Table 5.
Clinical pharmacokinetic interactions between ARV and buprenorphine.
| ARV | Interaction | Mechanism | Reference |
|---|---|---|---|
| Atazanavir (ATZ) and atazanavir/ritonavir(RIT) |
Both ATZ alone and ATZ/RIT combination after five days of exposure caused significant ↑ in AUC and ↓ clearance of buprenorphine and its glucoronide metabolites |
Via inhibition of CYP3A4 or inhibition of secretion of glucoronides into the bile |
(McCance-Katz et al., 2007) |
| Efavirenz, delaverdine, nelfinavir, RIT, and lopinavir/RIT |
Altered metabolism M1 ↓and ↑M3 by efavirenz and ↑M1 and ↓ M3 by delavirdine. Both nelfinavir and ritonavir caused M1 and M3↓. |
While efavirenz induced CYP3A, delaverdine, nelfinavir and ritonavir inhibited CYP3A |
(Moody et al., 2009) |
| Delaverdine and RIT | Prolongation of QT intervals in opiod dependent subjects. | Inhibition of CYP3A4 | (Baker et al., 2006) |
| Tiprinavir/RIT | AUC and Cmax of tiprinavir ↓ by 19% and 25% respectively | Mechanism unclear | (Bruce et al., 2009) |
| Didanosine, atazanavir, tenofovir and RIT |
Three patients received the ARV combination therapy and resulted in ↑ levels and clinical symptoms of opiate excess |
Inhibition of CYP3A metabolism of buprenorphine by atazanavir/ritonavir |
(Bruce and Altice, 2006) |
M1, M3=Known metabolites of buprenorphine.