Biocatalysis
... serum half-life for a drug. Metabolites are not always the source of negative data for a drug. In a number of cases metabolites have been shown to display biological activities superior to or different from that of the drug from which they are derived. The identification of these so-called ‘active m ...
... serum half-life for a drug. Metabolites are not always the source of negative data for a drug. In a number of cases metabolites have been shown to display biological activities superior to or different from that of the drug from which they are derived. The identification of these so-called ‘active m ...
Side Effects of ARVs
... To describe the major side effects of HIV treatment To know useful lab tests for HIV side effect monitoring To review case studies of how to choose initial HIV regimen, and what regimen to switch to in the event of side effects Benefits of treatment ...
... To describe the major side effects of HIV treatment To know useful lab tests for HIV side effect monitoring To review case studies of how to choose initial HIV regimen, and what regimen to switch to in the event of side effects Benefits of treatment ...
Infection, Genetics and Evolution
... Global trends in antiretroviral resistance in treatment-naive individuals with HIV after rollout of antiretroviral treatment in resourcelimited settings: a global collaborative study and meta-regression analysis ...
... Global trends in antiretroviral resistance in treatment-naive individuals with HIV after rollout of antiretroviral treatment in resourcelimited settings: a global collaborative study and meta-regression analysis ...
Side Effects of ARVs
... To describe the major side effects of HIV treatment To know useful lab tests for HIV side effect monitoring To review case studies of how to choose initial HIV regimen, and what regimen to switch to in the event of side effects Benefits of treatment ...
... To describe the major side effects of HIV treatment To know useful lab tests for HIV side effect monitoring To review case studies of how to choose initial HIV regimen, and what regimen to switch to in the event of side effects Benefits of treatment ...
![[3]-Drug Metabolism-Lect [Compatibility Mode]](http://s1.studyres.com/store/data/014976812_1-98aead36b4cf9a08acaf1a5ae778ddf3-300x300.png)
[3]-Drug Metabolism-Lect [Compatibility Mode]
... the biochemical changes of the drugs and other foreign substances in the body. ...
... the biochemical changes of the drugs and other foreign substances in the body. ...
RIFAMPIN
... Isoniazid is well absorbed from GIT. It diffuses readily into all tissues, body fluids, (CSF, Pleural fluids etc… ) Isoniazid is metabolized in the liver by acetylation then isoniazid and it is metabolites are excreted by the ...
... Isoniazid is well absorbed from GIT. It diffuses readily into all tissues, body fluids, (CSF, Pleural fluids etc… ) Isoniazid is metabolized in the liver by acetylation then isoniazid and it is metabolites are excreted by the ...
Lecture 12, computers CORRECTED
... 1. The known structure is used as a template. The backbone of the new receptor is constructed on a computer to match that of the known protein. 2. Side chains are added in favorable conformations, and the energy is minimized by computer. 3. Key residues in the new receptor are identified and tested ...
... 1. The known structure is used as a template. The backbone of the new receptor is constructed on a computer to match that of the known protein. 2. Side chains are added in favorable conformations, and the energy is minimized by computer. 3. Key residues in the new receptor are identified and tested ...
... (HIVdb or HIV-SEQ), AntiRetroScan (ARS), and Visible Genetics/Bayer Diagnostics (VGI), have been developed for estimating the level of resistance mutations in HIV-1 protease and transcriptase based on this approach [18,19]. HIVdb scans a sequence for known resistance mutations and generates scores f ...
Viral Binding and Fusion—The Next Targets in - IAS-USA
... that mechanically brings the viral and target cell membranes together. Rational drug discovery is based on an understanding at the molecular level of the process to be inhibited. Since the induction of membrane fusion by HIV is a complex process, there are discrete steps at which interference with t ...
... that mechanically brings the viral and target cell membranes together. Rational drug discovery is based on an understanding at the molecular level of the process to be inhibited. Since the induction of membrane fusion by HIV is a complex process, there are discrete steps at which interference with t ...
| Bedaquiline: 10 years later, the drug susceptibility testing protocol is still pending
... The World Health Organization (WHO)-recommended regimens include at least four drugs divided into five groups. Among them, pyrazinamide should be administered with a later-generation fluoroquinolone, ethionamide or prothionamide, cycloserine or para-aminosalicylic acid, and second-line injectable dr ...
... The World Health Organization (WHO)-recommended regimens include at least four drugs divided into five groups. Among them, pyrazinamide should be administered with a later-generation fluoroquinolone, ethionamide or prothionamide, cycloserine or para-aminosalicylic acid, and second-line injectable dr ...
Considerations for Target Selection in CNS Drug Discovery Programs
... Simple physicochemical guidelines and computational models can be helpful in altering the probability of encountering P-gp efflux; however, it is abundantly evident that compounds with identical physicochemical properties can have vastly different efflux properties. As with any small molecule–protei ...
... Simple physicochemical guidelines and computational models can be helpful in altering the probability of encountering P-gp efflux; however, it is abundantly evident that compounds with identical physicochemical properties can have vastly different efflux properties. As with any small molecule–protei ...
Powerpoint
... kinase-like superfamily can be traced with careful analysis • So taking this a step further … The Role of Evolution ...
... kinase-like superfamily can be traced with careful analysis • So taking this a step further … The Role of Evolution ...
Poison Control Centers Synthetic Drugs of Abuse
... “I'm concerned that it could hurt people…We made this as a research compound and published it and did what we were supposed to do. You can’t be responsible for what idiots are going to do.” ...
... “I'm concerned that it could hurt people…We made this as a research compound and published it and did what we were supposed to do. You can’t be responsible for what idiots are going to do.” ...
The Development of Deuterium-Containing Drugs
... Figure 3) (9). Minor CYP2D6 inhibition was observed at higher CTP-347 doses, consistent with reversible, competitive inhibition seen in vitro. The study is also ...
... Figure 3) (9). Minor CYP2D6 inhibition was observed at higher CTP-347 doses, consistent with reversible, competitive inhibition seen in vitro. The study is also ...
The Development of Deuterium-Containing Drugs
... Figure 3) (9). Minor CYP2D6 inhibition was observed at higher CTP-347 doses, consistent with reversible, competitive inhibition seen in vitro. The study is also ...
... Figure 3) (9). Minor CYP2D6 inhibition was observed at higher CTP-347 doses, consistent with reversible, competitive inhibition seen in vitro. The study is also ...
Dr. Reddy Qs - Website of Neelay Gandhi
... All are true about vancomycin resistance except: a) VRE vancomycin resistant enterococci has decreased affinity to cell wall precursors, D-alanyl-D-lactate. b) Resistance could occur due to decreased access to the site of action. c) Flushing, pruritus, redness of face & neck could occur with I.V. ad ...
... All are true about vancomycin resistance except: a) VRE vancomycin resistant enterococci has decreased affinity to cell wall precursors, D-alanyl-D-lactate. b) Resistance could occur due to decreased access to the site of action. c) Flushing, pruritus, redness of face & neck could occur with I.V. ad ...
Antiviral Agents: Structural Basis of Action and Rational Design
... Viral uptake occurs through different mechanisms such as endocytosis (as for example, in the case of influenza virus) or the fusion of the cellular membrane with the viral envelope, as demonstrated in the case of retroviruses (see Chap. 16). These events allow the internalization of the capsid conta ...
... Viral uptake occurs through different mechanisms such as endocytosis (as for example, in the case of influenza virus) or the fusion of the cellular membrane with the viral envelope, as demonstrated in the case of retroviruses (see Chap. 16). These events allow the internalization of the capsid conta ...
Characterization of Human Immunodeficiency Viruses Resistant to
... Additional preclinical studies have demonstrated that the 5'-triphosphates of (-)-FTC and (-)-BCH-189 are competitive inhibitors of HIV-1 reverse transcriptase (RT) and are potent DNA chain terminators when HIV-1 RT is used (13, 35). (-)-BCH-189 has progressed to phase I clinical trials, and studies ...
... Additional preclinical studies have demonstrated that the 5'-triphosphates of (-)-FTC and (-)-BCH-189 are competitive inhibitors of HIV-1 reverse transcriptase (RT) and are potent DNA chain terminators when HIV-1 RT is used (13, 35). (-)-BCH-189 has progressed to phase I clinical trials, and studies ...
Counterfeit, Black-Market and Off-Label Drug Use
... vanish from a UM pharmacy? Technician is charged with stealing $14 million in expensive cancer drugs over three years before he was discovered. ...
... vanish from a UM pharmacy? Technician is charged with stealing $14 million in expensive cancer drugs over three years before he was discovered. ...
Drug Discovery Pipeline Brief Report 2011
... of leading compounds with strong intellectual property. In vitro data show that the novel compound, D824 has an activity 1000 times more potent than Gleevec on chronic myloid leukemia cells containing no mutations, but more importantly exhibits excellent activities on all cell lines that are resista ...
... of leading compounds with strong intellectual property. In vitro data show that the novel compound, D824 has an activity 1000 times more potent than Gleevec on chronic myloid leukemia cells containing no mutations, but more importantly exhibits excellent activities on all cell lines that are resista ...
汤慧芳
... Moxifloxacin is the most active against M tuberculosis by weight in vitro. Levofloxacin tends to be slightly more active than ciprofloxacin against M tuberculosis, Ciprofloxacin is slightly more active against atypical mycobacteria. Fluoroquinolones are an important addition to the drugs available f ...
... Moxifloxacin is the most active against M tuberculosis by weight in vitro. Levofloxacin tends to be slightly more active than ciprofloxacin against M tuberculosis, Ciprofloxacin is slightly more active against atypical mycobacteria. Fluoroquinolones are an important addition to the drugs available f ...
Development of new drugs for chemoprophylaxis of malaria.
... for mefloquine in a collaborative effort between the US Army and SmithKline Beecham. Halfan® is US Food and Drug Administration (FDA) approved and marketed in many areas of the world. However, its usefulness is limited by possible cross-resistance with mefloquine, cardiac toxicity, and poor absorpti ...
... for mefloquine in a collaborative effort between the US Army and SmithKline Beecham. Halfan® is US Food and Drug Administration (FDA) approved and marketed in many areas of the world. However, its usefulness is limited by possible cross-resistance with mefloquine, cardiac toxicity, and poor absorpti ...
Some Principles in the Chemotherapy of Bacterial Infections—I
... bactericidal drugs, may give the clinician very useful guidance in therapy (Garrod and Waterworth, 1962). In general there is virtually never a synergistic effect between bacteriostatic drugs. With marginal doses the effect is purely additive. Clinically a more than adequate dose of both drugs is us ...
... bactericidal drugs, may give the clinician very useful guidance in therapy (Garrod and Waterworth, 1962). In general there is virtually never a synergistic effect between bacteriostatic drugs. With marginal doses the effect is purely additive. Clinically a more than adequate dose of both drugs is us ...
Pharm_Essays!
... inhibitors of the HMG-CoA reductase enzyme which converts HMG-CoA to mevalonic acid. This is the rate-limiting step in hepatic cholesterol synthesis. As a result there is a decrease in cholesterol synthesis followed by up-regulation of LDL-receptors at the hepatocyte surface leading to increased LDL ...
... inhibitors of the HMG-CoA reductase enzyme which converts HMG-CoA to mevalonic acid. This is the rate-limiting step in hepatic cholesterol synthesis. As a result there is a decrease in cholesterol synthesis followed by up-regulation of LDL-receptors at the hepatocyte surface leading to increased LDL ...
Lecture 13, Inhibitors - Cal State LA
... •Resemble the substrate, so targeted to binding site; •Contain an electrophilic group (below, or alpha-halo ketones, or diazoketones) that reacts with a nucleophilic group of the enzyme in or near the active site to form a covalent bond. ...
... •Resemble the substrate, so targeted to binding site; •Contain an electrophilic group (below, or alpha-halo ketones, or diazoketones) that reacts with a nucleophilic group of the enzyme in or near the active site to form a covalent bond. ...
Discovery and development of non-nucleoside reverse-transcriptase inhibitors
Non-nucleoside reverse-transcriptase inhibitors (NNRTIs) are antiretroviral drugs used in the treatment of human immunodeficiency virus (HIV). NNRTIs inhibit reverse transcriptase (RT), an enzyme that controls the replication of the genetic material of HIV. RT is one of the most popular targets in the field of antiretroviral drug development.Discovery and development of NNRTIs began in the late 1980s and in the end of 2009 four NNRTI had been approved by regulatory authorities and several others were undergoing clinical development. Drug resistance develops quickly if NNRTIs are administered as monotherapy and therefore NNRTIs are always given as part of combination therapy, the highly active antiretroviral therapy (HAART).