In vitro availability studies of enoxacin in presence of H2 receptor antagonists.
Enoxacin is a second-generation quinolone with increased antibacterial activity both in potency as well as in terms of broad spectrum against a wide range of clinically important pathogens over the first generation quinolones and produces its effect by inhibiting bacterial enzyme DNA gyrase. There are a number of drug interactions reported for enoxacin. On the other hand H2-receptor antagonists block gastric acid secretion and some cardiovascular effects of histamine. As the later drugs are used for a long-term therapy, they may be coadministered with other drugs. In present study in vitro release of enoxacin in presence of cimetidine, ranitidine and famotidine has been studied on a B.P. 2003 dissolution test apparatus and compared with the availability of enoxacin and H2-receptor antagonists alone. The interacting drugs were analyzed spectrophotometrically. These studies were carried out in simulated gastric juice, simulating empty stomach, simulated intestinal juice (pH 9) and buffers of pH 7.4 simulating blood pH at 37 degrees C. In order to support these interaction studies, the effect of H2-receptor antagonists on the antibacterial efficacy (MIC) of enoxacin was also studied by turbidity method and compared with parent drug against Staphylococcus aureus, Streptococcus pyogens, Streptococcus pneumoniae, Enterococcus, Escherichia coli, Salmonella typhi, Pseudomonas aeruginosa, Klebsiella pneumoniae, Proteus mirabilis and Bacillus subtilis. On the basis of these results, it is suggested that enoxacin should be coadministered with care along with H2-receptor antagonists especially in case of ranitidine, although chances of adverse reactions are rare but decrease in MIC of enoxacin may result in delayed effect or require prolonged use of the drug.
Arayne
M Saeed
MS
Department of Chemistry, University of Karachi. Karachi-75270, Pakistan.
Sultana
Najma
N
Haroon
Urooj
U
Hamza
Erum
E
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D000897:Anti-Ulcer Agents / Q000737:chemistry*; D002927:Cimetidine / Q000737:chemistry / Q000494:pharmacology; D004347:Drug Interactions; D015365:Enoxacin / Q000737:chemistry* / Q000494:pharmacology; D015738:Famotidine / Q000737:chemistry / Q000494:pharmacology; D005750:Gastric Juice / Q000737:chemistry; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D008826:Microbial Sensitivity Tests; D011899:Ranitidine / Q000737:chemistry / Q000494:pharmacology; D012995:Solubility; D013696:Temperature
D000900:Anti-Bacterial Agents; D000897:Anti-Ulcer Agents; D006635:Histamine H2 Antagonists; D015365:Enoxacin; D015738:Famotidine; D002927:Cimetidine; D011899:Ranitidine