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Hiv and pharmacokinetics

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https://www.readbyqxmd.com/read/28231276/alterations-in-cellular-pharmacokinetics-and-pharmacodynamics-of-elvitegravir-in-response-to-ethanol-exposure-in-hiv-1-infected-monocytic-u1-cells
#1
Narasimha M Midde, Namita Sinha, Pradeep B Lukka, Bernd Meibohm, Santosh Kumar
Ethanol consumption is negatively associated with antiretroviral therapy (ART) adherence and general health in HIV positive individuals. Previously, we demonstrated ethanol-mediated alterations to metabolism of elvitegravir (EVG) in human liver microsomes. In the current study, we investigated ethanol influence on the pharmacokinetic and pharmacodynamic interactions of EVG in HIV infected monocytic (U1) cells. U1 cells were treated with 5 μM EVG, 2 μM Cobicistat (COBI), a booster drug, and 20 mM ethanol for up to 24 hours...
2017: PloS One
https://www.readbyqxmd.com/read/28219799/uplc-ms-ms-method-for-the-simultaneous-quantification-of-three-new-antiretroviral-drugs-dolutegravir-elvitegravir-and-rilpivirine-and-other-thirteen-antiretroviral-agents-plus-cobicistat-and-ritonavir-boosters-in-human-plasma
#2
Marco Simiele, Alessandra Ariaudo, Amedeo De Nicolò, Fabio Favata, Martina Ferrante, Chiara Carcieri, Stefano Bonora, Giovanni Di Perri, Antonio De Avolio
Rilpivirine (RPV), dolutegravir (DTG) and elvitegravir (EVG) are the latest antiretroviral drugs approved for treatment of HIV infection. Currently, poor information is currently available concerning their pharmacokinetic and pharmacodynamic properties, thus making the use of therapeutic drug monitoring for these drugs not useful. This lack of information is partially due to the absence of an high-throughput method for their simultaneous quantification together with other antiretroviral drugs. In this work, we describe the development and validation of a new UPLC-MS/MS method to quantify these drugs, together with other fourteen antiretroviral agents, in human plasma...
February 3, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28206979/effect-of-gender-and-age-on-the-relative-bioavailability-of-doravirine-results-of-a-phase-i-trial-in-healthy-subjects
#3
Martin O Behm, Ka L Yee, Li Fan, Paul Fackler
BACKGROUND: Doravirine is a potent, once-daily, non-nucleoside reverse transcriptase inhibitor with a distinct resistance profile in Phase 3 development for the treatment of HIV-1. As doravirine may be administered to women and the elderly, we investigated the impact of gender and age in doravirine pharmacokinetics. METHODS: In this Phase 1, open-label, single-period, parallel-group investigation, doravirine 100 mg was administered to 36 healthy subjects in 3 groups: elderly men (n=12, 65-80 years), elderly women (n=12, 65-80 years), and young women (n=12, 18-50 years)...
February 16, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28198203/enteral-administration-of-twice-daily-dolutegravir-and-rilpivirine-as-a-part-of-a-triple-therapy-regimen-in-a-critically-ill-patient-with-hiv
#4
Sarah Lynn Turley, Patricia Pecora Fulco
The administration of antiretroviral therapy (ART) in intubated critically ill patients may be challenging. Limited pharmacokinetic data exist characterizing the effects of crushed ART with subsequent enteral administration on antiretroviral drug concentrations or the clinical impact on HIV virologic suppression. We report a case of a 27-year-old HIV-positive male with presumed multidrug-resistant HIV and a diagnosis of lymphoma who required enteral ART administration after intensive care unit admission. Crushed twice-daily dolutegravir (separated from enteral nutrition by 2 hours) and rilpivirine (concurrently with a bolus feed) were administered via an orogastric tube...
January 1, 2017: Journal of the International Association of Providers of AIDS Care
https://www.readbyqxmd.com/read/28196003/antiviral-activity-safety-and-pharmacokinetics-of-bictegravir-as-10-day-monotherapy-in-hiv-1-infected-adults
#5
Joel E Gallant, Melanie Thompson, Edwin DeJesus, Gene W Voskuhl, Xuelian Wei, Heather Zhang, Kirsten White, Andrew Cheng, Erin Quirk, Hal Martin
OBJECTIVE: to evaluate antiviral activity, safety, and pharmacokinetics of short-term monotherapy with bictegravir (bic), a novel, potent hiv integrase strand-transfer inhibitor (insti) DESIGN:: Phase 1b, randomized, double-blinded, adaptive, sequential cohort, placebo-controlled study METHODS:: HIV-infected adults not taking antiretroviral therapy were randomized to receive BIC (5, 25, 50, or 100 mg) or placebo once daily for 10 days. Primary endpoint was time-weighted average change from baseline to Day 11 (DAVG11) for plasma HIV-1 RNA...
February 8, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/28193650/interaction-of-rifampicin-and-darunavir-ritonavir-or-darunavir-cobicistat-in-vitro
#6
Owain Roberts, Saye Khoo, Andrew Owen, Marco Siccardi
Treatment of HIV patients co-infected with tuberculosis (TB) is challenging due to drug-drug interactions (DDIs) between antiretrovirals (ARVs) and anti-TB drugs. The aim of this study was to quantify the effects of cobicistat (COBI), or ritonavir (RTV), in modulating DDIs between darunavir (DRV) and rifampicin (RIF) in a human hepatocyte-based in vitro model. Human primary hepatocyte cultures were incubated with RIF alone, or in combination with either COBI or RTV for three days, followed by co-incubation with DRV for one hour...
February 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28188763/hiv-antiretroviral-drug-efavirenz-induces-anxiety-like-and-depression-like-behavior-in-rats-evaluation-of-neurotransmitter-alterations-in-the-striatum
#7
Giuliana Ignácio Teixeira Cavalcante, Adriano José Maia Chaves Filho, Maria Isabel Linhares, Camila Nayane de Carvalho Lima, Edith Teles Venâncio, Emiliano Ricardo Vasconcelos Rios, Francisca Cléa Florenço de Souza, Silvânia Maria Mendes Vasconcelos, Danielle Macêdo, Marta Maria de França Fonteles
Efavirenz (EFV) is an effective antiretroviral drug with a favorable pharmacokinetic profile and widely used in combination regimens to treat HIV infection. However, there are major concerns about the safety of this drug. Patients treated with EFV often experience neuropsychiatric adverse effects, which frequently lead to switching to alternative EFV-free regimens. The mechanisms involved in the central action of EFV are intrinsically unclear. Thus, this study aimed to investigate the effects of acute and subchronic (2 weeks) EFV administration in a series of behavioral tests for anxiety-like and depression-like behavior in healthy rats...
February 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28187506/the-effect-of-gene-variants-on-levonorgestrel-pharmacokinetics-when-combined-with-antiretroviral-therapy-containing-efavirenz-or-nevirapine
#8
M Neary, M Lamorde, A Olagunju, K M Darin, C Merry, P Byakika-Kibwika, D J Back, M Siccardi, A Owen, K K Scarsi
Reduced levonorgestrel concentrations from the levonorgestrel contraceptive implant was previously seen when given concomitantly with efavirenz. We sought to assess whether single nucleotide polymorphisms (SNPs) in genes involved in efavirenz and nevirapine metabolism were linked to these changes in levonorgestrel concentration. SNPs in CYP2B6, CYP2A6, NR1I2 and NR1I3 were analysed. Associations of participant demographics and genotype with levonorgestrel pharmacokinetics were evaluated in HIV-positive women using the levonorgestrel implant plus efavirenz- or nevirapine-based ART, in comparison to ART-naïve women using multivariate linear regression...
February 10, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28182610/pharmacokinetics-and-safety-of-darunavir-ritonavir-in-hiv-infected-pregnant-women
#9
Saye Khoo, Gilles Peytavin, David Burger, Andrew Hill, Kimberley Brown, Christiane Moecklinghoff, Charles La Porte, Maria Blanca Hadacek
The dosage of darunavir/ritonavir is 800/100 mg once daily for treatment-naive patients or treatment-experienced patients with no prior darunavir resistance associated mutations, and 600/100 mg twice daily for treatment-experienced patients with one or more darunavir resistance associated mutations. Results from the five available pharmacokinetic studies show reductions in total darunavir plasma concentrations of between 20-50% during the third trimester of pregnancy. The unbound darunavir concentrations have been measured only in subsets of patients in two of the five pharmacokinetic studies...
January 2017: AIDS Reviews
https://www.readbyqxmd.com/read/28168828/relative-bioavailability-of-a-dolutegravir-dispersible-tablet-and-the-effects-of-low-and-high-mineral-content-water-on-the-tablet-in-healthy-adults
#10
Ann M Buchanan, Michael Holton, Ian Conn, Mark Davies, Mike Choukour, Brian R Wynne
Dolutegravir (DTG) is approved in the United States to treat HIV-1-infected patients weighing ≥30 kg. A dispersible DTG tablet formulation was recently developed for pediatric patients. This study compares the pharmacokinetics (PK) of the dispersible tablet with that of a previously evaluated granule formulation. In this randomized, open-label, crossover study, 15 healthy adults received single oral doses of DTG 20 mg every 7 days across 5 treatment arms: granules consumed immediately after mixture with purified water, dispersible DTG consumed immediately after reconstitution in low-mineral-content (LMC) or high-mineral-content (HMC) water, and dispersible DTG consumed 30 minutes after dispersal in LMC or HMC water...
February 7, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/28167742/structural-and-preclinical-studies-of-computationally-designed-non-nucleoside-reverse-transcriptase-inhibitors-for-treating-hiv-infection
#11
Shalley N Kudalkar, Jagadish Beloor, Albert H Chan, Won-Gil Lee, William L Jorgensen, Priti Kumar, Karen S Anderson
The clinical benefits of human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase (RT) inhibitors (NNRTIs) are hindered by their unsatisfactory pharmacokinetic (PK) properties along with the rapid development of drug-resistant variants. However, the clinical efficacy of these inhibitors can be improved by developing compounds with enhanced pharmacological profiles and heightened antiviral activity. We used computational and structure-guided design to develop two next-generation NNRTI drug candidates, compounds I and II, which are members of a class of catechol diethers...
February 6, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28165830/pharmacokinetic-drug-evaluation-of-velpatasvir-plus-sofosbuvir-for-the-treatment-of-hepatitis-c-virus-infection
#12
Teresa Brieva, Antonio Rivero, Antonio Rivero-Juarez
The fixed-dose combination therapy of sofosbuvir (SOF) plus velpatasvir (VEL) is the first pangenotypic, direct-acting antiviral (DAA), single-treatment regimen (STR) for the treatment of hepatitis C virus (HCV) infection to be commercialized. It is approved for the treatment of HCV genotypes 1, 2, 3, 4, 5, and 6. Following approval in 2016, new pharmacokinetic and pharmacodynamic data were reported, which led to important clinical applications. Areas covered: This review provides a summary of the pharmacokinetics, pharmacodynamics, efficacy and safety of SOF/VEL therapy for treatment of HCV infection...
February 6, 2017: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/28160772/renal-safety-of-lithium-in-hiv-infected-patients-established-on-tenofovir-disoproxil-fumarate-containing-antiretroviral-therapy-analysis-from-a-randomized-placebo-controlled-trial
#13
Eric H Decloedt, Maia Lesosky, Gary Maartens, John A Joska
BACKGROUND: The prevalence of bipolar disorder in HIV-infected patients is higher than the general population. Lithium is the most effective mood stabiliser, while tenofovir disoproxil fumarate (TDF) is frequently used as part of combination antiretroviral therapy (ART). Both TDF and lithium are associated with renal tubular toxicity, which could be additive, or a pharmacokinetic interaction may occur at renal transporters with a decrease in TDF elimination. OBJECTIVE: We report on the change in estimated glomerular filtration rate (eGFR) using the modification of diet in renal disease formula in participants who received ART including TDF and were enrolled in a 24 week randomised trial of lithium versus placebo in patients with HIV-associated neurocognitive impairment...
February 4, 2017: AIDS Research and Therapy
https://www.readbyqxmd.com/read/28160272/suboptimal-exposure-to-anti-tb-drugs-in-a-tbm-hiv-population-is-not-related-to-anti-retroviral-therapy
#14
M E Török, G Aljayyoussi, D Waterhouse, Tth Chau, Nth Mai, N H Phu, T T Hien, W Hope, J J Farrar, S A Ward
A placebo-controlled trial that compares the outcomes of immediate versus deferred initiation of antiretroviral therapy in HIV+ve Tuberculous Meningitis (TBM) patients was conducted in Vietnam in 2011. Here, the pharmacokinetics of Rifampicin, Isoniazid, Pyrazinamide and Ethambutol were investigated in the presence and absence of anti-HIV treatment in 85 patients. Pharmacokinetic analyses show that HIV therapy has no significant impact upon the pharmacokinetics of TB drugs in this cohort. The same population, however, displayed generally low CSF and systemic exposures to rifampicin compared to previously reported HIV -ve cohorts...
February 4, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28145472/predicting-hiv-pre-exposure-prophylaxis-efficacy-for-women-using-a-preclinical-pharmacokinetic-pharmacodynamic-in-vivo-model
#15
Angela Wahl, Phong T Ho, Paul W Denton, Katy L Garrett, Michael G Hudgens, Glenn Swartz, Cynthia O'Neill, Fulvia Veronese, Angela D Kashuba, J Victor Garcia
The efficacy of HIV pre-exposure prophylaxis (PrEP) relies on adherence and may also depend on the route of HIV acquisition. Clinical studies of systemic tenofovir disoproxil fumarate (TDF) PrEP revealed reduced efficacy in women compared to men with similar degrees of adherence. To select the most effective PrEP strategies, preclinical studies are critically needed to establish correlations between drug concentrations (pharmacokinetics [PK]) and protective efficacy (pharmacodynamics [PD]). We utilized an in vivo preclinical model to perform a PK-PD analysis of systemic TDF PrEP for vaginal HIV acquisition...
February 1, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28145050/cytochrome-2b6-polymorphism-and-efavirenz-induced-central-nervous-system-symptoms-a-substudy-of-the-anrs-alize-trial
#16
S Gallien, V Journot, M-A Loriot, H Sauvageon, P Morlat, J Reynes, V Reliquet, G Chêne, J-M Molina
OBJECTIVES: Single nucleotide polymorphisms in the cytochrome P450 (CYP) 2B6 gene have been associated with high interindividual variation in efavirenz pharmacokinetics. However, clinical data on the relationship of CYP2B6 polymorphisms with the occurrence of efavirenz-induced central nervous system (CNS) symptoms are limited. METHODS: We analysed four polymorphisms in the CYP2B6 (516 G>T), CYP3A5 (6986 A>G) and ATP-binding cassette, sub-family B, member 1 (ABCB1) (2677 G>T/A and 3435 C>T) genes in HIV-infected adults virologically suppressed on a protease inhibitor-based regimen who switched to a regimen containing emtricitabine, didanosine and efavirenz in the setting of the ANRS ALIZE trial...
February 1, 2017: HIV Medicine
https://www.readbyqxmd.com/read/28128004/long-acting-slow-effective-release-antiretroviral-therapy
#17
Benson Edagwa, JoEllyn McMillan, Brady Sillman, Howard E Gendelman
Advances in long-acting antiretroviral therapy (ART) can revolutionize current HIV/AIDS treatments. We coined the term 'long-acting slow effective release ART' (LASER ART) to highlight the required formulation properties of slow drug dissolution, poor water-solubility, bioavailability, little-to-no off-target toxicities and improved regimen adherence. Drug carrier technologies characterized by high antiretroviral drug (ARV) payloads in a single carrier improve the pharmacokinetic and pharmacodynamic profiles...
February 6, 2017: Expert Opinion on Drug Delivery
https://www.readbyqxmd.com/read/28114388/multicompartmental-pharmacokinetic-model-of-tenofovir-delivery-to-the-rectal-mucosa-by-an-enema
#18
Yajing Gao, David F Katz
Rectal enemas that contain prophylactic levels of anti-HIV microbicides such as tenofovir have emerged as a promising dosage form to prevent sexually transmitted HIV infections. The enema vehicle is promising due to its likely ability to deliver a large amount of drug along the length of the rectal canal. Computational models of microbicide drug delivery by enemas can help their design process by determining key factors governing drug transport and, more specifically, the time history and degree of protection...
2017: PloS One
https://www.readbyqxmd.com/read/28114187/nevirapine-pharmacokinetics-and-safety-in-neonates-receiving-combination-antiretroviral-therapy-for-prevention-of-vertical-hiv-transmission
#19
Elaine Lau, Jason Brophy, Lindy Samson, Fatima Kakkar, Douglas Campbell, Mark H Yudin, Kellie Murphy, Winnie Seto, David Colantonio, Stanley E Read, Ari Bitnun
BACKGROUND: Nevirapine (NVP)-based combination antiretroviral therapy (cART) is routinely prescribed to infants deemed at high risk of vertical HIV infection in our centers. We evaluated NVP pharmacokinetics and safety of this regimen. METHODS: Neonates were recruited prospectively between September 2012 and April 2015 or enrolled retrospectively if treated similarly prior to prospective study initiation. NVP was dosed at 150 mg/m daily for 14 days, then twice daily for 14 days...
January 20, 2017: Journal of Acquired Immune Deficiency Syndromes: JAIDS
https://www.readbyqxmd.com/read/28109702/population-pharmacokinetics-and-dose-optimisation-of-ritonavir-boosted-atazanavir-in-thai-hiv-infected-patients
#20
Baralee Punyawudho, Narukjaporn Thammajaruk, Kiat Ruxrungtham, Anchalee Avihingsanon
There is evidence that Thai patients receiving standard doses of ritonavir (RTV)-boosted atazanavir (ATV/r) have high exposure to atazanavir (ATV) leading to a higher risk of toxicity. A lower dose of ATV/r may provide adequate exposure in this population. However, pharmacokinetic data on ATV/r in Thai patients required for dose adjustment are limited. This study aimed to develop a population pharmacokinetic model of ATV/r and to determine the influence of patient characteristics on ATV pharmacokinetics. Monte Carlo simulations were performed to estimate the proportion of patients achieving target ATV trough concentration (Ctrough) with the standard ATV/r dose of 300/100 mg and a low dose of 200/100 mg once daily (OD)...
January 18, 2017: International Journal of Antimicrobial Agents
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