Table 5.
PK parameters | Dosage | ||
---|---|---|---|
Single dose of 0.4 mg/kg [22] median (Q1, Q3) | Initial infusion 1 mg/kg/h for 0.5 h + 0.4 mg/kg/h for 3.5 h [23] mean (CV%) | Bolus-loading dose 0.4 mg/kg + 0.4 mg/kg/h for 12 h [23] mean (CV%) | |
C max (ng/mL) | 1330.0 (985.0, 1710.0) | 550.7 (13.4) | 1282.4 (83.9) |
AUC0–t (ng·h/mL) | 254.33 (226.67, 423.33) | 2496.4 (46.3) | 4417.9 (12.7) |
AUC0−∞ (ng·h/mL) | 271.67 (245.00, 505.00) | 2211.6 (16.5) | 4647.2 (13.2) |
T max (min) | 2.00 (2.00, 3.00) | 55.20 (30.00, 720.00)# | 3.60 (1.80, 17.40)# |
T 1/2 (h) | 2.09 (1.86, 2.47) | 12.78 (41.7) | 9.91 (17.3) |
CL (L/h/kg) | 1.47 (0.79, 1.63) | 1.00 (19.0) | 1.09 (22.9) |
Vd (L/kg) | 4.3 (2.1, 5.0) | 18.94 (49.7) | 15.45 (21.7) |
λ z (L/h) | 0.34 (0.28, 0.37) | 0.061 (32.8) | 0.072 (15.3) |
MRT (h) | 2.36 (1.89, 2.37) | 3.68 (62.5) | 3.31 (16.9) |
Notes: #these data of Tmax are presented as median (range). Abbreviations: PK: pharmacokinetics; Cmax: maximum plasma concentration; AUC: area under the curve; CV: coefficient of variation; Tmax: time of maximum plasma concentration; T1/2: terminal elimination half-life; CL: clearance after adjusting for weight; Vd: apparent volume of distribution; λz: elimination rate constant; MRT: mean residence time.