Table 1

Plasma and pulmonary tissue pharmacokinetic studies conducted in MTB exposed NZW rabbitsa

Drug(s) administered (no. of animals)Dosing regimenSampling timesNo., type, and diam of granulomas sampled
INH, RIF, PZA, and MXF (n = 13)All 4 drugs given once to each animal at the following doses: INH, 50 mg/kg; RIF, 30 mg/kg; PZA, 125 mg/kg; MXF, 25 mg/kgPlasma samples at 2-4 practical times during the expt; tissue samples at euthanasia (between 0.5 and 7 h)46 solid granulomas, 1 to 4 mm
INH (n = 4)30 mg/kg daily for 8 daysPlasma samples at 0, 0.5-1, and 1-2 h; tissue samples at euthanasia (between 2 and 4 h)8 caseous, 1.5 to 3 mm; 3 suppurative, 1.5 to 3 mm
RIF (n = 4)24 mg/kg daily for 8 daysPlasma samples at 0, 0.5-1, and 1-2 h; tissue samples at euthanasia (between 1 and 3 h)3 solid, 1 to 4 mm; 3 caseous, 2.5 to 3 mm; 3 suppurative, 1.5 to 3 mm
INH, RIF, PZA, and MXF (n = 12)All 4 drugs given to each animal once daily for 5 to 6 days: INH, 50 mg/kg; RIF, 30 mg/kg; PZA, 125 mg/kg; MXF, 25 mg/kgPlasma samples at 2 to 4 practical times during the expt; tissue samples at euthanasia (between 1 and 17 h)24 solid, 1 to 4 mm; 25 caseous, 1.5 to 4 mm; 5 suppurative, 1 to 2.5 mm; 6 coalescing, >4 mm, irregular shape; 2 cavity caseous cores, ND; 3 cavity walls, ND
  • a For each study, serial plasma samples were drawn before euthanasia. Pulmonary tissue samples were obtained at study end. ND, not determined.