Quinolone antibiotic drug

Synthesis of intermediate for quinolone antibiotic drug (LG Chem/Daejeon) [13,14]... 

Five different types of reactors, including tube reactors, static mixers and a microstructured reactor, were tested for the synthesis of an intermediate to 3deld a quinolone antibiotic drug, named Gemifloxacin (FACTIVE ) [13,14]. 

LG Chem in Daejeon, Korea, performed the multistep synthesis of Gemifloxacin (FACTIVE), a quinolone antibiotic drug with enhanced activity against G(+) bacteria [30]. This drug has high activity against G(—) bacteria, atypical strains and major respiratory pathogens. 

Synthesis of Intermediate for Quinolone Antibiotic Drug (LG Chem/Daejeon IMM Tools)... 

Antacids also have clinically significant drug interactions with tetracycline, ferrous sulfate, isoniazid, quinidine, sul-fonylureas, and quinolone antibiotics. Antacid-drug interactions are influenced by antacid composition, dose, dosage schedule, and formulation. 

The potential for sunlight (or selected other light frequencies) to transform a drug or product is both a useful tool for activating some drugs and a cause of significant adverse effects for others (such as the quinolone antibiotics [Horio et al., 1995 and... 

Several drug classes, including tetracycline, sulfonamide, and quinolone antibiotics, as well as chlorothiazide, chlorpromazine, and amiodarone hydrochloride, have been shown to be photoantigens. Photosensitivity may persist even after withdrawal of the drug, as has been observed with the antiarrhythmic drug amiodarone hydrochloride, since it is lipophilic and can be stored for extended periods in the body fat (Unkovic et al., 1984). In addition, it is quite common for cross-reactions to occur between structurally related drugs of the same class. 

The quinolone antibiotics feature as the one main gronp of antibacterial agents that is totally synthetic, and not derived from or based upon natural products, as are penicillins, cephalosporins, macrolides, tetracyclines, and aminoglycosides. The first of these compounds to be employed clinically was nalidixic acid more recent drugs in current use include ciprofloxacin, norfloxacin, and ofloxacin... 

With IV CyC - - 5FU - - MTX it cannot be established which IMN in the combination is effective and which induces adverse effects. Immediate allergic reactions arising during IV drips may indicate the IMN concerned. Drug interactions among 5FU, MTX and CyC by IVT and oral CyS, MMF, and MTX have not been studied. It has been established however that quinolone antibiotics may interact with IMNs. 

The lead compound for this series, nalidixic acid (38-6), which is acmally a naphthyridine rather than a quinolone, was first introduced over four decades ago. That compound for many years found its niche as a rather effective drug for the treatment of urinary tract infection. The rediscovery of the general stmcmral class in the early 1980s hinged on the discovery of the importance of fluorine at the 6 position and basic nitrogen at position 7. This renewed research led to the development of a very large series of potent broad spectmm antibiotics. This is reflected in the fact that more than 20 quinolone antibiotics have been granted U.S. nonproprietary names. 

For more information on absorption of quinolones, see Drugs to Treat Infections, Antibiotics - quinolones Drugs Acting on the Gastrointestinal Tract, Antacids. 

Finally, it has to be noted that glycopeptides only represent one option to combat infections by gram-positive bacteria. Current research is focused on other cell wall biosynthesis inhibitors (e.g., (3-lactams, cephalosporins) or even on the development of antibacterial agents (e.g., tetracyclines, ketohdes, and quinolone antibiotics) against other targets.An important drug candidate in this context is hnezolid (Zyvox), which is an entirely synthetic oxazolidinone antibiotic with in vitro and in vivo efficiency against MRS A and VRE. ... 

Alternative or reserve drugs are used where there are problems of drug intolerance and bacterial resistance. They are in this class because of either greater toxicity or of lesser efficacy and include ethionamide (gastrointestinal irritation, allergic reactions), capreomycin (nephrotoxic), and cycloserine (effective but neurotoxic). Quinolone antibiotics such as ciprofloxacin and the more recently introduced macrolides such as clarithromycin and azithromycin also have useful activity against mycobacteria. 

Drug-induced tubulointerstitial nephritides represent 1-10% of cases of acute renal failure and is characterized by infiltrates of mononuclear cells associated with tubular cell injury. A lot of drugs are incriminated, including antibiotics (P-lactams, sulfonamides, aminoglycosides, quinolones), antiepileptic drugs, diuretics, proton pump inhibitors, foscarnet and non-steroidal anti-inflammatory drugs [73]. Most often, withdrawal of the drug, with or without concomitant administration of steroids improves the renal functions. 

FIGURE 6.5 The striking analogy between the vasodilator drug flosequinan and the quinolone antibiotic norfloxacin. 

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