Trovafloxacin

416.35

416.35

9F388J00UK

DTXSID0041145

J01MA13|J - Antiinfectives for systemic use

99.8

3.7

Solid

1.612±0.06 g/cm3(Predicted)

246ºC

630.5±55.0 °C(Predicted)

335.1ºC

1.672

7.04e-02 g/L

Symptoms of overdose include convulsions, decreased activity, diarrhea, sleepiness, tremors, and/or vomiting.

The mean plasma protein bound fraction is approximately 76%, and is concentration-independent.

For treatment of infections caused by susceptible strains of the designated microorganisms in uncomplicated urethral gonorrhea in males and endocervical and rectal gonorrhea in females caused by Neisseria gonorrhoeae as well as non gonoccocal urethritis and cervicitis due to Chlamydia trachomatis.|Trovafloxacin is a synthetic broad spectrum quinolone antibacterial agent indicated for the treatment of the following infections in adults:Pneumonia: Community Acquired Pneumonia and Nosocomial Pneumonia (mild, moderate, and severe).Note: Efficacy in patients with very severe nosocomial pneumonia and in particular infections due to less susceptible pathogens e.g. P. aeruginosa, has not been established. See also section 4.2.Acute Exacerbations of Chronic BronchitisAcute SinusitisComplicated Intra-abdominal Infections and Acute Pelvic InfectionsSalpingitisUncomplicated Gonococcal Urethritis and CervicitisChlamydial CervicitisComplicated Skin and Soft Tissue InfectionsConsideration should be given to official guidance on the appropriate use of antibacterial agents.|Trovafloxacin is a synthetic broad spectrum quinolone antibacterial agent indicated for the treatment of the following infections in adults:Pneumonia:Community Acquired Pneumonia and Nosocomial Pneumonia (mild, moderate, and severe).Note: Efficacy in patients with very severe nosocomial pneumonia and in particular infections due to less susceptible pathogens e.g. P. aeruginosa, has not been established. See also section 4.2.Acute Exacerbations of Chronic BronchitisAcute SinusitisComplicated Intra-abdominal Infections and Acute Pelvic InfectionsSalpingitisUncomplicated Gonococcal Urethritis and CervicitisChlamydial CervicitisComplicated Skin and Soft Tissue InfectionsConsideration should be given to official guidance on the appropriate use of antibacterial agents.

Trovafloxacin is a broad spectrum antibiotic that inhibits DNA supercoiling in various bacteria by blocking the activity of DNA gyrase and topoisomerase IV. It is not used widely due to the risk of hepatotoxicity. It tends to have better gram-positive bacterial coverage and less gram-negative coverage than the previous fluoroquinolones. Mechanism of action of fluoroquinolones including trovafloxacin is different from that of penicillins, cephalosporins, aminoglycosides, macrolides, and tetracyclines. Therefore fluoroquinolones may be active against pathogens that are resistant to these antibiotics. There is no cross-resistance between trovafloxacin and the mentioned classes of antibiotics. The overall results obtained from in vitro synergy studies, testing combinations of trovafloxacin with beta-lactams and aminoglycosides, indicate that synergy is strain specific and not commonly encountered. This agrees with results obtained previously with other fluoroquinolones. Resistance to trovafloxacin in vitro develops slowly via multiple-step mutation in a manner similar to other fluoroquinolones. Resistance to trovafloxacin in vitro occurs at a general frequency of between 1x10^-7 to 10^-10. Although cross-resistance has been observed between trovafloxacin and some other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to trovafloxacin.

Compounds that inhibit the activity of DNA TOPOISOMERASE II. Included in this category are a variety of ANTINEOPLASTIC AGENTS which target the eukaryotic form of topoisomerase II and ANTIBACTERIAL AGENTS which target the prokaryotic form of topoisomerase II. (See all compounds classified as Topoisomerase II Inhibitors.)|Substances that prevent infectious agents or organisms from spreading or kill infectious agents in order to prevent the spread of infection. (See all compounds classified as Anti-Infective Agents.)

Well-absorbed from the gastrointestinal tract after oral administration and does not depend on concomitant food intake. The absolute bioavailability is approximately 88%.|Approximately 50% of an oral dose is excreted unchanged (43% in the feces and 6% in the urine).

Metabolism Trovafloxacin is metabolized by conjugation (the role of cytochrome P450 oxidative metabolism of trovafloxacin is minimal). The major metabolites include the ester glucuronide, which appears in the urine (13% of the administered dose); and the N -acetyl metabolite, which appears in the feces and serum (9% and 2.5% of the administered dose, respectively). Other minor metabolites include diacid, hydroxycarboxylic acid, and sulfamate, which have been identified in both the feces and the urine in small amounts (< 4% of the administered dose).|Trovafloxacin has known human metabolites that include (2S,3S,4S,5R)-6-[7-[(1R,5S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,8-naphthyridine-3-carbonyl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid.

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.

Trovafloxacin is a fluoronaphthyridone related to the fluoroquinolones with in vitro activity against a wide range of gram-negative and gram-positive aerobic and anaerobic microorganisms. The bactericidal action of trovafloxacin results from inhibition of DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription, and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.

CP 99,219

Human drugs -> Turvel -> EMA Drug Category|Antibacterials for systemic use -> Human pharmacotherapeutic group|Human drugs -> Turvel IV -> EMA Drug Category|Human drugs -> Trovan IV -> EMA Drug Category|Human drugs -> Trovan -> EMA Drug Category|Pharmaceuticals