Fluoroquinolones ofloxacin

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). 

Among fluoroquinolones, ofloxacin, pefloxacin and sparfloxacin can be used in alternative regimen, when drugs like rifampicin can not be used. Detailed pharmacology of quinolones is discussed in chapter Sulfonamides, nitrofurans and quinolones. ... 

Csem iczky G, Alvendal C, Landgren B-M. Risk for ovulation in women taking a low-dose oal contraceptive (Micrc ynon) when receiving antibacterial treatment with a fluoroquinolone (ofloxacin). A Crmtraceja (1996) 12,101-9. 

Ce(IV)/sulfite Fluoroquinolones (ofloxacin norfloxacin ciprofloxacin lomefloxacin) (Ph) benzamides (sulpiride sultopride tiapride) (Ph and BF) ofloxacin (Ph). 

Tris(2,2 -bipyridyl) Fluoroquinolone (ofloxacin, norfloxacin, ciprofloxacin) (Ph) thioxanthenes... 

The fluoroquinolones include ciprofloxacin (Cipro), enoxacin (Penetrex), gatifloxacin (Tequin), lome-floxacin (Maxaquin), moxifloxacin (Avelox), ofloxacin (Floxin), and sparfloxacin (Zagain). 

The fluoroquinolones are used in the treatment of infections caused by susceptible microorganisms. The fluoroquinolones are effective in the treatment of infections caused by gram-positive and gram-negative microorganisms. They are primarily used in the treatment of susceptible microorganisms in lower respiratory infections, infections of the skin, urinary tract infections, and sexually transmitted diseases. Ciprofloxacin, norfloxacin, and ofloxacin are available in ophthalmic forms for infections in the eyes. 

Ciprofloxacin, gatifloxacin, and ofloxacin are the only fluoroquinolones given intravenously (IV). None of the fluoroquinolones are given intramuscularly (IM). 

The majority of patients can be managed with oral antimicrobial agents, such as trimethoprim-sulfamethoxazole or the fluoroquinolones (ciprofloxacin, levofloxacin). When IV treatment is necessary, IV to oral sequential therapy with trimethoprim-sulfamethoxazole or a fluoroquinolone, such as ciprofloxacin or ofloxacin, would be appropriate. 

The first members of the new fluoroquinolone class (such as norfloxacin (2a), enoxacin (5), pefloxacin (6), ciprofloxacin (2b) and ofloxacin (7)), are generally somewhat less active versus Gram-positive species than Gram-negative... 

The data on the adverse reactions of the fluoroquinolones which have received the most extensive clinical evaluation (ciprofloxacin, ofloxacin, pefloxacin, norfloxacin and enoxacin), involving about 30,000 patients, have been the subject of a review [54a], An important point noted in this review involves the difficulty in detecting an important severe adverse reaction if it is of relatively low frequency, until there has been a very large patient exposure (some examples are provided in which at least 150,000-300,000 exposures would be required to observe the importance of side-effects, resulting in an alert, which have been discovered with specific drugs). However, the majority of side-effects observed thus far with the fluoroquinolones have been minor,... 

J.Y. Shen, M.R. Kim, C.J. Lee, I.S. Kim, K.B. Lee and J.H. Shim, Supercritical fluid extraction of the fluoroquinolones norfloxacin and ofloxacin from orally heated chicken breast muscles. Anal. Chim. Acta 513 (2004) 451-455. 

We then used this Caco-2 cell assay to categorize representative fluoroquinolone drug substance permeability [50], The drugs demonstrated some concentration-dependent permeability indicative of active drug transport. Based upon comparison to labetalol, ciprofloxacin was classified as a LP drug, whereas levofloxacin, lomefloxacin, and ofloxacin were classified as HP drugs, which matched their human in vivo bioavailabilities. All four fluoroquinolone drugs were subject to efflux transport (ciprofloxacin > lomefloxacin > rhodamine 123 > levofloxacin > ofloxacin). 

Thus quinolone antibacterial agents, such as ciprofloxacin CPFX 143 [201], ofloxacin OFLX144 [202],sparfloxacin SPFX145 [203] and trovaflaxin 146 [204] are members of a major class of antibacterial drugs. These fluoroquinolones show broad-spectrum antibacterial activity and are widely used to treat patients with infections, Eq. (58). 

Benzoyl ester 55a was then hydrolyzed with aqueous sodium bicarbonate to enantio-merically pure alcohol 56 in 91% yield (Scheme 4.6). The alcohol was converted to iodide 57 with triphenylphosphite methyliodide in excellent yield. Iodide 57 was next reduced under radical conditions, and the resulting core was hydrolyzed with hydrochloric acid in acetic acid to furnish carboxylic acid 58 in 44% yield over two steps. Finally, the 7-fluoroquinolone was allowed to react with iV-methylpiperazine in DMSO at 130-140°C to deliver (—)-ofloxacin, levofloxacin (1), in 52% yield. 

Most of the fluoroquinolones antibiotics (see Chapter 44) have activity against M. tuberculosis and M. avium-intracellulare. Ciprofloxacin, ofloxacin, and levofloxacin inhibit 90% of the strains of susceptible tubercula bacilli at concentrations of less than 2 xg/mL. Levofloxacin is preferred because it is the active L-optical isomer of ofloxacin and is approved for once-daily use. The... 

Fluoroquinolones are well tolerated. The most common adverse effects are nausea, vomiting, diarrhoea, headache, insomnia, skin rash and occasionally abnormal liver function tests (with trovafloxacin). Phototoxicity has been particularly reported with pefloxacin, lomefloxacin, sparfloxacin and ofloxacin. Tendinitis is a serious side effect rarely reported in adults. Because of cartilage damage in children it must be used under close supervision. 

It is the levoisomer of ofloxacin and having better activity than ciprofloxacin and ofloxacin against S. pneumoniae. It is also used in chronic bronchitis, sinusitis, pyelonephritis, and other related infections of soft tissues. Due to high oral bioavailability, patient can be shifted from IV to oral therapy. It can be administered just once a day regimen as an alternate to other fluoroquinolones in the treatment of respiratory infections. 

Fluoroquinolones like ciprofloxacin, ofloxacin Macrolide antibiotics like clarithromycin, azithromycin. ... 

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