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Antimicrobials during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
An integrase inhibitor, elvitegravir is used to treat HIV infection. 213 women used it during the first trimester (Antiretroviral Registry, 2018). The frequency of congenital anomalies was not increased above background (www.apregistry.com/forms/interim_report.pdf).
Human immunodeficiency virus (HIV)
Published in Hung N. Winn, Frank A. Chervenak, Roberto Romero, Clinical Maternal-Fetal Medicine Online, 2021
Richard Basilan, William Salzer
Nucleoside reverse transcriptase inhibitors (NRTIs) were the first drugs active against HIV to be developed with the introduction of zidovudine or azidothymidine in 1987. The NRTIs are nucleoside analogs and require intracellular phosphorylation in order to become active. They are incorporated into the DNA chain and terminate DNA chain elongation by acting as nonactive substrates for the viral reverse transcriptase. Nonnucleoside reverse transcriptase inhibitors (NNRTIs), on the other hand, bind to the reverse transcriptase enzyme and induce conformational changes at the active site, thereby rendering the enzyme nonfunctional. Protease inhibitors (PIs) target the viral protease, an enzyme required for cleavage of precursor proteins (gag and gag-pol), thereby preventing the final assembly of the inner core of viral particles (22). Entry inhibitors block the penetration of HIV virions into their target cells by either preventing fusion (enfuvirtide) or by blocking the CCR5 coreceptor required for entry (Maraviroc). A newer class of ARVs act by inhibiting the enzyme required for integration of the transcribed viral genome into the host DNA (integrase), aptly named integrase inhibitors. Available ARV agents are summarized in Table 1.
Efavirenz
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Alan C. Street, Irani Thevarajan
Integrase inhibitors are potent and well-tolerated agents with few drug interactions, and over the past few years evidence has accumulated of their superiority over the previous gold standard of efavirenz when combined with two nucleoside/nucleotide agents for initial antiretroviral therapy. The three integrase inhibitors in current use are raltegravir, elvitegravir, and dolutegravir.
The association between neutrophil to lymphocyte ratio and endothelial dysfunction in people living with HIV on stable antiretroviral therapy
Published in Expert Review of Anti-infective Therapy, 2022
Vanessa Bianconi, Elisabetta Schiaroli, Massimo R. Mannarino, Amirhossein Sahebkar, Francesco Paciosi, Sara Benedetti, Ettore Marini, Matteo Pirro, Daniela Francisci
At the enrollment the median CD4 T cell count was 609 cells/µL (versus 332 cells/µL before ART initiation) and HIV-1 RNA was undetectable in 88% of patients. The median ART duration was 8 years. Among PLWH with undetectable HIV-1 RNA levels, viral suppression had been documented since a median of 98 (48–180) months. At the enrollment 36%, 34%, and 29% of patients were receiving an integrase inhibitor-based, a non-nucleoside reverse transcriptase inhibitor-based, and a protease inhibitor-based ART regimen for at least six months, respectively. The median NLR value was 1.47 and the median bFMD value was 4.55%. Table 1 shows the characteristics of the study population dichotomized according to the median NLR value [i.e. high-NLR group (NLR ≥1.47) and low-NLR group (NLR <1.47)]. Fasting glucose levels were significantly higher in the high-NLR group as compared to the low-NLR group (p = 0.011). Significantly lower pre-ART CD4 T cell counts emerged in the high-NLR group as compared to the low-NLR group (p = 0.021). A borderline significantly older age was found in the high-NLR group as compared to the low-NLR group (p = 0.052).
Antiretroviral treatment for HIV infection: Swedish recommendations 2019
Published in Infectious Diseases, 2020
Jaran Eriksen, Christina Carlander, Jan Albert, Leo Flamholc, Magnus Gisslén, Lars Navér, Veronica Svedhem, Aylin Yilmaz, Anders Sönnerborg
HIV-drugs are categorized into six groups according to their antiretroviral activity into six groups (Table 1). Cross-resistance is not seldom seen within these groups, but not between groups. Virus entry into the cell can be inhibited by enfuvirtide (which blocks fusion by binding to the viral surface protein gp41), ibalizumab (a monoclonal anti-CD4-antibody that prevents HIV from infecting the cell – currently not available in Sweden) and maraviroc (binding to the cell’s CCR5-receptor thus preventing entry of CCR5-trophic virus). These medicines are rarely used. Nucleoside reverse transcriptase inhibitors (NRTI) and non-nucleoside reverse transcriptase inhibitors (NNRTIs) inhibit reverse transcriptase (RT) (which synthesizes HIV DNA using HIV RNA as a template). Integrase inhibitors (INSTI) block the virus-specific enzyme integrase, thereby preventing viral DNA from being integrated into cellular DNA. Finally, protease inhibitors (PI) inhibit the viral protease and thereby the production of mature virus.
Current pharmacotherapy for the treatment of dyslipidemia associated with HIV infection
Published in Expert Opinion on Pharmacotherapy, 2019
Anna Gebhardt, Carl J. Fichtenbaum
Current guidelines for the use of antiretroviral therapy recommend regimens that tend to minimize the risk of alterations in lipid metabolism [30]. Most guidelines recommend or suggest clinicians consider switching older regimens to avoid specific toxicities like dyslipidemia. The USPHS Guidelines generally recommend the use of an integrase inhibitor in conjunction with 1–2 NRTIs as first-line therapy for most patients [30]. Although lipid alterations are not common with many of these regimens, some recent studies have noted weight gain with the use of integrase inhibitors though not all [31,32]. The mechanism behind weight gain observed in persons taking integrase inhibitors is not clear. However, obesity is a well-known risk factor for dyslipidemia. Initiation of therapy with any of the antiretrovirals typically results in modest increases in most lipid levels, typically felt to be related to a reduction in HIV-induced dyslipidemic changes (see Table 1). Many of the older antiretrovirals that often led to more pronounced dyslipidemic changes are in less common use. However, treatment failure remains a common problem with the use of antiretrovirals and requires switching to different classes to suppress HIV replication. Thus, many PWH continue to use antiretrovirals known to alter lipids directly or indirectly.