Antiretroviral treatment in HIV-1 infected pediatric patients: focus on efavirenz

Abstract

Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI), used for the treatment of human immunodeficiency virus (HIV)-1 infection. Approved by the US Food and Drug Administration in 1998, its indication was recently extended to include children as young as 3 months of age. The World Health Organization and many national guidelines consider efavirenz to be the preferred NNRTI for first-line treatment of children over the age of 3 years. Clinical outcomes of patients on three-drug antiretroviral regimens which include efavirenz are as good as or better than those for patients on all other currently approved HIV medications. Efavirenz is dosed once daily and has pediatric-friendly formulations. It is usually well tolerated, with central nervous system side effects being of greatest concern. Efavirenz increases the risk of neural tube defects in nonhuman primates and therefore its use during the first trimester of pregnancy is limited in some settings. With minimal interactions with antituberculous drugs, efavirenz is preferred for use among patients with HIV/tuberculosis coinfection. Efavirenz can be rendered inactive by a single point mutation in the reverse transcriptase enzyme. Newer NNRTI drugs such as etravirine, not yet approved for use in children under the age of 6 years, may maintain their activity following development of efavirenz resistance. This review highlights key points from the existing literature regarding the use of efavirenz in children and suggests directions for future investigation.

Survey of Pretreatment HIV Drug Resistance and Genetic Transmission Network Analysis Among HIV Patients in a High Drug-Use Area of Southwest China

“…EFV and NVP, which are both NNRTIs, had the highest drug resistance rate in this study which was mainly caused by K103N, V179D, V106M and E138G/Q mutations [ 56 , 57 ]. NVP and EFV both have some adverse effects [ 58 - 60 ], but studies showed that they had an effective viral suppression effect in the treatment of HIV-infected individuals [ 61 , 62 ], and the 2015 Guideline for HIV/AIDS Treatment in China recommended first-line ART drugs containing NVP or EFV. Given the high rates of resistance to these drugs, drug resistance monitoring is critical.…”

Synthetic Transformations and Medicinal Significance of 1,2,3-Thiadiazoles Derivatives: An Update

“…Rossignol et al reported that most of the antiviral agents are specifically targeted oriented while some other antivirals have a broad spectrum against a vast variety of viral infections [97]. Some antiviral drugs such as ribavirin (89; Figure 3) are being used against both RNA and DNA viruses [98][99][100], efavirenz (90; Figure 3) used for the treatment of HIV/AIDS [101][102][103] and arbidol (91; Figure 3) was used against influenza viruses [104,105]. Zhan et al prepared 1,2,3-thiadiazole thioacetanilide by adopting a multi-step methodology and exhibited their anti-HIV (Human Immunodeficiency Virus) activity against MT-4 cells.…”

Efavirenz-based simplification after successful early lopinavir-boosted-ritonavir-based therapy in HIV-infected children in Burkina Faso and Côte d’Ivoire: the MONOD ANRS 12206 non-inferiority randomised trial

“…Consequently, we explored whether it would be possible to substitute this initial LPV-based regimen in children with confirmed virological suppression with a once-daily ART that is easier to handle and more acceptable, while saving protease inhibitors for later use if virological failure occurs, in the context of poor access to second-line treatments. We selected efavirenz (EFV) dosed once daily with paediatric-friendly formulations, which is well tolerated and can be used in combination with anti-tuberculous drugs [ 15 ].…”