Ciprofloxacin studies

The complexation of 6, ciprofloxacin, and lomefloxacin with metals ions were studied in aqueous solution (pD 2.5 37 °C) by and NMR spectroscopy (99MI18). Titration experiments have revealed that the binding ability of 6 towards Al " " ion is much stronger than that of ciprofloxacin and lomefloxacin. Other metal ions (Ca " " and Mg " ") formed much weaker complexes. 

The results showed that the compounds studied with more frequency in the aquatic environment, and of which, logically, there is more information, are the antibiotics, analgesics and anti-inflammatories (like diclofenac, ibuprofen, naproxen, acetylsalicylic acid, and paracetamol), as well as the p-blocker atenolol. In the category of antibiotics, several families are included, like the macrolides (erythromycin), the fluoroquinolones (ofloxacin and ciprofloxacin), sulfonamides (sulfamethoxazole), penicillins (amoxicillin), the metronidazol, and trimethoprim. Other therapeutic groups also widely studied and frequently found in the environmental waters are the lipid regulators (gemfibrozil and bezafibrat), antiepileptic carbamaze-pine, and antidepressants (diazepam, fluoxetine, paroxetine) (see Table 3). 

Antibiotics have been studied based on the rationale that they may interrupt the inflammatory response directed against endogenous bacterial flora. Metronidazole and ciprofloxacin have been the two most widely-studied agents.32 Metronidazole may benefit some patients with pouchitis (inflammation of surgically-created intestinal pouches) and patients with CD who have had ileal resection or have perianal fistulas. Ciprofloxacin has shown some efficacy in refractory active CD. Both drugs may cause diarrhea, and long-term use of metronidazole is associated with the development of peripheral neuropathy. 

Absorption of antimicrobial agents such as fluoroquinolones and tetracyclines that can be bound by divalent and trivalent cations potentially could be compromised by administration with EN formulas containing these cations. The fluoroquinolones (e.g., levofloxacin and ciprofloxacin) have been best studied in this regard, and results of studies are not consistent. Mechanisms for an interaction between fluoroquinolones and EN formulas other than chelation by cations have been postulated.40 Some institutions hold tube feedings for 30 to 60 minutes or more before and after enteral dosages of fluoroquinolones. Because ciprofloxacin absorption has been shown to be decreased with jejunal administration, this drug probably should not be given by jejunal tube.41... 

In a recent study, Walters et al. [141] described the occurrence and loss of several PhC from biosolid-soil mixtures exposed at ambient outdoor conditions for 3 years. Some compounds showed no detectable loss over the monitoring period, including diphenhydramine, fluoxetine, thiabendazole and triclosan, while half-life estimates ranging from 182 to 3,466 days were determined for others such as azithromycin, carbamazepine, ciprofloxacin, doxycycline, tetracycline, 4-epitetracycline, gemfibrozil, norfloxacin and triclosan. These findings highlight the potential use of T. versicolor to reduce the impact of biosolids once released to the environment, which could reduce the concentrations of PhC in much shorter periods of treatment. 

Ciprofloxacin has been tested in a randomized, place-bo-controlled study 70 patients with mildly to moderately active UC were randomized to receive ciprofloxacin 250 mg b.i.d. or placebo for 14 days. At the end of the study, 70.5% of patients in the ciprofloxacin group versus 72% in the placebo group showed an improvement [31], Nevertheless, in a more recent randomized, placebo-controlled trial, ciprofloxacin was administered for 6 months to patients with active UC poorly responding to conventional therapy with steroids and mesalazine. At the end of the study, the treatment failure rate was 21% in the ciprofloxacin-treated group and 44% in the placebo group (p < 0.002). Also endoscopic and histological evaluation showed a better improvement in the ciprofloxacin group [32],... 

Ciprofloxacin has an excellent activity against enteric pathogens and Gram-negative Enterobacteriaceae associated with immunosuppressive properties. Ciprofloxacin 1 g/daily was compared to mesalazine 4 g/daily in a controlled study in mildly to moderately active CD. After 6 weeks an equivalence in efficacy was registered, offering an alternative treatment in active CD [39],... 

In a small study ciprofloxacin was shown to be effective in association with standard treatment in patients with resistant disease [40], The results of this study were challenged by a controlled study in which ciprofloxacin (1 g/day) was associated with budesonide (9 mg/day) in ileocolic active CD. No difference was found compared to placebo, but surprisingly the overall response in both groups was lower than that reported in previous studies with budesonide [41],... 

Turunen UM, Farkkila MA, Hakala K, Seppala K, Sivonen A, Ogren M, Vuoristo M, Valtonen VV, Miettinen TA Long-term treatment of ulcerative colitis with ciprofloxacin A prospective, double-blind, placebo-controlled study. Gastroenterology 1998 115 1072-1078. 

Arnold GL, Beaves MR, Prydun VO, Mook WJ Preliminary study of ciprofloxacin in active Crohn s disease. Inflamm Bowel Dis 2002 8 10-15. 

Surprisingly, in the light of the results of studies such as those described above, the 1-t-butyl analogues (36) exhibit excellent antibacterial properties [83], The results for the in vitro evaluation of these agents relative to ciprofloxacin are shown in Table 6.14. Compound (36a), the 1-/-butyl analogue of... 

In a study aimed at examining both the electronic influence of attaching a phenyl ring to the cyclopropyl ring of ciprofloxacin and the tolerance to this added steric bulk, the enantiomeric fraiu-disubstituted cyclopropane analogues (60) and (61) were prepared [94]. In general, the (1 S,2R)-enantiomer (61) is... 

Maurer N, Wong KF, Hope MJ, Cullis PR. Anomalous solubility behavior of the antibiotic ciprofloxacin encapsulated in liposomes a IH-NMR study. Biochim Biophys Acta 1998 1374 9. 

Turiel E, Bordin G, Rodriguez AR (2005) Study of the evolution and degradation products of ciprofloxacin and oxolinic acid in river water samples by HPLC-UV/MS/MS-MS. J Environ Monit 7 189-195... 

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