SOLITHROMYCIN

Pharmaceutical Applications

A 2-fluoroketolide. The side chain substituting the C11–C12 carbamate is composed of a substituted triazolyl (aminophenyl) ring. It displays good in-vitro and in-vivo activity against Streptococcus spp., including Str. pneumoniae (MIC 0.0015–0.25 mg/L), Str. pyogenes (MIC ≤0.008–0.015 mg/L)and viridians group streptococci (MIC ≤0.008–0.06 mg/L). Activity against H. influenzae is close to that of azithromycin (MIC 1.0–2.0 mg/L). Vancomycin-susceptible strains of E. faecalis are inhibited by 0.003–2.0 mg/L and E. faecium by 0.25–2.0 mg/L. It exhibits good activity against Ch. pneumoniae (MIC 0.25–1.0 mg/L), C. trachomatis (MIC 0.123–0.5 mg/L) and Mycoplasma spp. (MIC ≤0.0008 mg/L). In vitro H. pylori is susceptible (MIC 0.006–0.25 mg/L), but C. jejuni less so (MIC 1–4 mg/L). It is extremely active in vitro against B. anthracis (MIC <0.008–0.015 mg/L) and other agents of bioterrorism such as Francisella tularensis (MIC <0.08–4.0 mg/L), Yersinia pestis and Burkholderia mallei (MIC 0.25–2.0 mg/L). It exhibits a good activity against the M. avium complex.
In healthy adult volunteers the proposed therapeutic dose of 400 mg achieved a peak plasma concentration of 0.78 mg/L after 4 h. The apparent elimination half-life was 5.1 h.