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A1980KP91000001
A1980KP91000001

... of the benzodiazepines. Over 2,300 papers had been published on the clinical activity of these compounds. The laboratory and clinical work on 22 benzodiazepines that had been subjected to tolerance testing in man was summarized It was reported that the best correlation of animal testing methods with ...
A1986A667000002
A1986A667000002

... explain the phenomenon of tolerance to drug action. They believed the cause to be reduced semitivity of the receptor site, since no experiments had shown increased drug metabolism. The in vitro procedures published by Aselrod and Brodie, who had first described the drug.metabolizing enzyme ...
ENZYMES
ENZYMES

... the cytochrome P450 (CYP) system that are responsible for many of the phase 1 biotransformations of drugs. These metabolic transformations, such as oxidation, reduction and hydrolysis, produce a molecule that is suitable for conjugation. Those of importance in the metabolism of psychotropic drugs ar ...
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... Thus, NSAIDs drugs are not sufficiently selective to affect COX2 without shutting down COX-1 as well. ...
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2-Renal tubular excretion

... • -Manipulation of urine pH is e.g. by given sod. Bicarbonate to alkalinize the urine is useful in aspirin overdose ...
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... Sustained viral response: 49.6% for all, 35.6% for genotype 1, 32.6% for genotype 4, 72.4% for genotype 3 Cf. APRICOT 29% for G1 and 62% for G2-3 ...
Pharmacokinetic drug interaction
Pharmacokinetic drug interaction

... dissolution and absorption of these compounds is heavily dependent on acidic gastric conditions in the stomach ,Drugs that increase gastric pH (e.g.,H2 antagonists, proton pump inhibitors) slow the dissolution of the solid dosage forms and decrease drug available for absorption in the gastric lumen. ...
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q-dips: computer-based prediction of known and potential drug
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... Drug metabolism interactions are and will probably remain difficult to predict for clinicians. To help improve their management, we have developed an «expert» computer application: Q-DIPS (Quantitative Drug Interactions Prediction System). Q-DIPS gives extensive information, in dynamic tables, on wh ...
Table 2 - Bahrain Medical Bulletin
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... protease inhibitor2. Monotherapy should be avoided because it is clearly inferior to combination therapies. Also, the use of dual NRTI-only containing regimens should be avoided because initial viral suppression may not be sustained8,9,19,20. Two types of initial HAART strategies – NNRTI or PI-based ...
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... •Urine and tears become pink/red which may be a useful guide to compliance. ...
Quiz 1 Key - chem.uwec.edu
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Action of and Resistance to drugs and toxic metals

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... also have a key role in regulating growth across a range of organisms, including fungi. Several compounds in Lixte’s LB-200 series have been examined for activity in model systems against various fungal pathogens. A topical version of LB-201 cures two of the most common fungal skin infections of hum ...
Rilpivirine: a new non-nucleoside reverse transcriptase inhibitor
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... Introduction Non-nucleoside reverse transcriptase inhibitors (NNRTIs), such as efavirenz and nevirapine, are important components of highly active antiretroviral therapy. Combination therapy including an NNRTI has become a standard of care because of the low pill burden, improved adherence and high ...
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PolyMedix Presents Antibiotic Data at the 50th Interscience

... starting at doses as low as 0.1 to 0.3 mg/kg. These data suggest that administration of PMX-30063 below the identified limitingdose may have a bactericidal effect on MSSA and MRSA in human subjects. “Antimicrobial Activities of Structurally Diverse Host Defense Protein Mimics” R. Scott, CE Budu, A. ...
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... • It is often found that a drug fails clinical trials because of its toxic side effects. • This may be due to toxic metabolites, in which case the drug should be made more resistant to metabolism as described previously. • It is know that functional groups such as aromatic nitro groups, aromatic am ...
Lecture 7 Bio3124 - University of Ottawa
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Twenty-Six Years of Anti-HIV Drug Discovery
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... resistant strains with the codon 69 insertion.45 Although phase I/II studies showed significant reduction in HIV-1 RNA levels in HIV-infected subjects, 5 out of the 18 subjects used in this study demonstrated lens opacities during the study.46 Compound 10 also showed good activity in vivo when used ...
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Pharm II-Ch 8-PPT
Pharm II-Ch 8-PPT

... • GOAL OF ANTI-INFECTIVE THERAPY IS REDUCTION OF THE POPULATION OF THE INVADING ORGANISM. • DRUGS THAT WOULD ELIMINATE ALL TRACES OF ANY INVADING PATHOGEN MIGHT BE TOXIC TO THE HOST AS WELL. • IMMUNE RESPONSE IS A COMPLEX PROCESS INVOLVING CHEMICAL MEDIATORS, LEUKOCYTES, LYMPHOCYTES, ANTIBODIES, AND ...
Human Immunodeficiency Virus and Antiretroviral Therapy
Human Immunodeficiency Virus and Antiretroviral Therapy

... 2. Reverse Transcription and Integration Viral enzyme reverse transcriptase is used to copy viral RNA into viral DNA – Viral DNA is transported into cell nucleus and spliced into cell’s DNA by HIV enzyme integrase – Viral DNA persists in latent state until cell ...
Origins of multicellularity
Origins of multicellularity

... being explored. In a popular one, known as double decoupling, the free-energy changes associated with making the inhibitor ‘disappear’ from the complex with the enzyme and for making the inhibitor disappear in bulk water are computed. The difference in these results yields ΔGb. However, such calcula ...
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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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