Darunavir can cause transient and usually asymptomatic elevations in serum aminotransferase levels and has been linked to rare instances of clinically apparent, acute liver injury. In HBV or HCV coinfected patients, highly active antiretroviral therapy with darunavir may result of an exacerbation of the underlying chronic hepatitis B or C.
Darunavir (dar ue' na vir) is a proteinomimetic, azapeptide that blocks the catalytic site of the HIV protease preventing cleavage of viral polyprotein precursors into mature, functional proteins that are necessary for viral replication. When given in combination with other antiretroviral agents, darunavir has been shown to lower HIV RNA levels and delay onset of AIDS related complications.
Darunavir was approved for use in the United States in 2003 and is indicated for the treatment of HIV, typically in combination with low “booster” doses of ritonavir, a potent CYP 3A4 inhibitor. Darunavir is available under the brand name Prezista in tablets of 75, 150, 400, 600 and 800 mg and as an oral suspension (100 mg/mL).
The usual adult dosage is 800 mg with ritonavir (100 mg) once daily. Higher doses and twice daily administration are sometimes recommended for patients with darunavir resistance mutations. A fixed combination of darunavir (800 mg) with the CYP 3A4 inhibitor cobicistat (150 mg) was approved for use in HIV infection in 2016 under the brand name Prezcobix, the recommended dose being one tablet daily.
Common side effects of darunavir are nausea, diarrhea, gastrointestinal upset, headache, fatigue, rash and, with long term use, hyperlipidemia and lipodystrophy. Severe adverse events can include hypersensitivity reactions including Stevens Johnson syndrome. The combination of darunavir with a CYP 3A4 inhibitor also predisposes to significant drug-drug interactions.
Drugs for HIV Infection, in the Subclass Antiretroviral Agents
- Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
- Nucleoside Analogues (HIV)
- Protease Inhibitors (HIV)
HCV NS5A Inhibitors
HCV NS5B (Polymerase) Inhibitors
- Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir
Drugs for Herpes Virus Infections (HSV, CMV, others)
Drugs for Influenza