Characteristic | Value | Species | Source |
Onset of action after oral administration | 30-45 min | Human | McEnvoy, 1991 |
Onset (time to initial detection in blood) | 30 min | Human | Whinnery, 1984 |
Duration of action after oral administration | 3-6 hr | Human | McEnvoy, 1991 |
Intravenous elimination half-life | 30 min | Human ("clinical results") | Lietman, 1993 |
97 min | Human | Breyer-Pfaff, 1985 | |
1.9 hrs | Sidell, 1990, based on Cronnelly, 1980; Breyer-Pfaff, 1985; Kornhauser, 1988 | ||
Oral elimination half-life | 200 min | Human | Breyer-Pfaff, 1985 |
3.7±1.0 hours | Human | Sidell, 1990, based on Cronnelly, 1980; Breyer-Pfaff, 1985; Kornhauser, 1988 | |
1.78±0.24 hr | Human | Whinnery, 1984, citing Eur J Clin Pharm, 423-428, 1980 | |
Bioavailability | 7.6±2.4% 14% 29% | Human Human Human | Whinnery, 1984 Breyer-Pfaff, 1985 Kornhauser, 1988 |
Mean concentration at which 50% of the red blood cell AChE activity was inhibited (IC50) | 31.8 ng/ml | Human | Lietman, 1993 |
Characteristic | Value | Species | Source |
Time to peak plasma concentration, fasting | 1.7 hr | Human | Whinnery, 1984 |
Time to peak plasma level after oral dosing | 1.5-2.5 hrs | Human? | Kolka, 1991, citing Aquilonius 1980 |
Time to peak plasma concentration, with food | 3.2 hr | Human | Whinnery, 1984 |
Plasma clearance | 44.62L/hr or 744 ml/min | Human | Lietman, 1993 |
0.66±0.22 l/kgahr | Human | Whinnery, 1984 | |
Time at which 95% of the drug is eliminated | 8-10 hours | Human | Kolka, 1991, citing Aquilonius 1980 |
Total clearance | 8.5 (SD 8.7) (ml/min/kg) | Human | Sidell, 1990, based on Cronnelly, 1980; Breyer-Pfaff, 1985; Kornhauser, 1988 |
Volume of distribution | 1.1 (SD 0.3) L/kg | Human | Sidell, 1990, based on Cronnelly, 1980; Breyer-Pfaff, 1985; Kornhauser, 1988 |
Mean rate constant of elimination | 1.365/hr | Human | Lietman, 1993 |
Urinary excretion | 80-90% (SD 0.3) | Sidell, 1990, based on Cronnelly, 1980; Breyer-Pfaff, 1985; Kornhauser, 1988 |
aWhinnery:
from 5 males given 120 mg PB orally.
Characteristic |
Value |
Species |
Source |
Urinary Excretion |
90% |
rat |
Yamamoto, Sawada, et al., 1995 |
Metabolite, 3-hydroxy-N-methylpyridium, as fraction of excreted dose |
1/3 |
rat |
Yamamoto, Sawada, et al., 1995 |
Plasma elimination half life (iv) |
19 min |
rat |
Yamamoto, Sawada, et al., 1995 |
Additional information derived from rats: