ABSTRACT
Objective: To evaluate the clinical efficacy and safety of Levornidazole and sodium chloride injection in treating patients with bacterial liver abscess. Methods: 94 patients with bacterial liver abscess who need anti-anaerobion treatment were enrolled in this study. And all of them were divided into observation group (47 cases) and control group (47 cases). The patients of observation group received intravenous drip infusion of Levornidazole and sodium chloride injection, while patients of control group received intravenous drip infusion of Omidazole injection. The dosage of two groups was 0.5g, 2 times/d, 5-10d per a course. The clinical efficiency, bacteriology efficiency and the occurrence rate of adverse reaction between two groups were compared and researched. Results: The differences of clinically effective rate and clearance rate of bacteria between observation group (95.74% and 93.33%) and control group (89.36% and 88.23%) were not significant (x2=0.62, x2=1.30, P>0.05). The difference of average hospital stay time between observation group (13.47 d) and control group (14.86 d) also was no significant (t=0.96, P>0.05). After the drug therapy, the occurrence rates of adverse reactions, included of gastrointestinal reaction, anaphylaxis and abnormal liver function, of observation group was no significantly lower than that of control group (x2=0.26, x2=0.51, x2=0.51, P>0.05). While the adverse reaction rate of central nervous system of observation group (0) was significant lower than that of control group(14.89%) (x2=5.56, P<0.05). Conclusion: Levornidazole treating the bacterial liver abscess can obtain significant efficacy and safety, and it has higher clinical application value.
ABSTRACT
This study was carried out to investigate the pharmacokinetics/bioequivalence of levornidazole disodium phosphate by using stable isotope labeled drug, evaluated the pharmacokinetic profile and confirmed the prodrug characteristics of levornidazole disodium phosphate in monkey. Levornidazole (Drug A) and stable isotope 15N labeled levornidazole disodium phosphate (Drug B) were mixed with equal mole amount (experiment I); stable isotope 15N labeled levornidazole disodium phosphate (Drug B) and levornidazole disodium phosphate (Drug C) were mixed with equal mole amount, respectively. After giving the mixed drugs to the monkey, the concentration of 15N-levornidazole disodium phosphate, levornidazole disodium phosphate, 15N-levornidazole and levornidazole in plasma samples of pre-dosing and 24 h after administration were analyzed by a liquid chromatography-mass spectrometry/mass spectrometry (LC-MS/MS) method. Pharmacokinetic calculations were performed through non-compartmental analysis using WinNonlin software. Two-sided 90% confidence intervals (CI) were used to evaluate the bioequivalence of two drugs. The results showed that levornidazole disodium phosphate was metabolized to levornidazole rapidly after administration, the body exposure were increased with the dosage. The method of bioequivalence used in this study was different from the traditional two periods, crossover design. By using the method of this study, the effects of administration period, intra-individual variability, and sequence of administration on bioequivalence were avoided. The results of this study had successfully supported the pharmacokinetic and bioequivalence study of this drug in human using the same approach.
ABSTRACT
Objective To determine the in vitro antibacterial activity of levornidazole against 375 anaerobic isolates.Methods Agar dilution method was used to determine the minimum inhibitory concentrations (MICs)of levornidazole,3 comparators (metronidazole,ornidazole and dextrornidazole)against 375 anaerobic isolates.Results For anaerobic gram-negative and gram-positive bacilli,and anaerobic gram-positive cocci,levornidazole displayed activity similar to or slightly higher than that of met-ronidazole,ornidazole and dextrornidazole.Levornidazole showed good activity against B.fragilis,Bacteroides thetaiotaomi-cron ,Clostridium difficile ,Clostridium perfringens ,and Peptostreptococcus magnus .The MIC90 value of levornidazole a-gainst the above-mentioned anaerobes was 0.5,1,0.25,2 and 1 mg/L,respectively.However,levornidazole and the compa-rators had poor antibacterial activity against Veillonella spp.among anaerobic gram-negative cocci.Conclusions The in vitro anti-anaerobic activity of levornidazole is similar to or slightly higher than that of metronidazole, ornidazole and dex-trornidazole.Levornidazole has good activity against both gram-negative and gram-positive anaerobic bacilli,and gram-positive anaerobic cocci,suggesting its promising clinical use.