TABLE 2

Pharmacokinetics of various antibacterials in adult CF patients following oral, intravenous, or aerosolized administration

Agent, dose, and routeCmax (mg/liter) in serumCmax (mg/liter) in sputumCmax (mg/liter) in lung or ELFt1/2 (h) in serum/sputumUrinary recovery (%)Reference(s)
CPX, 500 mg, p.o.2.5–3.80.7–1.93.9–293.7–5.135.7 144 146
CPX, 750 mg, p.o.3.4–4.5 3.6–4.5 144, 145
CPX, 1,000 mg, p.o.4.6–5.61.8 3.7–5.140.8 144 147
CPX, 200 mg, i.v.4.9 16.9 148
CPX, 32.5 mg, ae0.05633.0 9.5/9.04 149
LVX, 200 mg, p.o.2.1 3.9 151
LVX, 500 mg, p.o.4.1–5.3 (4 h) 9.9–15.2* 152 155
LVX, 750 mg, p.o.12.0 (4 h) 22.1* 152 155
LVX, 500 mg, i.v.6.6 18.3 156
LVX, 180 mg, ae0.95–1.32,563-2,932 6.4–6.8/3.5–4.3 157
TOB, 1.7–3.5, mg/kg q.d. i.v.3.6–11.3 2 1.1-0.7 85 158,160
TOB, 10 mg/kg, q.d. i.v.22–29 1.7–2.2 221, 223, 224, 369
TOB, 600 mg, ae b 1.3 1317.5 164
TOB, 300 mg, ae b <4489–6953.6–5.58.9–11.25.5 165 168
TOB, 112 mg, ae c 1.021,048 3.1/2.2 169
TOB, 300 mg, ae b 1.04737 3.0/1.7 169
AMI, 30 mg/kg, i.v.83–121 (AUC = 235 mg · h/liter)6.3–10.9 (AUC = 83.7 mg · h/liter) 0.6–2.683 369, 225, 299, 370, 371
AMI, 500 mg, aeAUC = 8.3 mg · h/literAUC = 3,830 mg · h/liter 2.9 170
AMI, 560 mg, ae1.292,286 25–50 171
AZM, 2 g80–2285.2 1.872 172 175
AZM, 75 mg, ae0.42–0.49324–677 2.1 176, 177
COL, 2.4 mg/kg2.5–10 (range) 4.2 179
COL, 66 mg0.17–0.18∼40 4.1–4.54.3 180
  • a The broad range of ciprofloxacin lung tissue concentrations following oral (p.o.) or i.v. administration is due to the fact that some investigators administered the drugs once and others administered them repeatedly; the higher values represent steady-state concentrations. The range of levofloxacin concentrations following aerosolized (ae) administration is due to the fact that the dose of 180 mg was administered in two different formulations (50 mg/ml and 100 mg/ml) (lung, lung tissue homogenate; ELF, epithelial lining fluid; AUC, area under the concentration-versus-time curve; t 1/2, half-life, either in serum or in sputum; CPX, ciprofloxacin; LVX, levofloxacin; TOB, tobramycin; AMI, amikacin; AZM, aztreonam; COL, colistin). Asterisks indicate values for ELF.

  • b Tobramycin solution for inhalation.

  • c Tobramycin dry powder for inhalation.