darunavir
Regulatory sources consulted
Approved indications
- Combination treatment of HIV-1 infection, always boosted with ritonavir and with other antiretrovirals.
Contraindications
Absolute
- Hypersensitivity; severe hepatic impairment; expressly contraindicated CYP3A combinations, including rifampin, St John s wort, simvastatin/lovastatin, pimozide, oral midazolam, triazolam, ergots, lopinavir/ritonavir, sildenafil for pulmonary arterial hypertension, ticagrelor, and colchicine in renal or hepatic impairment.
Clinical warnings
- It may cause severe or fatal hepatitis; monitor liver function, especially with hepatitis B/C or prior liver disease. — CIMA/AEMPS, ficha técnica 82143
- It may cause rash, DRESS, SJS/TEN, and sulfonamide reactions; discontinue for severe reactions. — CIMA/AEMPS, ficha técnica 82143
Drug interactions
- HighCYP3A substrates, inhibitors, or inducers
Mechanism: Boosted darunavir causes clinically important bidirectional interactions.
Recommendation: Perform complete reconciliation, avoid contraindicated combinations, and adjust permitted ones.
CIMA/AEMPS, ficha técnica 82143
Adverse events
Common (≥1%)
Diarrhea, nausea, headache, and rash
Rare but serious
Hepatitis, DRESS, SJS/TEN, pancreatitis, and bleeding in hemophilia
Pregnancy and lactation
It may be used during pregnancy with ritonavir when clinically indicated. Do not extrapolate cobicistat regimens. Do not breastfeed if you have HIV and receive treatment.
Recent literature (PubMed)
The COVID-19 pandemic has been inflicted upon humanity by the SARS-CoV-2 virus, the latest insidious incarnation of the coronaviruses group. While in its wake intense scientific research has produced breakthrough vaccines and cures, there still exists an immediate need to further understand the origin, mechanobiology and biochemistry, and destiny of this virus so that future pandemics arising from similar coronaviruses may be contained more effectively. In this Perspective, we discuss the various evidential findings of virus propagation and connect them to respective underpinning cellular biomechanical states leading to corresponding manifestations of the viral activity. We further propose avenues to tackle the virus, including from a "musical" vantage point, and contain its relentless strides that are currently afflicting the global populace.
Microbial infections continue to pose significant threats to global health, necessitating the development of innovative therapeutic strategies. One promising avenue is the use of protease inhibitors, with darunavir (DRV) emerging as a potent candidate in the field. Designed to combat resistance to standard HIV therapy, DRV is a second-generation protease inhibitor. Regarding microbial infections, this study sheds light on the internal processes behind the impact of DRV within cells. Novel protease inhibitor DRV targets essential proteolytic enzymes that are essential for microbial survival and growth in order to achieve its antimicrobial actions. By interfering with the proteolytic digestion of important microbial proteins, its inhibitory effect prevents infectious particles from being assembled and maturing. DRV is a viable treatment option for microbial infections as its selective suppression reduces the possibility of off-target consequences. DRV efficiently penetrates the intracellular milieu of host cells, where it prevents the proteolytic cleavage of vital viral and bacterial proteins, hence combating pathogenic infections. Microbial infections may be treated in a variety of ways using DRV as it disrupts the cycle of pathogen reproduction. The present review explores the molecular principles behind the effectiveness of DRV against microbial infections, emphasizing the drug's ability to fight a wide range of pathogens. The comprehension of the intracellular activity of DRV is promising for the creation of novel treatment approaches, providing encouragement in the continuous fight against microbial diseases.