Darunavir is a second-generation protease inhibitor, boosted by ritonavir. It has activity against many strains resistant to other protease inhibitors and a high genetic barrier to resistance.
Also known as: Prezista, DRV
Ketoconazole may raise darunavir levels via CYP3A4 inhibition. Limit ketoconazole dose to 200 mg/day.
Ketoconazole is a potent CYP3A4 inhibitor. Darunavir, when boosted by ritonavir or cobicistat, already has significantly elevated plasma levels. Adding ketoconazole may cause excessive accumulation, increasing the risk of side effects (nausea, hepatotoxicity, QT prolongation). The darunavir label (Prezista) recommends limiting ketoconazole dose to 200 mg/day when coadministered. Preferred alternative: itraconazole (different metabolism) or topical antifungals. If ketoconazole is necessary, monitor transaminases and signs of toxicity.
Darunavir + ketoconazole: CYP3A4 inhibition may raise darunavir levels. Limit ketoconazole to 200 mg/day.
Ketoconazole is a potent CYP3A4 inhibitor. Darunavir (boosted by ritonavir) already has elevated levels — adding ketoconazole may cause toxicity.
Transaminases, toxicity symptoms (nausea, jaundice).
Hepatotoxicity, excessive elevation of darunavir levels.
Limit ketoconazole to 200 mg/day. Monitor liver function and signs of toxicity.
DailyMed/FDA (NIH/NLM) — approved Darunavir (Prezista) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=814301f9-c990-46a5-b481-2879a521a16f
Food slightly increases darunavir absorption. Can be taken with or without food.
Can be taken with or without food. Do not chew or crush the tablets.
DailyMed/FDA (NIH/NLM) — approved Darunavir (Prezista) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=814301f9-c990-46a5-b481-2879a521a16f
No documented disease interactions.
Limited human data. Animal studies did not demonstrate teratogenicity. Can be used when other options are exhausted.
Can be used in the 2nd and 3rd trimesters with caution. 1st trimester data are limited.
Excreted in breast milk. Artificial feeding is recommended for HIV-positive mothers.
Reliable contraceptive methods are recommended.
DailyMed/FDA (NIH/NLM) — approved Darunavir (Prezista) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=814301f9-c990-46a5-b481-2879a521a16f
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Darunavir is a second-generation protease inhibitor with a high genetic barrier to resistance, boosted by ritonavir or cobicistat.
Binds to multiple residues of HIV-1 protease, maintaining activity against strains resistant to other PIs. Ritonavir or cobicistat boost darunavir exposure by inhibiting CYP3A4.
Oral bioavailability: 82% (with ritonavir). Tmax: 2.5-4 hours. Food slightly increases absorption. Plasma protein binding 95%.
Metabolised by CYP3A4 (primarily) and CYP2D6. Boosted by ritonavir or cobicistat (CYP3A4 inhibitors). Dose is adjusted depending on the booster used.
Half-life: 15 hours (with ritonavir). Elimination: ~80% faeces, ~14% urine. Monitor lipid profile.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
