TABLE 1

Classification of each drug based on P450 isozyme selectivity and P-gp affinity

TypeCompoundsF in HumansP450 IsozymeP-gp AffinityReference
ALithium94.5%Arancibia et al., 1986
Hydrochlorothiazide60.2%Patel et al., 1984
BDexamethasone81.4%3A4±Duggan et al., 1975
Nifedipine41.2%3A4Holtbecker et al., 1996
Midazolam30.0%3A4±Thummel et al., 1996
CQuinidine79.5%3A4+Greenblatt et al., 1977
Tacrolimus23.3%3A4+Moller et al., 1999
Verapamil18.0%3A4+McAllister and Kirsten, 1982
DDigoxin65.3%+Hinderling and Hartmann, 1991
EPropranolol29.0%2D6, 1A2Borgström et al., 1981
Amitriptyline47.7%2C19, 2D6, 3A4±Schulz et al., 1983
Timolol61.0%2D6Wilson et al., 1982
Ibuprofen100%2C9Martin et al., 1990
  • −, Drugs generally not considered to be P-gp substrates; ±, drugs known to be P-gp substrates; +, drugs generally known to be P-gp substrates.