Inhibition of Excretion Pumps

5 and 4, respectively, while the corresponding uptake ratios were 10-58, 63 90, 17-64, 15 and 6-14, respectively (Shitara et al, 2013). The conclusion was that statins except cerivastatin and fluvastatin were highly concentrated in hepatocytes. 

TPSA and lipoidal permeability are not absolute rules in terms of transporter involvement. Actual transport rate is obviously important, and it is likely that some compounds are substrates for multiple transporters, which could give 

FIGURE 5.2 Correlation of in vitro and in vivo CNS pharmacological effects of opioid agonists and their physicochemical properties. The weaker in vivo effects of morphine are explainable in contrast to those of loperamide. 

Acharya, P., O Connor, M.P., Polli, J.W., Ayrton, A., Ellens, H., and Bentz, J. (2008) Kinetic identification of membrane transporters that assist P-glycoprotein-mediated transport of digoxin and loperamide through a confluent monolayer of MDCKII-hMDRl cells. Drug Metab. Dispos., 36,452-460. 

Wakenhut, E, and Whitlock, G. (2011) Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space. Med. Chem. Commun., 2, 669-674. 

---