Table 1.
Mean (SD) steady‐state concentrations of (+)‐ and (−)‐perhexiline, and the OH‐metabolites, in DA rats administered 200 mg/kg per day of (±)‐, (+)‐ or (−)‐perhexiline maleate for 8 weeks in rat chow pellets provided each day at 1700 hour
| Dosage form | |||
|---|---|---|---|
| (±) | (+) | (−) | |
| Plasma (mg/L) | |||
| (+)‐Perhexiline | 0.38 (0.29) | 0.67 (0.13) | n.d. |
| (−)‐Perhexiline | 0.19 (0.12) | n.d. | 0.30 (0.09) |
| cis‐OH‐perhexiline | 0.42 (0.14) | 0.21 (0.06) | 0.60 (0.06) |
| trans1‐OH‐perhexiline | 0.03 (0.01) | 0.05 (0.03) | <LLOQ |
| trans2‐OH‐perhexiline | 0.03 (0.02) | n.d. | <LLOQ |
| Liver (μg/g) | |||
| (+)‐Perhexiline | 19.4 (14.0) | 104.9 (36.8) | n.d. |
| (−)‐Perhexiline | 8.9 (6.0) | n.d. | 17.1 (2.8) |
| cis‐OH‐perhexiline | 11.8 (3.2) | 13.9 (6.6) | 15.5 (6.6) |
| trans1‐OH‐perhexiline | 1.1 (0.4) | 4.0 (1.7) | 0.6 (0.2) |
| trans2‐OH‐perhexiline | 1.1 (0.5) | 0.8 (0.7) | 1.9 (1.2) |
| Heart (μg/g) | |||
| (+)‐Perhexiline | 15.6 (6.8) | 65.1 (39.1) | |
| (−)‐Perhexiline | 6.3 (2.4) | 6.5 (3.3) | |
See Figure 1 for statistical analysis of dose‐corrected (+)‐ and (−)‐perhexiline concentrations. Samples were taken in the morning after the last dose (n.d. = not detectable; <LLOQ, below lower limit of quantification, 0.01 mg/L or μg/g).