Indinavir + Grapefruit Juice = Precautionary

Effect on Concentration

Indinavir
Increase
Applies within class?
No
Grapefruit Juice
Unknown
Applies within class?
No

Pharmacologic Effects

Indinavir
Effect
N/A
Applies within class?
No
Grapefruit Juice
Effect
N/A
Applies within class?
No

Interaction History

N/A

Last Updated 02-Jul-2018

Summary

Grapefruit juice at high concentrations may increase boosted protease inhibitor concentrations, but given manufacturer diversity, the exact effects of specific juices is difficult to predict.

Sources

Effects of grapefruit juice on pharmacokinetic exposure to indinavir in HIV‐positive subjects. ^

Study Design

In a study by Shelton, et al, 14 HIV positive subjects took 800 mg of indinavir with 6 ounces (180 ml) of water or double‐strength grapefruit juice. Gastric pH was measured and blood samples were collected for 5 hours after indinavir dosing

Study Results

Grapefruit juice increased the mean gastric pH (from 1.39 ± 0.4 to 3.20 ± 0.3; p < 0.05) and slightly delayed the absorption of indinavir (tmax increased from 1.12 ± 0.8hto 1.56± 0.6 h; p < 0.05). However, there were no significant differences in indinavir exposure. Cmax was 16.7 ± 7.3 μ with water versus 13.9 ± 4.2 μ with grapefruit juice (p = NS), and AUC0–8 was 37.5 ± 19 with water versus 36.9 ± 15 with grapefruit juice (p = NS).

Study Conclusions

The authors concluded that concomitant administration of grapefruit juice increases gastric pH and delays indinavir absorption but does not uniformly affect the systemic bioavailability of indinavir in HIV‐infected subjects. The magnitude of the potential interaction between boosted protease inhibitors and grapefruit juice is difficult to predict as the effect of grapefruit juice is concentration, dose and preparation dependent and varies widely across brands.

References

Shelton MJ, Wynn HE, Hewitt RG, DiFrancesco R. Effects of grapefruit juice on pharmacokinetic exposure to indinavir in hiv‐positive subjects. Journal Of Clinical Pharmacology. 2001; 4: 435-442.