Pharmacokinetic outcomes of loperamide and N-desmethylloperamide in 16 healthy volunteers administered loperamide (16 mg) with 240 ml of water or GFJ
Values denote the geometric mean (90% confidence intervals) unless indicated otherwise.
| Outcome | Water | GFJ | GFJ/Water Ratio |
|---|---|---|---|
| Loperamide | |||
| Cmax (nM) | 6.5 (5.3–8.1) | 10 (8.2–13) | 1.58 (1.33–1.88)a |
| AUC0-72h (nM · h) | 105 (87–126) | 180 (149–220) | 1.72 (1.58–1.87)a |
| AUC0-inf (nM · h) | 118 (96–145) | 203 (165–250) | 1.73 (1.58–1.89)a |
| Cl/F (l/h) | 285 (232–351) | 165 (134–203) | 0.57 (0.53–0.62)a |
| Terminal t1/2 (h) | 23.3 (20.7–26.3) | 23.2 (20.8–26.0) | 1.04 (0.94–1.16) |
| Tmax (h) [median (range)] | 3.0 (0.5–12) | 5.0 (2.0–6.0)b | |
| N-Desmethylloperamide | |||
| Cmax (nM) | 7.9 (6.7–9.2) | 7.7 (6.6–9.0) | 0.98 (0.83–1.15) |
| AUC0-72h (nM · h) | 271 (253–290) | 290 (270–310) | 1.04 (0.99–1.10) |
| Tmax (h) [median (range)] | 5.5 (2.0–12) | 7.0 (4.0–26)b | |
| Metabolite/parent AUC ratio | |||
| (AUCm/AUCp)0-72h | 2.6 (2.2–3.1) | 1.6 (1.3–1.9) |