Identification

Name
Grepafloxacin
Accession Number
DB00365  (APRD01003)
Type
Small Molecule
Groups
Approved, Investigational, Withdrawn
Description

Grepafloxacin 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 Grepafloxacin was withdrawn in the United States due to its side effect of lengthening the QT interval on the electrocardiogram, leading to cardiac events and sudden death.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
Synonyms
Not Available
Product Ingredients
IngredientUNIICASInChI Key
Grepafloxacin hydrochlorideA4ER1Z8N9N161967-81-3IEPMBYOIQGCVHO-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
RaxarTablet200 mgOralOtsuka Pharma Gmbh1998-07-011999-10-27Canada
Categories
UNII
L1M1U2HC31
CAS number
119914-60-2
Weight
Average: 359.3947
Monoisotopic: 359.16451979
Chemical Formula
C19H22FN3O3
InChI Key
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

Pharmacology

Indication

For treatment of adults with mild to moderate infections caused by susceptible strains of Haemophilus influenzae, Streptococcus pneumoniae, or Moraxella catarrhalis.

Structured Indications
Not Available
Pharmacodynamics

Grepafloxacin has in vitro activity against a wide range of gram-positive and gram-negative aerobic microorganisms, as well as some atypical microorganisms.

Mechanism of action

Grepafloxacin exerts its antibacterial activity by inhibiting bacterial topoisomerase II (DNA gyrase) and topoisomerase IV, essential enzymes for duplication, transcription, and repair of bacterial DNA.

TargetActionsOrganism
ADNA gyrase subunit A
inhibitor
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
ADNA topoisomerase 4 subunit A
inhibitor
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Absorption

Rapidly and extensively absorbed following oral administration. The absolute bioavailability is approximately 70%.

Volume of distribution
Not Available
Protein binding

50%

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 elimination
Not Available
Half life

15 ± 3 hours

Clearance
Not Available
Toxicity

Withdrawn 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
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
(4R)-limonene(4R)-limonene may increase the neuroexcitatory activities of Grepafloxacin.Investigational
16-BromoepiandrosteroneThe risk or severity of adverse effects can be increased when 16-Bromoepiandrosterone is combined with Grepafloxacin.Investigational
19-norandrostenedioneThe risk or severity of adverse effects can be increased when 19-norandrostenedione is combined with Grepafloxacin.Experimental, Illicit
5-androstenedioneThe risk or severity of adverse effects can be increased when 5-androstenedione is combined with Grepafloxacin.Experimental, Illicit
AbirateroneThe serum concentration of Grepafloxacin can be increased when it is combined with Abiraterone.Approved
AcarboseGrepafloxacin may increase the hypoglycemic activities of Acarbose.Approved, Investigational
AceclofenacAceclofenac may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
AcemetacinAcemetacin may increase the neuroexcitatory activities of Grepafloxacin.Approved, Experimental, Investigational
AcenocoumarolGrepafloxacin may increase the anticoagulant activities of Acenocoumarol.Approved, Investigational
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Grepafloxacin.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Grepafloxacin.Experimental
Acetylsalicylic acidAcetylsalicylic acid may increase the neuroexcitatory activities of Grepafloxacin.Approved, Vet Approved
AdapaleneAdapalene may increase the neuroexcitatory activities of Grepafloxacin.Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Grepafloxacin.Approved
AlbiglutideGrepafloxacin may increase the hypoglycemic activities of Albiglutide.Approved
AlclofenacAlclofenac may increase the neuroexcitatory activities of Grepafloxacin.Approved, Withdrawn
AlclometasoneThe risk or severity of adverse effects can be increased when Alclometasone is combined with Grepafloxacin.Approved
AldosteroneThe risk or severity of adverse effects can be increased when Aldosterone is combined with Grepafloxacin.Experimental, Investigational
AlmasilateAlmasilate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental
AlminoprofenAlminoprofen may increase the neuroexcitatory activities of Grepafloxacin.Experimental
AlogliptinGrepafloxacin may increase the hypoglycemic activities of Alogliptin.Approved
AloglutamolAloglutamol can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
AluminiumAluminium can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational
Aluminium acetoacetateAluminium acetoacetate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminium glycinateAluminium glycinate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational
Ambroxol acefyllinateThe metabolism of Ambroxol acefyllinate can be decreased when combined with Grepafloxacin.Experimental, Investigational
AmcinonideThe risk or severity of adverse effects can be increased when Amcinonide is combined with Grepafloxacin.Approved
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Grepafloxacin.Approved
AmiodaroneThe metabolism of Grepafloxacin can be decreased when combined with Amiodarone.Approved, Investigational
AncestimThe risk or severity of cytotoxicity can be increased when Ancestim is combined with Grepafloxacin.Approved, Investigational, Withdrawn
AndrographolideAndrographolide may increase the neuroexcitatory activities of Grepafloxacin.Investigational
AndrostenedioneThe risk or severity of adverse effects can be increased when Androstenedione is combined with Grepafloxacin.Experimental, Illicit
AnecortaveThe risk or severity of adverse effects can be increased when Anecortave is combined with Grepafloxacin.Investigational
anecortave acetateThe risk or severity of adverse effects can be increased when anecortave acetate is combined with Grepafloxacin.Investigational
AnisodamineAnisodamine may increase the neuroexcitatory activities of Grepafloxacin.Investigational
AntipyrineAntipyrine may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
ApalutamideThe serum concentration of Grepafloxacin can be decreased when it is combined with Apalutamide.Approved, Investigational
ApocyninApocynin may increase the neuroexcitatory activities of Grepafloxacin.Investigational
ApremilastApremilast may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
AprepitantThe serum concentration of Grepafloxacin can be increased when it is combined with Aprepitant.Approved, Investigational
AtamestaneThe risk or severity of adverse effects can be increased when Atamestane is combined with Grepafloxacin.Investigational
AtazanavirThe metabolism of Grepafloxacin can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Grepafloxacin can be decreased when combined with Atomoxetine.Approved
AzapropazoneAzapropazone may increase the neuroexcitatory activities of Grepafloxacin.Withdrawn
AzelastineAzelastine may increase the neuroexcitatory activities of Grepafloxacin.Approved
AzithromycinThe metabolism of Grepafloxacin can be decreased when combined with Azithromycin.Approved
BalsalazideBalsalazide may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Grepafloxacin.Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Grepafloxacin.Approved, Investigational
BendazacBendazac may increase the neuroexcitatory activities of Grepafloxacin.Experimental
BenorilateBenorilate may increase the neuroexcitatory activities of Grepafloxacin.Experimental
BenoxaprofenBenoxaprofen may increase the neuroexcitatory activities of Grepafloxacin.Withdrawn
BenzydamineBenzydamine may increase the neuroexcitatory activities of Grepafloxacin.Approved
BetamethasoneThe risk or severity of adverse effects can be increased when Betamethasone is combined with Grepafloxacin.Approved, Vet Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Grepafloxacin.Approved, Investigational
BevoniumBevonium may increase the neuroexcitatory activities of Grepafloxacin.Experimental
Bismuth SubcitrateBismuth Subcitrate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational
Bismuth subnitrateBismuth subnitrate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
BoceprevirThe metabolism of Grepafloxacin can be decreased when combined with Boceprevir.Approved, Withdrawn
BortezomibThe metabolism of Grepafloxacin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Grepafloxacin can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Grepafloxacin.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Grepafloxacin.Approved, Investigational
BromfenacBromfenac may increase the neuroexcitatory activities of Grepafloxacin.Approved
BromocriptineGrepafloxacin may increase the hypoglycemic activities of Bromocriptine.Approved, Investigational
BucillamineBucillamine may increase the neuroexcitatory activities of Grepafloxacin.Investigational
BudesonideThe risk or severity of adverse effects can be increased when Budesonide is combined with Grepafloxacin.Approved
BufexamacBufexamac may increase the neuroexcitatory activities of Grepafloxacin.Approved, Experimental
BumadizoneBumadizone may increase the neuroexcitatory activities of Grepafloxacin.Experimental
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Grepafloxacin.Approved
CaffeineThe metabolism of Grepafloxacin can be decreased when combined with Caffeine.Approved
Calcium AcetateCalcium Acetate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational
Calcium CarbonateCalcium Carbonate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational
Calcium ChlorideCalcium Chloride can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium CitrateCalcium Citrate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium glubionateCalcium glubionate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium GluceptateCalcium Gluceptate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium gluconateCalcium gluconate can cause a decrease in the absorption of Grepafloxacin 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 Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational, Vet Approved
Calcium lactate gluconateCalcium lactate gluconate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Calcium levulinateCalcium levulinate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental
Calcium pangamateCalcium pangamate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Calcium PhosphateCalcium Phosphate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium silicateCalcium silicate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
CanagliflozinGrepafloxacin may increase the hypoglycemic activities of Canagliflozin.Approved
CarbamazepineThe metabolism of Grepafloxacin can be increased when combined with Carbamazepine.Approved, Investigational
Carbaspirin calciumCarbaspirin calcium may increase the neuroexcitatory activities of Grepafloxacin.Experimental, Investigational
CarprofenCarprofen may increase the neuroexcitatory activities of Grepafloxacin.Approved, Vet Approved, Withdrawn
CaseinCasein can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CastanospermineCastanospermine may increase the neuroexcitatory activities of Grepafloxacin.Experimental
CelecoxibCelecoxib may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
CeritinibThe serum concentration of Grepafloxacin can be increased when it is combined with Ceritinib.Approved
ChloroquineChloroquine may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational, Vet Approved
ChlorpropamideGrepafloxacin may increase the hypoglycemic activities of Chlorpropamide.Approved, Investigational
Choline magnesium trisalicylateCholine magnesium trisalicylate may increase the neuroexcitatory activities of Grepafloxacin.Approved
CiclesonideThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Grepafloxacin.Approved, Investigational
CitalopramThe metabolism of Grepafloxacin can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Grepafloxacin can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Grepafloxacin can be decreased when combined with Clemastine.Approved, Investigational
ClobetasolThe risk or severity of adverse effects can be increased when Clobetasol is combined with Grepafloxacin.Approved, Investigational
Clobetasol propionateThe risk or severity of adverse effects can be increased when Clobetasol propionate is combined with Grepafloxacin.Approved
ClobetasoneThe risk or severity of adverse effects can be increased when Clobetasone is combined with Grepafloxacin.Approved
ClocortoloneThe risk or severity of adverse effects can be increased when Clocortolone is combined with Grepafloxacin.Approved
ClonixinClonixin may increase the neuroexcitatory activities of Grepafloxacin.Approved
ClorindioneGrepafloxacin may increase the anticoagulant activities of Clorindione.Experimental
ClotrimazoleThe metabolism of Grepafloxacin can be decreased when combined with Clotrimazole.Approved, Vet Approved
CobicistatThe metabolism of Grepafloxacin can be decreased when combined with Cobicistat.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Grepafloxacin.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Grepafloxacin.Approved, Investigational
Cortexolone 17α-propionateThe risk or severity of adverse effects can be increased when Cortexolone 17α-propionate is combined with Grepafloxacin.Investigational
CorticosteroneThe risk or severity of adverse effects can be increased when Corticosterone is combined with Grepafloxacin.Experimental
Cortisone acetateThe risk or severity of adverse effects can be increased when Cortisone acetate is combined with Grepafloxacin.Approved, Investigational
CrizotinibThe metabolism of Grepafloxacin can be decreased when combined with Crizotinib.Approved
CurcuminCurcumin may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Grepafloxacin.Approved, Investigational
CyclosporineThe metabolism of Grepafloxacin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Grepafloxacin.Experimental
Cyproterone acetateThe serum concentration of Grepafloxacin can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Grepafloxacin.Approved
DabrafenibThe serum concentration of Grepafloxacin can be decreased when it is combined with Dabrafenib.Approved, Investigational
DapagliflozinGrepafloxacin may increase the hypoglycemic activities of Dapagliflozin.Approved
DarunavirThe metabolism of Grepafloxacin can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Grepafloxacin can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Grepafloxacin can be decreased when it is combined with Deferasirox.Approved, Investigational
DeflazacortThe risk or severity of adverse effects can be increased when Deflazacort is combined with Grepafloxacin.Approved, Investigational
DelamanidGrepafloxacin may increase the QTc-prolonging activities of Delamanid.Approved, Investigational
DelavirdineThe metabolism of Grepafloxacin can be decreased when combined with Delavirdine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Grepafloxacin.Approved
DesonideThe risk or severity of adverse effects can be increased when Desonide is combined with Grepafloxacin.Approved, Investigational
DesoximetasoneThe risk or severity of adverse effects can be increased when Desoximetasone is combined with Grepafloxacin.Approved
Desoxycorticosterone acetateThe risk or severity of adverse effects can be increased when Desoxycorticosterone acetate is combined with Grepafloxacin.Approved
Desoxycorticosterone PivalateThe risk or severity of adverse effects can be increased when Desoxycorticosterone Pivalate is combined with Grepafloxacin.Experimental, Vet Approved
DeutetrabenazineGrepafloxacin may increase the QTc-prolonging activities of Deutetrabenazine.Approved, Investigational
DexamethasoneThe risk or severity of adverse effects can be increased when Dexamethasone is combined with Grepafloxacin.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Dexamethasone isonicotinate is combined with Grepafloxacin.Vet Approved
DiclofenacDiclofenac may increase the neuroexcitatory activities of Grepafloxacin.Approved, Vet Approved
DicoumarolGrepafloxacin may increase the anticoagulant activities of Dicoumarol.Approved
DidanosineThe serum concentration of Didanosine can be decreased when it is combined with Grepafloxacin.Approved
DifenpiramideDifenpiramide may increase the neuroexcitatory activities of Grepafloxacin.Experimental
DiflorasoneThe risk or severity of adverse effects can be increased when Diflorasone is combined with Grepafloxacin.Approved
DiflunisalDiflunisal may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
DifluocortoloneThe risk or severity of adverse effects can be increased when Difluocortolone is combined with Grepafloxacin.Approved, Investigational, Withdrawn
DifluprednateThe risk or severity of adverse effects can be increased when Difluprednate is combined with Grepafloxacin.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Grepafloxacin.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Grepafloxacin.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Grepafloxacin.Approved
DihydroergotamineThe metabolism of Grepafloxacin can be decreased when combined with Dihydroergotamine.Approved, Investigational
DiltiazemThe metabolism of Grepafloxacin can be decreased when combined with Diltiazem.Approved, Investigational
DiphenadioneGrepafloxacin may increase the anticoagulant activities of Diphenadione.Experimental
DisopyramideGrepafloxacin may increase the hypoglycemic activities of Disopyramide.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Grepafloxacin.Approved, Investigational
DosulepinThe metabolism of Grepafloxacin can be decreased when combined with Dosulepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Grepafloxacin.Approved, Investigational
DoxycyclineThe metabolism of Grepafloxacin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Grepafloxacin can be decreased when combined with Dronedarone.Approved
DroxicamDroxicam may increase the neuroexcitatory activities of Grepafloxacin.Withdrawn
DulaglutideGrepafloxacin may increase the hypoglycemic activities of Dulaglutide.Approved, Investigational
DuvelisibDuvelisib may increase the neuroexcitatory activities of Grepafloxacin.Investigational
DyphyllineThe metabolism of Dyphylline can be decreased when combined with Grepafloxacin.Approved
E-6201E-6201 may increase the neuroexcitatory activities of Grepafloxacin.Investigational
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Grepafloxacin.Approved
EmpagliflozinGrepafloxacin may increase the hypoglycemic activities of Empagliflozin.Approved
EnzalutamideThe serum concentration of Grepafloxacin can be decreased when it is combined with Enzalutamide.Approved
EpirizoleEpirizole may increase the neuroexcitatory activities of Grepafloxacin.Approved
EquileninThe risk or severity of adverse effects can be increased when Equilenin is combined with Grepafloxacin.Experimental
EquilinThe risk or severity of adverse effects can be increased when Equilin is combined with Grepafloxacin.Approved
ErythromycinThe metabolism of Grepafloxacin can be decreased when combined with Erythromycin.Approved, Investigational, Vet Approved
EstroneThe risk or severity of adverse effects can be increased when Estrone is combined with Grepafloxacin.Approved
Estrone sulfateThe risk or severity of adverse effects can be increased when Estrone sulfate is combined with Grepafloxacin.Approved
EtanerceptEtanercept may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
EthenzamideEthenzamide may increase the neuroexcitatory activities of Grepafloxacin.Experimental
Ethyl biscoumacetateGrepafloxacin may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtodolacEtodolac may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
EtoricoxibEtoricoxib may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
Evening primrose oilEvening primrose oil may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Grepafloxacin.Approved
ExenatideGrepafloxacin may increase the hypoglycemic activities of Exenatide.Approved, Investigational
ExisulindExisulind may increase the neuroexcitatory activities of Grepafloxacin.Investigational
FelbinacFelbinac may increase the neuroexcitatory activities of Grepafloxacin.Experimental
FenbufenFenbufen may increase the neuroexcitatory activities of Grepafloxacin.Approved
FenoprofenFenoprofen may increase the neuroexcitatory activities of Grepafloxacin.Approved
FentiazacFentiazac may increase the neuroexcitatory activities of Grepafloxacin.Experimental
FeprazoneFeprazone may increase the neuroexcitatory activities of Grepafloxacin.Experimental
Ferric CarboxymaltoseThe serum concentration of Grepafloxacin can be decreased when it is combined with Ferric Carboxymaltose.Approved
Ferric pyrophosphateThe serum concentration of Grepafloxacin can be decreased when it is combined with Ferric pyrophosphate.Experimental
Ferulic acidFerulic acid may increase the neuroexcitatory activities of Grepafloxacin.Experimental
FloctafenineFloctafenine may increase the neuroexcitatory activities of Grepafloxacin.Approved, Withdrawn
FluasteroneThe risk or severity of adverse effects can be increased when Fluasterone is combined with Grepafloxacin.Investigational
FluconazoleThe metabolism of Grepafloxacin can be decreased when combined with Fluconazole.Approved, Investigational
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Grepafloxacin.Approved, Investigational
FluindioneGrepafloxacin may increase the anticoagulant activities of Fluindione.Approved, Investigational
FlumethasoneThe risk or severity of adverse effects can be increased when Flumethasone is combined with Grepafloxacin.Approved, Vet Approved
FlunisolideThe risk or severity of adverse effects can be increased when Flunisolide is combined with Grepafloxacin.Approved, Investigational
FlunixinFlunixin may increase the neuroexcitatory activities of Grepafloxacin.Vet Approved
FlunoxaprofenFlunoxaprofen may increase the neuroexcitatory activities of Grepafloxacin.Experimental
Fluocinolone AcetonideThe risk or severity of adverse effects can be increased when Fluocinolone Acetonide is combined with Grepafloxacin.Approved, Investigational, Vet Approved
FluocinonideThe risk or severity of adverse effects can be increased when Fluocinonide is combined with Grepafloxacin.Approved, Investigational
FluocortoloneThe risk or severity of adverse effects can be increased when Fluocortolone is combined with Grepafloxacin.Approved, Withdrawn
FluorometholoneThe risk or severity of adverse effects can be increased when Fluorometholone is combined with Grepafloxacin.Approved, Investigational
FluprednideneThe risk or severity of adverse effects can be increased when Fluprednidene is combined with Grepafloxacin.Approved, Withdrawn
FluprednisoloneThe risk or severity of adverse effects can be increased when Fluprednisolone is combined with Grepafloxacin.Approved
FlurandrenolideThe risk or severity of adverse effects can be increased when Flurandrenolide is combined with Grepafloxacin.Approved
FlurbiprofenFlurbiprofen may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
Fluticasone furoateThe risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Grepafloxacin.Approved
Fluticasone propionateThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with Grepafloxacin.Approved
FluvoxamineThe metabolism of Grepafloxacin can be decreased when combined with Fluvoxamine.Approved, Investigational
FormestaneThe risk or severity of adverse effects can be increased when Formestane is combined with Grepafloxacin.Approved, Investigational, Withdrawn
FosamprenavirThe metabolism of Grepafloxacin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Grepafloxacin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Grepafloxacin can be increased when combined with Fosphenytoin.Approved, Investigational
Fusidic AcidThe serum concentration of Grepafloxacin can be increased when it is combined with Fusidic Acid.Approved, Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Grepafloxacin.Experimental
GliclazideGrepafloxacin may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideGrepafloxacin may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideGrepafloxacin may increase the hypoglycemic activities of Glipizide.Approved, Investigational
GlyburideGrepafloxacin may increase the hypoglycemic activities of Glyburide.Approved
GuacetisalGuacetisal may increase the neuroexcitatory activities of Grepafloxacin.Experimental
HalcinonideThe risk or severity of adverse effects can be increased when Halcinonide is combined with Grepafloxacin.Approved, Investigational, Withdrawn
HE3286The risk or severity of adverse effects can be increased when HE3286 is combined with Grepafloxacin.Investigational
HigenamineHigenamine may increase the neuroexcitatory activities of Grepafloxacin.Investigational
HydrocortisoneThe risk or severity of adverse effects can be increased when Hydrocortisone is combined with Grepafloxacin.Approved, Vet Approved
HydrotalciteHydrotalcite can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental, Investigational
IbuprofenIbuprofen may increase the neuroexcitatory activities of Grepafloxacin.Approved
IbuproxamIbuproxam may increase the neuroexcitatory activities of Grepafloxacin.Withdrawn
IcatibantIcatibant may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
IdelalisibThe metabolism of Grepafloxacin can be decreased when combined with Idelalisib.Approved
ImatinibThe metabolism of Grepafloxacin can be decreased when combined with Imatinib.Approved
Imidazole salicylateImidazole salicylate may increase the neuroexcitatory activities of Grepafloxacin.Experimental
IndinavirThe metabolism of Grepafloxacin can be decreased when combined with Indinavir.Approved
IndobufenIndobufen may increase the neuroexcitatory activities of Grepafloxacin.Investigational
IndomethacinIndomethacin may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
IndoprofenIndoprofen may increase the neuroexcitatory activities of Grepafloxacin.Withdrawn
Insulin AspartGrepafloxacin may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirGrepafloxacin may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineGrepafloxacin may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineGrepafloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanGrepafloxacin may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproGrepafloxacin may increase the hypoglycemic activities of Insulin Lispro.Approved
IronThe serum concentration of Grepafloxacin can be decreased when it is combined with Iron.Approved
Iron DextranThe serum concentration of Grepafloxacin can be decreased when it is combined with Iron Dextran.Approved, Vet Approved
Iron saccharateThe serum concentration of Grepafloxacin can be decreased when it is combined with Iron saccharate.Approved
IsavuconazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe metabolism of Grepafloxacin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsoxicamIsoxicam may increase the neuroexcitatory activities of Grepafloxacin.Withdrawn
IsradipineThe metabolism of Grepafloxacin can be decreased when combined with Isradipine.Approved, Investigational
IstaroximeThe risk or severity of adverse effects can be increased when Istaroxime is combined with Grepafloxacin.Investigational
ItraconazoleThe metabolism of Grepafloxacin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Grepafloxacin can be increased when it is combined with Ivacaftor.Approved
KebuzoneKebuzone may increase the neuroexcitatory activities of Grepafloxacin.Experimental
KetoconazoleThe metabolism of Grepafloxacin can be decreased when combined with Ketoconazole.Approved, Investigational
KetoprofenKetoprofen may increase the neuroexcitatory activities of Grepafloxacin.Approved, Vet Approved
KetorolacKetorolac may increase the neuroexcitatory activities of Grepafloxacin.Approved
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Grepafloxacin.Experimental
Lanthanum carbonateThe serum concentration of Grepafloxacin can be decreased when it is combined with Lanthanum carbonate.Approved
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Grepafloxacin.Approved
LeflunomideLeflunomide may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
LidocaineThe metabolism of Grepafloxacin can be decreased when combined with Lidocaine.Approved, Vet Approved
LiraglutideGrepafloxacin may increase the hypoglycemic activities of Liraglutide.Approved
LisofyllineLisofylline may increase the neuroexcitatory activities of Grepafloxacin.Investigational
LobeglitazoneThe metabolism of Grepafloxacin can be decreased when combined with Lobeglitazone.Approved, Investigational
LonazolacLonazolac may increase the neuroexcitatory activities of Grepafloxacin.Experimental
LopinavirThe metabolism of Grepafloxacin can be decreased when combined with Lopinavir.Approved
LornoxicamLornoxicam may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
LorpiprazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Lorpiprazole.Approved
LoteprednolThe risk or severity of adverse effects can be increased when Loteprednol is combined with Grepafloxacin.Approved
LovastatinThe metabolism of Grepafloxacin can be decreased when combined with Lovastatin.Approved, Investigational
LoxoprofenLoxoprofen may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
LuliconazoleThe serum concentration of Grepafloxacin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Grepafloxacin can be decreased when it is combined with Lumacaftor.Approved
LumiracoxibLumiracoxib may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
MacimorelinGrepafloxacin may increase the QTc-prolonging activities of Macimorelin.Approved, Investigational
MagaldrateMagaldrate can cause a decrease in the absorption of Grepafloxacin 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 Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium peroxideMagnesium peroxide can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Magnesium salicylateThe serum concentration of Grepafloxacin can be decreased when it is combined with Magnesium salicylate.Approved
Magnesium silicateMagnesium silicate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium sulfateThe serum concentration of Grepafloxacin can be decreased when it is combined with Magnesium sulfate.Approved, Investigational, Vet Approved
Magnesium TrisilicateMagnesium Trisilicate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
MasoprocolMasoprocol may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
ME-609The risk or severity of adverse effects can be increased when ME-609 is combined with Grepafloxacin.Investigational
MecaserminGrepafloxacin may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Meclofenamic acidMeclofenamic acid may increase the neuroexcitatory activities of Grepafloxacin.Approved, Vet Approved
MedrysoneThe risk or severity of adverse effects can be increased when Medrysone is combined with Grepafloxacin.Approved
Mefenamic acidMefenamic acid may increase the neuroexcitatory activities of Grepafloxacin.Approved
MelengestrolThe risk or severity of adverse effects can be increased when Melengestrol is combined with Grepafloxacin.Vet Approved
MeloxicamMeloxicam may increase the neuroexcitatory activities of Grepafloxacin.Approved, Vet Approved
MesalazineMesalazine may increase the neuroexcitatory activities of Grepafloxacin.Approved
MetamizoleMetamizole may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational, Withdrawn
MetforminGrepafloxacin may increase the hypoglycemic activities of Metformin.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Grepafloxacin.Approved, Vet Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Grepafloxacin.Experimental
MexiletineThe metabolism of Grepafloxacin can be decreased when combined with Mexiletine.Approved, Investigational
MidostaurinThe metabolism of Grepafloxacin can be decreased when combined with Midostaurin.Approved, Investigational
MifepristoneThe serum concentration of Grepafloxacin can be increased when it is combined with Mifepristone.Approved, Investigational
MiglitolGrepafloxacin may increase the hypoglycemic activities of Miglitol.Approved
MitotaneThe serum concentration of Grepafloxacin can be decreased when it is combined with Mitotane.Approved
MizoribineMizoribine may increase the neuroexcitatory activities of Grepafloxacin.Investigational
MofebutazoneMofebutazone may increase the neuroexcitatory activities of Grepafloxacin.Experimental
MometasoneThe risk or severity of adverse effects can be increased when Mometasone is combined with Grepafloxacin.Approved, Vet Approved
Mycophenolate mofetilMycophenolate mofetil may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
Mycophenolic acidThe serum concentration of Mycophenolic acid can be decreased when it is combined with Grepafloxacin.Approved
NabumetoneNabumetone may increase the neuroexcitatory activities of Grepafloxacin.Approved
NafamostatNafamostat may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
NaftifineNaftifine may increase the neuroexcitatory activities of Grepafloxacin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Grepafloxacin.Approved
NaproxenNaproxen may increase the neuroexcitatory activities of Grepafloxacin.Approved, Vet Approved
NateglinideGrepafloxacin 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 Grepafloxacin.Investigational
NefazodoneThe metabolism of Grepafloxacin can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Grepafloxacin can be decreased when combined with Nelfinavir.Approved
NepafenacNepafenac may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
NetupitantThe serum concentration of Grepafloxacin can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe metabolism of Grepafloxacin can be increased when combined with Nevirapine.Approved
NifenazoneNifenazone may increase the neuroexcitatory activities of Grepafloxacin.Experimental
Niflumic AcidNiflumic Acid may increase the neuroexcitatory activities of Grepafloxacin.Approved
NilotinibThe metabolism of Grepafloxacin can be decreased when combined with Nilotinib.Approved, Investigational
NimesulideNimesulide may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational, Withdrawn
NitroaspirinNitroaspirin may increase the neuroexcitatory activities of Grepafloxacin.Investigational
OlaparibThe metabolism of Grepafloxacin can be decreased when combined with Olaparib.Approved
OleandrinOleandrin may decrease the cardiotoxic activities of Grepafloxacin.Experimental, Investigational
Oleoyl-estroneThe risk or severity of adverse effects can be increased when Oleoyl-estrone is combined with Grepafloxacin.Investigational
OlopatadineOlopatadine may increase the neuroexcitatory activities of Grepafloxacin.Approved
OlsalazineOlsalazine may increase the neuroexcitatory activities of Grepafloxacin.Approved
OrgoteinOrgotein may increase the neuroexcitatory activities of Grepafloxacin.Vet Approved
OsimertinibThe serum concentration of Grepafloxacin can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Grepafloxacin.Approved
OxaprozinOxaprozin may increase the neuroexcitatory activities of Grepafloxacin.Approved
OxyphenbutazoneOxyphenbutazone may increase the neuroexcitatory activities of Grepafloxacin.Approved, Withdrawn
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Grepafloxacin.Approved, Vet Approved
PalbociclibThe serum concentration of Grepafloxacin can be increased when it is combined with Palbociclib.Approved, Investigational
ParamethasoneThe risk or severity of adverse effects can be increased when Paramethasone is combined with Grepafloxacin.Approved
ParecoxibParecoxib may increase the neuroexcitatory activities of Grepafloxacin.Approved
ParthenolideParthenolide may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Grepafloxacin.Approved
Peginterferon alfa-2bThe serum concentration of Grepafloxacin can be increased when it is combined with Peginterferon alfa-2b.Approved
PentamidineGrepafloxacin may increase the hypoglycemic activities of Pentamidine.Approved, Investigational
PentobarbitalThe metabolism of Grepafloxacin can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Grepafloxacin.Experimental
PhenindioneGrepafloxacin may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenobarbitalThe metabolism of Grepafloxacin can be increased when combined with Phenobarbital.Approved, Investigational
PhenprocoumonGrepafloxacin may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenylbutazonePhenylbutazone may increase the neuroexcitatory activities of Grepafloxacin.Approved, Vet Approved
PhenytoinThe metabolism of Grepafloxacin can be increased when combined with Phenytoin.Approved, Vet Approved
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Grepafloxacin.Approved
PimecrolimusPimecrolimus may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
PioglitazoneGrepafloxacin may increase the hypoglycemic activities of Pioglitazone.Approved, Investigational
PirfenidonePirfenidone may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
PiroxicamPiroxicam may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
PirprofenPirprofen may increase the neuroexcitatory activities of Grepafloxacin.Experimental
PitolisantThe serum concentration of Grepafloxacin can be decreased when it is combined with Pitolisant.Approved, Investigational
PosaconazoleThe metabolism of Grepafloxacin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PramlintideGrepafloxacin may increase the hypoglycemic activities of Pramlintide.Approved, Investigational
PranoprofenPranoprofen may increase the neuroexcitatory activities of Grepafloxacin.Experimental, Investigational
PrasteroneThe risk or severity of adverse effects can be increased when Prasterone is combined with Grepafloxacin.Approved, Investigational, Nutraceutical
Prasterone sulfateThe risk or severity of adverse effects can be increased when Prasterone sulfate is combined with Grepafloxacin.Investigational
PrednicarbateThe risk or severity of adverse effects can be increased when Prednicarbate is combined with Grepafloxacin.Approved, Investigational
PrednisoloneThe risk or severity of adverse effects can be increased when Prednisolone is combined with Grepafloxacin.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Prednisone is combined with Grepafloxacin.Approved, Vet Approved
PregnenoloneThe risk or severity of adverse effects can be increased when Pregnenolone is combined with Grepafloxacin.Approved, Experimental, Investigational
PrimidoneThe metabolism of Grepafloxacin can be increased when combined with Primidone.Approved, Vet Approved
ProbenecidThe serum concentration of Grepafloxacin can be increased when it is combined with Probenecid.Approved, Investigational
ProglumetacinProglumetacin may increase the neuroexcitatory activities of Grepafloxacin.Experimental
PropacetamolPropacetamol may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
PropyphenazonePropyphenazone may increase the neuroexcitatory activities of Grepafloxacin.Experimental
ProquazoneProquazone may increase the neuroexcitatory activities of Grepafloxacin.Experimental
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Grepafloxacin.Experimental
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Grepafloxacin.Approved
PTC299PTC299 may increase the neuroexcitatory activities of Grepafloxacin.Investigational
QuinaprilQuinapril can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Investigational
QuinineGrepafloxacin may increase the hypoglycemic activities of Quinine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Grepafloxacin.Approved, Investigational
RepaglinideGrepafloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
ResveratrolResveratrol may increase the neuroexcitatory activities of Grepafloxacin.Approved, Experimental, Investigational
RibociclibThe risk or severity of QTc prolongation can be increased when Ribociclib is combined with Grepafloxacin.Approved, Investigational
RifabutinThe metabolism of Grepafloxacin can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Grepafloxacin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Grepafloxacin can be increased when combined with Rifapentine.Approved, Investigational
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Grepafloxacin.Approved, Investigational
RimexoloneThe risk or severity of adverse effects can be increased when Rimexolone is combined with Grepafloxacin.Approved
RofecoxibRofecoxib may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational, Withdrawn
RopiniroleThe metabolism of Grepafloxacin can be decreased when combined with Ropinirole.Approved, Investigational
RosiglitazoneGrepafloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
RucaparibThe metabolism of Grepafloxacin can be decreased when combined with Rucaparib.Approved, Investigational
SalicylamideSalicylamide may increase the neuroexcitatory activities of Grepafloxacin.Approved
Salicylic acidSalicylic acid may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational, Vet Approved
SalsalateSalsalate may increase the neuroexcitatory activities of Grepafloxacin.Approved
SaquinavirThe metabolism of Grepafloxacin can be decreased when combined with Saquinavir.Approved, Investigational
SarilumabThe therapeutic efficacy of Grepafloxacin can be decreased when used in combination with Sarilumab.Approved, Investigational
SaxagliptinGrepafloxacin may increase the hypoglycemic activities of Saxagliptin.Approved
SemapimodSemapimod may increase the neuroexcitatory activities of Grepafloxacin.Investigational
SeratrodastSeratrodast may increase the neuroexcitatory activities of Grepafloxacin.Approved
SerrapeptaseSerrapeptase may increase the neuroexcitatory activities of Grepafloxacin.Investigational
SevelamerSevelamer can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
SildenafilThe metabolism of Grepafloxacin can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Grepafloxacin.Approved
SiltuximabThe serum concentration of Grepafloxacin can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Grepafloxacin can be increased when it is combined with Simeprevir.Approved
SitagliptinGrepafloxacin may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
Sodium bicarbonateSodium bicarbonate can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
SRT501SRT501 may increase the neuroexcitatory activities of Grepafloxacin.Investigational
St. John's WortThe serum concentration of Grepafloxacin can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Grepafloxacin can be increased when it is combined with Stiripentol.Approved
Strontium ranelateThe serum concentration of Grepafloxacin can be decreased when it is combined with Strontium ranelate.Approved, Withdrawn
SucralfateThe serum concentration of Grepafloxacin can be decreased when it is combined with Sucralfate.Approved
SulfadiazineGrepafloxacin may increase the hypoglycemic activities of Sulfadiazine.Approved, Investigational, Vet Approved
SulfamethoxazoleGrepafloxacin may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfasalazineSulfasalazine may increase the neuroexcitatory activities of Grepafloxacin.Approved
SulfisoxazoleThe metabolism of Grepafloxacin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulindacSulindac may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
SunitinibGrepafloxacin may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
SuprofenSuprofen may increase the neuroexcitatory activities of Grepafloxacin.Approved, Withdrawn
SuxibuzoneSuxibuzone may increase the neuroexcitatory activities of Grepafloxacin.Experimental
TarenflurbilTarenflurbil may increase the neuroexcitatory activities of Grepafloxacin.Investigational
TelaprevirThe metabolism of Grepafloxacin can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Grepafloxacin can be decreased when combined with Telithromycin.Approved
TenidapTenidap may increase the neuroexcitatory activities of Grepafloxacin.Experimental
Tenofovir disoproxilThe metabolism of Grepafloxacin can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TenoxicamTenoxicam may increase the neuroexcitatory activities of Grepafloxacin.Approved
TepoxalinTepoxalin may increase the neuroexcitatory activities of Grepafloxacin.Vet Approved
TeriflunomideThe serum concentration of Grepafloxacin can be increased when it is combined with Teriflunomide.Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Grepafloxacin.Approved
Tiaprofenic acidTiaprofenic acid may increase the neuroexcitatory activities of Grepafloxacin.Approved
TiclopidineThe metabolism of Grepafloxacin can be decreased when combined with Ticlopidine.Approved
TinoridineTinoridine may increase the neuroexcitatory activities of Grepafloxacin.Investigational
TioclomarolGrepafloxacin may increase the anticoagulant activities of Tioclomarol.Experimental
TixocortolThe risk or severity of adverse effects can be increased when Tixocortol is combined with Grepafloxacin.Approved, Withdrawn
TocilizumabThe serum concentration of Grepafloxacin can be decreased when it is combined with Tocilizumab.Approved
TolazamideGrepafloxacin may increase the hypoglycemic activities of Tolazamide.Approved, Investigational
TolbutamideGrepafloxacin may increase the hypoglycemic activities of Tolbutamide.Approved, Investigational
Tolfenamic AcidTolfenamic Acid may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
TolmetinTolmetin may increase the neuroexcitatory activities of Grepafloxacin.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Grepafloxacin.Approved, Investigational
TranilastTranilast may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Grepafloxacin.Approved, Investigational
TriamcinoloneThe risk or severity of adverse effects can be increased when Triamcinolone is combined with Grepafloxacin.Approved, Vet Approved
TribenosideTribenoside may increase the neuroexcitatory activities of Grepafloxacin.Experimental
TriptolideTriptolide may increase the neuroexcitatory activities of Grepafloxacin.Investigational
TromethamineTromethamine can cause a decrease in the absorption of Grepafloxacin 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 Grepafloxacin.Approved
ValdecoxibValdecoxib may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational, Withdrawn
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Grepafloxacin.Approved, Investigational
VemurafenibThe risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Grepafloxacin.Approved
VenlafaxineThe metabolism of Grepafloxacin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Grepafloxacin can be decreased when combined with Verapamil.Approved
VincristineThe excretion of Vincristine can be decreased when combined with Grepafloxacin.Approved, Investigational
VoriconazoleThe metabolism of Grepafloxacin can be decreased when combined with Voriconazole.Approved, Investigational
WarfarinGrepafloxacin may increase the anticoagulant activities of Warfarin.Approved
ZaltoprofenZaltoprofen may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational
ZileutonZileuton may increase the neuroexcitatory activities of Grepafloxacin.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Grepafloxacin can be decreased when combined with Ziprasidone.Approved
ZomepiracZomepirac may increase the neuroexcitatory activities of Grepafloxacin.Withdrawn
ZucapsaicinThe metabolism of Grepafloxacin can be decreased when combined with Zucapsaicin.Approved, Investigational
Food Interactions
  • Drink liberally but avoid coffee.
  • Take without regard to meals.

References

Synthesis Reference
US4920120
General References
Not Available
External Links
Human Metabolome Database
HMDB0014509
KEGG Compound
C11368
PubChem Compound
72474
PubChem Substance
46507253
ChemSpider
65391
BindingDB
50117924
ChEBI
5543
ChEMBL
CHEMBL583
Therapeutic Targets Database
DAP001005
PharmGKB
PA449812
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Grepafloxacin
ATC Codes
J01MA11 — Grepafloxacin
MSDS
Download (115 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingTreatmentOsteomyelitis1

Pharmacoeconomics

Manufacturers
  • Otsuka pharmaceutical co ltd
Packagers
  • GlaxoSmithKline Inc.
Dosage forms
FormRouteStrength
TabletOral200 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5563138No1993-10-082013-10-08Us
CA1340492No1999-04-132016-04-13Canada

Properties

State
Solid
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

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

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
Fluoroquinolones / N-arylpiperazines / Haloquinolines / Hydroquinolones / Aminoquinolines and derivatives / Hydroquinolines / Pyridinecarboxylic acids / Dialkylarylamines / Benzenoids / Aryl fluorides
show 12 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 29 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
quinolines, quinolone antibiotic, fluoroquinolone antibiotic (CHEBI:5543)

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, 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. 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
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. 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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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
Substrate
Inhibitor
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
Uniprot Name
Multidrug resistance protein 1
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, methotre...
Gene Name
ABCC1
Uniprot ID
P33527
Uniprot Name
Multidrug resistance-associated protein 1
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 ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
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, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
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 cat...
Gene Name
SLC22A5
Uniprot ID
O76082
Uniprot Name
Solute carrier family 22 member 5
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
Uniprot Name
Canalicular multispecific organic anion transporter 1
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]

Drug created on June 13, 2005 07:24 / Updated on May 02, 2018 01:21