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Identification
NameGrepafloxacin
Accession NumberDB00365  (APRD01003)
TypeSmall Molecule
GroupsWithdrawn
DescriptionGrepafloxacin is an oral broad-spectrum quinoline antibacterial agent used to treat bacterial infections. Grepafloxacin was withdrawn in the United States due to its side effect of lengthening the QT interval on the electrocardiogram, leading to cardiac events and sudden death. [Wikipedia]
Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Raxartablet200 mgoralOtsuka Pharma Gmbh1998-07-011999-10-27Canada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Grepafloxacin hydrochloride
ThumbNot applicableDBSALT000913
Categories
UNIIL1M1U2HC31
CAS number119914-60-2
WeightAverage: 359.3947
Monoisotopic: 359.16451979
Chemical FormulaC19H22FN3O3
InChI KeyInChIKey=AIJTTZAVMXIJGM-UHFFFAOYSA-N
InChI
InChI=1S/C19H22FN3O3/c1-10-8-22(6-5-21-10)15-7-14-16(11(2)17(15)20)18(24)13(19(25)26)9-23(14)12-3-4-12/h7,9-10,12,21H,3-6,8H2,1-2H3,(H,25,26)
IUPAC Name
1-cyclopropyl-6-fluoro-5-methyl-7-(3-methylpiperazin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
SMILES
CC1CN(CCN1)C1=C(F)C(C)=C2C(=O)C(=CN(C3CC3)C2=C1)C(O)=O
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassQuinolines and derivatives
Sub ClassQuinoline carboxylic acids
Direct ParentQuinoline carboxylic acids
Alternative Parents
Substituents
  • Quinoline-3-carboxylic acid
  • N-arylpiperazine
  • Fluoroquinolone
  • Dihydroquinolone
  • Aminoquinoline
  • Dihydroquinoline
  • Pyridine carboxylic acid or derivatives
  • Pyridine carboxylic acid
  • Dialkylarylamine
  • Fluorobenzene
  • Benzenoid
  • Pyridine
  • Piperazine
  • 1,4-diazinane
  • Aryl halide
  • Aryl fluoride
  • Heteroaromatic compound
  • Vinylogous amide
  • Tertiary amine
  • Azacycle
  • Secondary amine
  • Monocarboxylic acid or derivatives
  • Secondary aliphatic amine
  • Carboxylic acid
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor treatment of adults with mild to moderate infections caused by susceptible strains of Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis.
PharmacodynamicsGrepafloxacin has in vitro activity against a wide range of gram-positive and gram-negative aerobic microorganisms, as well as some atypical microorganisms.
Mechanism of actionGrepafloxacin exerts its antibacterial activity by inhibiting bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, essential enzymes for duplication, transcription, and repair of bacterial DNA.
Related Articles
AbsorptionRapidly and extensively absorbed following oral administration. The absolute bioavailability is approximately 70%.
Volume of distributionNot Available
Protein binding50%
Metabolism

Primarily hepatic via CYP1A2 and CYP3A4. The major metabolite is a glucuronide conjugate; minor metabolites include sulfate conjugates and oxidative metabolites. The oxidative metabolites are formed mainly by the cytochrome P450 enzyme CYP1A2, while the cytochrome P450 enzyme CYP3A4 plays a minor role. The nonconjugated metabolites have little antimicrobial activity compared with the parent drug, and the conjugated metabolites have no antimicrobial activity

Route of eliminationNot Available
Half life15 ± 3 hours
ClearanceNot Available
ToxicityWithdrawn from the US market in 1999 due to associations with QTc prolongation and adverse cardiovascular events.
Affected organisms
  • Enteric bacteria and other eubacteria
  • Streptococcus pneumoniae
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9886
Blood Brain Barrier-0.9855
Caco-2 permeable+0.5
P-glycoprotein substrateSubstrate0.8825
P-glycoprotein inhibitor INon-inhibitor0.9062
P-glycoprotein inhibitor IINon-inhibitor0.9228
Renal organic cation transporterNon-inhibitor0.7877
CYP450 2C9 substrateNon-substrate0.8299
CYP450 2D6 substrateNon-substrate0.9127
CYP450 3A4 substrateNon-substrate0.7079
CYP450 1A2 substrateNon-inhibitor0.8516
CYP450 2C9 inhibitorNon-inhibitor0.9197
CYP450 2D6 inhibitorNon-inhibitor0.9365
CYP450 2C19 inhibitorNon-inhibitor0.9064
CYP450 3A4 inhibitorNon-inhibitor0.8116
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.763
Ames testAMES toxic0.7309
CarcinogenicityNon-carcinogens0.8042
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.0923 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9009
hERG inhibition (predictor II)Non-inhibitor0.7785
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Otsuka pharmaceutical co ltd
Packagers
Dosage forms
FormRouteStrength
Tabletoral200 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1340492 No1999-04-132016-04-13Canada
US5563138 No1993-10-082013-10-08Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP2.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.632 mg/mLALOGPS
logP-0.12ALOGPS
logP0.12ChemAxon
logS-2.8ALOGPS
pKa (Strongest Acidic)5.88ChemAxon
pKa (Strongest Basic)8.77ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area72.88 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity97.4 m3·mol-1ChemAxon
Polarizability37.69 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

DrugSyn.org

US4920120
General ReferencesNot Available
External Links
ATC CodesJ01MA11
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (115 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Grepafloxacin can be increased when it is combined with Abiraterone.
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Grepafloxacin.
AcetaminophenThe serum concentration of Grepafloxacin can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Grepafloxacin.
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Grepafloxacin.
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Grepafloxacin.
AlbendazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Grepafloxacin can be decreased when it is combined with Aldosterone.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Grepafloxacin.
AlectinibThe serum concentration of Grepafloxacin can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Grepafloxacin can be increased when it is combined with Alfentanil.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Grepafloxacin.
AmantadineThe serum concentration of Grepafloxacin can be increased when it is combined with Amantadine.
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Grepafloxacin.
Aminohippuric acidThe serum concentration of Grepafloxacin can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Grepafloxacin can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Grepafloxacin can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Grepafloxacin can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Grepafloxacin can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Grepafloxacin can be increased when it is combined with Amsacrine.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Grepafloxacin.
AprepitantThe serum concentration of Grepafloxacin can be increased when it is combined with Aprepitant.
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Grepafloxacin.
AstemizoleThe serum concentration of Grepafloxacin can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Grepafloxacin.
AtenololThe serum concentration of Grepafloxacin can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Grepafloxacin can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Grepafloxacin can be increased when it is combined with Atorvastatin.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Grepafloxacin.
AzelastineThe serum concentration of Grepafloxacin can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Grepafloxacin can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Grepafloxacin can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Grepafloxacin can be increased when it is combined with Bepridil.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Grepafloxacin.
BevacizumabBevacizumab may increase the cardiotoxic activities of Grepafloxacin.
BexaroteneThe serum concentration of Grepafloxacin can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Grepafloxacin can be increased when it is combined with Biperiden.
BoceprevirThe metabolism of Grepafloxacin can be decreased when combined with Boceprevir.
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Grepafloxacin.
BortezomibThe metabolism of Grepafloxacin can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Grepafloxacin can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Grepafloxacin.
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Grepafloxacin.
BromocriptineThe serum concentration of Grepafloxacin can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Grepafloxacin can be increased when it is combined with Buprenorphine.
BuspironeThe serum concentration of Grepafloxacin can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Grepafloxacin.
CaffeineThe serum concentration of Grepafloxacin can be increased when it is combined with Caffeine.
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Grepafloxacin.
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Grepafloxacin.
CandesartanThe serum concentration of Grepafloxacin can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Grepafloxacin can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Grepafloxacin can be decreased when it is combined with Carbamazepine.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Grepafloxacin.
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Grepafloxacin.
CarvedilolThe serum concentration of Grepafloxacin can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Grepafloxacin can be increased when it is combined with Caspofungin.
CeritinibThe serum concentration of Grepafloxacin can be increased when it is combined with Ceritinib.
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Grepafloxacin.
ChloroquineThe serum concentration of Grepafloxacin can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Grepafloxacin can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Grepafloxacin can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Grepafloxacin can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Grepafloxacin can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Grepafloxacin can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Grepafloxacin can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Grepafloxacin can be decreased when it is combined with Cimetidine.
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Grepafloxacin.
CiprofloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Ciprofloxacin.
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Grepafloxacin.
CitalopramThe serum concentration of Grepafloxacin can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Grepafloxacin can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Grepafloxacin can be decreased when combined with Clemastine.
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Grepafloxacin.
ClofazimineThe serum concentration of Grepafloxacin can be increased when it is combined with Clofazimine.
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Grepafloxacin.
ClomipramineThe serum concentration of Grepafloxacin can be increased when it is combined with Clomipramine.
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Grepafloxacin.
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Grepafloxacin.
ClotrimazoleThe metabolism of Grepafloxacin can be decreased when combined with Clotrimazole.
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Grepafloxacin.
CobicistatThe serum concentration of Grepafloxacin can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Grepafloxacin.
ColchicineThe serum concentration of Grepafloxacin can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Grepafloxacin can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Grepafloxacin can be increased when it is combined with Conivaptan.
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Grepafloxacin.
CrizotinibThe metabolism of Grepafloxacin can be decreased when combined with Crizotinib.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Grepafloxacin.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Grepafloxacin.
CyclosporineThe metabolism of Grepafloxacin can be decreased when combined with Cyclosporine.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Grepafloxacin.
Cyproterone acetateThe serum concentration of Grepafloxacin can be decreased when it is combined with Cyproterone acetate.
Dabigatran etexilateThe serum concentration of Dabigatran etexilate can be increased when it is combined with Grepafloxacin.
DabrafenibThe serum concentration of Grepafloxacin can be decreased when it is combined with Dabrafenib.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Grepafloxacin.
DaclatasvirThe serum concentration of Grepafloxacin can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Grepafloxacin can be increased when it is combined with Dactinomycin.
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Grepafloxacin.
DarunavirThe metabolism of Grepafloxacin can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Grepafloxacin can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Grepafloxacin can be decreased when it is combined with Daunorubicin.
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Grepafloxacin.
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Grepafloxacin.
DeferasiroxThe serum concentration of Grepafloxacin can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Grepafloxacin can be decreased when combined with Delavirdine.
DesipramineThe serum concentration of Grepafloxacin can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Grepafloxacin.
DesloratadineThe serum concentration of Grepafloxacin can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Grepafloxacin can be decreased when it is combined with Dexamethasone.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Grepafloxacin.
DextromethorphanThe serum concentration of Grepafloxacin can be increased when it is combined with Dextromethorphan.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Grepafloxacin.
DiclofenacThe serum concentration of Grepafloxacin can be increased when it is combined with Diclofenac.
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Grepafloxacin.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Grepafloxacin.
DigitoxinThe serum concentration of Digitoxin can be increased when it is combined with Grepafloxacin.
DigoxinDigoxin may decrease the cardiotoxic activities of Grepafloxacin.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Grepafloxacin.
DihydroergotamineThe metabolism of Grepafloxacin can be decreased when combined with Dihydroergotamine.
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Grepafloxacin.
DiltiazemThe metabolism of Grepafloxacin can be decreased when combined with Diltiazem.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Grepafloxacin.
DipyridamoleThe serum concentration of Grepafloxacin can be increased when it is combined with Dipyridamole.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Grepafloxacin.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Grepafloxacin.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Grepafloxacin.
DoxazosinThe serum concentration of Grepafloxacin can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Grepafloxacin can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Grepafloxacin can be decreased when it is combined with Doxorubicin.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Grepafloxacin.
DoxycyclineThe metabolism of Grepafloxacin can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Grepafloxacin can be increased when it is combined with Dronabinol.
DronedaroneThe metabolism of Grepafloxacin can be decreased when combined with Dronedarone.
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Grepafloxacin.
EfavirenzThe serum concentration of Grepafloxacin can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Grepafloxacin can be increased when it is combined with Elbasvir.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Grepafloxacin.
EnalaprilThe serum concentration of Grepafloxacin can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Grepafloxacin can be increased when it is combined with Enzalutamide.
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Grepafloxacin.
ErgonovineThe serum concentration of Grepafloxacin can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Grepafloxacin can be increased when it is combined with Ergotamine.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Grepafloxacin.
ErythromycinThe metabolism of Grepafloxacin can be decreased when combined with Erythromycin.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Grepafloxacin.
Eslicarbazepine acetateThe serum concentration of Grepafloxacin can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Grepafloxacin.
EstramustineThe serum concentration of Grepafloxacin can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Grepafloxacin can be decreased when it is combined with Estriol.
EstriolThe serum concentration of Estriol can be increased when it is combined with Grepafloxacin.
EstroneThe serum concentration of Grepafloxacin can be decreased when it is combined with Estrone.
EstroneThe serum concentration of Estrone can be increased when it is combined with Grepafloxacin.
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Grepafloxacin.
EtoposideThe serum concentration of Grepafloxacin can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Grepafloxacin can be decreased when it is combined with Etravirine.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Grepafloxacin.
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Grepafloxacin.
FelodipineThe serum concentration of Grepafloxacin can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Grepafloxacin can be increased when it is combined with Fentanyl.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Grepafloxacin.
FexofenadineThe serum concentration of Grepafloxacin can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Grepafloxacin.
FluconazoleThe metabolism of Grepafloxacin can be decreased when combined with Fluconazole.
FluoxetineThe serum concentration of Grepafloxacin can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Grepafloxacin can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Grepafloxacin can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Grepafloxacin can be increased when it is combined with Flurazepam.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Grepafloxacin.
FluvoxamineThe metabolism of Grepafloxacin can be decreased when combined with Fluvoxamine.
FosamprenavirThe metabolism of Grepafloxacin can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Grepafloxacin can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Grepafloxacin can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Grepafloxacin can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Grepafloxacin can be increased when it is combined with Gefitinib.
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Grepafloxacin.
GenisteinThe serum concentration of Grepafloxacin can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Grepafloxacin can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Grepafloxacin can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Grepafloxacin can be increased when it is combined with Gramicidin D.
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Grepafloxacin can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Grepafloxacin can be increased when it is combined with Hydrocortisone.
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Grepafloxacin.
IdelalisibThe serum concentration of Grepafloxacin can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Grepafloxacin can be decreased when combined with Imatinib.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Grepafloxacin.
ImipramineThe serum concentration of Grepafloxacin can be increased when it is combined with Imipramine.
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Grepafloxacin.
IndinavirThe serum concentration of Grepafloxacin can be decreased when it is combined with Indinavir.
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Grepafloxacin.
IndomethacinThe serum concentration of Grepafloxacin can be increased when it is combined with Indomethacin.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Grepafloxacin.
IsavuconazoniumThe metabolism of Grepafloxacin can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Grepafloxacin can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Grepafloxacin can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Grepafloxacin can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Grepafloxacin can be increased when it is combined with Ketamine.
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Grepafloxacin.
KetoconazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Ketoconazole.
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Grepafloxacin.
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Grepafloxacin.
LansoprazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Grepafloxacin can be increased when it is combined with Lapatinib.
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Grepafloxacin.
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Grepafloxacin.
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Grepafloxacin.
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Grepafloxacin.
LevofloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Levofloxacin.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Grepafloxacin.
LevothyroxineThe serum concentration of Grepafloxacin can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Grepafloxacin can be increased when it is combined with Lidocaine.
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Grepafloxacin.
LiothyronineThe serum concentration of Grepafloxacin can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Grepafloxacin can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Grepafloxacin can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Grepafloxacin can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Grepafloxacin can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Grepafloxacin can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Grepafloxacin can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Grepafloxacin can be increased when it is combined with Losartan.
LovastatinThe metabolism of Grepafloxacin can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Grepafloxacin can be decreased when it is combined with Lumacaftor.
MannitolThe serum concentration of Mannitol can be increased when it is combined with Grepafloxacin.
MaprotilineThe serum concentration of Grepafloxacin can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Grepafloxacin can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Grepafloxacin can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Grepafloxacin can be increased when it is combined with Meprobamate.
MethadoneThe serum concentration of Grepafloxacin can be increased when it is combined with Methadone.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Grepafloxacin.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Grepafloxacin.
MetoprololThe serum concentration of Grepafloxacin can be increased when it is combined with Metoprolol.
MexiletineThe metabolism of Grepafloxacin can be decreased when combined with Mexiletine.
MibefradilThe serum concentration of Grepafloxacin can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Grepafloxacin can be decreased when it is combined with Midazolam.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Grepafloxacin.
MifepristoneThe metabolism of Grepafloxacin can be decreased when combined with Mifepristone.
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Grepafloxacin.
MitomycinThe serum concentration of Grepafloxacin can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Grepafloxacin can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Grepafloxacin can be decreased when it is combined with Mitoxantrone.
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Grepafloxacin.
ModafinilThe serum concentration of Grepafloxacin can be decreased when it is combined with Modafinil.
MorphineThe serum concentration of Grepafloxacin can be increased when it is combined with Morphine.
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Grepafloxacin.
NadololThe serum concentration of Nadolol can be increased when it is combined with Grepafloxacin.
NafcillinThe serum concentration of Grepafloxacin can be decreased when it is combined with Nafcillin.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Grepafloxacin.
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Grepafloxacin.
NaltrexoneThe serum concentration of Grepafloxacin can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Grepafloxacin can be increased when it is combined with Naringenin.
NefazodoneThe serum concentration of Grepafloxacin can be decreased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Grepafloxacin can be decreased when it is combined with Nelfinavir.
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Grepafloxacin.
NeostigmineThe serum concentration of Grepafloxacin can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Grepafloxacin can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Grepafloxacin can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Grepafloxacin can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Grepafloxacin can be decreased when it is combined with Nifedipine.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Grepafloxacin.
NilotinibThe metabolism of Grepafloxacin can be decreased when combined with Nilotinib.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Grepafloxacin.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Grepafloxacin.
NisoldipineThe serum concentration of Grepafloxacin can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Grepafloxacin can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Grepafloxacin can be increased when it is combined with Nitrendipine.
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Grepafloxacin.
NorethisteroneThe serum concentration of Grepafloxacin can be decreased when it is combined with Norethisterone.
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Grepafloxacin.
OlaparibThe metabolism of Grepafloxacin can be decreased when combined with Olaparib.
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Grepafloxacin.
OmeprazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Grepafloxacin can be increased when it is combined with Osimertinib.
OuabainOuabain may decrease the cardiotoxic activities of Grepafloxacin.
P-NitrophenolThe serum concentration of Grepafloxacin can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Grepafloxacin can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Grepafloxacin can be increased when it is combined with Palbociclib.
Palmitic AcidThe serum concentration of Grepafloxacin can be increased when it is combined with Palmitic Acid.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Grepafloxacin.
PantoprazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Grepafloxacin can be increased when it is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Grepafloxacin.
Peginterferon alfa-2bThe serum concentration of Grepafloxacin can be increased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Grepafloxacin can be increased when combined with Pentobarbital.
PerindoprilThe serum concentration of Grepafloxacin can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Grepafloxacin can be decreased when it is combined with Phenobarbital.
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Grepafloxacin.
PhenytoinThe metabolism of Grepafloxacin can be increased when combined with Phenytoin.
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Grepafloxacin.
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Grepafloxacin.
PimozideThe serum concentration of Grepafloxacin can be increased when it is combined with Pimozide.
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Grepafloxacin.
Platelet Activating FactorThe serum concentration of Grepafloxacin can be decreased when it is combined with Platelet Activating Factor.
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Grepafloxacin.
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Grepafloxacin.
PosaconazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Grepafloxacin can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Grepafloxacin can be increased when it is combined with Prazosin.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Grepafloxacin.
PrednisoneThe serum concentration of Grepafloxacin can be increased when it is combined with Prednisone.
PrimidoneThe metabolism of Grepafloxacin can be increased when combined with Primidone.
ProbenecidThe serum concentration of Grepafloxacin can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Grepafloxacin can be decreased when it is combined with Progesterone.
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Grepafloxacin.
PromethazineThe serum concentration of Grepafloxacin can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Grepafloxacin can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Grepafloxacin can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Grepafloxacin can be increased when it is combined with Protriptyline.
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Grepafloxacin.
QuercetinThe serum concentration of Grepafloxacin can be increased when it is combined with Quercetin.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Grepafloxacin.
QuinacrineThe serum concentration of Grepafloxacin can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Grepafloxacin can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Grepafloxacin can be increased when it is combined with Quinine.
RanitidineThe serum concentration of Grepafloxacin can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Grepafloxacin.
ReboxetineThe serum concentration of Grepafloxacin can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Grepafloxacin can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Grepafloxacin can be decreased when it is combined with Reserpine.
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Grepafloxacin.
RifabutinThe metabolism of Grepafloxacin can be increased when combined with Rifabutin.
RifampicinThe serum concentration of Grepafloxacin can be decreased when it is combined with Rifampicin.
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Grepafloxacin.
RifapentineThe metabolism of Grepafloxacin can be increased when combined with Rifapentine.
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Grepafloxacin.
RilpivirineThe serum concentration of Grepafloxacin can be increased when it is combined with Rilpivirine.
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Grepafloxacin.
RitonavirThe serum concentration of Grepafloxacin can be decreased when it is combined with Ritonavir.
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Grepafloxacin.
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Grepafloxacin.
RolapitantThe serum concentration of Grepafloxacin can be increased when it is combined with Rolapitant.
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Grepafloxacin.
RopiniroleThe metabolism of Grepafloxacin can be decreased when combined with Ropinirole.
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Grepafloxacin.
SaquinavirThe serum concentration of Grepafloxacin can be decreased when it is combined with Saquinavir.
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Grepafloxacin.
ScopolamineThe serum concentration of Grepafloxacin can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Grepafloxacin can be increased when it is combined with Selegiline.
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Grepafloxacin.
SertralineThe serum concentration of Grepafloxacin can be increased when it is combined with Sertraline.
SildenafilThe metabolism of Grepafloxacin can be decreased when combined with Sildenafil.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Grepafloxacin.
SiltuximabThe serum concentration of Grepafloxacin can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Grepafloxacin can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Grepafloxacin can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Grepafloxacin can be decreased when it is combined with Sirolimus.
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Grepafloxacin.
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Grepafloxacin.
SorafenibThe serum concentration of Grepafloxacin can be increased when it is combined with Sorafenib.
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Grepafloxacin.
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Grepafloxacin.
SpironolactoneThe serum concentration of Grepafloxacin can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Grepafloxacin can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Grepafloxacin can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Grepafloxacin can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Grepafloxacin can be decreased when it is combined with Streptozocin.
SulfinpyrazoneThe serum concentration of Grepafloxacin can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe metabolism of Grepafloxacin can be decreased when combined with Sulfisoxazole.
SumatriptanThe serum concentration of Grepafloxacin can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Grepafloxacin can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Grepafloxacin can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Grepafloxacin can be decreased when it is combined with Tacrolimus.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Grepafloxacin.
TamoxifenThe serum concentration of Grepafloxacin can be decreased when it is combined with Tamoxifen.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Grepafloxacin.
Taurocholic AcidThe serum concentration of Grepafloxacin can be increased when it is combined with Taurocholic Acid.
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Grepafloxacin.
TelaprevirThe metabolism of Grepafloxacin can be decreased when combined with Telaprevir.
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Grepafloxacin.
TelithromycinThe metabolism of Grepafloxacin can be decreased when combined with Telithromycin.
TelmisartanThe serum concentration of Grepafloxacin can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Grepafloxacin.
TenofovirThe metabolism of Grepafloxacin can be decreased when combined with Tenofovir.
TerazosinThe serum concentration of Grepafloxacin can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Grepafloxacin can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Grepafloxacin can be decreased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Grepafloxacin can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Grepafloxacin can be increased when it is combined with Testosterone.
TheophyllineThe metabolism of Grepafloxacin can be decreased when combined with Theophylline.
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Grepafloxacin.
TiclopidineThe metabolism of Grepafloxacin can be decreased when combined with Ticlopidine.
TimololThe serum concentration of Timolol can be increased when it is combined with Grepafloxacin.
TocilizumabThe serum concentration of Grepafloxacin can be decreased when it is combined with Tocilizumab.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Grepafloxacin.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Grepafloxacin.
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Grepafloxacin.
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Grepafloxacin.
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Grepafloxacin.
TrazodoneThe serum concentration of Grepafloxacin can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Grepafloxacin can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Grepafloxacin can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Grepafloxacin can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Grepafloxacin can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Grepafloxacin can be increased when it is combined with Troleandomycin.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Grepafloxacin.
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Grepafloxacin.
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Grepafloxacin.
VemurafenibThe serum concentration of Grepafloxacin can be increased when it is combined with Vemurafenib.
VenlafaxineThe metabolism of Grepafloxacin can be decreased when combined with Venlafaxine.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Grepafloxacin.
VerapamilThe metabolism of Grepafloxacin can be decreased when combined with Verapamil.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Grepafloxacin.
VinblastineThe serum concentration of Grepafloxacin can be decreased when it is combined with Vinblastine.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Grepafloxacin.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Grepafloxacin.
VincristineThe serum concentration of Grepafloxacin can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Grepafloxacin can be increased when it is combined with Vinorelbine.
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Grepafloxacin.
VoriconazoleThe metabolism of Grepafloxacin can be decreased when combined with Voriconazole.
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Grepafloxacin.
ZimelidineThe serum concentration of Grepafloxacin can be increased when it is combined with Zimelidine.
ZiprasidoneThe metabolism of Grepafloxacin can be decreased when combined with Ziprasidone.
Food Interactions
  • Drink liberally but avoid coffee.
  • Take without regard to meals.

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:
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, including catenanes and knotted rings.
Gene Name:
gyrA
Uniprot ID:
P43700
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. Stewart BA, Johnson AP, Woodford N: Relationship between mutations in parC and gyrA of clinical isolates of Streptococcus pneumoniae and resistance to ciprofloxacin and grepafloxacin. J Med Microbiol. 1999 Dec;48(12):1103-6. [PubMed:10591164 ]
  4. Jorgensen JH, Weigel LM, Ferraro MJ, Swenson JM, Tenover FC: Activities of newer fluoroquinolones against Streptococcus pneumoniae clinical isolates including those with mutations in the gyrA, parC, and parE loci. Antimicrob Agents Chemother. 1999 Feb;43(2):329-34. [PubMed:9925527 ]
  5. Griggs DJ, Marona H, Piddock LJ: Selection of moxifloxacin-resistant Staphylococcus aureus compared with five other fluoroquinolones. J Antimicrob Chemother. 2003 Jun;51(6):1403-7. Epub 2003 Apr 25. [PubMed:12716775 ]
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
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. Ernst EJ, Klepser ME, Petzold CR, Doern GV: Evaluation of survival and pharmacodynamic relationships for five fluoroquinolones in a neutropenic murine model of pneumococcal lung infection. Pharmacotherapy. 2002 Apr;22(4):463-70. [PubMed:11939681 ]
  4. Morris JE, Pan XS, Fisher LM: Grepafloxacin, a dimethyl derivative of ciprofloxacin, acts preferentially through gyrase in Streptococcus pneumoniae: role of the C-5 group in target specificity. Antimicrob Agents Chemother. 2002 Feb;46(2):582-5. [PubMed:11796384 ]
  5. Kawamura-Sato K, Hasegawa T, Torii K, Ito H, Ohta M: Prevalence of Ile-460-Val/ParE substitution in clinical Streptococcus pneumoniae isolates that were less susceptible to fluoroquinolones. Curr Microbiol. 2005 Jul;51(1):27-30. Epub 2005 May 31. [PubMed:15942701 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Rodighiero V: Effects of liver disease on pharmacokinetics. An update. Clin Pharmacokinet. 1999 Nov;37(5):399-431. [PubMed:10589374 ]
  2. Bril F, Gonzalez CD, Di Girolamo G: Antimicrobial agents-associated with QT interval prolongation. Curr Drug Saf. 2010 Jan;5(1):85-92. [PubMed:20210724 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
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 performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Pal D, Mitra AK: MDR- and CYP3A4-mediated drug-drug interactions. J Neuroimmune Pharmacol. 2006 Sep;1(3):323-39. Epub 2006 Aug 2. [PubMed:18040809 ]
  2. Owens RC Jr: QT prolongation with antimicrobial agents: understanding the significance. Drugs. 2004;64(10):1091-124. [PubMed:15139788 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Yamaguchi H, Yano I, Hashimoto Y, Inui KI: Secretory mechanisms of grepafloxacin and levofloxacin in the human intestinal cell line caco-2. J Pharmacol Exp Ther. 2000 Oct;295(1):360-6. [PubMed:10992002 ]
  2. Naruhashi K, Tamai I, Inoue N, Muraoka H, Sai Y, Suzuki N, Tsuji A: Active intestinal secretion of new quinolone antimicrobials and the partial contribution of P-glycoprotein. J Pharm Pharmacol. 2001 May;53(5):699-709. [PubMed:11370709 ]
  3. Yamaguchi H, Yano I, Saito H, Inui K: Effect of cisplatin-induced acute renal failure on bioavailability and intestinal secretion of quinolone antibacterial drugs in rats. Pharm Res. 2004 Feb;21(2):330-8. [PubMed:15032316 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Tamai I, Yamashita J, Kido Y, Ohnari A, Sai Y, Shima Y, Naruhashi K, Koizumi S, Tsuji A: Limited distribution of new quinolone antibacterial agents into brain caused by multiple efflux transporters at the blood-brain barrier. J Pharmacol Exp Ther. 2000 Oct;295(1):146-52. [PubMed:10991972 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one molecule of endogenous dicarboxylic acid (glutarate, ketoglutarate, etc). Mediates the sodium-independent uptake of 2,3-dimercapto-1-propanesulfonic acid (DMPS) (By similarity). Mediates the sodium-in...
Gene Name:
SLC22A6
Uniprot ID:
Q4U2R8
Molecular Weight:
61815.78 Da
References
  1. Uwai Y, Okuda M, Takami K, Hashimoto Y, Inui K: Functional characterization of the rat multispecific organic anion transporter OAT1 mediating basolateral uptake of anionic drugs in the kidney. FEBS Lett. 1998 Nov 6;438(3):321-4. [PubMed:9827570 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Urakami Y, Akazawa M, Saito H, Okuda M, Inui K: cDNA cloning, functional characterization, and tissue distribution of an alternatively spliced variant of organic cation transporter hOCT2 predominantly expressed in the human kidney. J Am Soc Nephrol. 2002 Jul;13(7):1703-10. [PubMed:12089365 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Symporter activity
Specific Function:
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Also relative uptake activity ratio of carnitine to TEA is 11.3.
Gene Name:
SLC22A5
Uniprot ID:
O76082
Molecular Weight:
62751.08 Da
References
  1. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. [PubMed:10525100 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular Weight:
174205.64 Da
References
  1. Sasabe H, Tsuji A, Sugiyama Y: Carrier-mediated mechanism for the biliary excretion of the quinolone antibiotic grepafloxacin and its glucuronide in rats. J Pharmacol Exp Ther. 1998 Mar;284(3):1033-9. [PubMed:9495864 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23