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Antimicrobials during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
This agent (atazanavir) is a protease inhibitor used to treat HIV. 1309 women used Atazanavir during the first trimester, and the frequency of birth defects was not increased (http://pregnancyregistry.gsk.com). The drug was not teratogenic in rabbits and rats given the usual therapeutic dose during pregnancy.
How Artificial Intelligence and IoT Aid in Fighting COVID-19
Published in Fadi Al-Turjman, AI-Powered IoT for COVID-19, 2020
Abdullahi Umar Ibrahim, Mehmet Ozsoz, Fadi Al-Turjman, Pwadubashiyi Pwavodi Coston, Basil Bartholomew Duwa
Different systems are being tried in China, including drug repurposing. A pre-trained deep learning-based drug-target interaction model, termed Molecule Transformer-Drug Target Interaction (MT-DTI), was utilized to distinguish industrially accessible medications that could follow up on viral proteins of SARS-CoV-2. Atazanavir, an antiretroviral prescription used to treat and forestall the human immunodeficiency infection (HIV), was analyzed as the best substance (Luo et al., 2020).
Atazanavir
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
Atazanavir was a welcome addition to the armamentarium of antiretroviral drugs for the treatment of HIV-1-infected adults in 2003 and in 2008 for the treatment of HIV-1-infected children. At the time of licensing, it had many advantages over other, older protease inhibitors not the least of which is potency (at least in the treatment-naive setting), a more favorable lipid profile than many other protease inhibitors (even when co-administered with ritonavir), low pill burden, and once-daily dosing. However, more recent data from properly conducted clinical trials have shown a more favorable toxicity profile of ritonavir-boosted darunavir or raltegravir leading to the demotion of atazanavir to an “alternative” drug, at least for naive patients. It still remains an important drug globally, both in the adult and pediatric setting, most especially now that the powder formulation is approved for use in infants aged 6 months or older. Further refinement of genetic testing to predict who is at the greatest risk of atazanavir-related hyperbilirubinemia will inform the extent to which switching away from boosted atazanavir could have been avoided, which has had a direct impact on the drug being used less, particularly in resource-rich settings.
Alteration of liver immunity by increasing inflammatory response during co-administration of methamphetamine and atazanavir
Published in Immunopharmacology and Immunotoxicology, 2020
Yanfei Li, Sangsang Li, Yang Xia, Xiangrong Li, Tingjun Chen, Jie Yan, Yong Wang
Human hepatic cell line LO2 (Zhongqiao Xinzhou Biotech, Shanghai, China) and human monocyte cell line THP-1 (Zhongqiao Xinzhou Biotech) were cultured in 1640 medium supplemented with 10% fetal bovine serum and 1% penicillin/streptomycin. Incubator for cell culture was set to 5% carbon dioxide and 37 °C. THP-1 was initially suspended cells. After THP-1 cells were treated with phorbol 12-myristate 13-acetate (PMA) (final concentration of 100 ng/mL) for 24 h, the cells differentiated into macrophages and adhered to the wall of cell culture dish for growth. LO2 cells in logarithmic growth phase were washed with PBS twice. Then, after trypsin-EDTA (Ethylenediaminetetraacetic acid) digestion, single-cell suspensions of LO2 cells were prepared by pipette light mixing. Cell density (5 × 106) was calculated by cell counting in six-well plates, and cell adhesion was observed the next day. Atazanavir powder (Meilun Biotech, Dalian, China) was dissolved in dimethyl sulphoxide to 1 M and stored at −20 °C. METH solution was prepared in ultra-pure water at 1 M and stored at −20 °C. Atazanavir or METH was diluted further in serum-free media before cell treatment. The same volume of drug solutions at various concentrations was added to cells. LO2 cells were initially incubated with atazanavir (0, 40, 200, or 1 μM) and METH (0, 0.05, 0.2, or 1 mM) for 24 h. Then, after centrifugation of LO2 cells, the cell culture supernatant was collected and transferred to THP-1-derived macrophages to culture for another 24 h.
Managing antiretroviral therapy in the elderly HIV patient
Published in Expert Review of Clinical Pharmacology, 2018
Giovanni Guaraldi, Ines Pintassilgo, Jovana Milic, Cristina Mussini
Parsons et al. compared lopinavir trough concentrations in two age-differentiated cohorts of treatment-naïve PLWH [37]. A significant positive correlation existed between age and lopinavir trough concentration after adjusting for sex at 24 weeks, but not at 36 or 96 weeks. Other study including 44 OALWH showed that older age was associated with higher lopinavir concentration [38]. However, other reports have not confirmed any age-related differences in the pharmacokinetics of lopinavir/ritonavir [39,40]. In a prospective pharmacokinetic study, no clinically significant effect of age or gender on single-dose atazanavir in 60 healthy volunteers was reported [41]. On the contrary, a study including 51 OALWH receiving darunavir showed decreased clearance of 14% with every 10 years increase in age [42]. So far, we cannot ascertain that boosted PI plasma concentrations are higher in OALWH.
Unraveling enhanced brain delivery of paliperidone-loaded lipid nanoconstructs: pharmacokinetic, behavioral, biochemical, and histological aspects
Published in Drug Delivery, 2022
Saleha Rehman, Bushra Nabi, Amaan Javed, Tahira Khan, Ashif Iqubal, Mohammad Javed Ansari, Sanjula Baboota, Javed Ali
Additionally, there was no observation of chromatolysis, vacuolization, neuronal damage, or pyknosis in any part of the brain. As observed from the histological finding, the conventional (drug suspension) group did not exhibit any signs of toxicity. Thus, it was concluded that the prepared formulation PPD-LNC is safe for administration via oral route as no toxicity was observed. Khan et al. showed that no signs of toxicity or neuronal damage were observed in histopathological images of atazanavir-NLC. and is thus safe for oral administration (Khan et al., 2020). Additionally, Rahman et al. also revealed that histopathological images of Zerumbone-loaded NLC displayed no degenerative, vacuolar, or hemorrhagic alterations in the brain tissues (Rahman et al., 2014).