The first generation is rarely used today. Nalidixic acid was added to the OEHHA Prop 65 list as a carcinogen on 15 May 1998. A number of the second-, third-, and fourth-generation drugs have been removed from clinical practice due to severe toxicity issues or discontinued by their manufacturers.
The drugs most frequently prescribed today consist of Avelox (moxifloxacin), Cipro (ciprofloxacin), Levaquin (levofloxacin), and, to some extent, their generic equivalents.
- cinoxacin (Cinobac) (discontinued by manufacturer)
- nalidixic acid (NegGram, Wintomylon)
- oxolinic acid (Uroxin)
- piromidic acid (Panacid)
- pipemidic acid (Dolcol)
- rosoxacin (Eradacil)
The second-generation class is sometimes subdivided into “Class 1” and “Class 2”.
- ciprofloxacin (Alcipro,Ciprobay, Cipro, Ciproxin, ultracipro)
- enoxacin (Enroxil, Penetrex)
- fleroxacin (Megalone, Roquinol)
- lomefloxacin (Maxaquin)
- nadifloxacin (Acuatim, Nadoxin, Nadixa)
- norfloxacin (Lexinor, Noroxin, Quinabic, Janacin)
- ofloxacin (Floxin, Oxaldin, Tarivid)
- pefloxacin (Peflacine)
- rufloxacin (Uroflox)
Unlike the first- and second-generations, the third-generation is active against streptococci.
- balofloxacin (Baloxin)
- grepafloxacin (Raxar) (removed from clinical use)
- levofloxacin (Cravit, Levaquin, Tavanic)
- pazufloxacin (Pasil, Pazucross)
- sparfloxacin (Zagam)
- temafloxacin (Omniflox) (removed from clinical use)
- tosufloxacin (Ozex, Tosacin)
Fourth-generation fluoroquinolones act at DNA gyrase and topoisomerase IV. This dual action slows development of resistance.
- gatifloxacin (Zigat, Tequin) (Zymar -opth.) (Tequin removed from clinical use)
- gemifloxacin (Factive)
- moxifloxacin (Acflox Woodward, Avelox,Vigamox)
- sitafloxacin (Gracevit)
- trovafloxacin (Trovan) (removed from clinical use)
- prulifloxacin (Quisnon)
- delafloxacin — an anionic fluoroquinoline in clinical trials
- JNJ-Q2 — completed Phase II for MRSA
The quinolones have been widely used in agriculture, and several agents have veterinary, but not human, applications.
- danofloxacin (Advocin, Advocid) (for veterinary use)
- difloxacin (Dicural, Vetequinon) (for veterinary use)
- enrofloxacin (Baytril) (for veterinary use)
- ibafloxacin (Ibaflin) (for veterinary use)
- marbofloxacin (Marbocyl, Zenequin) (for veterinary use)
- orbifloxacin (Orbax, Victas) (for veterinary use)
- sarafloxacin (Floxasol, Saraflox, Sarafin) (for veterinary use)