Penetration of roxithromycin into gingival tissue.

Roxithromycin is a new macrolide with an antibacterial spectrum similar to that of erythromycin. Absorption is rapid and complete, resulting in high serum levels and a long half-life. Tissue distribution is extensive and sustained, as shown by the high concentrations measured in the lung, prostate, ovaries, liver, kidney, and skin. In this study, we measured the penetration of roxithromycin into gingival tissue at steady state in 30 patients treated orally with 150 mg every 12 hr for 5 days. Tissue specimens were sampled at 2, 4, 6, 8, or 12 hr (n = 6 each time) after dose 10, and blood samples were taken simultaneously. Serum and tissue concentrations of roxithromycin were measured by high-performance liquid chromatography. The peak serum level, reached 4 hr after dosing, was 6.60 +/- 1.15 micrograms/ml. The peak tissue level was 4.63 +/- 1.84 micrograms/g and was reached after 8 hr. From 4 to 10 hr after dosing, tissue concentrations were greater than 2 micrograms/g, that is, higher than the MIC90 of roxithromycin against most oral pathogens. These data support the use of roxithromycin in the treatment of oral infections.

Comparison of two oral antibiotics, roxithromycin and amoxicillin plus clavulanic acid, in lower respiratory tract infections.

In a randomized, multicenter, open-label study, 490 ambulatory adult patients with lower respiratory tract infection (LRTI) were randomized to roxithromycin (ROX) 150 mg b.i.d. orally (n = 244) or amoxicillin plus clavulanic acid (AMX + CA) as 500 mg AMX + 125 mg CA t.i.d orally (n = 24). Clinical results were analyzed in 477 patients with acute bronchitis (79%), chronic bronchitis (CB) (14%), and pneumonia (7%). There were significantly more patients with underlying disease (cardiovascular diseases, p = 0.045; and alcoholism, (p less than 0.001), and more patients over the age of 65 years (p = 0.045) in the ROX group. Overall clinical efficacy was similar in both groups: 88% (206:235) in the ROX group and 85% (205:242) in the AMX + CA group. Side effects were reported in 67 cases (28%) in the AMX + CA group and in 21 cases (9%) in the ROX group (p less than 0.0001), causing withdrawal in 21 and three cases, respectively (p less than 0.001). Thus, despite being administered to a significantly older and more ill group of patients with LRTI, roxithromycin was as effective as amoxicillin plus clavulanic acid and better tolerated.

[Diffusion of roxithromycin in gingival tissue]. / Diffusion gingivale de la roxithromycine.

The gingival penetration of roxithromycin was evaluated at steady-state in twenty nine patients treated by 150 mg orally every 12 h during five days. Tissue specimen were sampled at 2 h (n = 6), 4 h (n = 6), 6 h (n = 5), 8 h (n = 6) and 12 h (n = 6) after the 10th administration. One blood sample was drawn at the same times. Serum and tissue concentrations of roxithromycin were measured by high performance liquid chromatography (HPLC). Serum peak level, measured at the 4th h, reached 6.60 +/- 1.15 micrograms/ml. The tissue peak concentration was 4.63 +/- 1.84 micrograms/g at the 8th h. Between the 4th and 10th hour after administration, the tissue concentrations are above 2 micrograms/g, i.e. above roxithromycin MIC 90 against most of the encountered pathogens in stomatologic infections.

[Bone diffusion of cefotiam in men]. / Etude de la diffusion osseuse du céfotiam chez l'homme.

A 2g single dose of cefotiam was given by rapid intravenous injection to 17 patients undergoing total hip replacement as a prophylaxis. The concentrations of the antibiotic in plasma and femoral head (cancellous bone, cortical bone and capsule) were measured at different time (40 to 250 minutes) following the injection of the drug. Evaluation was done by liquid chromatography. Mean antibiotic concentrations were 70.5 micrograms/ml, 41.4 micrograms/g, 16.9 micrograms/g and 8.1 micrograms/g respectively in plasma, capsule, cancellous and cortical bones. 240 minutes following the injection, mean concentrations of cefotiam were higher than 2.3 micrograms/ml in plasma and 1.8 micrograms/g in bone. Diffusion in cancellous bone is twofold high as in cortical bone and elimination half lif is higher in bone than in plasma (248.8 minutes versus 59.6 minutes in plasma). These results suggest that a 2g intravenous bolus injection of cefotiam given at the induction of anaesthesia should provide an effective prophylaxis during total hip replacement.

[Course of the diffusion of cefotiam in infected ascitic fluid]. / Evolution de la diffusion du céfotiam dans le liquide d'ascite infecté.

The cefotiam (CFT) penetration in infected ascitic fluid was investigated in 12 cirrhotic patients. CFT (1 g every 8 h) was given intravenously and measured by HPLC in plasmatic and ascitic samples. The mean ascitic concentrations (+/- SEM), 1 h, 3 h and 8 h after the first injection (J1) were 14.6 +/- 4.6, 11.8 +/- 3 and 8.4 +/- 2.9 micrograms/ml respectively. These values were 38, 62 and 88% of the corresponding mean plasmatic concentrations and higher than the MIC's for the organisms most commonly involved. The mean plasmatic and ascitic concentrations, a few days later (4.5 or 6 days) (Jn) were not significantly different from the corresponding values at J1. A significant decrease of polymorphonuclear cell count was observed between J1 and Jn. These results suggest that CFT diffusion into ascitic fluid is independent of inflammation and CFT is an adequate antibiotic in cirrhotic patients with infected ascitic fluid.