Levocil Mechanism of Action

Pharmacology: Antibacterial Activity: Levocil is a wide-spectrum antibacterial agent against gram-positive and gram-negative bacteria, including anaerobes. Levocil has shown strong antibacterial activities against Staphylococcus spp., Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus haemolyticus, Enterobacter spp., Escherichia coli, Klebsiella spp., Serratia spp., Enterococcus spp., Proteus spp., and other glucose non-fermentative gram-negative rods, Pseudomonas aeruginosa, Haemophilus influenzae, and Neisseria gonorrhoeae. Moreover, Levocil has shown antibacterial activity against Chlamydia trachomatis. Levocil has excellent protective and treatment effects in mice.
Mechanism of Action: The main mechanism of action of Levocil is the inhibition of DNA gyrase. It is two fold stronger than that of ofloxacin. There is not much difference between the MIC and MBC. The activity of Levocil is bactericidal. In the observation of bacterial morphology, bacteriolysis can be seen in the concentration around MIC.
Pharmacokinetics: Distribution in Plasma: Approximately 30-40% of Levofloxacin is bound to serum protein. 500mg once daily multiple dosing with Levofloxacin showed negligible accumulation. There is modest but predictable accumulation of Levofloxacin after doses of 500mg twice daily. Steady-state is achieved within 3 days.
Penetration into tissues and body fluids: Penetration into Bronchial mucosa, Epithelial Lining Fluid (ELF). Maximum Levofloxacin concentrations in bronchial mucosa and epithelial lining fluid were 8.3 ug/ml and 10.8 ug/ml respectively. These were reached approximately one hour after administration.
Penetration into lung tissue: Maximum Levofloxacin concentrations in lung tissue were approximately 11.3 ug/ml and were reached between 4 and 6 hours after administration. The concentration in the lungs consistently exceeded those in plasma.
Metabolism: Levofloxacin is metabolised to a very small extent, the metabolites being desmethyl-levofloxacin and levofloxacin N-oxide. These metabolites account for < 5% of the dose excreted in urine. Levofloxacin is stereochemically stable and does not undergo chiral inversion.
Elimination: Following oral and intravenous administration, Levofloxacin is eliminated relatively slowly from the plasma (t_½ : 6-8 h). Excretion is primarily by the renal route (> 85% of the administered dose). There are no major differences in the pharmacokinetics of Levofloxacin following intravenous and oral administration, suggesting that the oral and intravenous routes are interchangeable.
Tablet: Absorption: Orally administered Levofloxacin is rapidly and almost completely absorbed with peak plasma concentrations being obtained within 1 hr. The absolute bioavailability is approximately 100%. Food has little effect on the absorption of Levofloxacin.
Subjects with renal insufficiency: The pharmacokinetics of Levofloxacin are affected by renal impairment. With decreasing renal function, renal elimination and clearance are decreased, and elimination half-lives increased as shown in the table as follows. (See Table 1.)

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Elderly subjects: There are no significant differences in Levofloxacin kinetics between young and elderly subjects, except those associated with differences in clearance.
Gender differences: Separate analysis for male and female subjects did not show clinical relevant gender differences in Levofloxacin pharmacokinetics.