Page 193 - HIV/AIDS Guidelines

Table 15a. Drug Interactions between Protease Inhibitors* and Other Drugs (Page 5 of 11)

Concomitant Effect on PI or Concomitant Drug Dosing Recommendations and Clinical
Drug PI Concentrations Comments

Anti-mycobacterials

ATV +/− RTV clarithromycin AUC ↑ 94% May cause QTc prolongation. Reduce
clarithromycin dose by 50%. Consider
alternative therapy (e.g., azithromycin).
DRV/r, FPV/r, DRV/r ↑ clarithromycin AUC 57% Monitor for clarithromycin-related toxicities
LPV/r, SQV/r, FPV/r ↑ clarithromycin possible or consider alternative macrolide (e.g.,
TPV/r LPV/r ↑ clarithromycin expected azithromycin).
Clarithromycin RTV 500 mg BID ↑ clarithromycin 77%
SQV unboosted ↑ clarithromycin 45% Reduce clarithromycin dose by 50% in
TPV/r ↑ clarithromycin 19% patients with CrCl 30−60 mL/min.
clarithromycin ↑ unboosted SQV 177% Reduce clarithromycin dose by 75% in
clarithromycin ↑ TPV 66% patients with CrCl <30 mL/min.

FPV APV AUC ↑ 18% No dosage adjustment necessary.

RTV-boosted PIs
ATV/r rifabutin (150 mg once daily)
AUC ↑ 110% and metabolite
AUC ↑ 2101% compared with rifabutin (300
mg daily) administered alone

DRV/r rifabutin (150 mg every other day) AUC not
significantly changed and metabolite AUC ↑
881% compared with rifabutin (300 mg once Rifabutin 150 mg once daily or 300 mg three
daily) administered alone times a week. Monitor for antimycobacterial
activity and consider therapeutic drug
FPV/r rifabutin (150 mg every other day) and monitoring.
metabolite AUC ↑ 64% compared with
Rifabutin rifabutin (300 mg once daily) administered PK data reported in this table are results from
alone healthy volunteer studies. Lower rifabutin
exposure has been reported in HIV-infected
LPV/r rifabutin (150 mg once daily) and metabolite patients than in the healthy study participants.
AUC ↑ 473% compared with rifabutin (300
mg daily) administered alone

SQV/r ↑ rifabutin with unboosted SQV
TPV/r rifabutin (150 mg x 1 dose) and metabolite
AUC ↑ 333%

PIs without RTV
ATV, FPV ↑ rifabutin AUC expected Rifabutin 150 mg daily or 300 mg three times a
week

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents K-23

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