Pseudomonas polycolor...

  • Colistimethate sodium may be used to treat Pseudomonas aeruginosa infections in cystic fibrosis patients and it has come into recent use for treating multidrug-resistant Acinetobacter infection, although resistant forms have been reported.[1][2] Colistimethate sodium has also been given intrathecally and intraventricularly in Acinetobacter baumanii and Pseudomonas aeruginosa meningitis/ventriculitis [3][4][5][6] Some studies have indicated that colistin may be useful for treating infections caused by carbapenem-resistant isolates of Acinetobacter baumannii.[2]
  • Colistin sulfate may be used to treat intestinal infections, or to suppress colonic flora. Colistin sulfate is also used as topical creams, powders, and otic solutions.

Species A. baumannii A. lwoffii etc. ... Acinetobacter is a genus of Proteobacteria. ... It has been suggested that this article or section be merged with Large intestine. ...

Dosage

Colistin sulfate and colistimethate sodium may both be given intravenously, but the dosing is complicated. Colistimethate sodium manufactured by Dumex-Alpharma (Colomycin injection®) is prescribed in international units, but colistimethate sodium manufactured by Parkdale Pharmaceuticals (Coly-Mycin M Parenteral®) is prescribed in milligrams of colistin base:

  • Colomycin 1,000,000 units is 80mg colistimethate;[7]
  • Coly-mycin M 150mg "colistin base" is 360mg colistimethate or 4,500,000 units.[8]

Because colistin was introduced into clinical practice over 50 years ago, it was never subject to the regulations that modern drugs are subject to, and therefore there is no standardised dosing of colistin and no detailed trials on pharmacology or pharmacokinetics: the optimal dosing of colistin for most infections is therefore unknown. Colomycin has a recommended intravenous dose of 1 to 2 million units thrice daily for patients weighing 60kg or more with normal renal function, Coly-Mycin has a recommended dose of 2.5 to 5mg/kg colistin base a day, which is equivalent to 6 to 12 mg/kg colistimethate sodium per day. For a 60kg man, therefore, the recommended dose for Colomycin is 240 to 480mg of colistimethate sodium, yet the recommended dose for Coly-Mycin is 360 to 720mg of colistimethate sodium. Likewise, the recommended "maximum" dose for each preparation is different (480mg for Colomycin and 720mg for Coly-Mycin). Each country has different generic preparations of colistin and the recommended dose will depend on the manufacturer. This complete absence of any regulation or standardisation of dose makes intravenous colistin dosing a nightmare for any physician.


Colistin has been used in combination with rifampicin, and there is in-vitro evidence of synergy,[9][10] and the combination has been used successfully in patients.[11] There is also in-vitro evidence of synergy for colistimethate sodium used in combination with other antipseudomonal antibiotics [12]. Rifampicin (INN) (IPA: ) or rifampin (USAN) is a bacteriocidal antibiotic drug of the rifamycin group. ...


Colistimethate sodium aerosol (Promixin®; Colomycin Injection®) is used to treat pulmonary infections, especially in cystic fibrosis. In the UK, the recommended adult dose is 1 - 2 million units (80 - 160mg) nebulised colistimethate twice daily.[13][14]


Mode of action

Colistin is polycationic and has both hydrophilic and lipophilic moieties. These interact with the bacterial cytoplasmic membrane, changing its permeability. This effect is bactericidal. In chemistry, a cationic species is one that contains a full positive charge. ... The adjective hydrophilic describes something that likes water (from Greek hydros = water; philos = friend). ... This article or section does not cite its references or sources. ... Drawing of a cell membrane A component of every biological cell, the cell membrane (or plasma membrane) is a thin and structured bilayer of phospholipid and protein molecules that encapsulate the cell. ...


Resistance

Resistance to colistin is currently rare, but is described. At present there is no agreement about how to look for colistin resistance. The Société Française de Microbiologie uses a cut off of 2mg/l, whereas the British Society for Antimicrobial Chemotherapy sets a cutoff of 4mg/l or less as sensitive, and 8mg/ml or more as resistant. There are not currently any US standards for measuring colistin sensitivity.


Pharmacokinetics

There is no clinically useful absorption of colistin from the gastrointestinal tract. For systemic infection, colistin must therefore be given by injection. Colistimethate is eliminated by the kidneys, but colistin is supposed to be eliminated by non-renal mechanism(s) that are as yet not characterised.[15][16]


Adverse reactions

The main toxicities described with intravenous treatment are nephrotoxicity (damage to the kidneys) and neurotoxicity (damage to the nerves),[17][18][19][20] but this may reflect the very high doses given, which are much higher than the doses currently recommended by any manufacturer and for which no adjustment was made for renal disease. Neuro- and nephrotoxic effects appear to be transient and subside on discontinuation of therapy or reduction in dose [21].


At a dose of 160mg colistimethate IV every eight hours, very little nephrotoxicity is seen.[22][23] Indeed, colistin appears to have less toxicity than the aminoglycosides that subsequently replaced it, and colistin has been used for extended periods of up to six months with no ill effects.[24]


The main toxicity described with aerosolised treatment is bronchospasm [25] which can be treated or prevented with the use of beta2-agonists such as salbutamol [26] or following a desensitisation protocol[27]. Bronchospasm is a difficulty in breathing caused by a sudden constriction of the muscles in the walls of the bronchioles. ... Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and COPD. Salbutamol sulphate is usually given by the inhaled route for direct effect on bronchial smooth muscle. ...


Further reading

  • Li J, Nation RL, Tunridge JD, et al. (2006). "Colistin: the re-emerging antibiotic for multidrug-resistant Gram-negative bacterial infections". Lancet Infect Dis 6 (8): 589–601. 
  • Li J , Nation RL, Milne RW, et al. (2005). "Evaluation of colistin as an agent against multi-resistant Gram-negative bacteria". Int J Antimicrob Agents 25: 11–25. 

References

  1. ^ Reis AO, Luz DAM, Tognim MCB, Sader HS, and Gales AC (2003). "Polymyxin-Resistant Acinetobacter spp. Isolates: What Is Next?". Emerg Infect Dis 9: 1025–7. 
  2. ^ a b Towner K J (2008). "Molecular Basis of Antibiotic Resistance in Acinetobacter spp.", Acinetobacter Molecular Biology. Caister Academic Press. ISBN 978-1-904455-20-2. 
  3. ^ Benifla M, Zucker G, Cohen S and Alkan M (2004). "Successful treatment of Acinetobacter meningitis with intrathecal polymyxin". J Antimicrobial Chemotherapy 54: 290–293. 
  4. ^ Yagmur et al., (2006). "Intrathecal colistin for treatment of Pseudomonas aeruginosa ventriculitis: report of a case with successful outcome". Critical Care 10. 
  5. ^ Motaouakkil et al., (2006). "Colistin and rifampicin in the treatment of nosocomial infections from multiresistant Acinetobacter baumannii". Journal of Infection 53: 274–278. 
  6. ^ Karakitsos et al., (2006). "Is intraventricular colistin an effective and safe treatment for post-surgical ventriculitis in the intensive care unit?". Acta Anaesthesiol Scand. 50: 1309–1310. 
  7. ^ Colomycin injection [Summary of product characteristics]. http://emc.medicines.org.uk/emc/assets/c/html/displaydoc.asp?documentid=1590
  8. ^ http://www.emea.europa.eu/pdfs/vet/mrls/081502en.pdf; NB. Colistin base has an assigned potency of 30 000 IU/mg
  9. ^ Giamarellos-Bourboulis EJ, Sambatakou H, Galani I, Giamarellou H. (2003). "In vitro interaction of colistin and rifampin on multidrug-resistant Pseudomonas aeruginosa". J Chemother 15: 235–38. 
  10. ^ Hogg GM, Barr JG, Webb CH. (1998). "In-vitro activity of the combination of colistin and rifampicin against multidrug-resistant strains of Acinetobacter baumannii". J Antimicrob Chemother 41: 494–95. 
  11. ^ Petrosillo N, Chinello P, Proietti MF, et al. (2005). "Combined colistin and rifampicin therapy for carbapenem-resistant Acinetobacter baumannii infections: clinical outcome and adverse events". Clin Microbiol Infect 11: 682–83. 
  12. ^ MacGowan AP, Rynn C, Wootton M, Bowker KE, Holt HA, Reeves DS. (1999). "In vitro assessment of colistin's antipseudomonal antimicrobial interactions with other antibiotics". Clin Microbiol Infect. 5: 32–36. 
  13. ^ Promixin [Summary of Product Characteristics] http://emc.medicines.org.uk/emc/assets/c/html/displaydoc.asp?documentid=13532
  14. ^ Colomycin Injection [Summary of Product Characteristics] http://emc.medicines.org.uk/emc/assets/c/html/displaydoc.asp?documentid=1590
  15. ^ Li J, Milne RW, Nation RL, et al. (2004). "Pharmacokinetics of colistin methanesulphonate and colistin in rats following an intravenous dose of colistin methanesulphonate". J Antimicrob Chemother. 53. 
  16. ^ Li J, Milne RW, Nation RL, et al. (2003). "Use of high performance liquid chromatography to study the pharmacokinetics of colistin sulfate in rats following intravenous administration". Antimicrob Agents Chemother 47: 1766–70. 
  17. ^ Wolinsky E, Hines JD. (1962). "Neurotoxic and nephrotoxic effects of colistin in patients with renal disease". N Engl J Med 266: 759–68. 
  18. ^ Koch-Weser J, Sidel VW, Federman EB, et al. (1970). "Adverse effects of sodium colistimethate. Manifestations and specific reaction rates during 317 courses of therapy". Ann Intern Med 72: 857–68. 
  19. ^ Ledson MJ, Gallagher MJ, Cowperthwaite C, et al. (1998). "Four years' experience of intravenous colomycin in an adult cystic fibrosis unit". Eur Respir J 12: 592–94. 
  20. ^ Li J, Nation RL, Milne RW, et al. (2005). "Evaluation of colistin as an agent against multi-resistant Gram-negative bacteria". Int J Antimicrob Agents 25: 11–25. 
  21. ^ Beringer P. (2001). "The clinical use of colistin in patients with cystic fibrosis". Current Opinion in Pulmonary Medicine 7: 434–440. 
  22. ^ Conway SP, Etherington C, Munday J, et al. (2000). "Safety and tolerability of bolus intravenous colistin in acute respiratory exacerbation in adults with cystic fibrosis". Ann Pharmacother 34: 1238–42. 
  23. ^ Littlewood JM, Koch C, Lambert PA , et al. (2000). "A ten year review of Colomycin". Respir Med 94: 632–40. 
  24. ^ Stein A, Raoult D. (2002). "Colistin: an antimicrobial for the 21st century?" 35: 901–2. 
  25. ^ Maddison J, Dodd M, Webb AK. (1994). "Nebulized colistin causes chest tightness in adults with cystic fibrosis". Respir Med. 88: 145–147. 
  26. ^ Kamin W, Schwabe A, Kramer I. (2006). "Inhalation solutions: which one are allowed to be mixed? Physico-chemical compatibility of drug solutions in nebulizers". J Cyst Fibros. 5: 205–213. 
  27. ^ Dominguez-Ortega J, Manteiga E, Abad-Schilling C, Juretzcke MA, Sanchez-Rubio J, Kindelan C. (2007). "Induced tolerance to nebulized colistin after severe reaction to the drug". J Investig Allergol Clin Immunol. 17: 59–61. 

  Results from FactBites:
 
Reference.com/Encyclopedia/Colistin (865 words)
Colistin is a mixture of cyclic polypeptides colistin A and B. Colistin is effective against Gram-negative bacilli, except Proteus and Burkholderia cepacia.
Colistin sulfate is cationic, colistimethate sodium is anionic; colistin sulphate is stable, but colistimethate sodium is readily hydrolysed to a variety of methanesulfonated derivatives.
"Colistin: the re-emerging antibiotic for multidrug-resistant Gram-negative bacterial infections".
BioMed Central | Full text | Toxicity after prolonged (more than four weeks) administration of intravenous colistin (3669 words)
Colistin was given for long duration in patients mainly in the ICU setting, because of persistence of infections due to Gram-negative bacteria sensitive only to colistin or bacteria sensitive also to antibiotics of other classes that were previously administered (based on in-vitro susceptibility test results) but failed.
For the subgroup of 12 patients with 14 courses of prolonged colistin administration, with normal serum creatinine at the initiation of treatment, the median serum creatinine values at baseline and at the end of colistin treatment were 0,60 mg/dl and 0,55 mg/dl, respectively.
The conclusion in the majority of the published studies during 1960 – 1970 was that colistin must be used in serious infections where other antimicrobial agents have failed, always with close monitor of renal function, and with precaution in the co-administration of other possible nephrotoxic or neutotoxic agents [2,4].
  More results at FactBites »

 
 

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