[In vitro and in vivo activity of tiamulin against leptospires (author's transl)].
The minimal growth inhibiting concentration of tiamulin, a derivative of the diterpen antibiotic pleuromutilin, was evaluated in vitro against 11 different serogroups of leptospira interrogans by twofold serial dilution technique, in comparison to tetracyclin, dihydrostreptomycin and tylosin. The range of the MIC values of tiamulin is between 0.07 and 2.5 microgram/ml and thus comparable to the activities of the standard antibiotics tested (see table 1). The chemotherapeutic efficacy (ED50) of the compound was examined in two experimental leptospiral infections of the Syrian hamster, in comparison to tetracyclin. Both compounds were administered orally for 3 days. In the L. canicola infection, the ED50 values were 103.8 mg/kg and 306.3 mg/kg body-weight for tiamulin and tetracyclin, respectively. In the L. grippotyphosa infection, the ED50 values amounted to 35.16 and 277.5 mg/kg bodyweight for tiamulin and tetracyclin, respectively. Based on these values, tiamulin in comparison to tetracyclin showed 3-8 fold higher efficacy in vivo after oral administration.
D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology* / Q000627:therapeutic use; D006224:Cricetinae; D004096:Dihydrostreptomycin Sulfate / Q000494:pharmacology; D004195:Disease Models, Animal; D004224:Diterpenes; D004353:Drug Evaluation, Preclinical; D005260:Female; D007919:Leptospira / Q000187:drug effects*; D007922:Leptospirosis / Q000188:drug therapy; D007933:Leucomycins / Q000494:pharmacology; D008297:Male; D008647:Mesocricetus; D013045:Species Specificity; D013752:Tetracycline / Q000494:pharmacology / Q000627:therapeutic use
D000900:Anti-Bacterial Agents; D004224:Diterpenes; D007933:Leucomycins; D013752:Tetracycline; D004096:Dihydrostreptomycin Sulfate
Wirksamkeit von Tiamulin gegen Leptospiren in vitro und in vivo.