Biliary secretion of moxifloxacin in obstructive cholangitis and the non‐obstructed biliary tract

Abstract

Summary Background : Biliary secretion of antibiotic agents into the bile is considerably compromised by biliary obstruction, a precondition of bacterial cholangitis. Moxifloxacin may be advantageous according to secretion and antimicrobial spectrum. Aim : To establish the secretion of moxifloxacin into obstructed and non‐obstructed bile. Methods : Biliary excretion of moxifloxacin was determined in plasma and bile of 10 patients with biliary obstruction and cholangitis and 10 patients without biliary obstruction 30 min after administration of 400 mg of moxifloxacin intravenously. Results : The plasma concentration of moxifloxacin was similar in both groups (4.45 ± 1.58 μg/mL; 4.33 ± 1.23 μg/mL). The concentration of moxifloxacin in the bile was significantly lower in patients with biliary obstruction than without (4.63 ± 3.94 μg/mL; range 0.71–14.40; vs. 16.90 ± 13.77 μg/mL; range 1.79–42.50; P = 0.043). Although significantly different, the penetration index was extensively high in those without biliary obstruction (4.41 ± 4.40; range 0.35–14.45) but still sufficient in those patients with obstructive cholangitis (1.02 ± 0.74; range 0.29–2.83; P = 0.035). Conclusion : These findings are suggestive of an active secretion mechanism for moxifloxacin into the obstructed bile, producing a biliary concentration sufficiently above the minimal inhibitory concentrations for most of the expected bacteria.

Penetration of moxifloxacin into liver tissue

“…The results of subgroup analysis implicate that there is no relevant influence of liver cirrhosis on the concentrations in liver tissue. In accordance with findings of other recent studies, moxifloxacin shows exceptional penetration into the human hepatobiliary system including pancreatic tissue [11], the gallbladder wall [8], bile [19] and liver tissue.…”

“…As liver concentrations of moxifloxacin were analysed from wholetissue homogenates, the exact concentration of moxifloxacin in the different liver compartments could not be determined. However, considering the data from other groups demonstrating high concentrations of moxifloxacin within the bile and gallbladder wall [8,19], the current results emphasise the potential use of moxifloxacin in bacterial liver infections.…”

Involvement of Mrp2 (Abcc2) in biliary excretion of moxifloxacin and its metabolites in the isolated perfused rat liver

“…The involvement of an active transport system is also supported by a recent clinical study in patients which showed that moxifloxacin is secreted extensively into the bile duct system, even in the presence of biliary obstruction (Schwab et al 2005). Efficient transport of moxifloxacin and its conjugates by cmoat is also suggested by the fact that the addition of moxifloxacin stimulates bile flow in control rats but not in TR − rats.…”

Complications of Transcatheter Arterial Chemoembolization for Treatment of Primary Liver Cancer

“…10 Moxifloxacin has a high degree of biliary secretion. 15 Other biliary complications occurring after TACE include biliary strictures, biliary dilation, and the development of intrahepatic bilomas. These complications are uncommon (0.87%) 16,17 but can be exceedingly difficult to treat.…”