darunavir
Sources réglementaires consultées
Indications approuvées
- Traitement combiné de l’infection par le VIH-1, toujours potentialisé par ritonavir et associé à d’autres antirétroviraux.
Contre-indications
Absolues
- Hypersensibilite ; insuffisance hépatique severe ; associations CYP3A expressement contre-indiquees, notamment rifampicine, millepertuis, simvastatine/lovastatine, pimozide, midazolam oral, triazolam, dérivés de l’ergot, lopinavir/ritonavir, sildenafil pour hypertension arterielle pulmonaire, ticagrelor et colchicine en insuffisance rénale ou hépatique.
Mises en garde cliniques
- Il peut provoquer une hépatite sévère ou mortelle ; surveiller la fonction hépatique, surtout en cas d’hépatite B/C ou d’hépatopathie préalable. — CIMA/AEMPS, ficha técnica 82143
- Il peut provoquer éruption, DRESS, SJS/TEN et réactions liées aux sulfamides ; arrêter en cas de réaction grave. — CIMA/AEMPS, ficha técnica 82143
Interactions médicamenteuses
- SévèreSubstrats, inhibiteurs ou inducteurs du CYP3A
Mécanisme: Le darunavir potentialisé provoque des interactions bidirectionnelles cliniquement importantes.
Recommandation: Effectuer une conciliation complète, éviter les associations contre-indiquées et adapter celles qui sont permises.
CIMA/AEMPS, ficha técnica 82143
Effets indésirables
Communs (≥1%)
Diarrhée, nausées, céphalées et éruption
Rares mais graves
Hépatite, DRESS, SJS/TEN, pancréatite et saignement dans l’hémophilie
Grossesse et allaitement
Il peut être utilisé pendant la grossesse avec ritonavir lorsqu’il est indiqué. Ne pas extrapoler les schémas avec cobicistat. Ne pas allaiter en cas de VIH sous traitement.
Bibliographie récente (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.