Page 198 - HIV/AIDS Guidelines

Table 15a. Drug Interactions between Protease Inhibitors* and Other Drugs (Page 10 of 11)

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

RTV-boosted PIs

ATV/r, DRV/r, ATV/r, DRV/r, FPV/r Opioid withdrawal unlikely but may occur. No
d
FPV/r, LPV/r, ↓ R-methadone AUC 16%−18%; adjustment in methadone usually required but
SQV/r, TPV/r LPV/r ↓ methadone AUC 26%–53%; monitor for opioid withdrawal and increase methadone
SQV/r 1000/100 mg BID dose as clinically indicated.
d
↓ R-methadone AUC 19%;
d
TPV/r ↓ R-methadone AUC 48%
Methadone
PIs without RTV
ATV No significant effect No dosage adjustment necessary.
FPV No data with unboosted FPV Monitor and titrate methadone as clinically indicated.
d
APV ↓ R-methadone C min 21%, AUC no The interaction with FPV is presumed to be similar.
significant change

Phosphodiesterase Type 5 (PDE5) Inhibitors
All PIs DRV/r + sildenafil 25 mg similar to sildenafil For treatment of erectile dysfunction
100 mg alone; Start with sildenafil 25 mg every 48 hours and
RTV 500 mg BID ↑ sildenafil AUC 1000%; monitor for adverse effects of sildenafil.
Sildenafil
SQV unboosted ↑ sildenafil AUC 210%
For treatment of PAH
Contraindicated
All PIs RTV 200 mg BID ↑ tadalafil AUC 124%; For treatment of erectile dysfunction
TPV/r (1st dose) ↑ tadalafil AUC 133%; Start with tadalafil 5-mg dose and do not exceed a
TPV/r steady state: no significant effect single dose of 10 mg every 72 hours. Monitor for
adverse effects of tadalafil.
For treatment of PAH
In patients on a PI >7 days:
Start with tadalafil 20 mg once daily and increase to
40 mg once daily based on tolerability.
Tadalafil
In patients on tadalafil who require a PI:
Stop tadalafil >24 hours prior to PI initiation, restart
7 days after PI initiation at 20 mg once daily, and
increase to 40 mg once daily based on tolerability.
For treatment of benign prostatic hyperplasia
Maximum recommended daily dose is 2.5 mg per
day
Vardenafil All PIs RTV 600 mg BID ↑ vardenafil AUC Start with vardenafil 2.5 mg every 72 hours and
49-fold monitor for adverse effects of vardenafil.

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents K-28

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