Macrolide | Dosage | cmax | cmax | cport.vn | IC50 | References | |||
---|---|---|---|---|---|---|---|---|---|
OATP1B1 | OATP1B3 | ||||||||
mg | mg/l | μM | μM | ||||||
Azithromycin | 1 × 500a | 0.5a | 0.7 | 42 | >250 | N.D. | a Azithromycin (Zithromax) product information, Pfizer Pharma GmbH, Karlsruhe, Germany, 2004 | ||
Clarithromycin | 2 × 250b | 1-2b | 1.3-2.7 | 23 | 96 ± 5 | 32 ± 7 | b Clarithromycin (Klacid) product information, Abbott GmbH & Co. KG, Wiesbaden, Germany, 2004 | ||
Erythromycin | 1 × 1000c | 3.0c | 4.1 | 88 | 217 ± 19 | 34 ± 14 | c Erythromycin (Erythrocin) product information, Abbott GmbH & Co. KG, Wiesbaden, Germany, 2001 | ||
Roxithromycin | 1 × 300d | 9.7d | 11.6 | 34 | 153 ± 4 | 37 ± 6 | d Roxithromycin (Rulid), product information, Aventis Pharma Deutschland GmbH, Frankfurt am Main, 2004 | ||
Telithromycin | 1 × 800e | 2e | 2.5 | 64 | 121 ± 20 | 11 ± 0.3 | e Telithromycin (Ketek), product information, Aventis Pharma S.A., Antony, France, 2005 |
N.D., not determined, cmax, maximal plasma concentration in the systemic circulation, cport.vn, predicted concentration in portal venous blood (according to Ito et al., 1998).