Table 2.
Pharmacokinetics of S- and R- verapamil, PR prolongation and changes in blood pressure following single doses of 80 mg to healthy control and Crohn's patients in remission or with active disease
| Verapamil enantiomer | Control (n = 9) | Crohn's disease remission (n = 22) | Active (n = 14) |
|---|---|---|---|
| tmax (min) | |||
| S | 60 (40–60)a | 60 (40–60)a | 60 (40–120)a |
| 95% CI | 0.74, 1.46 | 0.81, 1.33 | 0.57, 1.83 |
| R | 60 (20–60)a | 60 (40–60)a | 60 (20–60)a |
| 95% CI | 0.60, 0.88 | 0.79, 1.21 | 0.67, 1.93 |
| Cmax (ng ml-1) | |||
| S | 19.9 ± 10.5a | 39.3 ± 51.6a | 189.7 ± 243.1b |
| 95% CI | 13.0, 26.8 | 17.7, 60.9 | 62.0, 317 |
| R | 278 ± 127a | 353 ± 313a | 558 ± 538b |
| 95% CI | 195, 361 | 222, 484 | 271, 840 |
| t1/2 (h) | |||
| S | 4.33 ± 1.93a | 3.56 ± 1.55a | 17.0 ± 22.7b |
| (n = 4) | (n = 11) | (n = 11) | |
| 95% CI | 2.44, 6.22 | 2.64, 4.48 | 3.59, 30.41 |
| R | 3.16 ± 1.04a | 3.13 ± 1.23a | 3.13 ± 1.54a |
| (n = 9) | (n = 22) | (n = 13) | |
| 95% CI | 2.48, 3.84 | 2.62, 3.64 | 2.29, 3.97 |
| AUC (ng ml-1 h) | |||
| S | 61.7 ± 46.8a | 95.5 ± 140.7a | 537 ± 598b |
| 95% CI | 31.1, 92.3 | 36.71, 154.3 | 222, 849 |
| R | 723 ± 453a | 720 ± 755a | 1714 ± 1693a |
| 95% CI | 427, 1019 | 396, 1044 | 827, 2601 |
| PR interval prolongation | |||
| % max/baseline | 21.4 ± 14.9a | 14.8 ± 9.8a | 17.0 ± 17.0a |
| 95% CI | 11.7, 31.1 | 10.7, 18.9 | 2.86, 31.1 |
| AUEC, %.h | 44.3 ± 45.1a | 36.0 ± 41.4a | 32.2 ± 67.8a |
| 95% CI | 14.8, 73.8 | 18.7, 53.3 | −3.32, 67.7 |
| Blood pressure (%) | |||
| Systolic | 13.4 ± 10.0a | 10.8 ± 4.4a | 12.2 ± 7.5a |
| 95% CI | 6.87, 19.9 | 8.96, 12.6 | 8.17, 16.2 |
| Diastolic | 12.6 ± 3.5a | 9.4 ± 3.0a | 9.9 ± 3.6a |
| 95% CI | 10.3, 14.9 | 8.15, 10.7 | 8.01, 11.8 |
| Heart rate (%) | 11.3 ± 5.8a | 10.9 ± 5.3a | 9.6 ± 5.0a |
| 95% CI | 7.51, 15.1 | 8.69, 13.1 | 6.98, 12.2 |
Different characters in the row indicate significant difference at α = 0.05. Blood pressure (mmHg) and heart rates are changes from baseline. Experimental points from fewer patients were used to calculate t1/2 due to fluctuation. Data are presented as mean ± SD except for Cmax, t1/2 and AUC that are geometric means ± SD and tmax is median (range).