Second-generation HIV protease inhibitor
ATC code: J05AE10 (Darunavir)
Brand names
Prezista, Prezcobix
Highly selective HIV-1 protease inhibitor with an improved resistance profile – active against strains resistant to earlier protease inhibitors. Metabolised by CYP3A4; itself inhibits CYP3A4 and CYP2D6. Always given with a pharmacokinetic booster (ritonavir or cobicistat).
Second line
Darunavir is a second-line HIV-1 protease inhibitor. GeSIDA 2024 recommends darunavir-based combinations (Symtuza, Rezolsta, Prezcobix) in patients with resistance to earlier protease inhibitors or when an integrase-inhibitor-free regimen is required. Booster (ritonavir 100 mg or cobicistat 150 mg) is mandatory.
4 pairs found. Sorted from critical to minor.
Mechanism
Carbamazepine is a strong CYP3A4 inducer. Darunavir falls 50% – ART failure and resistance risk.
Symptoms
Rising viral load.
Management
Combination contraindicated. Alternative anticonvulsant – levetiracetam.
Mechanism
CYP3A4 inhibition – fatal ergotism.
Symptoms
Limb ischaemia, stroke.
Management
Combination contraindicated.
Mechanism
Strong CYP3A4 induction – darunavir falls 80%. ART failure.
Symptoms
Rising viral load.
Management
Combination contraindicated. Alternative – rifabutin.
Mechanism
Darunavir inhibits CYP3A4. Simvastatin rises 10+ fold – fatal rhabdomyolysis.
Symptoms
Myalgia, CK above 50× ULN.
Management
Combination contraindicated. Pravastatin or rosuvastatin.
Opens the checker prefilled with this drug. Pick the second one from your regimen.
Can be used in pregnancy at the discretion of HIV specialist. Pregnancy registry shows no significant increase in defects.
Breastfeeding by HIV-positive women not recommended in Spain.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Darunavir is evaluated for the following indications with varying evidence strength: HIV infection (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Darunavir (≥ 1 in 100): Diarrhoea, Nausea, Headache, Rash, Transaminase rise. See the Safety section for uncommon and serious reactions.
FDA category C. Can be used in pregnancy at the discretion of HIV specialist. Pregnancy registry shows no significant increase in defects.
Breastfeeding by HIV-positive women not recommended in Spain.
Darunavir is contraindicated in: Simvastatin, lovastatin; Pimozide, ergotamine, dihydroergotamine, oral midazolam, cisapride; Rifampicin, St John's wort (loss of ARV effect); Severe hepatic impairment. Full list in the Safety section.