Antimycobacterial Drugs (抗分枝杆菌药)
... 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 ...
medicinal - American Chemical Society
... the amide substituent of lysergamides may have a significant influence on hallucinogenic activity, as reflected in the DD model. The relative potency of 4 (16% of 1) is in agreement with clinical evaluations (510% of thereby lending support to the validity of this model. It is particularly noteworth ...
... the amide substituent of lysergamides may have a significant influence on hallucinogenic activity, as reflected in the DD model. The relative potency of 4 (16% of 1) is in agreement with clinical evaluations (510% of thereby lending support to the validity of this model. It is particularly noteworth ...
Antimalarial drug discovery: efficacy models for compound
... “Origin”). These reflect the drug concentrations at which 50% and 90% of suppression of parasitemia is achieved. Note that with short half-life drugs it may be necessary to dose multiple times per day. Two other parameters measured in this study are relative potency compared to an appropriate standa ...
... “Origin”). These reflect the drug concentrations at which 50% and 90% of suppression of parasitemia is achieved. Note that with short half-life drugs it may be necessary to dose multiple times per day. Two other parameters measured in this study are relative potency compared to an appropriate standa ...
Antimycobacterial drugs
... 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 ...
Document
... The world's first pharmacogenomic microarray designed for clinical applications that provides comprehensive coverage of gene variations – including deletions and duplications – for the 2D6 and 2C19 genes, which play a role in the metabolism of about 25% of all prescription drugs. It is intended to b ...
... The world's first pharmacogenomic microarray designed for clinical applications that provides comprehensive coverage of gene variations – including deletions and duplications – for the 2D6 and 2C19 genes, which play a role in the metabolism of about 25% of all prescription drugs. It is intended to b ...
Productivity Shortfalls in Drug Discovery: Contributions from the
... (Enna and Williams, 2009a), to the exclusion of a more hierarchically integrated, pharmacologically based approach (Williams, 2005), has become increasingly problematic. It has been further compounded by NCEs that, although active against the in vitro target construct, gave less than stellar results ...
... (Enna and Williams, 2009a), to the exclusion of a more hierarchically integrated, pharmacologically based approach (Williams, 2005), has become increasingly problematic. It has been further compounded by NCEs that, although active against the in vitro target construct, gave less than stellar results ...
Strategies and Challenges Involved in the Discovery of
... those discovered from conventional screening and optimization methods. To this end, this rationale has led to ligand efficiency, which is described as the free energy of ligand binding to an enzyme-binding site averaged for each nonhydrogen atom [13]. Thus, the emphasis with this technique is to pri ...
... those discovered from conventional screening and optimization methods. To this end, this rationale has led to ligand efficiency, which is described as the free energy of ligand binding to an enzyme-binding site averaged for each nonhydrogen atom [13]. Thus, the emphasis with this technique is to pri ...
Antiepileptic drugs
... mal). Status epilepticus is a lifethreatening condition in which seizure activity is uninterrupted. ...
... mal). Status epilepticus is a lifethreatening condition in which seizure activity is uninterrupted. ...
IN SILICO QUINAZOLINONES AS NMDA RECEPTOR INHIBITORS FOR ANTICONVULSANT ACTIVITY Research Article
... inhibitor for anticonvulsant activity. Molecules from the series 6-bromo-3(substituted benzylideneamino) – 2 phenylquinazolin-4(3H)-one(BQSB 18 ), 3-(substituted-benzylamino)-2-phenylquinazolin-4(3H)-one (QSBR 1-8 ), 6-bromo3-(substituted-benzylamino)-2-phenylquinazolin-4(3H)-one (BQSBR 1-8 ) and 2- ...
... inhibitor for anticonvulsant activity. Molecules from the series 6-bromo-3(substituted benzylideneamino) – 2 phenylquinazolin-4(3H)-one(BQSB 18 ), 3-(substituted-benzylamino)-2-phenylquinazolin-4(3H)-one (QSBR 1-8 ), 6-bromo3-(substituted-benzylamino)-2-phenylquinazolin-4(3H)-one (BQSBR 1-8 ) and 2- ...
Statins forever: Is anything set to topple this class`s mighty reign?
... and evacetrapib, with Roche and Lilly both stating that discontinuation was down to “lack of clinically meaningful efficacy”. 6,7 These discontinuations have seriously bought into question the suitability of inhibiting CETP as a treatment for dyslipidaemia. Despite these notable failures, Merck is s ...
... and evacetrapib, with Roche and Lilly both stating that discontinuation was down to “lack of clinically meaningful efficacy”. 6,7 These discontinuations have seriously bought into question the suitability of inhibiting CETP as a treatment for dyslipidaemia. Despite these notable failures, Merck is s ...
slides
... MTN-020/ASPIRE participants and their communities; MTN-020 Community Working Group; MTN-020 Study Monitoring Committee; DAIDS MNDSMB The Microbicide Trials Network is funded by the National Institute of Allergy and Infectious Diseases (UM1AI068633, UM1AI068615, UM1AI106707), with co-funding from the ...
... MTN-020/ASPIRE participants and their communities; MTN-020 Community Working Group; MTN-020 Study Monitoring Committee; DAIDS MNDSMB The Microbicide Trials Network is funded by the National Institute of Allergy and Infectious Diseases (UM1AI068633, UM1AI068615, UM1AI106707), with co-funding from the ...
The amino acid Tyrosine
... preparations like marihuana are already used as dried material. So, it's not wide spread throughout the world like other addicted drugs. * When young leaves are kept in banana leaves ,they keep their freshness for 24 hours. * Usually , the leaves should be used within the first 24 hours of preparati ...
... preparations like marihuana are already used as dried material. So, it's not wide spread throughout the world like other addicted drugs. * When young leaves are kept in banana leaves ,they keep their freshness for 24 hours. * Usually , the leaves should be used within the first 24 hours of preparati ...
new-ff-Benzodiazepines-
... Compounds without 3-OH group have long half-lives and undergo conversion to the 3-hydroxyl compounds by hepatic oxidation. Compounds with 3-OH (oxazepam, lorazepam) are short-acting because they are rapidly conjugated and urinary excreted. So, they can be used in elderly or ...
... Compounds without 3-OH group have long half-lives and undergo conversion to the 3-hydroxyl compounds by hepatic oxidation. Compounds with 3-OH (oxazepam, lorazepam) are short-acting because they are rapidly conjugated and urinary excreted. So, they can be used in elderly or ...
The Microbial Pharmacy: FDA Approved Medicines
... being ejected today. It is also interesting that fungi have been the source of two of the best known hallucinogens, both of which are currently, or have been, used in clinical trials to treat terminally ill patients.(19-22) Cyclosporin A, a powerful immunosuppressant used following organ transplant ...
... being ejected today. It is also interesting that fungi have been the source of two of the best known hallucinogens, both of which are currently, or have been, used in clinical trials to treat terminally ill patients.(19-22) Cyclosporin A, a powerful immunosuppressant used following organ transplant ...
12472-0 Nat`l Academy.6B - National Academy of Sciences
... the United States, had isolated the responsible virus, HIV. The ensuing molecular studies of HIV by researchers around the world held the promise that a medical solution—a treatment, perhaps, if not a cure—would soon be at hand. Montagnier had identified HIV as a retrovirus, which, like all viruses, ...
... the United States, had isolated the responsible virus, HIV. The ensuing molecular studies of HIV by researchers around the world held the promise that a medical solution—a treatment, perhaps, if not a cure—would soon be at hand. Montagnier had identified HIV as a retrovirus, which, like all viruses, ...
Medicinal Lecture
... ionic group and in a third site I want hydrophobic bond. It is important to know the pharmacophore before starting random changes in the structure. We start with a lead and end with a drug; the structure of the drug may be very different from that of the lead BUT ...
... ionic group and in a third site I want hydrophobic bond. It is important to know the pharmacophore before starting random changes in the structure. We start with a lead and end with a drug; the structure of the drug may be very different from that of the lead BUT ...
Presentation
... Understanding of post-antibiotic effect (PAE) Mathematical modelling of data In vitro PK/PD Humanising dosing in efficacy models: Significant expertise in the translation of efficacy in pre-clinical models and microbiological assays to predict efficacy in humans Use and analysis of pharm ...
... Understanding of post-antibiotic effect (PAE) Mathematical modelling of data In vitro PK/PD Humanising dosing in efficacy models: Significant expertise in the translation of efficacy in pre-clinical models and microbiological assays to predict efficacy in humans Use and analysis of pharm ...
幻灯片 1
... withholding therapy is great, such as with bacterial meningitis or in clinically unstable patients, therapy should be started without delay even when the presence of a bacterial infection is uncertain. ...
... withholding therapy is great, such as with bacterial meningitis or in clinically unstable patients, therapy should be started without delay even when the presence of a bacterial infection is uncertain. ...
London NHSE guidance 14Jan2015 - HIV i-Base
... • Although once-‐daily combina-ons are preferred for adherence, many pa-ents would choose twice daily if it had fewer side effects or drug interac-ons. • The new lower price for twice-‐daily raltegravir mean ...
... • Although once-‐daily combina-ons are preferred for adherence, many pa-ents would choose twice daily if it had fewer side effects or drug interac-ons. • The new lower price for twice-‐daily raltegravir mean ...
Norepinephrine
... Phentermine is used together with diet and exercise to treat obesity (overweight) in people with risk factors such as high blood pressure, high cholesterol, or diabetes. Phentermine is used to counteract the effect of morphine in cancer patient ( narcotic effect) . The first sign that appears ...
... Phentermine is used together with diet and exercise to treat obesity (overweight) in people with risk factors such as high blood pressure, high cholesterol, or diabetes. Phentermine is used to counteract the effect of morphine in cancer patient ( narcotic effect) . The first sign that appears ...
Biotransformation Xenobiotic metabolism
... • First pass effects may so greatly limit the bioavailability of orally administered drugs. •The lower gut harbors intestinal microorganisms that are capable of many biotransformation reactions. •Although drug biotransformation in vivo can occur by spontaneous, noncatalyzed chemical reactions, the v ...
... • First pass effects may so greatly limit the bioavailability of orally administered drugs. •The lower gut harbors intestinal microorganisms that are capable of many biotransformation reactions. •Although drug biotransformation in vivo can occur by spontaneous, noncatalyzed chemical reactions, the v ...
CURRENT PERIOPERATIVE MANAGEMENT a b
... Chronic intestinal Isophoriasis lasting greater than 1 month ...
... Chronic intestinal Isophoriasis lasting greater than 1 month ...
Topic guide 9.1: Drugs and receptor sites
... sites Drugs used in medicine may alter the metabolism of cells and organs in the human body, or they may kill or inactivate pathogens such as bacteria, viruses and fungi. Regardless of their effect, all drugs work by binding to specific target molecules within the organism. These target sites can be ...
... sites Drugs used in medicine may alter the metabolism of cells and organs in the human body, or they may kill or inactivate pathogens such as bacteria, viruses and fungi. Regardless of their effect, all drugs work by binding to specific target molecules within the organism. These target sites can be ...
D Drug Discovery: A Historical Perspective
... by a compound that modifies the target constitute the lowest level of validation. If phenotypic changes can reproducibly be induced in an animal model that represents at least some disease-relevant mechanisms, the degree of validation is higher. The credibility of a target grows with the number of r ...
... by a compound that modifies the target constitute the lowest level of validation. If phenotypic changes can reproducibly be induced in an animal model that represents at least some disease-relevant mechanisms, the degree of validation is higher. The credibility of a target grows with the number of r ...
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).