Identification

Name
Pefloxacin
Accession Number
DB00487  (APRD00108)
Type
Small Molecule
Groups
Approved
Description

A synthetic broad-spectrum fluoroquinolone antibacterial agent active against most gram-negative and gram-positive bacteria. [PubChem]

Structure
Thumb
Synonyms
  • Labocton
  • Pefloxacin
  • Pefloxacine
  • Pefloxacino
  • Pefloxacinum
  • PFLX
Product Ingredients
IngredientUNIICASInChI Key
Pefloxacin mesylate5IAD0UV3FH70458-95-6HQQSBEDKMRHYME-UHFFFAOYSA-N
Pefloxacin mesylate dihydrateCX28QC6FU0149676-40-4LEULAXMUNMRLPW-UHFFFAOYSA-N
International/Other Brands
Labocton
Categories
UNII
2H52Z9F2Q5
CAS number
70458-92-3
Weight
Average: 333.3574
Monoisotopic: 333.148869726
Chemical Formula
C17H20FN3O3
InChI Key
FHFYDNQZQSQIAI-UHFFFAOYSA-N
InChI
InChI=1S/C17H20FN3O3/c1-3-20-10-12(17(23)24)16(22)11-8-13(18)15(9-14(11)20)21-6-4-19(2)5-7-21/h8-10H,3-7H2,1-2H3,(H,23,24)
IUPAC Name
1-ethyl-6-fluoro-7-(4-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
SMILES
CCN1C=C(C(O)=O)C(=O)C2=CC(F)=C(C=C12)N1CCN(C)CC1

Pharmacology

Indication

For the treatment of uncomplicated gonococcal urethritis in males and for gram-negative-bacterial infections in the gastrointestinal system and the genitourinary tract.

Structured Indications
Not Available
Pharmacodynamics

Pefloxacin is a fluoroquinolone antibiotic. Flouroquinolones such as pefloxacin possess excellent activity against gram-negative aerobic bacteria such as E.coli and Neisseria gonorrhoea as well as gram-positive bacteria including S. pneumoniae and Staphylococcus aureus. They also posses effective activity against shigella, salmonella, campylobacter, gonococcal organisms, and multi drug resistant pseudomonas and enterobacter.

Mechanism of action

The bactericidal action of pefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.

TargetActionsOrganism
ADNA topoisomerase 4 subunit A
inhibitor
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
ADNA gyrase subunit A
inhibitor
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
UDNA topoisomerase 2-alpha
inhibitor
Human
UDNA topoisomerase 1Not AvailableStaphylococcus aureus
Absorption

Well absorbed by the oral route.

Volume of distribution
Not Available
Protein binding

20-30%

Metabolism

Hepatic. Primary metabolites are pefloxacin N-oxide and norfloxacin.

Route of elimination
Not Available
Half life

8.6 hours

Clearance
Not Available
Toxicity

Adverse reactions include peripheral neuropathy, nervousness, agitation, anxiety, and phototoxic events (rash, itching, burning) due to sunlight exposure.

Affected organisms
  • Enteric bacteria and other eubacteria
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
16-BromoepiandrosteroneThe risk or severity of adverse effects can be increased when 16-Bromoepiandrosterone is combined with Pefloxacin.Investigational
19-norandrostenedioneThe risk or severity of adverse effects can be increased when 19-norandrostenedione is combined with Pefloxacin.Experimental, Illicit
5-androstenedioneThe risk or severity of adverse effects can be increased when 5-androstenedione is combined with Pefloxacin.Experimental, Illicit
AcarbosePefloxacin may increase the hypoglycemic activities of Acarbose.Approved, Investigational
AceclofenacAceclofenac may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
AcemetacinAcemetacin may increase the neuroexcitatory activities of Pefloxacin.Approved
AcenocoumarolPefloxacin may increase the anticoagulant activities of Acenocoumarol.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Pefloxacin.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Pefloxacin.Experimental
Acetylsalicylic acidAcetylsalicylic acid may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved
AdapaleneAdapalene may increase the neuroexcitatory activities of Pefloxacin.Approved
AlbiglutidePefloxacin may increase the hypoglycemic activities of Albiglutide.Approved
AlclofenacAlclofenac may increase the neuroexcitatory activities of Pefloxacin.Approved, Withdrawn
AlclometasoneThe risk or severity of adverse effects can be increased when Alclometasone is combined with Pefloxacin.Approved
AldosteroneThe risk or severity of adverse effects can be increased when Aldosterone is combined with Pefloxacin.Experimental, Investigational
AlmasilateAlmasilate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental
AlminoprofenAlminoprofen may increase the neuroexcitatory activities of Pefloxacin.Experimental
AlogliptinPefloxacin may increase the hypoglycemic activities of Alogliptin.Approved
AloglutamolAloglutamol can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
AluminiumAluminium can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Aluminium acetoacetateAluminium acetoacetate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminium glycinateAluminium glycinate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Ambroxol acefyllinateThe metabolism of Ambroxol acefyllinate can be decreased when combined with Pefloxacin.Experimental, Investigational
AmcinonideThe risk or severity of adverse effects can be increased when Amcinonide is combined with Pefloxacin.Approved
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Pefloxacin.Approved
AndrographolideAndrographolide may increase the neuroexcitatory activities of Pefloxacin.Investigational
AndrostenedioneThe risk or severity of adverse effects can be increased when Androstenedione is combined with Pefloxacin.Experimental, Illicit
AnecortaveThe risk or severity of adverse effects can be increased when Anecortave is combined with Pefloxacin.Investigational
anecortave acetateThe risk or severity of adverse effects can be increased when anecortave acetate is combined with Pefloxacin.Investigational
AnisodamineAnisodamine may increase the neuroexcitatory activities of Pefloxacin.Investigational
AntipyrineAntipyrine may increase the neuroexcitatory activities of Pefloxacin.Approved
ApocyninApocynin may increase the neuroexcitatory activities of Pefloxacin.Investigational
ApremilastApremilast may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
AtamestaneThe risk or severity of adverse effects can be increased when Atamestane is combined with Pefloxacin.Investigational
AzapropazoneAzapropazone may increase the neuroexcitatory activities of Pefloxacin.Withdrawn
AzelastineAzelastine may increase the neuroexcitatory activities of Pefloxacin.Approved
BalsalazideBalsalazide may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Pefloxacin.Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Pefloxacin.Approved, Investigational
BendazacBendazac may increase the neuroexcitatory activities of Pefloxacin.Experimental
BenorilateBenorilate may increase the neuroexcitatory activities of Pefloxacin.Experimental
BenoxaprofenBenoxaprofen may increase the neuroexcitatory activities of Pefloxacin.Withdrawn
BenzydamineBenzydamine may increase the neuroexcitatory activities of Pefloxacin.Approved
BetamethasoneThe risk or severity of adverse effects can be increased when Betamethasone is combined with Pefloxacin.Approved, Vet Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Pefloxacin.Approved, Investigational
BevoniumBevonium may increase the neuroexcitatory activities of Pefloxacin.Experimental
Bismuth SubcitrateBismuth Subcitrate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Bismuth subnitrateBismuth subnitrate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
BromfenacBromfenac may increase the neuroexcitatory activities of Pefloxacin.Approved
BromocriptinePefloxacin may increase the hypoglycemic activities of Bromocriptine.Approved, Investigational
BucillamineBucillamine may increase the neuroexcitatory activities of Pefloxacin.Investigational
BudesonideThe risk or severity of adverse effects can be increased when Budesonide is combined with Pefloxacin.Approved
BufexamacBufexamac may increase the neuroexcitatory activities of Pefloxacin.Experimental
BumadizoneBumadizone may increase the neuroexcitatory activities of Pefloxacin.Experimental
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Pefloxacin.Approved
Calcium AcetateCalcium Acetate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium CarbonateCalcium Carbonate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium ChlorideCalcium Chloride can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium CitrateCalcium Citrate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium glubionateCalcium glubionate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium GluceptateCalcium Gluceptate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium gluconateCalcium gluconate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Vet Approved
Calcium lactateCalcium lactate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental, Investigational, Vet Approved
Calcium lactate gluconateCalcium lactate gluconate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Calcium laevulateCalcium laevulate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Calcium pangamateCalcium pangamate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Calcium PhosphateCalcium Phosphate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium silicateCalcium silicate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
CanagliflozinPefloxacin may increase the hypoglycemic activities of Canagliflozin.Approved
CarprofenCarprofen may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved, Withdrawn
CaseinCasein can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CastanospermineCastanospermine may increase the neuroexcitatory activities of Pefloxacin.Experimental
CelecoxibCelecoxib may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
ChloroquineChloroquine may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved
ChlorpropamidePefloxacin may increase the hypoglycemic activities of Chlorpropamide.Approved
Choline magnesium trisalicylateCholine magnesium trisalicylate may increase the neuroexcitatory activities of Pefloxacin.Approved
CiclesonideThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Pefloxacin.Approved, Investigational
ClobetasolThe risk or severity of adverse effects can be increased when Clobetasol is combined with Pefloxacin.Investigational
Clobetasol propionateThe risk or severity of adverse effects can be increased when Clobetasol propionate is combined with Pefloxacin.Approved
ClobetasoneThe risk or severity of adverse effects can be increased when Clobetasone is combined with Pefloxacin.Approved
ClocortoloneThe risk or severity of adverse effects can be increased when Clocortolone is combined with Pefloxacin.Approved
ClonixinClonixin may increase the neuroexcitatory activities of Pefloxacin.Approved
ClorindionePefloxacin may increase the anticoagulant activities of Clorindione.Experimental
Cortexolone 17α-propionateThe risk or severity of adverse effects can be increased when Cortexolone 17α-propionate is combined with Pefloxacin.Investigational
CorticosteroneThe risk or severity of adverse effects can be increased when Corticosterone is combined with Pefloxacin.Experimental
Cortisone acetateThe risk or severity of adverse effects can be increased when Cortisone acetate is combined with Pefloxacin.Approved
CurcuminCurcumin may increase the neuroexcitatory activities of Pefloxacin.Investigational
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Pefloxacin.Approved, Investigational
CymarinCymarin may decrease the cardiotoxic activities of Pefloxacin.Experimental
D-LimoneneD-Limonene may increase the neuroexcitatory activities of Pefloxacin.Investigational
DapagliflozinPefloxacin may increase the hypoglycemic activities of Dapagliflozin.Approved
DeflazacortThe risk or severity of adverse effects can be increased when Deflazacort is combined with Pefloxacin.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Pefloxacin.Approved
DesonideThe risk or severity of adverse effects can be increased when Desonide is combined with Pefloxacin.Approved, Investigational
DesoximetasoneThe risk or severity of adverse effects can be increased when Desoximetasone is combined with Pefloxacin.Approved
Desoxycorticosterone acetateThe risk or severity of adverse effects can be increased when Desoxycorticosterone acetate is combined with Pefloxacin.Approved
Desoxycorticosterone PivalateThe risk or severity of adverse effects can be increased when Desoxycorticosterone Pivalate is combined with Pefloxacin.Experimental, Vet Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Dexamethasone is combined with Pefloxacin.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Dexamethasone isonicotinate is combined with Pefloxacin.Vet Approved
DiclofenacDiclofenac may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved
DicoumarolPefloxacin may increase the anticoagulant activities of Dicoumarol.Approved
DidanosineThe serum concentration of Didanosine can be decreased when it is combined with Pefloxacin.Approved
DifenpiramideDifenpiramide may increase the neuroexcitatory activities of Pefloxacin.Experimental
DiflorasoneThe risk or severity of adverse effects can be increased when Diflorasone is combined with Pefloxacin.Approved
DiflunisalDiflunisal may increase the neuroexcitatory activities of Pefloxacin.Approved
DifluocortoloneThe risk or severity of adverse effects can be increased when Difluocortolone is combined with Pefloxacin.Approved, Investigational
DifluprednateThe risk or severity of adverse effects can be increased when Difluprednate is combined with Pefloxacin.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Pefloxacin.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Pefloxacin.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Pefloxacin.Approved
DiphenadionePefloxacin may increase the anticoagulant activities of Diphenadione.Experimental
DisopyramidePefloxacin may increase the hypoglycemic activities of Disopyramide.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Pefloxacin.Approved, Investigational
DroxicamDroxicam may increase the neuroexcitatory activities of Pefloxacin.Approved
DulaglutidePefloxacin may increase the hypoglycemic activities of Dulaglutide.Approved
DuvelisibDuvelisib may increase the neuroexcitatory activities of Pefloxacin.Investigational
DyphyllineThe metabolism of Dyphylline can be decreased when combined with Pefloxacin.Approved
E-6201E-6201 may increase the neuroexcitatory activities of Pefloxacin.Investigational
EmpagliflozinPefloxacin may increase the hypoglycemic activities of Empagliflozin.Approved
EpirizoleEpirizole may increase the neuroexcitatory activities of Pefloxacin.Approved
EquileninThe risk or severity of adverse effects can be increased when Equilenin is combined with Pefloxacin.Experimental
EquilinThe risk or severity of adverse effects can be increased when Equilin is combined with Pefloxacin.Approved
EstroneThe risk or severity of adverse effects can be increased when Estrone is combined with Pefloxacin.Approved
Estrone sulfateThe risk or severity of adverse effects can be increased when Estrone sulfate is combined with Pefloxacin.Approved
EtanerceptEtanercept may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
EthenzamideEthenzamide may increase the neuroexcitatory activities of Pefloxacin.Experimental
Ethyl biscoumacetatePefloxacin may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtodolacEtodolac may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
EtoricoxibEtoricoxib may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
Evening primrose oilEvening primrose oil may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
ExenatidePefloxacin may increase the hypoglycemic activities of Exenatide.Approved, Investigational
exisulindexisulind may increase the neuroexcitatory activities of Pefloxacin.Investigational
FelbinacFelbinac may increase the neuroexcitatory activities of Pefloxacin.Experimental
FenbufenFenbufen may increase the neuroexcitatory activities of Pefloxacin.Approved
FenoprofenFenoprofen may increase the neuroexcitatory activities of Pefloxacin.Approved
FentiazacFentiazac may increase the neuroexcitatory activities of Pefloxacin.Experimental
FeprazoneFeprazone may increase the neuroexcitatory activities of Pefloxacin.Experimental
Ferric CarboxymaltoseThe serum concentration of Pefloxacin can be decreased when it is combined with Ferric Carboxymaltose.Approved
Ferric CitrateThe serum concentration of Pefloxacin can be decreased when it is combined with Ferric Citrate.Approved, Investigational
Ferric pyrophosphateThe serum concentration of Pefloxacin can be decreased when it is combined with Ferric pyrophosphate.Approved
Ferulic acidFerulic acid may increase the neuroexcitatory activities of Pefloxacin.Experimental
FloctafenineFloctafenine may increase the neuroexcitatory activities of Pefloxacin.Approved, Withdrawn
fluasteroneThe risk or severity of adverse effects can be increased when fluasterone is combined with Pefloxacin.Investigational
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Pefloxacin.Approved
FluindionePefloxacin may increase the anticoagulant activities of Fluindione.Investigational
FlumethasoneThe risk or severity of adverse effects can be increased when Flumethasone is combined with Pefloxacin.Approved, Vet Approved
FlunisolideThe risk or severity of adverse effects can be increased when Flunisolide is combined with Pefloxacin.Approved, Investigational
FlunixinFlunixin may increase the neuroexcitatory activities of Pefloxacin.Vet Approved
FlunoxaprofenFlunoxaprofen may increase the neuroexcitatory activities of Pefloxacin.Experimental
Fluocinolone AcetonideThe risk or severity of adverse effects can be increased when Fluocinolone Acetonide is combined with Pefloxacin.Approved, Investigational, Vet Approved
FluocinonideThe risk or severity of adverse effects can be increased when Fluocinonide is combined with Pefloxacin.Approved, Investigational
FluocortoloneThe risk or severity of adverse effects can be increased when Fluocortolone is combined with Pefloxacin.Approved, Withdrawn
FluorometholoneThe risk or severity of adverse effects can be increased when Fluorometholone is combined with Pefloxacin.Approved
FluprednideneThe risk or severity of adverse effects can be increased when Fluprednidene is combined with Pefloxacin.Approved, Withdrawn
FluprednisoloneThe risk or severity of adverse effects can be increased when Fluprednisolone is combined with Pefloxacin.Approved
FlurandrenolideThe risk or severity of adverse effects can be increased when Flurandrenolide is combined with Pefloxacin.Approved
FlurbiprofenFlurbiprofen may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
Fluticasone furoateThe risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Pefloxacin.Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Pefloxacin.Approved
FormestaneThe risk or severity of adverse effects can be increased when Formestane is combined with Pefloxacin.Approved, Investigational, Withdrawn
GitoformateGitoformate may decrease the cardiotoxic activities of Pefloxacin.Experimental
GliclazidePefloxacin may increase the hypoglycemic activities of Gliclazide.Approved
GlimepiridePefloxacin may increase the hypoglycemic activities of Glimepiride.Approved
GlipizidePefloxacin may increase the hypoglycemic activities of Glipizide.Approved
GlyburidePefloxacin may increase the hypoglycemic activities of Glyburide.Approved
GuacetisalGuacetisal may increase the neuroexcitatory activities of Pefloxacin.Experimental
HalcinonideThe risk or severity of adverse effects can be increased when Halcinonide is combined with Pefloxacin.Approved, Investigational, Withdrawn
HE3286The risk or severity of adverse effects can be increased when HE3286 is combined with Pefloxacin.Investigational
HigenamineHigenamine may increase the neuroexcitatory activities of Pefloxacin.Investigational
HydrocortisoneThe risk or severity of adverse effects can be increased when Hydrocortisone is combined with Pefloxacin.Approved, Vet Approved
HydrotalciteHydrotalcite can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental, Investigational
IbuprofenIbuprofen may increase the neuroexcitatory activities of Pefloxacin.Approved
IbuproxamIbuproxam may increase the neuroexcitatory activities of Pefloxacin.Withdrawn
IcatibantIcatibant may increase the neuroexcitatory activities of Pefloxacin.Approved
Imidazole salicylateImidazole salicylate may increase the neuroexcitatory activities of Pefloxacin.Experimental
IndobufenIndobufen may increase the neuroexcitatory activities of Pefloxacin.Investigational
IndomethacinIndomethacin may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
IndoprofenIndoprofen may increase the neuroexcitatory activities of Pefloxacin.Withdrawn
Insulin AspartPefloxacin may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirPefloxacin may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlarginePefloxacin may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisinePefloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanPefloxacin may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproPefloxacin may increase the hypoglycemic activities of Insulin Lispro.Approved
IronThe serum concentration of Pefloxacin can be decreased when it is combined with Iron.Approved
Iron DextranThe serum concentration of Pefloxacin can be decreased when it is combined with Iron Dextran.Approved, Vet Approved
Iron saccharateThe serum concentration of Pefloxacin can be decreased when it is combined with Iron saccharate.Approved
IsoxicamIsoxicam may increase the neuroexcitatory activities of Pefloxacin.Withdrawn
IstaroximeThe risk or severity of adverse effects can be increased when Istaroxime is combined with Pefloxacin.Investigational
KebuzoneKebuzone may increase the neuroexcitatory activities of Pefloxacin.Experimental
KetoprofenKetoprofen may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved
KetorolacKetorolac may increase the neuroexcitatory activities of Pefloxacin.Approved
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Pefloxacin.Experimental
Lanthanum carbonateThe serum concentration of Pefloxacin can be decreased when it is combined with Lanthanum carbonate.Approved
LeflunomideLeflunomide may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
LiraglutidePefloxacin may increase the hypoglycemic activities of Liraglutide.Approved
LisofyllineLisofylline may increase the neuroexcitatory activities of Pefloxacin.Investigational
LonazolacLonazolac may increase the neuroexcitatory activities of Pefloxacin.Experimental
LornoxicamLornoxicam may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
LoteprednolThe risk or severity of adverse effects can be increased when Loteprednol is combined with Pefloxacin.Approved
LoxoprofenLoxoprofen may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
LumiracoxibLumiracoxib may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
MagaldrateMagaldrate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Withdrawn
Magnesium HydroxideMagnesium Hydroxide can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium peroxideMagnesium peroxide can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Magnesium salicylateThe serum concentration of Pefloxacin can be decreased when it is combined with Magnesium salicylate.Approved
Magnesium silicateMagnesium silicate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental
Magnesium SulfateThe serum concentration of Pefloxacin can be decreased when it is combined with Magnesium Sulfate.Approved, Vet Approved
Magnesium TrisilicateMagnesium Trisilicate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
MasoprocolMasoprocol may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
ME-609The risk or severity of adverse effects can be increased when ME-609 is combined with Pefloxacin.Investigational
MecaserminPefloxacin may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Meclofenamic acidMeclofenamic acid may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved
MedrysoneThe risk or severity of adverse effects can be increased when Medrysone is combined with Pefloxacin.Approved
Mefenamic acidMefenamic acid may increase the neuroexcitatory activities of Pefloxacin.Approved
MelengestrolThe risk or severity of adverse effects can be increased when Melengestrol is combined with Pefloxacin.Vet Approved
MeloxicamMeloxicam may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved
MesalazineMesalazine may increase the neuroexcitatory activities of Pefloxacin.Approved
MetamizoleMetamizole may increase the neuroexcitatory activities of Pefloxacin.Investigational, Withdrawn
MetforminPefloxacin may increase the hypoglycemic activities of Metformin.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Pefloxacin.Approved, Vet Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Pefloxacin.Experimental
MifepristonePefloxacin may increase the hypoglycemic activities of Mifepristone.Approved, Investigational
MiglitolPefloxacin may increase the hypoglycemic activities of Miglitol.Approved
MizoribineMizoribine may increase the neuroexcitatory activities of Pefloxacin.Investigational
MofebutazoneMofebutazone may increase the neuroexcitatory activities of Pefloxacin.Experimental
MometasoneThe risk or severity of adverse effects can be increased when Mometasone is combined with Pefloxacin.Approved, Vet Approved
Mycophenolate mofetilMycophenolate mofetil may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
Mycophenolic acidThe serum concentration of Mycophenolic acid can be decreased when it is combined with Pefloxacin.Approved
NabumetoneNabumetone may increase the neuroexcitatory activities of Pefloxacin.Approved
NafamostatNafamostat may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
NaftifineNaftifine may increase the neuroexcitatory activities of Pefloxacin.Approved
NaproxenNaproxen may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved
NateglinidePefloxacin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NCX 1022The risk or severity of adverse effects can be increased when NCX 1022 is combined with Pefloxacin.Investigational
NepafenacNepafenac may increase the neuroexcitatory activities of Pefloxacin.Approved
NifenazoneNifenazone may increase the neuroexcitatory activities of Pefloxacin.Experimental
Niflumic AcidNiflumic Acid may increase the neuroexcitatory activities of Pefloxacin.Approved
NimesulideNimesulide may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational, Withdrawn
NitroaspirinNitroaspirin may increase the neuroexcitatory activities of Pefloxacin.Investigational
OleandrinOleandrin may decrease the cardiotoxic activities of Pefloxacin.Experimental, Investigational
Oleoyl-estroneThe risk or severity of adverse effects can be increased when Oleoyl-estrone is combined with Pefloxacin.Investigational
OlopatadineOlopatadine may increase the neuroexcitatory activities of Pefloxacin.Approved
OlsalazineOlsalazine may increase the neuroexcitatory activities of Pefloxacin.Approved
OrgoteinOrgotein may increase the neuroexcitatory activities of Pefloxacin.Vet Approved
OuabainOuabain may decrease the cardiotoxic activities of Pefloxacin.Approved
OxaprozinOxaprozin may increase the neuroexcitatory activities of Pefloxacin.Approved
OxyphenbutazoneOxyphenbutazone may increase the neuroexcitatory activities of Pefloxacin.Approved, Withdrawn
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Pefloxacin.Approved, Vet Approved
ParamethasoneThe risk or severity of adverse effects can be increased when Paramethasone is combined with Pefloxacin.Approved
ParecoxibParecoxib may increase the neuroexcitatory activities of Pefloxacin.Approved
ParthenolideParthenolide may increase the neuroexcitatory activities of Pefloxacin.Investigational
PentamidinePefloxacin may increase the hypoglycemic activities of Pentamidine.Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Pefloxacin.Experimental
PhenindionePefloxacin may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonPefloxacin may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenylbutazonePhenylbutazone may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Pefloxacin.Approved
PimecrolimusPimecrolimus may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
PioglitazonePefloxacin may increase the hypoglycemic activities of Pioglitazone.Approved, Investigational
PirfenidonePirfenidone may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
PiroxicamPiroxicam may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
PirprofenPirprofen may increase the neuroexcitatory activities of Pefloxacin.Experimental
PramlintidePefloxacin may increase the hypoglycemic activities of Pramlintide.Approved, Investigational
PranoprofenPranoprofen may increase the neuroexcitatory activities of Pefloxacin.Experimental, Investigational
PrasteroneThe risk or severity of adverse effects can be increased when Prasterone is combined with Pefloxacin.Approved, Nutraceutical
Prasterone sulfateThe risk or severity of adverse effects can be increased when Prasterone sulfate is combined with Pefloxacin.Investigational
PrednicarbateThe risk or severity of adverse effects can be increased when Prednicarbate is combined with Pefloxacin.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Prednisolone is combined with Pefloxacin.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Prednisone is combined with Pefloxacin.Approved, Vet Approved
PregnenoloneThe risk or severity of adverse effects can be increased when Pregnenolone is combined with Pefloxacin.Experimental, Investigational
ProbenecidThe serum concentration of Pefloxacin can be increased when it is combined with Probenecid.Approved
ProglumetacinProglumetacin may increase the neuroexcitatory activities of Pefloxacin.Experimental
PropacetamolPropacetamol may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
PropyphenazonePropyphenazone may increase the neuroexcitatory activities of Pefloxacin.Experimental
ProquazoneProquazone may increase the neuroexcitatory activities of Pefloxacin.Experimental
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Pefloxacin.Experimental
PTC299PTC299 may increase the neuroexcitatory activities of Pefloxacin.Investigational
QuinaprilThe serum concentration of Pefloxacin can be decreased when it is combined with Quinapril.Approved, Investigational
QuininePefloxacin may increase the hypoglycemic activities of Quinine.Approved
RepaglinidePefloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
ResveratrolResveratrol may increase the neuroexcitatory activities of Pefloxacin.Approved, Experimental, Investigational
RimexoloneThe risk or severity of adverse effects can be increased when Rimexolone is combined with Pefloxacin.Approved
RofecoxibRofecoxib may increase the neuroexcitatory activities of Pefloxacin.Investigational, Withdrawn
RosiglitazonePefloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
SalicylamideSalicylamide may increase the neuroexcitatory activities of Pefloxacin.Approved
Salicylic acidSalicylic acid may increase the neuroexcitatory activities of Pefloxacin.Approved, Vet Approved
SalsalateSalsalate may increase the neuroexcitatory activities of Pefloxacin.Approved
SaxagliptinPefloxacin may increase the hypoglycemic activities of Saxagliptin.Approved
SemapimodSemapimod may increase the neuroexcitatory activities of Pefloxacin.Investigational
SeratrodastSeratrodast may increase the neuroexcitatory activities of Pefloxacin.Approved
SerrapeptaseSerrapeptase may increase the neuroexcitatory activities of Pefloxacin.Investigational
SevelamerSevelamer can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
SitagliptinPefloxacin may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
Sodium bicarbonateSodium bicarbonate can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
SRT501SRT501 may increase the neuroexcitatory activities of Pefloxacin.Investigational
Strontium ranelateThe serum concentration of Pefloxacin can be decreased when it is combined with Strontium ranelate.Approved
SucralfateThe serum concentration of Pefloxacin can be decreased when it is combined with Sucralfate.Approved
SulfadiazinePefloxacin may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazolePefloxacin may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfasalazineSulfasalazine may increase the neuroexcitatory activities of Pefloxacin.Approved
SulfisoxazolePefloxacin may increase the hypoglycemic activities of Sulfisoxazole.Approved, Vet Approved
SulindacSulindac may increase the neuroexcitatory activities of Pefloxacin.Approved
SunitinibPefloxacin may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
SuprofenSuprofen may increase the neuroexcitatory activities of Pefloxacin.Approved, Withdrawn
SuxibuzoneSuxibuzone may increase the neuroexcitatory activities of Pefloxacin.Experimental
TarenflurbilTarenflurbil may increase the neuroexcitatory activities of Pefloxacin.Investigational
TenidapTenidap may increase the neuroexcitatory activities of Pefloxacin.Experimental
TenoxicamTenoxicam may increase the neuroexcitatory activities of Pefloxacin.Approved
TepoxalinTepoxalin may increase the neuroexcitatory activities of Pefloxacin.Vet Approved
TeriflunomideTeriflunomide may increase the neuroexcitatory activities of Pefloxacin.Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Pefloxacin.Approved
Tiaprofenic acidTiaprofenic acid may increase the neuroexcitatory activities of Pefloxacin.Approved
TinoridineTinoridine may increase the neuroexcitatory activities of Pefloxacin.Investigational
TioclomarolPefloxacin may increase the anticoagulant activities of Tioclomarol.Experimental
TixocortolThe risk or severity of adverse effects can be increased when Tixocortol is combined with Pefloxacin.Approved
TolazamidePefloxacin may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamidePefloxacin may increase the hypoglycemic activities of Tolbutamide.Approved
Tolfenamic AcidTolfenamic Acid may increase the neuroexcitatory activities of Pefloxacin.Approved
TolmetinTolmetin may increase the neuroexcitatory activities of Pefloxacin.Approved
TranilastTranilast may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Pefloxacin.Approved, Investigational
TriamcinoloneThe risk or severity of adverse effects can be increased when Triamcinolone is combined with Pefloxacin.Approved, Vet Approved
TribenosideTribenoside may increase the neuroexcitatory activities of Pefloxacin.Experimental
TriptolideTriptolide may increase the neuroexcitatory activities of Pefloxacin.Investigational
TromethamineTromethamine can cause a decrease in the absorption of Pefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
UlobetasolThe risk or severity of adverse effects can be increased when Ulobetasol is combined with Pefloxacin.Approved
ValdecoxibValdecoxib may increase the neuroexcitatory activities of Pefloxacin.Investigational, Withdrawn
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Pefloxacin.Approved, Investigational
WarfarinPefloxacin may increase the anticoagulant activities of Warfarin.Approved
ZaltoprofenZaltoprofen may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational
ZileutonZileuton may increase the neuroexcitatory activities of Pefloxacin.Approved, Investigational, Withdrawn
ZomepiracZomepirac may increase the neuroexcitatory activities of Pefloxacin.Withdrawn
Food Interactions
Not Available

References

Synthesis Reference
US4292317
General References
Not Available
External Links
Human Metabolome Database
HMDB14630
KEGG Drug
D02306
PubChem Compound
51081
PubChem Substance
46507338
ChemSpider
46291
BindingDB
57936
ChEBI
50199
ChEMBL
CHEMBL267648
Therapeutic Targets Database
DAP001001
PharmGKB
PA164742856
Wikipedia
Pefloxacin
ATC Codes
J01MA03 — Pefloxacin

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)271 dec °CPhysProp
water solubility11.4 mg/mL at 25 °CNot Available
logP0.27HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
Water Solubility1.23 mg/mLALOGPS
logP0.2ALOGPS
logP0.88ChemAxon
logS-2.4ALOGPS
pKa (Strongest Acidic)5.66ChemAxon
pKa (Strongest Basic)6.47ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area64.09 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity90.77 m3·mol-1ChemAxon
Polarizability34.42 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9914
Blood Brain Barrier-0.9651
Caco-2 permeable+0.9002
P-glycoprotein substrateSubstrate0.8136
P-glycoprotein inhibitor INon-inhibitor0.8781
P-glycoprotein inhibitor IINon-inhibitor0.8382
Renal organic cation transporterNon-inhibitor0.6812
CYP450 2C9 substrateNon-substrate0.8645
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6809
CYP450 1A2 substrateNon-inhibitor0.9275
CYP450 2C9 inhibitorNon-inhibitor0.9206
CYP450 2D6 inhibitorNon-inhibitor0.9112
CYP450 2C19 inhibitorNon-inhibitor0.8584
CYP450 3A4 inhibitorNon-inhibitor0.9524
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6784
Ames testAMES toxic0.9108
CarcinogenicityNon-carcinogens0.8816
BiodegradationNot ready biodegradable1.0
Rat acute toxicity1.9255 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7983
hERG inhibition (predictor II)Non-inhibitor0.7795
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 GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-001i-0198000000-230c93f5eaf4301ff8c6
MS/MS Spectrum - , positiveLC-MS/MSsplash10-014i-0910000000-593baa616326abe5f576

Taxonomy

Description
This compound belongs to the class of organic compounds known as quinoline carboxylic acids. These are quinolines in which the quinoline ring system is substituted by a carboxyl group at one or more positions.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Quinolines and derivatives
Sub Class
Quinoline carboxylic acids
Direct Parent
Quinoline carboxylic acids
Alternative Parents
N-arylpiperazines / Fluoroquinolones / Aminoquinolines and derivatives / Hydroquinolones / Haloquinolines / Hydroquinolines / Pyridinecarboxylic acids / Dialkylarylamines / N-methylpiperazines / Aryl fluorides
show 13 more
Substituents
Quinoline-3-carboxylic acid / Fluoroquinolone / N-arylpiperazine / Aminoquinoline / Haloquinoline / Dihydroquinolone / Dihydroquinoline / Pyridine carboxylic acid / Pyridine carboxylic acid or derivatives / Tertiary aliphatic/aromatic amine
show 30 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
N-arylpiperazine, N-alkylpiperazine, quinolone antibiotic, fluoroquinolone antibiotic, quinolone (CHEBI:50199)

Targets

Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function
Topoisomerase IV is essential for chromosome segregation. It relaxes supercoiled DNA. Performs the decatenation events required during the replication of a circular DNA molecule.
Gene Name
parC
Uniprot ID
P43702
Uniprot Name
DNA topoisomerase 4 subunit A
Molecular Weight
83366.24 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Varon E, Houssaye S, Grondin S, Gutmann L: Nonmolecular test for detection of low-level resistance to fluoroquinolones in Streptococcus pneumoniae. Antimicrob Agents Chemother. 2006 Feb;50(2):572-9. [PubMed:16436712]
  4. Rafii F, Park M, Novak JS: Alterations in DNA gyrase and topoisomerase IV in resistant mutants of Clostridium perfringens found after in vitro treatment with fluoroquinolones. Antimicrob Agents Chemother. 2005 Feb;49(2):488-92. [PubMed:15673722]
  5. Vila J, Sanchez-Cespedes J, Sierra JM, Piqueras M, Nicolas E, Freixas J, Giralt E: Antibacterial evaluation of a collection of norfloxacin and ciprofloxacin derivatives against multiresistant bacteria. Int J Antimicrob Agents. 2006 Jul;28(1):19-24. Epub 2006 Jun 14. [PubMed:16781123]
  6. Oyamada Y, Ito H, Fujimoto K, Asada R, Niga T, Okamoto R, Inoue M, Yamagishi J: Combination of known and unknown mechanisms confers high-level resistance to fluoroquinolones in Enterococcus faecium. J Med Microbiol. 2006 Jun;55(Pt 6):729-36. [PubMed:16687591]
Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function
DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, inc...
Gene Name
gyrA
Uniprot ID
P43700
Uniprot Name
DNA gyrase subunit A
Molecular Weight
97817.145 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Gootz TD, Zaniewski RP, Haskell SL, Kaczmarek FS, Maurice AE: Activities of trovafloxacin compared with those of other fluoroquinolones against purified topoisomerases and gyrA and grlA mutants of Staphylococcus aureus. Antimicrob Agents Chemother. 1999 Aug;43(8):1845-55. [PubMed:10428901]
  4. Bebear CM, Renaudin H, Charron A, Bove JM, Bebear C, Renaudin J: Alterations in topoisomerase IV and DNA gyrase in quinolone-resistant mutants of Mycoplasma hominis obtained in vitro. Antimicrob Agents Chemother. 1998 Sep;42(9):2304-11. [PubMed:9736554]
  5. Varon E, Houssaye S, Grondin S, Gutmann L: Nonmolecular test for detection of low-level resistance to fluoroquinolones in Streptococcus pneumoniae. Antimicrob Agents Chemother. 2006 Feb;50(2):572-9. [PubMed:16436712]
  6. Hombrouck C, Capmau ML, Moreau N: Overexpression, purification and photoaffinity labeling with a 3H-analogue of norfloxacin, of the GyrA and GyrB subunits of the DNA gyrase. Cell Mol Biol (Noisy-le-grand). 1999 May;45(3):347-52. [PubMed:10386791]
  7. Hooper DC: Quinolone mode of action--new aspects. Drugs. 1993;45 Suppl 3:8-14. [PubMed:7689456]
  8. Fukuda H, Hori S, Hiramatsu K: Antibacterial activity of gatifloxacin (AM-1155, CG5501, BMS-206584), a newly developed fluoroquinolone, against sequentially acquired quinolone-resistant mutants and the norA transformant of Staphylococcus aureus. Antimicrob Agents Chemother. 1998 Aug;42(8):1917-22. [PubMed:9687384]
  9. Drlica K, Zhao X: DNA gyrase, topoisomerase IV, and the 4-quinolones. Microbiol Mol Biol Rev. 1997 Sep;61(3):377-92. [PubMed:9293187]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Ubiquitin binding
Specific Function
Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segr...
Gene Name
TOP2A
Uniprot ID
P11388
Uniprot Name
DNA topoisomerase 2-alpha
Molecular Weight
174383.88 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Staphylococcus aureus
Pharmacological action
Unknown
General Function
Magnesium ion binding
Specific Function
Releases the supercoiling and torsional tension of DNA, which is introduced during the DNA replication and transcription, by transiently cleaving and rejoining one strand of the DNA duplex. Introdu...
Gene Name
topA
Uniprot ID
Q06AK7
Uniprot Name
DNA topoisomerase 1
Molecular Weight
79099.16 Da
References
  1. Tabary X, Moreau N, Dureuil C, Le Goffic F: Effect of DNA gyrase inhibitors pefloxacin, five other quinolones, novobiocin, and clorobiocin on Escherichia coli topoisomerase I. Antimicrob Agents Chemother. 1987 Dec;31(12):1925-8. [PubMed:2830840]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on June 13, 2005 07:24 / Updated on November 24, 2017 14:24