DIET/NUTRIENT INTERACTIONS WITH DRUG TRANSPORTERS - Drug Transporters: Molecular Characterization and Role in Drug Disposition - page 668

TABLE 22.1. Effects of Dietary Supplements on Drug Transporters
Dietary In Vitro/

Supplement In Vivo Substrate Effects Mechanisms Refs.

St. John's wort In vitro Rhodamine 123 ↑ Accumulation Inhibition of Pgp after

acute exposure
Induction of Pgp after
chronic exposure

43

↓ Accumulation due to
↑ Pgp protein level

43,44

In vitro Ritonavir ↓ Efflux Inhibition of Pgp 48

In vitro Daunorubicin/

calcein-AM

↓ Efflux Inhibition of Pgp 49

In vitro ↑ MRP2 mRNA level 50

↑

In vivo Pgp protein level Activation of PXR 31

↑

In vivo MRP2 protein level 51

In vivo Digoxin ↓ AUC, ↓ C max Induction of Pgp 24,31,53

In vivo Fexofenadine ↑ C max , ↓ clearance Inhibition of Pgp

(single dose)
Induction of Pgp
(chronic treatment)

57

↔ C max , ↔ AUC

In vivo Indinavir ↓ AUC, ↓ C trough Induction of Pgp/CYP3A4 59

In vivo Cyclosporine ↓ AUC, ↓ C plasma Induction of Pgp/CYP3A4 60,61

In vivo Tacrolimus ↓ AUC, ↑ clearance Induction of Pgp/CYP3A4 64

Grapefruit juice In vitro Talinolol/digoxin ↑ Absorptive transport Inhibition of Pgp 72,74

In vitro Rhodamine 123/

fexofenadine/
saquinavir

↓ Efflux Inhibition of Pgp 73,77,78

In vitro Vinblastine ↓ Efflux or ↑ uptake Inhibition of Pgp 71,79