• Raltegravir, Elvitegravir, Dolutegravir, and Bictegravir are the only HIV-1 integrase inhibitor being used to treat HIV infections S/GSK1349572. (wikipedia.org)
  • The investigational HIV integrase inhibitor elvitegravir taken once daily continued to perform as well as twice-daily raltegravir ( Isentress ) at 96 weeks for treatment-experienced people with extensive drug resistance, according to data presented last week at the 19th International AIDS Conference in Washington, DC. (aidsmap.com)
  • Richard Elion from Whitman-Walker Health presented long term data from a head-to-head phase III randomised controlled trial comparing 150mg elvitegravir once daily or 400mg raltegravir twice daily, both in combination with a fully active boosted protease inhibitor plus a third drug. (aidsmap.com)
  • The primary 48-week results, presented at the International AIDS Society meeting last summer in Rom e, showed that elvitegravir was well-tolerated and non-inferior to raltegravir in efficacy, with 59% vs 58% of participants in the two arms, respectively, achieving undetectable viral load. (aidsmap.com)
  • Of 2976 regimens started, 1901 (63.9%) contained dolutegravir, 631 (21.2%) elvitegravir and 444 (14.9%) raltegravir. (unl.pt)
  • The 1 year estimated probabilities of VF and INSTI-DC were 5.6% (95% CI 4.5-6.7) and 16.2% (95% CI 14.9-17.6), respectively, and were higher for raltegravir versus both elvitegravir and dolutegravir. (unl.pt)
  • There are four drugs within this family of medication: raltegravir, elvitegravir, dolutegravir and bictegravir. (eurekalert.org)
  • raltegravir and elvitegravir. (anatoliageneworks.com)
  • Cobicistat should be avoided in pregnancy due to the risk for lower concentrations of the drug and its boosted drugs - darunavir, atazanavir and elvitegravir - that can be seen in the second and third trimesters. (medscape.com)
  • Raltegravir (brand name Isentress) was granted accelerated approval from the U.S. Food and Drug Administration (FDA) in October 2007 and from EMEA (now EMA) in December 2007. (wikipedia.org)
  • The HIV integrase inhibitor raltegravir (Isentress) works well for both men and women and people of diverse racial/ethnic groups, according to data from the REALMRK trial presented at the 51st Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC 2011) this week in Chicago. (hivandhepatitis.com)
  • People with high baseline HIV viral load who used a NRTI-sparing regimen of ritonavir-boosted darunavir (Prezista) plus raltegravir (Isentress) had a higher than expected rate of virological failure and emergence of drug resistance mutations, according to research reported in the August 19, 2011, advance online edition of AIDS . (hivandhepatitis.com)
  • Raltegravir (Isentress) -- the sole approved integrase inhibitor -- plus tenofovir/emtricitabine remains the 'preferred' regimen. (hivandhepatitis.com)
  • Isentress HD contains the anti-HIV drug raltegravir. (catie.ca)
  • Isentress HD belongs to the class of drugs called integrase inhibitors. (catie.ca)
  • Causes of viral rebound can include drug resistance, poor adherence to an HIV treatment regimen or interrupting treatment. (aidsmap.com)
  • An ARV's intrinsic antiviral potency combined with its genetic barrier to resistance influences its ability to protect an ART regimen from VF (Fig 1.0). (ptmasterguide.com)
  • Lower rates of HIVDR have also been associated with routine viral load monitoring programs in which early detection of virological rebound provides the opportunity for adherence counseling or regimen modification as necessary, prior to the evolution of multiple DRMs (Charest et al. (ptmasterguide.com)
  • Globally, a dolutegravir-based regimen is currently recommended for treating HIV, and this is the first study to directly compare regimens including dolutegravir to other antiretroviral regimens, such as raltegravir-based regimens, that are also listed as 'Preferred' in U.S. perinatal guidelines" said Kunjal Patel , senior research scientist in the Department of Epidemiology at Harvard Chan School and lead author of the study. (harvard.edu)
  • Dolutegravir, a more recently approved antiretroviral drug, is part of a once-a-day regimen that has been shown to be more effective, easier to tolerate, and less likely to create new drug resistance in people with HIV-1 compared with other antiretroviral drugs. (harvard.edu)
  • We think the observed differences are due to dolutegravir's ability to rapidly decrease viral loads and its ease of use as part of a once-daily regimen that's available as a fixed-dose combination," said Patel. (harvard.edu)
  • In this study of [ viral load ] failure on lopinavir monotherapy, we found that patients often failed without PI mutations, but that resistance accumulated with longer time on the failing regimen," the researchers wrote. (infectiousdiseaseadvisor.com)
  • The key changes in this version focus on which drugs to start in a first-line regimen for treatment-naive patients. (hivandhepatitis.com)
  • Efavirenz (Sustiva) plus tenofovir/emtricitabine (the drugs in the Truvada coformulation) remains the sole 'preferred' first-line regimen, except for women during the first trimester of pregnancy. (hivandhepatitis.com)
  • The preferred regimen for pregnant women is lopinavir/ritonavir (Kaletra) plus zidovudine/lamivudine (the drugs in Combivir). (hivandhepatitis.com)
  • Namely, that it was risky to switch stable people from their "high resistance barrier" regimen of lopinavir/ritonavir plus NRTIs to raltegravir plus NRTIs if they harbored viruses with NRTI resistance. (lifeboat.com)
  • EDURANT is indicated in combination with VOCABRIA (cabotegravir), for short-term treatment of HIV-1 infection in adults and adolescents 12 years and older and weighing at least 35 kg who are virologically suppressed (HIV-1 RNA less than 50 copies/mL) on a stable regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine. (guidelinecentral.com)
  • When switching an ARV regimen in a patient with hepatitis B virus (HBV)/HIV coinfection, the patient should remain on an ARV agent that is active against HBV and has a high resistance barrier to HBV in order to avoid HBV rebound and hepatocellular damage. (hiv.gov)
  • Patients on antiretroviral therapy (ART) who do not achieve this treatment goal or who experience virologic rebound can develop resistance mutations to one or more components of their regimen. (hiv.gov)
  • Don't look now, but a two-drug lamivudine (3TC) + LPV/r strategy did just as well as a standard three-drug regimen of two NRTIs + LPV/r. (jwatch.org)
  • Better, actually, since virologic outcomes were the same and the two-drug regimen had fewer side effects. (jwatch.org)
  • Ah, but we're all thinking, what about the high viral load stratum - surely this group would need the extra potency of a three-drug regimen. (jwatch.org)
  • A two-drug regimen has never done better than a three-drug treatment in a fully powered study. (jwatch.org)
  • How would a two-drug, 3TC or FTC plus boosted-PI regimen fare as a maintenance strategy? (jwatch.org)
  • An initial antiretroviral regimen generally consists of two nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) in combination with a third active drug from one of the following classes: non-nucleoside reverse transcriptase inhibitor (NNRTI), protease inhibitor (PI) with a booster (ritonavir or cobicistat), or an integrase strand transfer inhibitor (INSTI). (medscape.com)
  • Selection of a regimen should be individualized based on virologic efficacy, potential adverse effects, pill burden, dosing frequency, drug-drug interaction potential, the patient's resistance test results, co-morbid conditions, drug availability, and cost. (medscape.com)
  • Patients must first achieve viral suppression on another regimen before switching. (medscape.com)
  • If a patient is virally suppressed while on a cobicistat containing regimen and becomes pregnant, they should be counseled on the risk for reduced drug concentration and their viral load should be monitored frequently. (medscape.com)
  • To characterize the HIV-2 integrase gene polymorphisms and the pathways to resistance of HIV-2 patients failing a raltegravir-containing regimen, we studied 63 integrase strand transfer inhibitors (INSTI)-naïve patients, and 10 heavily pretreated patients exhibiting virological failure while receiving a salvage raltegravir-containing regimen. (unl.pt)
  • To help guide the choice among regimens of similar efficacy, each table includes comments that address selected pertinent issues regarding each regimen, such as limitations based on a patient's kidney function and drug-drug interactions. (hivguidelines.org)
  • With the availability of new co-formulated HIV drugs, many patients could benefit from simplification of their ART regimen, guided by HIV DNA archive genotype testing (GenoSure Archive). (msdmanuals.com)
  • Nucleoside reverse transcriptase inhibitor (NRTI) transmitted drug resistance mutations (TDRMs) could increase the risk of virological failure (VF) of first-line integrase strand transfer inhibitor (InSTI)-based regimens. (nih.gov)
  • However, the presence of M184V/I independently predicted VF of raltegravir- but not dolutegravir-based therapy when compared with a fully-active backbone [adjusted hazard ratio (aHR) = 3.09, P = 0.035], particularly when associated with other non-thymidine analogue mutations (aHR = 27.62, P = 0.004). (nih.gov)
  • Many drugs have been discovered to treat the disease but mutations in the virus and resistance to the drugs make development difficult. (wikipedia.org)
  • Major INSTI mutations indicative of transmitted drug resistance occurred in 2/1114 (0.2%) individuals. (unl.pt)
  • The weakening of drug binding occurs due to a combined effect of mutations and a loss of key water molecules in the active site. (eurekalert.org)
  • We evaluated the mutations associated with INSTI resistance in naive HIV-1 infected patients and treated them with antiretrovirals (ART). (uludag.edu.tr)
  • INSTI resistance mutations were interpreted using the Stanford University HIVdb Program algorithm. (uludag.edu.tr)
  • In viral rebound under INSTI treatment, INSTI-resistant mutations follow typical INSTI resistance pathways and high resistance rates. (uludag.edu.tr)
  • Bosphore HBV Drug Resistance Mutation Sequencing Kit v1 analyzes the drug resistance mutations in the polymerase gene RT domain of the HBV DNA in human serum or plasma, encompassing all the HBV genotypes. (anatoliageneworks.com)
  • Bosphore HCV Drug Resistance Mutation Sequencing Kit v1 analyzes the drug resistance mutations in the NS3 region of the hepatitis C virus RNA in human serum or plasma, in HCV genotypes 1a and 1b, and enables to analyze the drug resistance mutations indicated below: Boceprevir, Telaprevir, Simetrevir, Faldaprevir. (anatoliageneworks.com)
  • Combination therapy has been shown to dramatically reduce the likelihood of drug resistance (many drug-resistant mutations are mutually exclusive) and to suppress viral replication to the point that progression to AIDS is significantly slowed. (medscape.com)
  • Antiviral-resistance mutations often affect more than one drug simultaneously because of similar development pipelines and the ultimate molecular structure of the drug, and combination choices should account for this possibility. (medscape.com)
  • Objectives: The objective of this studywas to improve the prediction of the impact of HIV-1 protease mutations in different viral subtypes on virological response to darunavir. (uu.nl)
  • The predictionmodel included weighted protease mutations, HIV RNA, CD4 and activity of accompanying drugs. (uu.nl)
  • Our model also allows quantification of the selective advantage of mutations by integrating their effects on viral fitness and drug susceptibility. (plos.org)
  • However, little data is available on the evolution, interaction and linkage of drug resistance mutations throughout the pol gene. (ucl.ac.uk)
  • In this study, we developed a single genome sequencing assay of the full-length HIV-1 pol gene and used it to investigate the development and linkage of drug resistance mutations in sequential samples from two patients failing INSTI-containing salvage therapy. (ucl.ac.uk)
  • Different phylogenetic methods were used to explore the evolution and dynamics of drug resistance mutations in the full-length HIV-1 pol gene. (ucl.ac.uk)
  • Our data indicate that the development of drug resistance mutations in IN is complex and is a fine balance between attaining high levels of drug resistance and decent replicative fitness. (ucl.ac.uk)
  • If more than 4 weeks have elapsed since non-long-acting ARV regimens were discontinued, resistance testing still can provide useful information to guide therapy, although it may not detect previously selected resistance mutations (CIII) . (hiv.gov)
  • We found that the reconstructed molecular clones of RVs lacked antiretroviral drug-resistant mutations, as well as G-to-A hypermutations. (biomedcentral.com)
  • Most ART regimens used for first-line therapy are sufficiently potent to completely block HIV-1 replication and have a genetic barrier to resistance high enough to maintain long-term virological suppression. (ptmasterguide.com)
  • At delivery, 96.7% of pregnancies of participants who received dolutegravir were virally suppressed, whereas those of participants who took atazanavir/ritonavir or raltegravir had viral suppression of 84.0% and 89.2%, respectively. (harvard.edu)
  • The interpretation was that despite the potency and excellent tolerability of raltegravir - massively better than lopinavir/ritonavir - it wasn't enough to maintain viral suppression reliably unless the NRTIs were also fully active. (lifeboat.com)
  • Pregnant individuals transitioning from efavirenz to dolutegravir might be at increased risk of insufficient viral suppression in the immediate postswitch period because both efavirenz- and pregnancy-related increases in hormone levels induce enzymes involved in dolutegravir metabolism, namely, cytochrome P450 3A4 and uridine 5'-diphospho-glucuronosyltransferase 1A1. (gwu.edu)
  • The goal of treatment for ART-experienced patients with drug resistance who are experiencing virologic failure is to establish virologic suppression (i.e. (hiv.gov)
  • For some rare highly ART-experienced patients with extensive drug resistance, maximal virologic suppression may not be possible. (hiv.gov)
  • While effective viral suppression with antiretroviral therapy has been proven to substantially reduce the risk of sexual transmission, a residual risk cannot be excluded. (medthority.com)
  • Integration to the retroviral genome is critical for gene expression and viral replication. (wikipedia.org)
  • Raltegravir is an INSTI integrase inhibitor which inhibits both HIV-1 and HIV-2 replication. (wikipedia.org)
  • The peripheral T-cell counts initially surge after therapy is initiated, but this represents redistribution of activated T cells from the viral replication centers in the lymph nodes rather than a true increase in total-body CD4 T-cell counts. (medscape.com)
  • HIV integrase inhibitors prevent the virus from inserting its genetic material into a host cell, a necessary step for viral replication. (aidsmap.com)
  • The selection of drug-resistant variants depends on the extent to which viral replication continues during incompletely suppressive therapy, the ease of acquisition of a particular drug resistance mutation (DRM), and the effect of DRMs on drug susceptibility and virus replica- tion. (ptmasterguide.com)
  • [ 3 ] In the late 1990s, the combined use of 3 or more antiretroviral medications was found to be highly successful at suppressing viral replication. (medscape.com)
  • The intermittent but prolonged detection of this replication-defective HIV variant in the patient′s plasma among other viral populations strongly suggests that this variant is released from highly stable productively infected cells present in vivo during therapy. (biomedcentral.com)
  • The process of continuous cycles of viral infection, integration, and production from target cells is referred to here as viral replication. (biomedcentral.com)
  • Combinations of 2, 3, or 4 drugs from different classes are usually necessary to fully suppress replication of wild-type HIV. (msdmanuals.com)
  • In the current observational study, the researchers compared dolutegravir use in pregnancy with atazanavir/ritonavir, darunavir/ritonavir, and raltegravir antiviral regimens that are currently classified as "Preferred" for use in pregnancy in the U.S. About half of the participants started ART before conception. (harvard.edu)
  • Changing treatment for viral failure can now be to a combination with two fully active drugs, so long as one of these has a high barrier to drug resistance (ie dolutegravir or boosted darunavir. (i-base.info)
  • The results indicate that annual viral load testing, which is the current World Health Organization recommendation, would identify failure during a timeframe when most patients would still benefit from switching to darunavir. (infectiousdiseaseadvisor.com)
  • Only 12 participants experienced resistance to darunavir, and only 1 participant had intermediate resistance. (infectiousdiseaseadvisor.com)
  • Darunavir plus abacavir/lamivudine (the drugs in the Epzicom coformulation) was reclassified as an 'alternative' due to additional data. (hivandhepatitis.com)
  • They include either of the first-line non-nucleoside reverse transcriptase inhibitor (NNRTI) drugs efavirenz and nevirapine, three boosted protease inhibitors (atazanavir, darunavir and lopinavir) and the integrase inhibitor raltegravir. (infohep.org)
  • Kaplan-Meier analyses assessed time to virological failure (VF), defined as one viral load (VL) ≥1000 copies/mL, two consecutive VLs ≥50 copies/mL, or one VL ≥50 copies/mL followed by treatment change after ≥24 weeks of follow-up, and time to INSTIs discontinuation (INSTI-DC) for any reason. (unl.pt)
  • Unboosted fosamprenavir (Lexiva) was removed due to inferior potency and risk of drug resistance in patients who experience virological failure. (hivandhepatitis.com)
  • Virological outcome prediction accuracy was compared with that from existing genotypic resistance interpretation systems (GISs) (ANRS 2013, Rega 9.1.0 and HIVdb 7.0). (uu.nl)
  • Amongst new recommendations are resistance testing at diagnosis, not just at virological failure and, where available, the B*5701 abacavir hypersensitivity test at diagnosis. (infohep.org)
  • Therefore, whenever possible, raltegravir should be administered with two other active ARTs to minimise the potential for virological failure and the development of resistance (see section 5.1). (medthority.com)
  • Patients starting two NRTIs (lamivudine/emtricitabine plus abacavir/tenofovir) plus raltegravir or dolutegravir were selected from the EuResist cohort. (nih.gov)
  • The original raltegravir 400 mg twice-daily version was compared to the new 2 x 600 mg once-daily formulation, with background NRTIs tenofovir DF + FTC for all participants. (i-base.info)
  • Raltegravir (RAL) 1200 mg once daily (QD) is non-inferior to RAL 400 mg twice daily (BID), in combination with tenofovir/emtricitabine, in treatment-naïve HIV-1-infected subjects: week 48 results. (i-base.info)
  • The new EACS guidelines recommend raltegravir only with tenofovir/emtricitabine. (hivandhepatitis.com)
  • For example, lack of efficacy of various formulations of tenofovir-based PrEP 17 in the VOICE trial were explained, in part, by undetectable drug levels in many participants 17 and imperfect adherence was also implicated for the lack of efficacy in the FEM-PrEP trial 18 . (nature.com)
  • In treatment-naïve patients, the clinical study data on use of raltegravir are limited to use in combination with two nucleotide reverse transcriptase inhibitors (NRTIs) (emtricitabine and tenofovir disoproxil fumarate). (medthority.com)
  • The dual combination of dolutegravir plus rilpivirine is also recommended as a switch option for people with undetectable viral load. (i-base.info)
  • Here we describe an oral dosage form composed of distinct drug-polymer matrices which achieved week-long systemic drug levels of the antiretrovirals dolutegravir, rilpivirine and cabotegravir in a pig. (nature.com)
  • NRTI backbone TDRMs increased the risk of VF with raltegravir-based but not dolutegravir-based regimens. (nih.gov)
  • For discussion of antiretroviral drugs and regimens, see Antiretroviral Therapy for HIV Infection . (medscape.com)
  • Treatment-experienced people may have taken several different regimens before and may have a strain of HIV that is resistant to multiple drug classes. (aidsmap.com)
  • Although all participants had used - and a majority had developed resistance to - at least two antiretroviral drug classes, they were able to construct viable regimens using a ritonavir-boosted protease inhibitor and an active third agent such as etravirine ( Intelence ), maraviroc ( Celsentri or Selzentry ) or a nucleoside/nucleotide reverse transcriptase inhibitor. (aidsmap.com)
  • Lamivudine is currently used in many HAART regimens but is now rarely used to treat hepatitis B because of a high rate of antiviral resistance when it is used as monotherapy as well as the availability of more potent agents with a higher barrier to resistance. (nih.gov)
  • Adherence to ARV regimens can be challenging for some patients, and poor adherence can result in detectable viral loads. (hiv.gov)
  • What remains unclear is why these two-drug regimens have been so disappointing. (jwatch.org)
  • Background In 2020, Zimbabwe adopted the WHO's recommendation to use raltegravir (RAL) granule-based regimens for treatment of neonates identified with HIV at the time of birth testing. (cdc.gov)
  • The NYSDOH AI Medical Care Criteria Committee recommendations for prescribing ART regimens for treatment-naive, nonpregnant adults (age ≥18 years) with HIV-1 and without acquired resistance are based on a comprehensive review of available clinical trial data. (hivguidelines.org)
  • So, in many cases they represent an indispensable escort for drugs, which otherwise would have to be discarded from therapeutic regimens. (infectiologyjournal.com)
  • Raltegravir plus abacavir/lamivudine was upgraded to 'alternative' due to accumulation of favorable data. (hivandhepatitis.com)
  • DHHS demoted abacavir/lamivudine from'preferred' to 'alternative' status in 2008 due to concerns that abacavir may increase the risk of cardiovascular problems and may not be as effective for people with high pre-treatment viral load. (hivandhepatitis.com)
  • Therapy should involve combinations of drugs-two nucleoside-analogue reverse-transcriptase inhibitors combined with either a protease inhibitor (PI) or a non-nucleoside-analogue reverse-transcriptase inhibitor. (medscape.com)
  • Nucleoside analogs ( NA s) are used to treat numerous viral infections and cancer. (plos.org)
  • Nucleoside analogs ( NA s) represent an important drug class for the treatment of viral infections and cancer. (plos.org)
  • Through mathematical modeling, we assess the mechanisms by which HIV-1 can develop resistance against nucleoside analog reverse transcriptase inhibitors (NRTI). (plos.org)
  • von Kleist M, Metzner P, Marquet R, Schütte C (2012) HIV-1 Polymerase Inhibition by Nucleoside Analogs: Cellular- and Kinetic Parameters of Efficacy, Susceptibility and Resistance Selection. (plos.org)
  • The viral genome is reversely transcribed into the DNA of the infected cell by viral reverse transcriptase, the DNA is then integrated into the host-cell chromosomes with the aid of the viral integrase. (wikipedia.org)
  • HIV-1 genetic variability results from the high rate of HIV-1 reverse transcriptase (RT) processing errors, recombination when more than one viral variants infect the same cell, and the accumulation of proviral variants during the course of infection (Abram et al. (ptmasterguide.com)
  • Lamivudine is phosphorylated intracellularly to the triphosphate which competes with the naturally occurring cytidine triphosphate for incorporation into the growing HIV or HBV DNA chain by the viral polymerase, thereby inhibiting polymerase (or reverse transcriptase) activity and causing chain termination. (nih.gov)
  • What agents are used to target reverse transcriptase conversion of viral RNA to DNA in HIV? (freezingblue.com)
  • The sole approved drug in this class, raltegravir, has demonstrated long-term efficacy and minimal toxicity, though it has a relatively low barrier to resistance. (aidsmap.com)
  • Hormonal contraceptives are safe and effective means to avoid unintended pregnancy, but there is concern that coadministration of antiretroviral drugs may alter contraceptive efficacy. (hindawi.com)
  • The safety and efficacy of raltegravir have not been established in patients with severe underlying liver disorders. (medicines.org.uk)
  • In other cases, enzymatic degradation of anti-infective drugs by mammalian enzymes in the liver (or kidney) can limit the efficacy of the drugs. (infectiologyjournal.com)
  • Typically, this is due to the development of resistances, for which numerous molecular mechanisms have been detected, in other cases, enzymatic degradation of anti-infective drugs by mammalian enzymes can limit the efficacy of the drugs. (infectiologyjournal.com)
  • As a result, most cases of VF and drug-resistance arise from incomplete adherence, which exposes a patient's virus to the incompletely suppressive ARV levels capable of exerting drug selective pressure. (ptmasterguide.com)
  • Accordingly, HIVDR appears to be less common in patients receiving FDCs containing ARVs that have similar half-lives because incomplete adherence to these combinations is less likely to expose a virus to selective drug pressure (Chi et al. (ptmasterguide.com)
  • Simulations of viral dynamics and patient adherence patterns indicate that such systems would significantly reduce therapeutic failures and epidemiological modelling suggests that using such an intervention prophylactically could avert hundreds of thousands of new HIV cases. (nature.com)
  • Evaluation of virologic failure should include an assessment of ART adherence, drug-drug and drug-food interactions, drug tolerability, HIV-RNA level and CD4 T lymphocyte (CD4) cell count trends over time, ART history, and prior and current drug-resistance test results. (hiv.gov)
  • That means without developing any resistance to drugs as long as their adherence is quite good. (jwatch.org)
  • However, few studies have examined the relative contributions of different patterns of drug use on adherence to antiretroviral therapy (ART). (biomedcentral.com)
  • We sought to estimate the effect of different types of illicit drug use on adherence in a setting of universal free HIV/AIDS treatment and care. (biomedcentral.com)
  • Using data from ongoing prospective cohorts of HIV-positive illicit drug users linked to comprehensive pharmacy dispensation records in Vancouver, Canada, we examined factors associated with ≥95% prescription refill adherence using generalized estimating equations (GEE) logistic regression. (biomedcentral.com)
  • Suboptimal adherence is associated with an increased risk of HIV/AIDS-associated mortality and morbidity [ 3 ] and elevated rates of viral resistance to treatment [ 4 ]. (biomedcentral.com)
  • In many studies, active illicit drug use among individuals living with HIV/AIDS is associated with decreased access to HIV treatment, reduced medication adherence and increased mortality [ 5 ]. (biomedcentral.com)
  • Thus, we sought to examine the relative contribution of different illicit drug use patterns on ART non-adherence among a group of HIV-positive illicit drug users. (biomedcentral.com)
  • Severe adverse events occur largely when it is withdrawn in patients with chronic hepatitis B or with the development of antiviral resistance. (nih.gov)
  • These elevations appear to be due to a transient flare in the underlying chronic hepatitis B and occur in three situations during and after therapy: upon initiation of therapy (treatment flares), upon development of antiviral resistance (breakthrough flares), and shortly after stopping therapy (withdrawal flares). (nih.gov)
  • However, some of the promising antibacterial and antiviral drugs lost activity after being used in therapy for some time. (infectiologyjournal.com)
  • However, we had to learn that some of the promising antibacterial, antifungal and antiviral drugs lost activity after being used in therapy for some time. (infectiologyjournal.com)
  • The study included 2164 stored plasma samples from 386 participants who had been randomly assigned to protease inhibitor (PI) monotherapy (ritonavir-boosted lopinavir after initial PI plus raltegravir induction) in the EARNEST trial. (infectiousdiseaseadvisor.com)
  • Overall, 107 participants experienced virologic failure, with 20% (n=21) having intermediate/high resistance to lopinavir. (infectiousdiseaseadvisor.com)
  • Some of the participants who had a history of treatment failure who switched ended up experiencing virologic rebound with integrase inhibitor resistance, which made the switch to raltegravir not noninferior (sorry for the double negative) to continuing lopinavir/ritonavir. (lifeboat.com)
  • Although naturally occurring drug-resistant viruses arise every day in untreated patients (Perelson and Ribeiro, 2013), these variants rarely rise to detectable levels because they are less fit than drug-susceptible viruses in the absence of selective drug pressure. (ptmasterguide.com)
  • People with extensive drug resistance and who still have detectable viral load are also recommended to consider pipeline drugs that are currently only available in research studies. (i-base.info)
  • 50 HIV-1 RNA copies/mL or a single viral load ≥ 200 copies/mL after 3 months from antiretroviral therapy start) was evaluated in the overall population and according to the InSTI employed. (nih.gov)
  • Laboratory tests showed a CD4 cell count of 11 cells/mL and HIV viral load of 44,201 copies/mL. (cdc.gov)
  • The patients CD4 count was 12 count cells/mm3 and HIV Viral Load was 1420045 copies/ml. (webmedcentral.com)
  • For pregnant women natural delivery is now preferred to Caesarean section if the mother has a viral load below 50 copies/ml. (infohep.org)
  • Integrase Strand Transfer Inhibitor (INSTI) Genotypic Resistance Analysis in Treatment-nNaive, INSTI Free Antiretroviral-Experienced and INSTI-Experienced Turkish Patients Infected with HIV-1. (uludag.edu.tr)
  • Results: INSTI resistance was not detected in ART naive patients. (uludag.edu.tr)
  • At least one INSTI resistance mutation was detected in 10% of the INSTI-free patients and 29% of the INSTI-treated patients. (uludag.edu.tr)
  • INSTI resistance genotypic analysis should be considered before any DTG-based regimes can be initiated in the future, and reduced DTG susceptibility should be carefully monitored and investigated. (uludag.edu.tr)
  • For patients with HIV who have used long acting cabotegravir as PrEP, INSTI resistance testing should be done before starting ART. (medscape.com)
  • Zidovudine/lamivudine was reclassified from 'alternative' to 'acceptable' overall, but remains the preferred NRTI combination for pregnant women receiving antiretroviral drugs to prevent perinatal HIV transmission. (hivandhepatitis.com)
  • We correctly predict that HIV-1 can develop resistance by decreasing NRTI incorporation rate, increasing its excision rate, or decreasing its affinity for the viral polymerase enzyme. (plos.org)
  • 14 , 15 Furthermore, in two studies among adults with HIV not receiving ART, persons who developed TB disease had higher viral loads 16 and a greater risk of HIV disease progression 16 and death 17 than CD4-matched control patients without TB. (hiv.gov)
  • These low viral loads in plasma during therapy are referred to as residual viremia. (biomedcentral.com)
  • INSTIs restrain the binding of pre-integration complex (PIC) and host DNA and INBIs restrain integrase and viral DNA binding. (wikipedia.org)
  • Conclusion: Our findings provide data for treatment and resistance management of INSTIs and may provide feedback for INSTIs resistance surveillance consensus-building efforts. (uludag.edu.tr)
  • Integrase inhibitors (INSTIs) such as dolutegravir and raltegravir. (targetwoman.com)
  • This has changed in the last few years with the development and approval for use of second-generation NNRTIs and PIs, and three new classes of drugs including integrase strand transfer inhibitors (INSTIs). (ucl.ac.uk)
  • Furthermore, we examined the effect of co-evolved PR and RT on the susceptibility of patient-derived viruses to INSTIs and viral replicative fitness. (ucl.ac.uk)
  • The patient also had genotypic testing for HIV drug resistance and antiretroviral therapy with truvada and raltegravir was started. (webmedcentral.com)
  • For instance in our host country Serbia, no Truvada or raltegravir are available. (infohep.org)
  • DRMs can be categorized as primary DRMs that directly reduce drug susceptibility and accessory DRMs that enhance fitness of variants containing primary DRMs or that contribute further reductions in susceptibility. (ptmasterguide.com)
  • In contrast, significant cross-resistance within a drug class is common because most DRMs reduce susceptibility to multiple ARVs of the same class (Melikian et al. (ptmasterguide.com)
  • Surprisingly, target cells with low dNTP/NTP levels may not confer hyper-susceptibility to inhibition, whereas cells with high dNTP/NTP contents are likely to confer natural resistance. (plos.org)
  • Resistance development also changes drug susceptibility distinctly and we show, for the first time, that selection of drug resistance can occur in particular target cells. (plos.org)
  • Taken together, the data suggests that larger regions of patient-derived HIV-1 genome should be examined in order to get a good understanding of HIV-1 drug susceptibility. (ucl.ac.uk)
  • If treatment fails, drug susceptibility (resistance) assays can determine the susceptibility of the dominant HIV strain to all available drugs. (msdmanuals.com)
  • Integrase inhibitors are a new class of drugs used in the treatment of HIV. (wikipedia.org)
  • Booster drugs are used to 'boost' the effects of protease inhibitors and some other antiretrovirals. (aidsmap.com)
  • As newer integrase inhibitors became available, the twice-daily formulation meant that even after lowering the price, raltegravir had a limited market. (i-base.info)
  • Today, a number of drugs are available which help to control HIV infection, including a group called integrase strand transfer inhibitors. (eurekalert.org)
  • BACKGROUND: Dolutegravir is approved for the treatment of HIV-1 patients exposed to other integrase inhibitors, but the decision to use dolutegravir in this setting should be informed by drug resistance testing. (unl.pt)
  • Protease inhibitors (PIs) inhibit the viral protease enzyme that is crucial to maturation of immature HIV virions after they bud from host cells. (msdmanuals.com)
  • Attachment inhibitors bind directly to the viral envelope glycoprotein 120 (gp120), close to the CD4+ binding site, which prohibits the conformational change necessary for initial interaction between the virus and the surface receptors on CD4 cells, thereby preventing attachment and subsequent entry into host T cells and other immune cells. (msdmanuals.com)
  • The first integrase inhibitor, raltegravir, was approved in 2007 and other drugs were in clinical trials in 2011. (wikipedia.org)
  • This research is an outstanding example of how we can use cryo-electron microscopy to reveal the intricate relationships between drugs and their targets, providing results that could lead to clinical benefit," explains Peter Rosenthal, the head of the Structural Biology of Cells and Viruses laboratory at the Francis Crick Institute. (eurekalert.org)
  • LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. (nih.gov)
  • A long, long time ago, back in the early exciting days of raltegravir, the first HIV integrase inhibitor, we learned something important from a clinical trial with disappointing results. (lifeboat.com)
  • Or maybe just the two drugs tested to date in these clinical studies? (jwatch.org)
  • We aimed to delineate mechanisms of T. vaginalis resistance using transcriptome profiling of metronidazole (MTZ)-resistant and sensitive T. vaginalis clinical isolates. (cdc.gov)
  • Although many studies have focused on the impact of heroin use on the clinical management of HIV infection [ 6 , 7 ] fewer studies have examined the influence of distinct illicit drug use patterns. (biomedcentral.com)
  • He received a blood transfusion, prophylactic antimicrobial drugs against opportunistic infections, analgesics, and supportive care. (cdc.gov)
  • Although most HIV-1 infections are initiated by a single viral variant (Keele et al. (ptmasterguide.com)
  • However, the risk varies widely depending on differences in factors such as co-occurrence with other sexually transmitted infections (STIs), level of viral load, stage of disease, and circumcision. (benthamscience.com)
  • Acute HIV seroconversion is often asymptomatic, although patients may manifest nonspecific symptoms that can be difficult to differentiate from other viral infections. (pcrm.org)
  • However, 5-nitroimidazole resistance has been increasingly recognized and may occur in up to 10% of infections. (cdc.gov)
  • Lamivudine is a very rare cause of clinically apparent drug induced liver injury, but is associated with flares of underlying hepatitis B during therapy or with abrupt withdrawal. (nih.gov)
  • For HBV infection the recommended dose of lamivudine in adults is 100 mg orally once daily, the drug being available in this dose under the trade name Epivir-HBV. (nih.gov)
  • An exacerbation of hepatitis also typically occurs after development of lamivudine resistance, a few weeks or months after the initial appearance of the mutant HBV strain and rise in HBV DNA levels (Case 2). (nih.gov)
  • According to all drug classes, drug resistance mutation prevalences were determined at the rate of 60%, 46%, and 46% in the RAL, EVG, and DTG groups, respectively. (uludag.edu.tr)
  • Bosphore HBV Drug Resistance Mutation Sequencing Kit v1, is a Real-Time PCR-based in vitro diagnostic medical device, IVD CE marked according to 98/79/EC Directive. (anatoliageneworks.com)
  • Bosphore HCV Drug Resistance Mutation Sequencing Kit v1, is a Real-Time PCR based in-vitro diagnostic medical device, IVD CE marked according to 98/79/EC Directive. (anatoliageneworks.com)
  • It should be noted that a couple of other reasons may be responsible for development of resistances of pathogenic microorganisms, like mutation of target proteins and expression of efflux pumps which eliminate the anti-infective drugs from the microbial cells, but these phenomena are poorly addressable by boosters and will be treated here only shortly 1 . (infectiologyjournal.com)
  • Initial ART selection should be guided by co-occurring conditions, including viral hepatitis, medications, and other factors such as pregnancy. (aafp.org)
  • Mechanistic Modeling of the Drug-Drug Interaction Between Efavirenz and Dolutegravir: Is This Interaction Clinically Relevant When Switching From Efavirenz to Dolutegravir During Pregnancy? (gwu.edu)
  • These findings suggest that dolutegravir exposure in the immediate post-efavirenz switch period during pregnancy may be suboptimal, leading to HIV viremia and, potentially, resistance. (gwu.edu)
  • For information regarding ART in individuals who are or who may become pregnant, see DHHS Recommendations for the Use of Antiretroviral Drugs During Pregnancy and Interventions to Reduce Perinatal HIV Transmission in the United States . (hivguidelines.org)
  • Evidence shows that HIV-positive people who are on ART, engaged in care, and have an ongoing undetectable viral load are substantially less likely to transmit HIV to others, be it through sex, when sharing equipment to use drugs or during pregnancy and birth. (catie.ca)
  • Higher rates of infection with HIV are exhibited among injection drug users mainly because of unsafe injecting behavior. (benthamscience.com)
  • A comprehensive laboratory evaluation, including HIV viral load and CD4 lymphocyte monitoring, is necessary to guide decision-making for treatment, opportunistic infection prophylaxis, and vaccinations. (aafp.org)
  • Each of these drug classes includes more than 25 HIV medicines that are approved to treat HIV infection. (targetwoman.com)
  • Perinatal infection can occur if the mother's viral load is not suppressed, with transmissibility rising in direct proportion to the HIV viral load. (pcrm.org)
  • Trichomonas vaginalis is the most common non-viral sexually transmitted infection. (cdc.gov)
  • These compounds are used in combination with the primary anti-infective agent, but not for their direct effects on the infection itself, but since they enhance or restore the activity of the drug. (infectiologyjournal.com)
  • HIV-1 infection, documented by any licensed rapid HIV test or HIV-1 E/CIA test kit at any time prior to entry and confirmed by a licensed Western blot or a second antibody test by a method other than the initial rapid HIV and/or E/CIA, or by HIV-1 antigen or plasma HIV-1 RNA viral load. (who.int)
  • Mechanistic Modeling of the Drug-Drug Interaction Between Efavirenz an" by André Dallmann, John van den Anker et al. (gwu.edu)
  • To this end, the drug-drug interaction between efavirenz and the uridine 5'-diphospho-glucuronosyltransferase 1A1 substrates dolutegravir and raltegravir was first simulated in nonpregnant subjects. (gwu.edu)
  • The number of DRMs required and the effect of each DRM on virus fitness contribute to the ARV's genetic barrier to resistance. (ptmasterguide.com)
  • Fig. 1.0 ARV potency versus genetic barrier to resistance. (ptmasterguide.com)
  • Raltegravir has a relatively low genetic barrier to resistance. (medthority.com)
  • National treatment guidelines include ART options that can be offered immediately after diagnosis, even before the results of baseline HIV drug-resistance testing are available. (aafp.org)
  • Since 2005, persons who used illicit drugs and were HIV-seropositive at baseline or during the study are subsequently followed in ACCESS. (biomedcentral.com)
  • The section on women and ART includes significant additions on weight gain, drug interactions with hormone treatment and considerations related to the menopause. (i-base.info)
  • Tables on drug interactions and side effects have been updated to include latest treatments. (i-base.info)
  • CDC (Vernon A.) Announcement: Updated guidelines on managing drug interactions in the treatment of HIV-related tuberculosis. (cdc.gov)
  • We performed a literature search of PubMed and Ovid databases of articles published between January 1980 and February 2012 to identify English-language reports of drug-drug interactions between hormonal contraceptives (HCs) and antiretroviral drugs (ARVs). (hindawi.com)
  • As access to both modern methods of contraception and antiretroviral drugs (ARVs) expands, women with HIV enter the largely uncharted territory of potential drug interactions. (hindawi.com)
  • There are new tables of the most common and serious HIV drug side effects, and also of interactions with drugs commonly used for other illnesses. (infohep.org)
  • Provide dosing considerations for individuals with renal or hepatic impairment and important drug-drug and food interactions. (hivguidelines.org)
  • Integrase is a viral enzyme that integrates retroviral DNA into the host cell genome. (wikipedia.org)
  • Although the drugs are normally very effective at binding and blocking integrase, over time, the virus can weaken this bond and thus enable its key enzyme to work again. (eurekalert.org)
  • This technique uses a powerful microscope which fires electrons at a frozen sample of the drug-enzyme complex. (eurekalert.org)
  • The greatest risk factor for vertical transmission is thought to be advanced maternal disease, such as acquired immunodeficiency syndrome (AIDS), likely because of a high maternal HIV viral load. (medscape.com)
  • Resistance and withdrawal flares typically occur as HBV DNA levels are high or rising. (nih.gov)
  • Because disease-related complications can occur in untreated patients with high CD4 counts and because less toxic drugs have been developed, treatment with antiretroviral therapy (ART) is now recommended for all patients. (msdmanuals.com)
  • Each film-coated tablet contains 600 mg of raltegravir (as potassium). (medicines.org.uk)
  • This therapy helps prevent drug resistance in patients. (targetwoman.com)
  • If patients stop taking the drug, they may develop resistance to the drug and thereby will stop responding to the treatment when continued at a later stage. (targetwoman.com)
  • Patients may also have aseptic meningitis that appears to be of viral origin upon examination of spinal fluid. (pcrm.org)
  • Until recently, patients developing highly drug-resistant HIV-1 have had limited therapy options. (ucl.ac.uk)
  • Depending on their ARV treatment histories, some of these patients may have minimal or no drug resistance and others may have extensive resistance. (hiv.gov)
  • Many of these patients' viral control remains under control (undetectable level) for not less than 7- 10 years. (jwatch.org)
  • There is essentially no cross-resistance between drug classes. (ptmasterguide.com)
  • 2002). Knowledge of ARV cross-resistance profiles is therefore essential when using more than one drug from the same ARV class either in combination or in sequence. (ptmasterguide.com)
  • Viruses that are highly-resistant to drugs in one ARV class are completely susceptible to ARVs from unused classes (Larder, 1994). (ptmasterguide.com)
  • If only one drug is taken, HIV will become resistant to the drug very soon and the drug will stop working. (targetwoman.com)
  • We quantify the effects of treatment and estimate the fitness of drug resistant mutants. (plos.org)
  • This finding could provide an explanation of how clinically observed resistant viral mutants may arise. (plos.org)
  • Future studies with more T. vaginalis isolates with a broad range of MLCs are needed to determine which genes may represent the best alternative targets in drug-resistant strains. (cdc.gov)