gemifloxacin and sparfloxacin

The pharmaceutical industry of Pakistan is growing with an annual growth rate of 10%. Besides this growth, this industry is not complying with environmental standards, and discharging its effluent into domestic wastewater network. Only limited information is available about the occurrence of pharmaceutical compounds (PCs) in the environmental matrices of Pakistan that has motivated us to aim at the occurrence and ecological risk assessment of 11 PCs of different therapeutic classes in the wastewater of pharmaceutical industry and in its receiving environmental matrices such as sludge, solid waste and soil samples near the pharmaceutical formulation units along Shiekhupura road, Lahore, Pakistan. Target PCs (paracetamol, naproxen, diclofenac, ibuprofen, amlodipine, rosuvastatin, ofloxacin, ciprofloxacin, moxifloxacin, sparfloxacin and gemifloxacin) were quantified using in-house developed HPLC-UV. Ibuprofen (1673µg/L, 6046µg/kg, 1229µg/kg and 610µg/kg), diclofenac (836µg/L, 4968µg/kg, 6632µg/kg and 257µg/kg) and naproxen (464µg/L, 7273µg/kg, 4819µg/kg and 199µg/kg) showed the highest concentrations among 11 target PCs in wastewater, sludge, solid waste and soil samples, respectively. Ecological risk assessment, in terms of risk quotient (RQ), was also carried out based on the maximum measured concentration of PCs in wastewater. The maximum RQ values obtained were with paracetamol (64 against daphnia), naproxen (177 against fish), diclofenac (12,600 against Oncorhynchus mykiss), ibuprofen (167,300 against Oryzias latipes), ofloxacin (81,000 against Pseudomonas putida) and ciprofloxacin (440 against Microcystis aeruginosa). These results show a high level of ecological risk due to the discharge of untreated wastewater from pharmaceutical units. This risk may further lead to food web contamination and drug resistance in pathogens. Thus, further studies are needed to detect the PCs in crops as well as the government should strictly enforce environmental legislation on these pharmaceutical units.

Topics: Animals; Diclofenac; Ecology; Environmental Monitoring; Fishes; Fluoroquinolones; Gemifloxacin; Ibuprofen; Moxifloxacin; Naphthyridines; Pakistan; Risk Assessment; Sewage; Wastewater; Water Pollutants, Chemical

The in vitro activity of gemifloxacin against 316 bloodstream isolates of staphylococci, pneumococci, and enterococci was compared with the activities of six fluoroquinolones and three other antimicrobial agents. Of the antimicrobial agents tested, gemifloxacin was the most potent against penicillin-intermediate and -resistant pneumococci, methicillin-susceptible and -resistant Staphylococcus epidermidis isolates, and coagulase-negative staphylococci.

Topics: Anti-Bacterial Agents; Anti-Infective Agents; Aza Compounds; Bacteremia; Ciprofloxacin; Fluoroquinolones; Gemifloxacin; Gram-Positive Bacterial Infections; Gram-Positive Cocci; Humans; Microbial Sensitivity Tests; Moxifloxacin; Naphthyridines; Ofloxacin; Piperazines; Quinolines

Antimicrobial activity of gemifloxacin (SB-265805), a newly developed fluoroquinolone, to Japanese isolates of Neisseria gonorrhoeae was compared with those of various fluoroquinolones, including norfloxacin, ciprofloxacin, tosufloxacin, levofloxacin, sparfloxacin, and trovafloxacin. Among the fluoroquinolones tested, gemifloxacin was most active against N. gonorrhoeae isolates. The MIC90 values of gemifloxacin for 94 N. gonorrhoeae isolated from 1992 through 1993 and 100 isolated from 1996 through 1997 were 0.03 and 0.125 microg/ml, respectively. On the other hand, MIC90 values of the other fluoroquinolone for the 1992-1993 isolates and the 1996-1997 isolates ranged from 0.125 to 2 microg/ml and from 0.5 to 8 microg/ml, respectively. Gemifloxacin was also the most potent fluoroquinolone against 31 ciprofloxacin-resistant isolates with the ciprofloxacin MIC of 1 to 16 microg/ml, for which the gemifloxacin MIC50 and MIC90 values were 0.25 and 2 microg/ml, respectively. Moreover, the activity of gemifloxacin against fluoroquinolone-resistant gonococcal isolates containing multiple amino acid substitutions in both GyrA and ParC proteins was superior to those of the other compounds.

Topics: Amoxicillin; Anti-Infective Agents; Ciprofloxacin; Clavulanic Acid; Drug Resistance, Microbial; Fluoroquinolones; Gemifloxacin; Gonorrhea; Humans; Levofloxacin; Naphthyridines; Neisseria gonorrhoeae; Norfloxacin; Ofloxacin