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Drug

D0125 | Trovafloxacin

Molecular Formula C20H15F3N4O3
Molecular Weight 416.4
Structure
State solid
Route of elimination Approximately 50% of an oral dose is excreted unchanged (43% in the feces and 6% in the urine).
Protein binding The mean plasma protein bound fraction is approximately 76%, and is concentration-independent.
Half life Following oral administration, half-life ranged from 9.1 hours to 12.2 hours over the dosage range of 100 to 200 mg tablets. Following intravenous infusion, half-life ranged from 9.4 to 12.7 hours over a dosage range of 100 to 300 mg.
Absorption Well-absorbed from the gastrointestinal tract after oral administration and does not depend on concomitant food intake. The absolute bioavailability is approximately 88%.

J

J01MA13 Trovafloxacin


[J01MA] Fluoroquinolones


[J01M] QUINOLONE ANTIBACTERIALS


[J01] ANTIBACTERIALS FOR SYSTEMIC USE


[J] Antiinfectives for systemic use

Toxicity Dose Time Species Model Method Action Positive criterion Reference
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex I activity Negative p < 0.05 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex II + III activity Negative p < 0.05 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex II + III activity Negative p < 0.05 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex IV activity Negative p < 0.05 3
ELECTRON TRANSPORT CHAIN 50 μM bovine heart mitochondria Measurement of complex V activity Negative p < 0.05 3

Target Dose Time Species Model Method Action Positive criterion Reference
NADH:ubiquinone reductase 50 μM bovine heart mitochondria Measurement of complex I activity Negative p < 0.05 3
Succinate dehydrogenase 50 μM bovine heart mitochondria Measurement of complex II + III activity Negative p < 0.05 3
Quinol--cytochrome-c reductase 50 μM bovine heart mitochondria Measurement of complex II + III activity Negative p < 0.05 3
Cytochrome c oxidase 50 μM bovine heart mitochondria Measurement of complex IV activity Negative p < 0.05 3
ATP synthase 50 μM bovine heart mitochondria Measurement of complex V activity Negative p < 0.05 3

Organism Test type Route Dose (normalized dose) Effect Source
man TDLo intravenous 7mg/kg/2D-I (7mg/kg) blood: change in clotting factors Annals of Internal Medicine. Vol. 131, Pg. 72, 1999.
women TDLo intravenous 12mg/kg/3D-I (12mg/kg) blood: change in clotting factors Annals of Internal Medicine. Vol. 131, Pg. 72, 1999.
man TDLo oral 40mg/kg/4W-I (40mg/kg) New England Journal of Medicine. Vol. 342, Pg. 359, 2000.

  • Abdominal infection

  • Abortion infected

  • Diabetic foot infection

  • Endometritis

  • Infection

  • Osteomyelitis

  • Parametritis

  • Pelvic infection

  • Dermatitis (0.02)

  • Vaginal inflammation (0.02)

  • Abdominal pain

  • Dizziness

  • Gastrointestinal pain

  • Headache

  • Nausea

  • Vomiting

    • (1alpha,5alpha,6alpha)-7-(6-Amino-3-azabicyclo[3.1.0]hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid 1,8-Naphthyridine-3-carboxylic acid, 1,4-dihydro-7-(6-amino-3-azabicyclo(3.1.0)hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-, (1-alpha,5-alpha,6-alpha)- 1,8-Naphthyridine-3-carboxylic acid, 7-(6-amino-3-azabicyclo[3.1.0]hex-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-, (1alpha,5alpha,6alpha)-
    1,8-Naphthyridine-3-carboxylic acid, 7-[(1alpha,5alpha,6alpha)-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-, methanesulfonate (1:1) 147059-72-1 7-((1R,5S)-6-Amino-3-aza-bicyclo[3.1.0]hex-3-yl)-1-(2,4-difluoro-phenyl)-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid
    7-((1R,5S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid 7-((1R,5S,6S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl)-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid 7-[(1R,5S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
    7-[(1R,5S,6s)-6-Amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid 7-[(1R,5S,6s)-6-amino-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid 7-[(1S,5R)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid
    7-[(1alpha,5alpha)-6beta-Amino-3-azabicyclo[3.1.0]hexane-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid 9F388J00UK AKOS000277872
    AKOS015909896 API0004697 BCP12644
    C-22002 C07664 C20H15F3N4O3
    CC-35528 CHEBI:9763 CHEMBL428
    CP-99,219 CP99219 CTK4C5244
    D08654 DB00685 DTXSID0041145
    EX-A897 FT-0601549 Fluorinated quinolone
    LS-95890 Q544393 SC-47970
    SCHEMBL34465 SCHEMBL34466 SCHEMBL9177464
    TR6 TVFX Trovafloxacin
    Trovafloxacin (INN) Trovafloxacin [INN] Trovan (oral)
    UNII-9F388J00UK WVPSKSLAZQPAKQ-CDMJZVDBSA-N ZINC100030989
    ZINC12503149 ZINC147175374 trovafloxacine
    trovafloxacino trovafloxacinum

    DrugBank Name Trovafloxacin
    DrugBank DB00685
    CAS Number 146836-84-2, 147059-72-1, 147059-75-4
    PubChem Compound 62959
    KEGG Compound ID C07664
    KEGG Drug D08654
    PubChem.Substance 46508751
    ChEBI 9763
    PharmGKB PA164749184
    ChemSpider 16736478
    BindingDB 50146361.0
    TTD DAP000652
    Wikipedia Trovafloxacin
    HET TR6
    DPD 11817