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ANTIINFECTIVES FOR SYSTEMIC USE › ANTIVIRALS FOR SYSTEMIC USE › DIRECT ACTING ANTIVIRALS › Protease inhibitors
darunavir
J05AE10
Forms & Strengths
- Oral Tablets: 75 mg, 150 mg, 600 mg, 800 mg
- Oral Suspension: 100 mg/mL
Adult Dosing
- Treatment-naive or experienced with no darunavir resistance mutations: 800 mg co-administered with ritonavir (100 mg) or cobicistat (150 mg) once daily with food
- Treatment-experienced with at least one darunavir resistance mutation: 600 mg co-administered with ritonavir (100 mg) twice daily with food
Pediatric Dosing
- Patients 3 years of age and older weighing at least 15 kg: Dosing based on weight and treatment history, co-administered with ritonavir
- Not recommended in patients under 3 years of age due to toxicity concerns
Indications
- Treatment of HIV-1 infection in antiretroviral treatment-naive and treatment-experienced adult and pediatric patients aged 3 years and older
- Must be co-administered with ritonavir or cobicistat and other antiretroviral agents
Mechanism of Action
- Human immunodeficiency virus (HIV-1) protease inhibitor
- Inhibits the cleavage of Gag-Pol polyproteins, preventing the formation of mature, infectious viral particles
Contraindications
- Co-administration with drugs highly dependent on CYP3A for clearance and for which elevated plasma concentrations are associated with serious/life-threatening events (e.g., alfuzosin, amiodarone, colchicine, dronedarone, ivabradine, lomitapide, lovastatin, simvastatin, sildenafil for PAH, triazolam, oral midazolam, pimozide, ergot derivatives)
- Patients with severe hepatic impairment (Child-Pugh Class C)
- Known hypersensitivity to darunavir or ritonavir
Adverse Reactions
- Common: Diarrhea, nausea, rash, headache, abdominal pain, fatigue
- Serious: Severe skin reactions (Toxic Epidermal Necrolysis, Stevens-Johnson Syndrome, DRESS), hepatotoxicity, diabetes mellitus/hyperglycemia, immune reconstitution inflammatory syndrome, hemophilia bleeding complications
Drug Interactions
- CYP3A inhibitors and inducers (e.g., rifampin, St. John's wort significantly decrease darunavir levels)
- HMG-CoA reductase inhibitors (statins like atorvastatin, rosuvastatin require dose adjustments or caution)
- Antiarrhythmics, anticonvulsants (carbamazepine, phenobarbital, phenytoin decrease darunavir efficacy)
- Direct oral anticoagulants (DOACs) and certain antiplatelets may have altered concentrations
- Coadministration with other antiretrovirals requires careful monitoring for overlapping toxicities and pharmacokinetic alterations
Curated Content: Needs Vetting Before Put to Clinical Use