Page 194 - HIV/AIDS Guidelines

Table 15a. Drug Interactions between Protease Inhibitors* and Other Drugs (Page 6 of 11)

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

Rifampin All PIs ↓ PI >75% approximately Do not coadminister rifampin and PIs. Additional RTV
does not overcome this interaction and increases
hepatotoxicity.
Rifapentine All PIs ↓ PI expected Do not coadminister rifapentine and PIs.

Benzodiazepines
All PIs ↑ benzodiazepine possible Consider alternative benzodiazepines such as
Alprazolam RTV (200 mg BID for 2 days) lorazepam, oxazepam, or temazepam.
Diazepam ↑ alprazolam half-life 222% and AUC
248%
Lorazepam All PIs No data These benzodiazepines metabolized via non-CYP450
Oxazepam pathways; less interaction potential compared with other
Temazepam benzodiazepines.
Midazolam All PIs ↑ midazolam expected Do not coadminister oral midazolam and PIs.
SQV/r ↑ midazolam (oral) AUC Parenteral midazolam can be used with caution as a single
1144% and C max 327% dose and can be given in a monitored situation for
procedural sedation.

Triazolam All PIs ↑ triazolam expected Do not coadminister triazolam and PIs.
RTV (200 mg BID)
↑ triazolam half-life 1200% and AUC
2000%
Cardiac Medications
Bosentan All PIs LPV/r ↑ bosentan 48-fold (Day 4) Do not coadminister bosentan and ATV without RTV.
and 5-fold (Day 10) In patients on a PI (other than unboosted ATV) >10
↓ ATV expected days: start bosentan at 62.5 mg once daily or every
other day.
In patients on bosentan who require a PI (other than
unboosted ATV): stop bosentan >36 hours before PI
initiation and restart 10 days after PI initiation at 62.5 mg
once daily or every other day.

RTV, SQV/r RTV (200 mg BID) ↑ digoxin AUC Use with caution. Monitor digoxin levels. Digoxin dose
Digoxin 29% and half-life 43% may need to be decreased.
SQV/r ↑ digoxin AUC 49%
Dihydropyridine All PIs ↑ dihydropyridine possible Use with caution. Titrate CCB dose and monitor closely.
Calcium Channel ECG monitoring is recommended when CCB used with
Blockers (CCBs) ATV.

ATV +/– RTV diltiazem AUC ↑ 125% Decrease diltiazem dose by 50%. ECG monitoring is
recommended.

Diltiazem DRV/r, ↑ diltiazem possible Use with caution. Adjust diltiazem according to
FPV +/– RTV, clinical response and toxicities.
LPV/r, SQV/r,
TPV/r

Guidelines for the Use of Antiretroviral Agents in HIV-1-Infected Adults and Adolescents K-24

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