Table 2.

Potencies of anti-tuberculosis agents against M. tuberculosisa

AntibioticbMIC99 (μg/ml)cMPC (μg/ml)dDose (mg)eCmaxfMPC/ CmaxReference for Cmax
Rifampin0.02>806009.5>8 2
Streptomycin0.2>320100034>9 1,4
Isoniazid0.06202507.62.6 2
Capreomycin2.01601,000334.8 4
Kanamycin1.5>80050021>38 5
Cycloserine1470750352 23
Fluoroquinolones
 Ciprofloxacin0.158.07504.41.8 9
 Moxifloxacin0.0372.54004.50.55 17
 PD135432g 0.031.53003.70.41 15
 Sparfloxacin0.0752.52001.41.8 14
 PD1611480.071.5 NAh
  • a Experiments were performed with isolate TN6515.

  • b Unless indicated otherwise the source of all compounds was Sigma Biochemicals. The exceptions were as follows: ciprofloxacin, Miles Laboratories; moxifloxacin, Bayer AG; PD135432, Parke-Davis; sparfloxacin, Parke-Davis; and PD161148, Parke-Davis.

  • c MIC99, MIC at which 99% of isolates are inhibited.

  • d The MPC was determined as described in footnote a of Table 1. The MPC of each compound was determined twice, with results similar to those shown obtained each time.

  • e The dose recommended by the manufacturer. For determination of the maximum concentration of drug in serum, streptomycin, capreomycin, and kanamycin were administered as single, intramuscular doses; all other compounds except ciprofloxacin and PD135432 were administered as oral doses once daily; ciprofloxacin and PD135432 were delivered twice daily. The initial dose of sparfloxacin was 400 mg. During treatment of tuberculosis, kanamycin is administered twice daily.

  • f C max, maximum concentration of drug in serum. All are steady-state determinations except for those for streptomycin, capreomycin, and kanamycin, which were single-dose determinations.

  • g Structure identical to that of gatifloxacin.

  • h NA, not available.