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Problem Set 2: Cephalosporins: KEY Answer the following
Problem Set 2: Cephalosporins: KEY Answer the following

... metabolism and thus allow for acetaldehyde levels to accumulate like disulfiram treatment? Under which therapeutic conditions is this reaction of concern? Which may prolong PT times? Answer: D. The 3-N-methylthiotetrazole cephalosporins are capable of producing hypoprothrombinemia. Do you recall the ...
DESIGN, SYNTHESIS AND MOLECULAR DOCKING STUDIES OF BENZOTHIAZOLE  Research Article
DESIGN, SYNTHESIS AND MOLECULAR DOCKING STUDIES OF BENZOTHIAZOLE Research Article

... Benzothiazole is an aromatic heterocyclic compound with the chemical formula C7H5NS. They represent an extensive group of compounds having a thiazole fused with benzene ring [1]. It is a proved fact that heterocyclic compounds containing nitrogen and sulphur possess potential pharmacological activit ...
Bergamottin and “The Grapefruit Juice Effect”
Bergamottin and “The Grapefruit Juice Effect”

... is a potent inhibitor of cytochrome P450, an enzyme that is responsible for the metabolism of approximately 60% of clinically relevant drugs1. Although much is known about this “grapefruit juice effect,” the exact mechanism of this bergamottindrug interaction is not clear at this time and warrants f ...
Anti-TB - PharmaStreet
Anti-TB - PharmaStreet

... • It was first clinically useful antitubercular drug. • It is aminoglycoside antibiotic. • It is tuberculocidal but less effective than INH or rifampin; acts only on extracellular bacilli. • Thus, other drugs and host defense mechanisms are needed to eradicate the disease. • It penetrates tubercular ...
Antifungal Agents Overview - Canadian Antimicrobial Resistance
Antifungal Agents Overview - Canadian Antimicrobial Resistance

... Another chemical group that is active against a number of fungi is the allylamines. Members of this group once again interfere with ergosterol biosynthesis by inhibiting the enzyme squalene epoxidase. One of the enzymes necessary for the production of lanosterol, an intermediate compound in the form ...
Antimicrobial resistance
Antimicrobial resistance

... 1-Restrict the use of antimicrobials to reduce the risk of antimicrobial resistance: Phase out and ban the use of antibiotics for non-therapeutic uses. 2-Clarify definitions estimates for drug use: Non-therapeutic and therapeutic antibiotics. 3- Improvement of monitoring and reporting of antimicrobi ...
local anaesthetics
local anaesthetics

...  Substitution of hydrophilic centre showed that as the no. of C atoms increase the partition coefficient and activity increase ...
Mebendazole
Mebendazole

... • Drugs that are active against schistosomiasis – Currently, praziquantel is the most common drug used for the treatment of all species of schistosomes – The drug artemisinin, an antimalarial, is also effective against schistosomes ...
Mechanism of Action
Mechanism of Action

... Influenza A virus subtype H1N1, also known as A(H1N1), is a subtype of influenzavirus A and the most common cause of influenza (flu) in humans. Some strains of H1N1 are endemic in humans, including the strain(s) responsible for the 1918 flu pandemic which killed 50–100 million people worldwide. H1N1 ...
Tuberculosis: New Drug Discovery Pipelines
Tuberculosis: New Drug Discovery Pipelines

... amikacin or kanamycin. The principles used for MDR-TB and XDRTB treatment are the same. The main difference is that XDR-TB is associated with a much higher mortality rate than MDR-TB, because of the reduced number of effective treatment options. Totally drug-resistant tuberculosis (TDR-TB) [23] This ...
log P
log P

... (Pharm 5219): Section A ...
combinatorx
combinatorx

... A phase II trial of a new anti-inflammatory combination drug, CRx140, in patients with severe psoriasis; Alice Gottlieb, Yanzhen Zhang, Melissa Nichols, CRx-140 group at CombinatoRx, Incorporated and CRx-140 group of investigators UMDNJ & Robert Wood Johnson Med. Ctr., Nexx Brunswick, NJ and Combina ...
The Why and How of Absorption, Distribution, Metabolism, Excretion
The Why and How of Absorption, Distribution, Metabolism, Excretion

... compounds, with less interest being given to their behavior in the body. However, the R&D paradigm in the pharmaceutical industry has undergone dramatic changes since the 1970’s and particularly since the mid-1990’s. High-throughput biological assays were developed which have enabled large series of ...
The Effect of Cytochrome P450 Metabolism on Drug Response
The Effect of Cytochrome P450 Metabolism on Drug Response

... CYP2D6, and CYP3A4).13 Drugs that cause CYP450 metabolic drug interactions are referred to as either inhibitors or inducers (Table 110,14-16). Inhibitors block the metabolic activity of one or more CYP450 enzymes. The extent to which an inhibitor affects the metabolism of a drug depends upon factors ...
Chapater 12 - IND/NDA/ANDA/AADA
Chapater 12 - IND/NDA/ANDA/AADA

... definitive clinical trials, which must be well underway, if not almost finished. An immediately lifethreatening disease means a stage of a disease in which there is a reasonable likelihood that death will occur within a matter of months or in which premature death is likely without early treatment. ...
malaria
malaria

... • Which of the following drugs should be used for oral treatment of the entomologist's acute attack of P vivax malaria? • (A) Chloroquin • (B) Mefloquine • (C) Primaquin • (D) Pyrimethamine-sulfadoxine • (E) Quinine ...
- Wiley Online Library
- Wiley Online Library

... to produce ATP and simple carbon compounds, class II reactions utilising energy and class I compounds to make small molecules such as amino acids and lastly, class III reactions that convert small molecules into macromolecules such as proteins, nucleic acids and peptidoglycans.5 Class I reactions ar ...
steam distillation of a spice
steam distillation of a spice

... the round bottomed flask. Clamp an addition flask or separatory funnel to the flask, and cover the remaining hole with a septum. Wrap the top of the 250-mL round bottom flask and the 3-way connector with some glass wool to insulate it so that the steam vapors don’t condense there (Figure 1). Start s ...
Open slides - CTN Dissemination Library
Open slides - CTN Dissemination Library

... and cost-effectiveness of 3 HIV testing strategies in substance abuse treatment centers evaluated in the CTN Rapid Testing and Counseling Study randomized controlled trial (CTN 0032) ...
View Full Text-PDF
View Full Text-PDF

... compound are shown in table1. Infrared identification was done by KBr disc aiming the proof of their formation, functional groups and structures and the bands are listed on table2. Ultraviolet spectroscopy was applied on DMSO solutions and the related λmaxs were appeared as per table.3. Antibacteria ...
Lopinavir/low dose ritonavir - WHO archives
Lopinavir/low dose ritonavir - WHO archives

... Trials of anti-retroviral compounds have relied heavily on measuring the effects of drugs on surrogate markers, usually CD4 cell counts and plasma HIV-1 RNA levels. The validity of these markers depends on showing that they are correlated with clinical outcomes, and that they should be able to captu ...
Drugs used to treat hypertension
Drugs used to treat hypertension

... - useful interaction ACEIs with diuretics: Converting enzyme inhibitors interrupt by diuretics increased plasma renin activity (and the consequent activation of angiotensin II and aldosterone) and enhance the antihypertensive efficacy of diuretics, as well as reducing thiazide-induced hypokalemia. - ...
Studies of Retroviral Reverse Transcriptase and
Studies of Retroviral Reverse Transcriptase and

... All existing drugs on the market together hit only about 500 drug targets, representing less than 1% of potential targets of the presumed druggable proteome. Similarly, the existing drugs (slightly over a thousand in number) represent a tiny portion of the chemical space of potential drug-like molec ...
Document
Document

... Clinical Considerations in Prescribing Antimicrobial Drugs ...
Medicinal chemistry strategies in follow
Medicinal chemistry strategies in follow

... phase 2 trials [5]. Therapeutically useful targets are rare commodities and only a small number of drugs targeting novel mechanisms are discovered every year [6] (between two and six per year in the past ten years [7]). These factors have prompted the pharmaceutical industry to exploit validated tar ...
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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).
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