TABLE 5

Uptake clearance of drugs in rat kidney slices

Time-dependent uptake of drugs into rat kidney slices was measured in the presence of tracer amount of drugs in the incubation buffer (0.1 μM for [3H]pravastatin, [3H]pitavastatin, [3H]rosuvastatin, [3H]valsartan, and [3H]olmesartan; 6.3 μM for [14C]temocaprilat; 1.7 μM for [14C]PCG; 10 μM for enalaprilat, benazeprilat, cefmetazole, and ceftizoxime). The in vitro intrinsic uptake clearance (P1 kid) was calculated by dividing initial uptake velocity by the drug concentration in the incubation buffer. Each value is expressed as mean ± S.E. of triplicate determinations.


Compound

P1KID
ml/min/g kidney
Pravastatin 0.236 ± 0.110
Pitavastatin 0.912 ± 0.173
Rosuvastatin 0.310 ± 0.110
Valsartan 1.21 ± 0.29
Olmesartan 0.644 ± 0.175
Candesartan 0.796 ± 0.363
Temocaprilat 0.290 ± 0.115
Enalaprilat 0.220 ± 0.135
Benazeprilat 0.122 ± 0.047
PCG 0.521 ± 0.106
Ceftizoxime 0.0415 ± 0.0272
Cefmetazole
0.0953 ± 0.0176