Reyataz ® (atazanavir) - Bristol
... Nephrolithiasis and Cholelithiasis: Cases of nephrolithiasis and/or cholelithiasis were reported during post-marketing surveillance in HIV-infected patients receiving atazanavir therapy. Some patients required hospitalization for additional management and some had complications. Because these events ...
... Nephrolithiasis and Cholelithiasis: Cases of nephrolithiasis and/or cholelithiasis were reported during post-marketing surveillance in HIV-infected patients receiving atazanavir therapy. Some patients required hospitalization for additional management and some had complications. Because these events ...
PPT - IAS-USA
... – RPV/TDF/FTC superior to EFV/TDF/FTC if VL <100,0001 – Don’t use RPV if VL >100,000, CD4 <200 – Food requirement; avoid PPI; stagger H2 blocker Slide 30 of 44 ...
... – RPV/TDF/FTC superior to EFV/TDF/FTC if VL <100,0001 – Don’t use RPV if VL >100,000, CD4 <200 – Food requirement; avoid PPI; stagger H2 blocker Slide 30 of 44 ...
Reyataz label - HIV Drug Resistance Database
... REYATAZ (atazanavir sulfate) is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. This indication is based on analyses of plasma HIV-1 RNA levels and CD4+ cell counts from controlled studies of 96 weeks duration in antiretroviral-naive and 48 weeks durat ...
... REYATAZ (atazanavir sulfate) is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. This indication is based on analyses of plasma HIV-1 RNA levels and CD4+ cell counts from controlled studies of 96 weeks duration in antiretroviral-naive and 48 weeks durat ...
Promega`s P450-GloTM Luminescent Cytochrome
... Great Sensitivity - Low background levels and a large dynamic range result in sensitive assays that require less P450 enzyme Soluble Substrates - P450-Glo™ substrates are highly soluble in aqueous solutions. Single readout - Multiple P450 isoforms with multiple substrates can be assayed at a s ...
... Great Sensitivity - Low background levels and a large dynamic range result in sensitive assays that require less P450 enzyme Soluble Substrates - P450-Glo™ substrates are highly soluble in aqueous solutions. Single readout - Multiple P450 isoforms with multiple substrates can be assayed at a s ...
Technical Guide for countries to set targets for universal
... areas such as cities and for specific settings such as prisons. It is important to define the scope of the areas or settings under consideration. While this Technical guide focuses primarily on IDUs, it may also be useful for setting targets for HIV interventions targeting problematic drug users who ...
... areas such as cities and for specific settings such as prisons. It is important to define the scope of the areas or settings under consideration. While this Technical guide focuses primarily on IDUs, it may also be useful for setting targets for HIV interventions targeting problematic drug users who ...
Comparison of Four-Drug Regimens and Pairs of Sequential Three
... lthough many drugs are approved for the treatment of human immunodeficiency virus type 1 (HIV-1) infection, the cause of the acquired immunodeficiency syndrome (AIDS), they belong to just four different classes: nucleoside or nucleotide reverse-transcriptase inhibitors (nucleoside analogues), nonnuc ...
... lthough many drugs are approved for the treatment of human immunodeficiency virus type 1 (HIV-1) infection, the cause of the acquired immunodeficiency syndrome (AIDS), they belong to just four different classes: nucleoside or nucleotide reverse-transcriptase inhibitors (nucleoside analogues), nonnuc ...
Inhibiting the breakdown of endogenous opioids and
... Outside the cells, enkephalins interact with opioid receptors only, and their signal is interrupted by the concomitant action of two zinc metallopeptidases — NEP and APN — that generate inactive metabolites. The circulating concentrations of enkephalins, which modulate the physiological analgesic re ...
... Outside the cells, enkephalins interact with opioid receptors only, and their signal is interrupted by the concomitant action of two zinc metallopeptidases — NEP and APN — that generate inactive metabolites. The circulating concentrations of enkephalins, which modulate the physiological analgesic re ...
Inhibitory Effects of Fruit Juices on Cytochrome P450
... activities observed with 0.25 ml (0.05% v/v) of pineapple juice at preincubation periods of 0, 5, 15, and 30 min were 79.4%, 72.4%, 64.9%, and 55.1% respectively. These data suggest that pineapple juice causes irreversible inhibition of human CYP2C9 activity. Thus, we discovered that pineapple juice ...
... activities observed with 0.25 ml (0.05% v/v) of pineapple juice at preincubation periods of 0, 5, 15, and 30 min were 79.4%, 72.4%, 64.9%, and 55.1% respectively. These data suggest that pineapple juice causes irreversible inhibition of human CYP2C9 activity. Thus, we discovered that pineapple juice ...
drug interactions with calcium channel blockers: possible
... Chemically, CCBs (Fig. 1) are classified into three classes, benzothiazepines (e.g., diltiazem), dihydropyridines (e.g., amlodipine, felodipine, nicardipine, and nifedipine), and phenylalkylamines (e.g., verapamil). Like diltiazem, most of these CCBs contain an amine functional group and undergo N-d ...
... Chemically, CCBs (Fig. 1) are classified into three classes, benzothiazepines (e.g., diltiazem), dihydropyridines (e.g., amlodipine, felodipine, nicardipine, and nifedipine), and phenylalkylamines (e.g., verapamil). Like diltiazem, most of these CCBs contain an amine functional group and undergo N-d ...
Final Program - International Society for Antiviral Research
... The Society was organized in 1987 as a non‐profit scientific organization for the purpose of advancing and disseminating knowledge in all areas of antiviral research. To achieve this objective, the Society organizes an annual meeting. The Society is now in its twenty fifth year of existence, and has ...
... The Society was organized in 1987 as a non‐profit scientific organization for the purpose of advancing and disseminating knowledge in all areas of antiviral research. To achieve this objective, the Society organizes an annual meeting. The Society is now in its twenty fifth year of existence, and has ...
Return on Investment in Needle and Syringe Programs in Australia
... In this study, NCHECR repeated the ecological study of change in HIV prevalence in cities with and without NSPs because several countries have introduced NSPs since the previous study (Hurley et al. 1997). The study also used a similar methodology to assess the effectiveness of NSPs for prevention o ...
... In this study, NCHECR repeated the ecological study of change in HIV prevalence in cities with and without NSPs because several countries have introduced NSPs since the previous study (Hurley et al. 1997). The study also used a similar methodology to assess the effectiveness of NSPs for prevention o ...
The role of metabolic inhibition
... nicotine, aminoglycosides, ethylene oxide, CO) are directly toxic while many chemicals exert ...
... nicotine, aminoglycosides, ethylene oxide, CO) are directly toxic while many chemicals exert ...
Reaction Phenotyping Methods using Recombinant Enzymes and
... P450s. Use Relative Activity Factors (RAFs) approach and/or relative hepatic abundance of the enzymes to determine relative importance when multiple CYPs involved. Scaled to predict in vivo clearance. • The effect of co-incubated CYP-selective chemical or monoclonal antibody inhibitors on rates of m ...
... P450s. Use Relative Activity Factors (RAFs) approach and/or relative hepatic abundance of the enzymes to determine relative importance when multiple CYPs involved. Scaled to predict in vivo clearance. • The effect of co-incubated CYP-selective chemical or monoclonal antibody inhibitors on rates of m ...
Mechanism-based Inhibition: Deriving KI and kinact
... The potential of enzyme inhibition is frequently quantified in terms of IC50 values, characterizing the degree to which the enzyme activity is inhibited, which are then used, e.g., for ranking of new chemical entities in terms of their inhibitory potency. Inhibition of cytochrome P450 enzymes is a p ...
... The potential of enzyme inhibition is frequently quantified in terms of IC50 values, characterizing the degree to which the enzyme activity is inhibited, which are then used, e.g., for ranking of new chemical entities in terms of their inhibitory potency. Inhibition of cytochrome P450 enzymes is a p ...
PerspectiVe
... engaged in fragment-based research has increased, and as a consequence, there has been continued development and refinement of techniques and methods. From its inception, the fragment-based approach had two central tenets that were critical to its success and that have set it apart from HTS and othe ...
... engaged in fragment-based research has increased, and as a consequence, there has been continued development and refinement of techniques and methods. From its inception, the fragment-based approach had two central tenets that were critical to its success and that have set it apart from HTS and othe ...
New Hepatitis C Therapies: The Toolbox, Strategies, and
... The HCV life cycle is now well understood.1–4 In theory, every step of the viral life cycle can be the target of specific inhibitory approaches through various mechanisms.5 However, antiviral drugs already on the market or in clinical development include only inhibitors of HCV polyprotein maturation ...
... The HCV life cycle is now well understood.1–4 In theory, every step of the viral life cycle can be the target of specific inhibitory approaches through various mechanisms.5 However, antiviral drugs already on the market or in clinical development include only inhibitors of HCV polyprotein maturation ...
Product Monograph Template - Standard
... HIV and hepatitis C virus (HCV) co-infected patients with mild to moderate hepatic impairment (see ACTION AND CLINICAL PHARMACOLOGY, Pharmacokinetics). Patients with underlying hepatitis B or C or marked elevations in transaminases prior to treatment may be at increased risk for developing or worsen ...
... HIV and hepatitis C virus (HCV) co-infected patients with mild to moderate hepatic impairment (see ACTION AND CLINICAL PHARMACOLOGY, Pharmacokinetics). Patients with underlying hepatitis B or C or marked elevations in transaminases prior to treatment may be at increased risk for developing or worsen ...
A Novel Model for the Prediction of Drug
... studying clinical pharmacokinetic drug-drug interactions (DDIs) of drugs that are primarily metabolized by CYP3A4/5. However, ketoconazole at therapeutic, high concentrations also inhibits cytochromes P450 (P450) other than CYP3A4/5, which has made the predictions of DDIs less accurate. Determining ...
... studying clinical pharmacokinetic drug-drug interactions (DDIs) of drugs that are primarily metabolized by CYP3A4/5. However, ketoconazole at therapeutic, high concentrations also inhibits cytochromes P450 (P450) other than CYP3A4/5, which has made the predictions of DDIs less accurate. Determining ...
HIV Research Inventory
... Salix Pharmaceuticals – CFHD3092: This study is being conducted to evaluate the safety and tolerability of crofelemer 125 mg twice a day, taken orally, over 48 weeks of therapy in human immunodeficiency virus-positive (HIV+) subjects with diarrhea. ...
... Salix Pharmaceuticals – CFHD3092: This study is being conducted to evaluate the safety and tolerability of crofelemer 125 mg twice a day, taken orally, over 48 weeks of therapy in human immunodeficiency virus-positive (HIV+) subjects with diarrhea. ...
zidovudine and lamivudine - WHO archives
... 83% of patients on triple therapy had unquantifiable viral load measures. For the most part, side effects have been minimal and easily managed and there are support groups to encourage adherence.8 At HIV clinics in Pune and Ahmedabad, India, a recent study demonstrated the benefit of triple combinat ...
... 83% of patients on triple therapy had unquantifiable viral load measures. For the most part, side effects have been minimal and easily managed and there are support groups to encourage adherence.8 At HIV clinics in Pune and Ahmedabad, India, a recent study demonstrated the benefit of triple combinat ...
Advances in and applications of proteasome inhibitors
... C derivative (Figure 2) having an IC50 in the low nanomolar level [29]. Other natural proteasome inhibitors include the TMC-95 family of cyclic peptides from the fungus Apiospora montagnei [30], with TMC-95A being the only natural product inhibitor to non-covalently block all active sites of the pro ...
... C derivative (Figure 2) having an IC50 in the low nanomolar level [29]. Other natural proteasome inhibitors include the TMC-95 family of cyclic peptides from the fungus Apiospora montagnei [30], with TMC-95A being the only natural product inhibitor to non-covalently block all active sites of the pro ...
Integrated Post-Exposure Protocol for HIV, HBV and HCV
... 1) The exposure incident (for health care workers and emergency responders) must be reported immediately to the appropriate administrative personnel, usually the immediate supervisor of the unit/facility where the exposure occurred. 2) The forms and requisitions that must be completed, as well as in ...
... 1) The exposure incident (for health care workers and emergency responders) must be reported immediately to the appropriate administrative personnel, usually the immediate supervisor of the unit/facility where the exposure occurred. 2) The forms and requisitions that must be completed, as well as in ...
Macrocycles in new drug discovery
... core, suggesting that an evolutionary advantage may be associated with the production of second ary metabolites based upon these scaffolds [1,11] . There are different classes that macrocycles could fall into, including peptidic and nonpeptidic nat ural products, non-natural (synthetic) peptides a ...
... core, suggesting that an evolutionary advantage may be associated with the production of second ary metabolites based upon these scaffolds [1,11] . There are different classes that macrocycles could fall into, including peptidic and nonpeptidic nat ural products, non-natural (synthetic) peptides a ...
Pathway-Dependent Inhibition of Paclitaxel Hydroxylation by Kinase
... samples were prepared as described previously, and the levels of 6a-hydroxypaclitaxel and p-39-hydroxypaclitaxel were quantified. For the time-dependent inhibition component of this assay, kinase inhibitors at a concentration of 10 mM were first incubated with HLMs in the presence of NADPH. After a ...
... samples were prepared as described previously, and the levels of 6a-hydroxypaclitaxel and p-39-hydroxypaclitaxel were quantified. For the time-dependent inhibition component of this assay, kinase inhibitors at a concentration of 10 mM were first incubated with HLMs in the presence of NADPH. After a ...
Discovery and development of HIV-protease inhibitors
Many major physiological processes depend on regulation of proteolytic enzyme activity and there can be dramatic consequences when equilibrium between an enzyme and its substrates is disturbed. In this prospective, the discovery of small-molecule ligands, like protease inhibitors, that can modulate catalytic activities has an enormous therapeutic effect. Hence, inhibition of the HIV protease is one of the most important approaches for the therapeutic intervention in HIV infection and their development is regarded as major success of structure-based drug design. They are highly effective against HIV and have, since the 1990s, been a key component of anti-retroviral therapies for HIV/AIDS.