RESUMO
Darunavir is a synthetic non-peptidic protease inhibitor that has been shown to be extremely potent against wild-type HIV, and it is an important component of highly active antiretroviral treatment (HAART), which is considered as one of the most significant advances in the field of HIV therapy. However, there are some concerns about darunavir quality control. Darunavir shows pseudo-polymorphism: in different ambient conditions one pseudo-polymorphic form can change to another. This behavior of darunavir is problematic because the dosage form is exposed to different ambient conditions around the world, since HIV/AIDS is prevalent globally. Issues around differences in the solubility and effects that different forms of darunavir can cause are of concern, and a more stable form is preferable. Important investigations of darunavir such as dissolution behavior, polymorphism, stability and degradation studies, and the impact of that on the quality of the product are being conducted by our working group. A cure for HIV/AIDS remains a long-term commitment, and there is much yet to achieve. This article discusses, by a critical review of the literature, the impact of the use of darunavir in the treatment of HIV-infected patients, its physical-chemical properties, the analytical methods to determine it, and challenges that remain in order to ensure the quality and stability of darunavir.
Assuntos
Inibidores da Protease de HIV , Sulfonamidas , Darunavir , Sistemas de Liberação de Medicamentos , Infecções por HIV/tratamento farmacológico , Inibidores da Protease de HIV/administração & dosagem , Inibidores da Protease de HIV/análise , Inibidores da Protease de HIV/química , Humanos , Controle de Qualidade , Sulfonamidas/administração & dosagem , Sulfonamidas/análise , Sulfonamidas/químicaRESUMO
Darunavir is a synthetic nonpeptidic protease inhibitor which has been shown to be extremely potent against wild-type HIV as well as a large panel of PI-resistant clinical isolates and shows a high genetic barrier to the development of antiretroviral resistance. The treatment of HIV/AIDS requires combinations of multiple antiretroviral drugs. In addition, patients frequently need to coadminister other medications for reasons including the prevention or treatment of opportunistic infections, treatment of concomitant illnesses and management of antiretroviral side effects. Drug interactions have been observed between darunavir and other drugs. New and more comprehensive drug interaction studies will be required since the increase in life expectancy of patients often brings new comorbidities and the concomitant use of different drugs. This paper discusses the impact of the use of darunavir in the treatment of HIV-infected patients, its pharmacological and physical-chemical properties, its drug interactions, and challenges that remain in order to ensure safety and compliance of treatment.