- Recent Trends and Effectiveness of Antiretroviral Regimens Among Men Who Have Sex With Men Living With HIV in the United States: The Multicenter AIDS Cohort Study (MACS) 2008-2017. [Journal Article]Open Forum Infect Dis 2019; 6(9):ofz333OF
- CONCLUSIONS: Consistent with guidelines, recent cART initiators started with INSTI-cART, which was associated with less switching early after initiation. Factors beyond those studied here, such as need for salvage therapy, unique personal characteristics, drug interactions, and cost may influence treatment decisions.
- LiverTox: Clinical and Research Information on Drug-Induced Liver Injury: Antiviral Agents [BOOK]National Institute of Diabetes and Digestive and Kidney Diseases: Bethesda (MD)BOOK
- The antivirals are a large and diverse group of agents that are typically classified by the virus infections for which they are used, their chemical structure and their mode of action. Most antiviral agents have been developed in the last 20 to 25 years, many as a result of the major research efforts to develop therapies and means of prevention of human immunodeficiency virus (HIV) infection and …
The antivirals are a large and diverse group of agents that are typically classified by the virus infections for which they are used, their chemical structure and their mode of action. Most antiviral agents have been developed in the last 20 to 25 years, many as a result of the major research efforts to develop therapies and means of prevention of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS). Some of the agents developed to treat HIV infection, AIDS and its complications were found to also inhibit other viruses, and the novel approaches taken in development of antiretroviral therapy have been applied to develop therapies of other viral infections. Antiretroviral Agents for HIV Infection. The antiretroviral agents include nucleoside analogues with reverse transcriptase activity (such as tenofovir, emtricitabine, lamivudine, abacavir, stavudine, didanosine, zidovudine), the nonnucleoside reverse transcriptase inhibitors (such as delavirdine, efavirenz, etravirine, nevirapine and rilpivirine), protease inhibitors (atazanavir, darunavir, indinavir, ritonavir, tipranavir and many others), and miscellaneous agents such as maraviroc that inhibits binding of the HIV virus its T cell receptor (CCR5 coreceptor antagonist), enfuvirtide that blocks the uptake of HIV into cells (fusion inhibitor), and integrase inhibitors (raltegravir, elvitegravir and dolutegravir) that block the integrase enzyme of HIV. Hepatitis B Agents. The agents active against hepatitis B virus (HBV) include several nucleoside analogues that are also active against and used to treat HIV infection (tenofovir, emtricitabine, lamivudine), as well as agents that are poorly if at all active against HIV (adefovir, entecavir and telbivudine). Alpha interferon and peginterferon (its long acting pegylated form) are also active against hepatitis B, but are no longer commonly used for this indication.
- In vitro-in vivo correlation of the drug-drug interaction potential of antiretroviral HIV treatment regimens on CYP1A1 substrate riociguat. [Journal Article]Expert Opin Drug Metab Toxicol 2019; 15(11):975-984EO
- CONCLUSIONS: Antiretroviral treatment containing the potent CYP1A1 inhibitor abacavir had the greatest impact on riociguat metabolic clearance. The impact of comedications containing only strong CYP3A4 inhibitors e.g. ritonavir was less pronounced, suggesting a benefit of riociguat over PAH-targeting medications with contraindications for use with strong CYP3A4 inhibitors.
- Lipid profile changings after switching from rilpivirine/tenofovir disoproxil fumarate/emtricitabine to rilpivirine/tenofovir alafenamide/emtricitabine: Different effects in patients with or without baseline hypercholesterolemia. [Journal Article]PLoS One 2019; 14(10):e0223181Plos
- Tenofovir alafenamide (TAF) has similar efficacy compared to tenofovir disoproxil fumarate (TDF), but a less favorable effect on lipids. Aim of this retrospective multicentre study was to evaluate the impact on lipids of switching from rilpivirine (RPV)/ emtricitabine (FTC)/TDF to RPV/FTC/TAF in a cohort of HIV-1 infected patients. Total cholesterol (TC), high density lipoproteins (HDL) and low d…
Tenofovir alafenamide (TAF) has similar efficacy compared to tenofovir disoproxil fumarate (TDF), but a less favorable effect on lipids. Aim of this retrospective multicentre study was to evaluate the impact on lipids of switching from rilpivirine (RPV)/ emtricitabine (FTC)/TDF to RPV/FTC/TAF in a cohort of HIV-1 infected patients. Total cholesterol (TC), high density lipoproteins (HDL) and low density lipoproteins (LDL) were compared at the moment of the switch and at the first following evaluation, by using paired t-test. Overall, 573 patients were considered, 99% with HIV-RNA <50 copies/ml, with mean age of 49.7 (±0.4) years and median 13.4 (6.9-22.5) years of HIV infection. In the study population with available data (431/573, 75%), mean TC changed from 173 ±1.7 to 188 ±1.8 mg/dl; mean HDL from 46 ±0.7 to 51± 0.7 mg/dl; mean LDL from 111 ±1.5 to 120 ±1.8 mg/dl (p<0.0001 for all). Neither LDL/HDL nor TC/HDL ratio changed significantly, with LDL/HDL from 2.6 ±0.5 to 2.5 ±0.5 (p = 0.12) and TC/HDL from 4.0 ±0.6 to 3.9 ±0.6 (p = 0.11). In patients with baseline diagnosis of hypercholesterolemia (TC>200 mg/dl, N = 87), there was no significant change in TC (224 ±2.2 to 228 ±3.4 mg/dl, p = 0.286) or LDL (150±2.5 to 151±3.2 mg/dl, p = 0.751), while HDL increased from 51 ±1.6 to 55 ±1.7 mg/dl (p<0.0001) and both LDL/HDL and TC/HDL ratio decreased significantly, from 3.2±0.1 to 3.0 ±0.1 (p = 0.025) and from 4.7±0.1 to 4.4 ±0.1 (p = 0.004). In this real life study, a slight increase in lipids was found after switching from RPV/FTC/TDF to RPV/FTC/TAF, but these results were not confirmed in people with hypercholesterolemia, in which lipids did not change and LDL/HDL and TC/HDL ratio decreased.
- Dolutegravir/lamivudine (Dovato)--a two-drug complete regimen for HIV-1 infection. [Review]Med Lett Drugs Ther 2019; 61(1579):134-136ML
- Switching from efavirenz to rilpivirine improves sleep quality and self-perceived cognition but has no impact on neurocognitive performances. [Journal Article]AIDS 2020; 34(1):53-61AIDS
- CONCLUSIONS: Our results do not support the hypothesis that switching to RPV improves cognitive function in patient under stable treatment with EFV. Nonetheless, improvements in neuropsychiatric symptoms, sleep quality and self-perceived cognition were observed.
- Pharmacokinetics of Coencapsulated Antiretrovirals with Ingestible Sensors. [Journal Article]AIDS Res Hum Retroviruses 2019AR
- We investigated the use of a system with an ingestible sensor (Proteus Digital Health Feedback system) coencapsulated with antiretrovirals (ARVs) to measure real-time adherence. To assess the safety and impact, if any, coencapsulation might have on ARV concentrations, we evaluated the pharmacokinetics of ARVs coencapsulated with an ingestible sensor for eight commonly used fixed-dose combination …
We investigated the use of a system with an ingestible sensor (Proteus Digital Health Feedback system) coencapsulated with antiretrovirals (ARVs) to measure real-time adherence. To assess the safety and impact, if any, coencapsulation might have on ARV concentrations, we evaluated the pharmacokinetics of ARVs coencapsulated with an ingestible sensor for eight commonly used fixed-dose combination ARVs: emtricitabine (FTC)/tenofovir disoproxil fumarate (TDF); FTC/tenofovir alafenamide (TAF); efavirenz (EFV)/FTC/TDF; abacavir (ABC)/lamivudine (3TC); dolutegravir (DTG)/ABC/3TC; rilpivirine (RPV)/TAF/FTC; elvitegravir (EVG)/cobicistat (COBI)/FTC/TAF; and bictegravir (BIC)/FTC/TAF. The steady-state apparent peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) were determined from plasma concentrations measured at predose, 1, 2, 4, and 6 h postdose, and compared with literature values. A total of 49 unique patients on stable regimens for at least 12 weeks with undetectable viral loads were recruited. Cmax and AUC values were not statistically significantly different from literature values for all of the formulations except the Cmax of FTC/TDF, Cmax of BIC, and the Cmax of RPV. In a subsequent evaluation of FTC/TDF and BIC/FTC/TAF using a crossover design, the geometric mean ratio (GMR) between the coencapsulated and the unencapsulated formulations for FTC/TDF were the following: FTC, 84.6% (90% confidence interval [CI] 66.6-107.4) for AUC and 77.5% (60.1-99.9) for Cmax. For tenofovir (TFV), the GMR was 96.2% (90% CI 89.2-103.8) for AUC and 87.3% (64.2-118.7) for Cmax. The GMR for BIC (from the BIC/FTC/TAF formulation) was 98.0% (90% CI 84.5-113.5) for AUC and 89.9% (84.5-95.7) for Cmax. The observed deviation in FTC/TDF (Truvada) may be due to participant characteristics, fasted/fed conditions, and/or random variation and may warrant further investigations with a larger sample size. These findings provide assurance for use of coencapsulated ARVs for future HIV treatment-adherence research.
- Drug-Drug Interactions of Glecaprevir and Pibrentasvir Coadministered with Human Immunodeficiency Virus Antiretrovirals. [Journal Article]J Infect Dis 2019JI
- CONCLUSIONS: Atazanavir is contraindicated with glecaprevir/pibrentasvir and use of boosted protease inhibitors or efavirenz is not recommended. No clinically significant interactions were observed with other studied antiretrovirals.
- Choice of the initial antiretroviral treatment for HIV-positive individuals in the era of integrase inhibitors. [Journal Article]PLoS One 2019; 14(8):e0221598Plos
- CONCLUSIONS: The choice of initial ART regimens is consistent with Spanish guidelines' recommendations, but is also clearly influenced by physician's perception based on patient's clinical and sociodemographic variables and by the prescribing hospital location.
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- Tenofovir DF/emtricitabine/rilpivirine as HIV post-exposure prophylaxis: results from a multicentre prospective study-authors' response. [Journal Article]J Antimicrob Chemother 2019; 74(11):3403-3404JA