Table 3. Antiretrovirals that can be or cannot be used by crushing or dissolving.
Antiretrovirals | Information | References | |
---|---|---|---|
STR | |||
BIC/TAF/FTC | Dissolving in water and taking it immediately can be considered | [37] | |
DTG/ABC/3TC | Can be crushed and administered with enteral nutrition | [38] | |
DTG/3TC | Can be crushed and administered with enteral nutrition | [38] | |
DOR/TDF/3TC | There has yet to be PK data on crushed and dissolved. The tablet must be swallowed whole | [43] | |
NRTI | |||
TAF/FTC | Dissolving in water and taking it immediately can be considered. Crushing tablets could reduce the TAF bioavailability but does not significantly impact TAF/FTC PK | [37,42] | |
TDF/FTC | Dissolving in water and taking it immediately can be considered | [18] | |
3TC | Can be crushed and administered with enteral nutrition | [38] | |
FTC | Dissolving in water and taking it immediately can be considered | [37] | |
ABC | Can be crushed and administered with enteral nutrition | [38] | |
INSTI | |||
DTG | Can be crushed and administered with enteral nutrition. Crushing DTG leads to higher DTG exposure but does not exceed exposure intake with food or twice-daily dosing | [38] | |
RAL | Chewing the tablets has higher drug absorption and lower drug inter-subject PK variability | [44] | |
PI | |||
DRV | Can be crushed and administered with enteral nutrition | [39,40,41] | |
DRV/c | Can be crushed and administered with enteral nutrition | [42] | |
LPV/r | Significantly lower AUC with crushed tablets | [45] | |
NNRTI | |||
DOR | Crushing or dissolving tablets is not recommended | [43] | |
ETV | Dispersed in ≥5 mL water showed bioequivalence to the whole tablet | [46] |
STR, single-tablet regimen; BIC, bictegravir; TAF, tenofovir alafenamide; FTC, emtricitabine; DTG, dolutegravir; ABC, abacavir; 3TC, lamivudine; DOR, doravirine; TDF, tenofovir disoproxil fumarate; PK, pharmacokinetics; NRTI, nucleoside reverse transcriptase inhibitors; INSTI, integrase strand transfer inhibitor; RAL, raltegravir; PI, protease inhibitor; DRV, darunavir; DRV/r, ritonavir boosted darunavir; DRV/c, cobicistat boosted darunavir; LPV/r, ritonavir boosted lopinavir; NNRTI, non-nucleoside reverse transcriptase inhibitors; ETV, etravirine.