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Psychoactive Medications: ARV Interactions

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Psychoactive Medications: ARV Interactions

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Class of MedicationInteractionsComments
Antidepressants
SSRI

Citalopram, escitalopram:

  • RTV causes no change in levels

Fluoxetine:

  • RTV: ↑ RTV AUC 19%, no change in Cmax

Paroxetine:

  • DRV/r: paroxetine AUC and Cmin ↓ 38%
  • FPV/r: paroxetine AUC ↓ 58%

Sertraline:

  • DRV/r: sertraline AUC and Cmin ↓ 49%
Interactions with ARVs are incompletely studied.

RTV may ↑ SSRI levels; this usually is not significant but there are case reports of SSRI toxicity. Start at low dosage, monitor for adverse effects.

No dosage adjustment of citalopram or escitalopram required.

Titrate paroxetine to effect.




Titrate sertraline to effect.
SNRIVenlafaxine, duloxetine:
  • No data; PIs may ↑ SNRI levels
Start at low dosage, use lowest effective dosage; monitor for adverse effects.
Tricyclic (TCA)Amitriptyline, nortriptyline, imipramine, desipramine, and others:
  • NFV, RTV known to ↑ TCA levels; other PIs may ↑ TCA levels
Start at low dosage, use lowest effective dosage; monitor for adverse effects.
Other antidepressantsBupropion:
  • EFV: ↓ bupropion AUC 55%
  • TPV: ↓ bupropion AUC 46%
  • LPV: ↓ bupropion AUC 57%
Monitor for efficacy; may need increased dosage.
Mirtazapine:
  • No data; RTV may ↑ mirtazapine levels
Start at low dosage, use lowest effective dosage; monitor for adverse effects.
Nefazodone:
  • RTV may ↑ nefazodone levels
  • Nefazodone may ↑ MVC levels
  • Start at low dosage, use lowest effective dosage; monitor for adverse effects.
  • MVC dosage: 150 mg BID
Trazodone:
  • RTV: ↑ trazodone AUC >200%
  • DRV, IDV, LPV/r: ↑ trazodone AUC
  • SQV/r may ↑ trazodone and ↑ risk of arrhythmia
Start at low dosage, use lowest effective dosage; monitor for adverse effects.






Avoid trazodone for patients taking SQV/r.
St. John's wort:
  • Substantial ↓ in levels of most PIs, NNRTIs, and MVC
Do not coadminister.
Sedatives, Hypnotics
Benzodiazepine



Midazolam:
  • SQV/r: ↑ oral midazolam AUC 1,144%
  • Other PIs: large ↑ in serum midazolam levels expected
Higher risk of benzodiazepine adverse effects in elderly patients; avoid if possible,


Avoid midazolam and triazolam for patients taking PIs. For procedures, may consider single-dose IV midazolam with close monitoring.
Triazolam:
  • RTV: ↑ triazolam half-life 1,900%; ↑ AUC 20%
  • Other PIs: large ↑ in serum triazolam levels expected
Alprazolam:
  • RTV: ↑ alprazolam half-life 200%
Avoid for patients taking PIs.
Diazepam:
  • All PIs: ↑ diazepam levels
  • ETR: ↑ diazepam levels
  • Start at low dosage, use lowest effective dosage; monitor for adverse effects.
  • Alternatives:
  • Consider use of the following benzodiazepines: lorazepam, oxazepam, temazepam (these benzodiazepines are, in part, metabolized via non-CYP450 pathways; lower potential for interactions). Start at low dosage, use lowest effective dosage; monitor for adverse effects.
OtherZolpidem:
  • RTV: ↑ zolpidem AUC 27%
Start at low dosage, use lowest effective dosage; monitor for adverse effects.
Antipsychotics: Few data on interactions between ARVs and antipsychotics
Olanzapine:
  • RTV: ↓ olanzapine AUC 53%, half-life ↓ 50%
Start at low dosage, use lowest effective dosage; monitor for adverse effects.
Pimozide:
  • PIs and EFV may ↑ pimozide levels
Contraindicated with PIs and with EFV.

From Psychoactive Medications: ARV Interactions
Primary Care of Veterans with HIV
Office of Clinical Public Health Programs
Veterans Health Administration, 2009