TABLE 2

Impact of decreasing fraction unbound in plasma

Administration route and drug characteristics.

ParameterPar Low E Low VPar Low E High VPar High E Low VPar High E High VOral Low E Low VOral Low E High VOral High E Low VOral High E High V
CL total
Cmax total
Css total
Cmax unbound
Css unbound
  • CL, total drug clearance; high E, high extraction ratio; high V, high volume of distribution (distributes extensively to peripheral tissues); low E, low extraction ratio; low V, low volume of distribution (confined primarily to central compartment); oral, oral administration; par, parenteral administration.