Trovafloxacin Mesilate

(rINNM)
Trovafloxacin Mesilate Chemical formula
Synonyms: CP-99219-27; CP-99219 (trovafloxacin); Mesilato de trovafloxacino; Trovafloxacin Mesylate Trovafloxacini Mesilas. 7-[(1R,5S,6S)-6-Amino-3-azabicyclo[3.1.0]hex-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-1,4-dihydro-4oxo-1,8-naphthyridine-3-carboxylic acid monomethanesulphonate.
Cyrillic synonym: Тровафлоксацина Мезилат.

💊 Chemical information

Chemical formula: C20H15F3N4O3,CH4O3S = 512.5.
CAS — 147059-72-1 (trovafloxacin); 147059-75-4 (trovafloxacin mesilate).
ATC — J01MA13.
ATC Vet — QJ01MA13.

💊 Adverse Effects and Precautions

As for Ciprofloxacin. Dizziness was the most common adverse effect reported with trovafloxacin. Trovafloxacin preparations have been withdrawn worldwide after reports of unpredictable severe hepatic adverse effects, including some fatalities. Symptomatic pancreatitis was also reported.

💊 Antimicrobial Action

As for Ciprofloxacin. It is more active against pneumococci.

💊 Pharmacokinetics

Trovafloxacin is readily absorbed from the gastrointestinal tract after an oral dose, peak plasma concentrations occurring after about 1 to 2 hours. After intravenous use, alatrofloxacin is rapidly converted to trovafloxacin. Oral bioavailability is 88%. Trovafloxacin is widely distributed into body tissues and is about 76% bound to plasma proteins. It appears in breast milk. The serum half-life of trovafloxacin ranges from about 9 to 12 hours. Trovafloxacin is metabolised by conjugation, 13% of a dose appearing in the urine as the glucuronide and 9% in the faeces as the N-acetyl metabolite; other metabolites appear in both the urine and faeces in minor amounts, but about 50% of an oral dose is excreted unchanged, mainly in the faeces but also in the urine.

💊 Uses and Administration

Trovafloxacin is a fluoroquinolone antibacterial with actions and uses similar to those of ciprofloxacin. It was given orally as the mesilate for the treatment of susceptible infections. The prodrug alatrofloxacin was used as the mesilate for intravenous infusion. Trovafloxacin and alatrofloxacin preparations have been withdrawn worldwide after reports of unpredictable severe hepatic adverse effects, including some fatalities.

💊 Preparations

Proprietary Preparations

Canad.: Trovan†; Gr.: Trovan†; Mex.: Trovan†; USA: Trovan†.
Published May 08, 2019.