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Brand names,
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Analogs
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Brand Names Mixture
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Chemical_Formula
C58H105N16Na5O28S5
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RX_link
http://www.rxlist.com/cgi/generic2/colistimethate.htm
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fda sheet
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msds (material safety sheet)
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Synthesis Reference
No information avaliable
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Molecular Weight
1749.82 g/mol
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Melting Point
No information avaliable
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H2O Solubility
Appreciable
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State
Solid
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LogP
No information avaliable
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Dosage Forms
Vials containing colistimethate sodium or pentasodium colistinmethanesulfonate (150 mg colistin base activity) for injection.
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Indication
For the treatment of acute or chronic infections due to sensitive strains of certain gram-negative bacilli, particularly Pseudomonas aeruginosa.
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Pharmacology
Colistimethate is a polymyxin antibiotic agent. Originally, colistimethate sodium was thought to be less toxic than polymyxin B; however, if the drugs are administered at comparable doses, their toxicities may be similar. 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.
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Absorption
Very poor absorption from gastrointestinal tract.
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side effects and Toxicity
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.
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Patient Information
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Organisms Affected
Gram-negative bacilli