Colistimethate

Identification

Name
Colistimethate
Accession Number
DB01111  (APRD00885)
Type
Small Molecule
Groups
Approved, Vet approved
Description

Colistimethate is an antibiotic that has been shown to have bactericidal activity against aerobic gram-negative microorganisms. Colistimethate is particularly indicated when the infection is caused by sensitive strains of Pseudomonas aeruginosa.

Structure
Thumb
Synonyms
  • Colistin methanesulfonic acid
  • Colistin sulfomethate
  • Colistinmethanesulfonic acid
Product Ingredients
IngredientUNIICASInChI Key
Colistimethate sodiumXW0E5YS77G8068-28-8BSSIRFLGSWHWDE-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ColobreatheCapsule1662500 IURespiratory (inhalation)Teva B.V.2012-02-13Not applicableEu
ColobreatheCapsule1662500 IURespiratory (inhalation)Teva B.V.2012-02-13Not applicableEu
ColobreatheCapsule1662500 IURespiratory (inhalation)Teva B.V.2012-02-13Not applicableEu
Coly-Mycin MInjection150 mg/2mLIntramuscular; IntravenousPar Pharmaceutical2007-11-01Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ColistimethateInjection150 mg/2mLIntramuscular; IntravenousXellia Pharmaceuticals, Ap S2012-11-22Not applicableUs
ColistimethateInjection, powder, lyophilized, for solution150 mg/2mLIntramuscular; IntravenousX Gen Pharmaceuticals, Inc.2011-01-01Not applicableUs
ColistimethateInjection, powder, lyophilized, for solution150 mg/2mLIntramuscular; IntravenousFresenius Kabi2009-12-04Not applicableUs
ColistimethateInjection, powder, lyophilized, for solution150 mg/2mLIntramuscular; IntravenousPaddock Laboratories, Inc.2004-03-202018-06-30Us
ColistimethateInjection150 mg/2mLIntramuscular; IntravenousX Gen Pharmaceuticals, Inc.2016-07-01Not applicableUs
ColistimethateInjection, powder, lyophilized, for solution150 mg/2mLIntramuscular; IntravenousSagent Pharmaceuticals2014-12-29Not applicableUs
ColistimethateInjection150 mg/2mLIntramuscular; IntravenousPar Pharmaceutical2012-06-01Not applicableUs
Colistimethate SodiumInjection, powder, lyophilized, for solution150 mg/4mLIntramuscular; IntravenousHeritage2012-10-22Not applicableUs
Categories
UNII
DL2R53P963
CAS number
12705-41-8
Weight
Average: 1634.87
Monoisotopic: 1633.588775306
Chemical Formula
C58H105N16O28S5
InChI Key
BSSIRFLGSWHWDE-UHFFFAOYSA-I
InChI
InChI=1S/C58H110N16O28S5/c1-9-35(6)12-10-11-13-46(77)65-38(14-20-59-28-103(88,89)90)53(82)74-48(37(8)76)58(87)70-41(17-23-62-31-106(97,98)99)50(79)68-43-19-25-64-57(86)47(36(7)75)73-54(83)42(18-24-63-32-107(100,101)102)67-49(78)39(15-21-60-29-104(91,92)93)69-55(84)44(26-33(2)3)72-56(85)45(27-34(4)5)71-52(81)40(66-51(43)80)16-22-61-30-105(94,95)96/h33-45,47-48,59-63,75-76H,9-32H2,1-8H3,(H,64,86)(H,65,77)(H,66,80)(H,67,78)(H,68,79)(H,69,84)(H,70,87)(H,71,81)(H,72,85)(H,73,83)(H,74,82)(H,88,89,90)(H,91,92,93)(H,94,95,96)(H,97,98,99)(H,100,101,102)/p-5
IUPAC Name
[(3-{3-hydroxy-2-[2-(6-methyloctanamido)-4-[(sulfonatomethyl)amino]butanamido]butanamido}-3-{[3-(1-hydroxyethyl)-12,15-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-6,9,18-tris({2-[(sulfonatomethyl)amino]ethyl})-1,4,7,10,13,16,19-heptaazacyclotricosan-21-yl]carbamoyl}propyl)amino]methanesulfonate
SMILES
CCC(C)CCCCC(=O)NC(CCNCS([O-])(=O)=O)C(=O)NC(C(C)O)C(=O)NC(CCNCS([O-])(=O)=O)C(=O)NC1CCNC(=O)C(NC(=O)C(CCNCS([O-])(=O)=O)NC(=O)C(CCNCS([O-])(=O)=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CCNCS([O-])(=O)=O)NC1=O)C(C)O

Pharmacology

Indication

For the treatment of acute or chronic infections due to sensitive strains of certain gram-negative bacilli, particularly Pseudomonas aeruginosa.

Associated Conditions
Pharmacodynamics

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.

Mechanism of action

Colistimethate is a surface active agent which penetrates into and disrupts the bacterial cell membrane. Colistimethate 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.

TargetActionsOrganism
ABacterial outer membrane
incorporation into and destabilization
Absorption

Very poor absorption from gastrointestinal tract.

Volume of distribution
Not Available
Protein binding
Not Available
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.

Route of elimination
Not Available
Half life

2-3 hours following either intravenous or intramuscular administration in adults and in the pediatric population, including premature infants.

Clearance
Not Available
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.

Affected organisms
  • Gram-negative bacilli
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AlcuroniumColistimethate may increase the neuromuscular blocking activities of Alcuronium.Experimental
AmikacinThe risk or severity of adverse effects can be increased when Colistimethate is combined with Amikacin.Approved, Investigational, Vet Approved
Amphotericin BAmphotericin B may increase the nephrotoxic activities of Colistimethate.Approved, Investigational
ApramycinApramycin may increase the nephrotoxic activities of Colistimethate.Experimental, Vet Approved
ArbekacinArbekacin may increase the nephrotoxic activities of Colistimethate.Approved, Investigational
AtracuriumColistimethate may increase the neuromuscular blocking activities of Atracurium.Approved, Experimental, Investigational
Atracurium besylateColistimethate may increase the neuromuscular blocking activities of Atracurium besylate.Approved
BacitracinColistimethate may increase the nephrotoxic activities of Bacitracin.Approved, Vet Approved
BekanamycinBekanamycin may increase the nephrotoxic activities of Colistimethate.Experimental
BenzphetamineThe risk or severity of adverse effects can be increased when Benzphetamine is combined with Colistimethate.Approved, Illicit
Benzyl alcoholThe risk or severity of adverse effects can be increased when Benzyl alcohol is combined with Colistimethate.Approved
BrompheniramineThe risk or severity of adverse effects can be increased when Brompheniramine is combined with Colistimethate.Approved
BupropionThe risk or severity of adverse effects can be increased when Bupropion is combined with Colistimethate.Approved
CapreomycinCapreomycin may increase the neuromuscular blocking activities of Colistimethate.Approved
CarbamazepineThe risk or severity of adverse effects can be increased when Carbamazepine is combined with Colistimethate.Approved, Investigational
CetirizineThe risk or severity of adverse effects can be increased when Cetirizine is combined with Colistimethate.Approved
ChlorphenamineThe risk or severity of adverse effects can be increased when Chlorphenamine is combined with Colistimethate.Approved
CisatracuriumColistimethate may increase the neuromuscular blocking activities of Cisatracurium.Approved
ClemastineThe risk or severity of adverse effects can be increased when Clemastine is combined with Colistimethate.Approved, Investigational
ClindamycinThe risk or severity of adverse effects can be increased when Clindamycin is combined with Colistimethate.Approved, Vet Approved
CodeineThe risk or severity of adverse effects can be increased when Codeine is combined with Colistimethate.Approved, Illicit
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Colistimethate.Approved
CyclosporineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Cyclosporine.Approved, Investigational, Vet Approved
DecamethoniumColistimethate may increase the neuromuscular blocking activities of Decamethonium.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Desvenlafaxine.Approved, Investigational
DexbrompheniramineThe risk or severity of adverse effects can be increased when Dexbrompheniramine is combined with Colistimethate.Approved
DibekacinDibekacin may increase the nephrotoxic activities of Colistimethate.Experimental
DiclofenacThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Diclofenac.Approved, Vet Approved
DihydrostreptomycinDihydrostreptomycin may increase the nephrotoxic activities of Colistimethate.Investigational, Vet Approved
DimenhydrinateThe risk or severity of adverse effects can be increased when Dimenhydrinate is combined with Colistimethate.Approved
DiphenhydramineThe risk or severity of adverse effects can be increased when Diphenhydramine is combined with Colistimethate.Approved, Investigational
Domoic AcidColistimethate may increase the neuromuscular blocking activities of Domoic Acid.Experimental
DotarizineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Dotarizine.Investigational
DoxacuriumColistimethate may increase the neuromuscular blocking activities of Doxacurium chloride.Approved
DoxylamineDoxylamine may increase the central nervous system depressant (CNS depressant) activities of Colistimethate.Approved, Vet Approved
EperisoneThe risk or severity of adverse effects can be increased when Eperisone is combined with Colistimethate.Approved, Investigational
EthanolColistimethate may increase the central nervous system depressant (CNS depressant) activities of Ethanol.Approved
EthosuximideThe risk or severity of adverse effects can be increased when Ethosuximide is combined with Colistimethate.Approved
EtomidateThe risk or severity of adverse effects can be increased when Etomidate is combined with Colistimethate.Approved
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Colistimethate.Approved, Illicit, Investigational, Vet Approved
FlunarizineThe risk or severity of adverse effects can be increased when Flunarizine is combined with Colistimethate.Approved
FluoxetineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Fluoxetine.Approved, Vet Approved
FluspirileneThe risk or severity of adverse effects can be increased when Fluspirilene is combined with Colistimethate.Approved, Investigational
Fluticasone propionateThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Colistimethate.Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Fluvoxamine.Approved, Investigational
FramycetinFramycetin may increase the nephrotoxic activities of Colistimethate.Approved
GabapentinThe risk or severity of adverse effects can be increased when Gabapentin is combined with Colistimethate.Approved, Investigational
GallamineColistimethate may increase the neuromuscular blocking activities of Gallamine.Experimental
Gallamine TriethiodideColistimethate may increase the neuromuscular blocking activities of Gallamine Triethiodide.Approved
GeneticinGeneticin may increase the nephrotoxic activities of Colistimethate.Experimental
GentamicinGentamicin may increase the nephrotoxic activities of Colistimethate.Approved, Vet Approved
GENTAMICIN C1AGENTAMICIN C1A may increase the nephrotoxic activities of Colistimethate.Experimental
GuanfacineThe risk or severity of adverse effects can be increased when Guanfacine is combined with Colistimethate.Approved, Investigational
HydrocodoneColistimethate may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.Approved, Illicit
HydroxyzineHydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Colistimethate.Approved
Hygromycin BHygromycin B may increase the nephrotoxic activities of Colistimethate.Vet Approved
IbandronateThe risk or severity of nephrotoxicity and hypocalcemia can be increased when Colistimethate is combined with Ibandronate.Approved, Investigational
IbuprofenThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Ibuprofen.Approved
IsepamicinIsepamicin may increase the nephrotoxic activities of Colistimethate.Experimental
KanamycinKanamycin may increase the nephrotoxic activities of Colistimethate.Approved, Investigational, Vet Approved
KetorolacThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Ketorolac.Approved
LamotrigineThe risk or severity of adverse effects can be increased when Lamotrigine is combined with Colistimethate.Approved, Investigational
LevetiracetamThe risk or severity of adverse effects can be increased when Levetiracetam is combined with Colistimethate.Approved, Investigational
LevodopaThe risk or severity of adverse effects can be increased when Levodopa is combined with Colistimethate.Approved
LoratadineThe risk or severity of adverse effects can be increased when Loratadine is combined with Colistimethate.Approved, Investigational
Magnesium carbonateThe risk or severity of adverse effects can be increased when Colistimethate is combined with Magnesium carbonate.Approved, Investigational
Magnesium citrateThe risk or severity of adverse effects can be increased when Colistimethate is combined with Magnesium citrate.Approved
Magnesium hydroxideThe risk or severity of adverse effects can be increased when Colistimethate is combined with Magnesium hydroxide.Approved, Investigational
Magnesium sulfateThe therapeutic efficacy of Colistimethate can be increased when used in combination with Magnesium sulfate.Approved, Investigational, Vet Approved
Magnesium TrisilicateThe risk or severity of adverse effects can be increased when Colistimethate is combined with Magnesium Trisilicate.Approved
MecamylamineColistimethate may increase the neuromuscular blocking activities of Mecamylamine.Approved, Investigational
MeclizineThe risk or severity of adverse effects can be increased when Meclizine is combined with Colistimethate.Approved
MethsuximideThe risk or severity of adverse effects can be increased when Methsuximide is combined with Colistimethate.Approved
MetocurineColistimethate may increase the neuromuscular blocking activities of Metocurine.Approved
Metocurine IodideColistimethate may increase the neuromuscular blocking activities of Metocurine Iodide.Approved, Withdrawn
MicronomicinMicronomicin may increase the nephrotoxic activities of Colistimethate.Experimental
MivacuriumColistimethate may increase the neuromuscular blocking activities of Mivacurium.Approved
NaproxenThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Naproxen.Approved, Vet Approved
NeamineNeamine may increase the nephrotoxic activities of Colistimethate.Experimental
NeomycinThe risk or severity of adverse effects can be increased when Colistimethate is combined with Neomycin.Approved, Vet Approved
NeosaxitoxinColistimethate may increase the neuromuscular blocking activities of Neosaxitoxin.Investigational
NetilmicinNetilmicin may increase the nephrotoxic activities of Colistimethate.Approved, Investigational
NicotineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Nicotine.Approved
NimesulideThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Nimesulide.Approved, Investigational, Withdrawn
OndansetronThe risk or severity of adverse effects can be increased when Ondansetron is combined with Colistimethate.Approved
OxycodoneThe risk or severity of adverse effects can be increased when Oxycodone is combined with Colistimethate.Approved, Illicit, Investigational
OxymorphoneThe risk or severity of adverse effects can be increased when Oxymorphone is combined with Colistimethate.Approved, Investigational, Vet Approved
PancuroniumColistimethate may increase the neuromuscular blocking activities of Pancuronium.Approved
ParomomycinThe risk or severity of adverse effects can be increased when Colistimethate is combined with Paromomycin.Approved, Investigational
ParoxetineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Paroxetine.Approved, Investigational
PenfluridolThe risk or severity of adverse effects can be increased when Penfluridol is combined with Colistimethate.Experimental
PhenobarbitalThe risk or severity of adverse effects can be increased when Phenobarbital is combined with Colistimethate.Approved, Investigational
PipecuroniumColistimethate may increase the neuromuscular blocking activities of Pipecuronium.Approved
PlazomicinPlazomicin may increase the nephrotoxic activities of Colistimethate.Approved, Investigational
Polymyxin B SulfatePolymyxin B Sulfate may increase the neuromuscular blocking activities of Colistimethate.Approved, Vet Approved
PramipexoleColistimethate may increase the sedative activities of Pramipexole.Approved, Investigational
PregabalinThe therapeutic efficacy of Colistimethate can be increased when used in combination with Pregabalin.Approved, Illicit, Investigational
ProchlorperazineThe risk or severity of adverse effects can be increased when Prochlorperazine is combined with Colistimethate.Approved, Vet Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Colistimethate.Approved, Investigational
PseudoephedrineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Pseudoephedrine.Approved
PuromycinPuromycin may increase the nephrotoxic activities of Colistimethate.Experimental
PyrantelThe therapeutic efficacy of Pyrantel can be increased when used in combination with Colistimethate.Approved, Vet Approved
QuetiapineThe risk or severity of adverse effects can be increased when Quetiapine is combined with Colistimethate.Approved
RapacuroniumColistimethate may increase the neuromuscular blocking activities of Rapacuronium.Withdrawn
RibostamycinRibostamycin may increase the nephrotoxic activities of Colistimethate.Approved, Investigational
RizatriptanThe risk or severity of adverse effects can be increased when Colistimethate is combined with Rizatriptan.Approved
RocuroniumColistimethate may increase the neuromuscular blocking activities of Rocuronium.Approved
RopiniroleColistimethate may increase the sedative activities of Ropinirole.Approved, Investigational
Salicylic acidThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Salicylic acid.Approved, Investigational, Vet Approved
ScopolamineThe risk or severity of adverse effects can be increased when Scopolamine is combined with Colistimethate.Approved, Investigational
SisomicinSisomicin may increase the nephrotoxic activities of Colistimethate.Investigational
StreptomycinStreptomycin may increase the nephrotoxic activities of Colistimethate.Approved, Vet Approved
SuccinylcholineColistimethate may increase the neuromuscular blocking activities of Succinylcholine.Approved
SulfasalazineThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Sulfasalazine.Approved
SulindacThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Sulindac.Approved, Investigational
SumatriptanThe risk or severity of adverse effects can be increased when Colistimethate is combined with Sumatriptan.Approved, Investigational
TetracyclineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Tetracycline.Approved, Vet Approved
TetrahydropalmatineThe risk or severity of adverse effects can be increased when Tetrahydropalmatine is combined with Colistimethate.Investigational
TobramycinTobramycin may increase the nephrotoxic activities of Colistimethate.Approved, Investigational
Tolfenamic AcidThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Tolfenamic Acid.Approved, Investigational
TopiramateThe risk or severity of adverse effects can be increased when Topiramate is combined with Colistimethate.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Colistimethate.Approved, Investigational
TrimethadioneThe risk or severity of adverse effects can be increased when Trimethadione is combined with Colistimethate.Approved
Trolamine salicylateThe risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Trolamine salicylate.Approved
TubocurarineColistimethate may increase the neuromuscular blocking activities of Tubocurarine.Approved
Valproic AcidThe risk or severity of adverse effects can be increased when Valproic Acid is combined with Colistimethate.Approved, Investigational
VancomycinVancomycin may increase the nephrotoxic activities of Colistimethate.Approved
VecuroniumThe therapeutic efficacy of Vecuronium can be increased when used in combination with Colistimethate.Approved
VenlafaxineThe risk or severity of adverse effects can be increased when Colistimethate is combined with Venlafaxine.Approved
VinpocetineThe risk or severity of adverse effects can be increased when Vinpocetine is combined with Colistimethate.Investigational
ZiconotideThe risk or severity of adverse effects can be increased when Ziconotide is combined with Colistimethate.Approved
Zoledronic acidThe risk or severity of nephrotoxicity and hypocalcemia can be increased when Colistimethate is combined with Zoledronic acid.Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Colistimethate is combined with Zolmitriptan.Approved, Investigational
ZolpidemColistimethate may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.Approved
ZonisamideThe risk or severity of adverse effects can be increased when Zonisamide is combined with Colistimethate.Approved, Investigational
Food Interactions
Not Available

References

General References
Not Available
External Links
Human Metabolome Database
HMDB0015243
PubChem Compound
70789202
PubChem Substance
46508586
ChemSpider
26329515
ChEBI
59662
Therapeutic Targets Database
DAP001329
PharmGKB
PA164749509
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Colistimethate
FDA label
Download (66.2 KB)
MSDS
Download (50.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentPseudomonas Infections1
2Unknown StatusTreatmentPneumonia, Hospital-Acquired1
3CompletedTreatmentAcute Pyelonephritis (AP) Due to CRE / Bloodstream Infections (BSI) Due to CRE / Complicated Urinary Tract Infection (cUTI) Due to CRE / Hospital-Acquired Bacterial Pneumonia (HABP) Due to CRE / Ventilator-Associated Bacterial Pneumonia (VABP) Due to CRE1
3CompletedTreatmentBacterial Infections1
3RecruitingPreventionNon Cystic Fibrosis Bronchiectasis2
3RecruitingTreatmentBlood Stream Infections / Pneumonia1
3TerminatedTreatmentColistin Adverse Reaction / Infection Due to Multidrug Resistant Acinetobacter / Infection Resistant to Multiple Drugs / Ventilator-Associated Pneumonia (VAP)1
4CompletedPreventionHematological Infection1
4CompletedTreatmentCystic Fibrosis (CF)1
4CompletedTreatmentGram-Negative Bacterial Infections1
4RecruitingTreatmentGram Negative Bacterial Infections1
Not AvailableActive Not RecruitingNot AvailableColistin1
Not AvailableCompletedNot AvailableAcinetobacter Infections1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • APP Pharmaceuticals
  • Ben Venue Laboratories Inc.
  • Draxis Specialty Pharmaceuticals Inc.
  • JHP Pharmaceuticals LLC
  • Monarch Pharmacy
  • Paddock Labs
  • X-Gen Pharmaceuticals
Dosage forms
FormRouteStrength
InjectionIntramuscular; Intravenous150 mg/2mL
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous150 mg/2mL
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous150 mg/4mL
CapsuleRespiratory (inhalation)1662500 IU
Prices
Unit descriptionCostUnit
Coly-mycin m 150 mg vial72.98USD vial
Colistimethate 150 mg vial57.0USD vial
Coly-Mycin S 3.3-3-10 mg/ml Suspension 5ml Bottle49.17USD bottle
Colistimethate For Injection 150 mg/vial35.42USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityAppreciableNot Available
Predicted Properties
PropertyValueSource
Water Solubility4.17 mg/mLALOGPS
logP-1.2ALOGPS
logP-17ChemAxon
logS-2.6ALOGPS
pKa (Strongest Acidic)-4.3ChemAxon
pKa (Strongest Basic)6.46ChemAxon
Physiological Charge-5ChemAxon
Hydrogen Acceptor Count33ChemAxon
Hydrogen Donor Count18ChemAxon
Polar Surface Area706.71 Å2ChemAxon
Rotatable Bond Count44ChemAxon
Refractivity370.19 m3·mol-1ChemAxon
Polarizability161.9 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.8904
Blood Brain Barrier-0.8404
Caco-2 permeable-0.6453
P-glycoprotein substrateSubstrate0.7147
P-glycoprotein inhibitor INon-inhibitor0.6292
P-glycoprotein inhibitor IINon-inhibitor0.9498
Renal organic cation transporterNon-inhibitor0.9643
CYP450 2C9 substrateNon-substrate0.8963
CYP450 2D6 substrateNon-substrate0.7999
CYP450 3A4 substrateSubstrate0.5172
CYP450 1A2 substrateNon-inhibitor0.7722
CYP450 2C9 inhibitorNon-inhibitor0.7827
CYP450 2D6 inhibitorNon-inhibitor0.8721
CYP450 2C19 inhibitorNon-inhibitor0.7391
CYP450 3A4 inhibitorNon-inhibitor0.9385
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9888
Ames testNon AMES toxic0.6102
CarcinogenicityNon-carcinogens0.5677
BiodegradationReady biodegradable0.9192
Rat acute toxicity2.6289 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8368
hERG inhibition (predictor II)Non-inhibitor0.6834
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues.
Kingdom
Organic compounds
Super Class
Organic Polymers
Class
Polypeptides
Sub Class
Not Available
Direct Parent
Polypeptides
Alternative Parents
Cyclic peptides / Macrolactams / N-acyl-alpha amino acids and derivatives / Alpha amino acid amides / N-acyl amines / Organosulfonic acids / Alkanesulfonic acids / Sulfonyls / Secondary alcohols / Lactams
show 8 more
Substituents
Polypeptide / Cyclic alpha peptide / N-acyl-alpha amino acid or derivatives / Macrolactam / Alpha-amino acid amide / N-substituted-alpha-amino acid / Alpha-amino acid or derivatives / N-acyl-amine / Fatty acyl / Fatty amide
show 28 more
Molecular Framework
Aliphatic heteromonocyclic compounds
External Descriptors
Not Available

Targets

1. Bacterial outer membrane
Kind
Group
Organism
Not Available
Pharmacological action
Yes
Actions
Incorporation into and destabilization
References
  1. Vaara M: Polymyxins and their novel derivatives. Curr Opin Microbiol. 2010 Oct;13(5):574-81. doi: 10.1016/j.mib.2010.09.002. Epub 2010 Sep 24. [PubMed:20869908]
  2. Soon RL, Nation RL, Cockram S, Moffatt JH, Harper M, Adler B, Boyce JD, Larson I, Li J: Different surface charge of colistin-susceptible and -resistant Acinetobacter baumannii cells measured with zeta potential as a function of growth phase and colistin treatment. J Antimicrob Chemother. 2011 Jan;66(1):126-33. doi: 10.1093/jac/dkq422. Epub 2010 Nov 16. [PubMed:21081544]
  3. Evans ME, Feola DJ, Rapp RP: Polymyxin B sulfate and colistin: old antibiotics for emerging multiresistant gram-negative bacteria. Ann Pharmacother. 1999 Sep;33(9):960-7. [PubMed:10492501]

Drug created on June 13, 2005 07:24 / Updated on August 02, 2018 07:41