Pulmonary Antihypertensives & ARVs

Legend
↑     Potential elevated exposure of the pulmonary antihypertensive
↓     Potential decreased exposure of the pulmonary antihypertensive
↔   No significant effect
D     Potential decreased exposure of ARV drug
E     Potential elevated exposure of ARV drug

Numbers refer to increased or decreased AUC as observed in drug-drug interaction studies

ATV/c:
ATV co-formulated with COBI (300/150 mg qd)

DRV/c:
DRV co-formulated with COBI (800/150 mg qd)

CAB/RPV:
CAB and RPV im long acting injections

ERA (endothelin receptor antagonists)
Ipr (IP receptor agonists)
PA (prostacyclin analogues)
PDE5 (phosphodiesterase type 5 inhibitors)
sGC (soluble guanylate cyclase stimulators)

Interactions with ABC, FTC, 3TC, ZDV
ABC, FTC, 3TC, ZDV:
No clinically relevant interactions expected

Interactions with cabotegravir (oral)
None

Interactions with ibalizumab
None

Comments

1. Co-administration is not recommended in the European labels, but the US labels suggest the following dose modifications: When starting bosentan in persons already on PI/b or EVG/c use a bosentan dose of 62.5 mg qd or every other day. Discontinue bosentan at least 36 h prior to starting PI/b or EVG/c and restart after at least 10 days at 62.5 mg qd or every other day.
2. Potential additive liver toxicity.
3. Exposure of parent drug increased but exposure of active metabolite unchanged.
4. This change is unlikely to be clinically relevant.

^ LEN causes moderate inhibition of CYP3A4 and, when discontinued, remains in the circulation for prolonged periods. Residual concentrations of LEN may affect the exposure of sensitive CYP3A4 substrates and/or narrow therapeutic index drugs that are initiated within 9 months after the last subcutaneous dose of LEN.

# At least a 2-week (moderate inducers) or 4-week (strong inducers) cessation period is recommended prior to initiation of LEN due to the persisting inducing effect after discontinuation of an inducer.

Further Information
For additional drug-drug interactions and for more detailed pharmacokinetic interaction data and dosage adjustments, please refer to: http://www.hiv-druginteractions.org (University of Liverpool)