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PPT
PPT

... Inhibition effect extends beyond elimination of drug due to enzyme inactivation. Effect tends to accumulate after each dose. Inhibition effect is generally greater than predicted based on ‘reversible’ IC50 or Ki values. Most compounds will have non-linear pharmacokinetics. Rare cases of hepatotoxici ...
8th Lecture 1433
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Fig 4.9a Synaptic Transmission
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Drug interactions
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... The risk of drug interactions increases with the number of drugs used. The rate of ADR in patients taking 6–10 drugs was 7%, rising to 40% in those taking 16–20 drugs, with the exponential rise being largely attributable to drug interactions. In a high-risk group of emergency department patients, th ...
Substance Abuse
Substance Abuse

... the APA as those listed above including at least 3 of the following in a 12 month period:.  1. Tolerance-need more of the drug to produce desired effect  2. Withdrawal-occurs when they stop using, must take the drug or alcohol to avoid these symptoms  3. Use larger amounts of the drug  4. Would ...
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BIOM 255: Molecular basis of drug action and disease therapy
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... The inter-individual variability in xenobiotic metabolism and drug response is extensive. The drug level in plasma can vary more than 1000-fold between two individuals having the same weight and with the same drug dosage. The causes for this variation are of genetic, physiological, pathophysiologica ...
SUSTAINED RELAEASE MULTIPARTICULATE DRUG DELIVERY
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... of the drug since multiparticulates are known to disperse freely in the gastric fluids covering greater surface of absorption. In addition they also offer benefits of reducing the dose required, and providing uniform drug delivery. So in the present study, attempts will be made to establish a optimu ...
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Answer Key of MCQ of AMO Exam

... 1. Total 110 multiple choice questions are provided out of which any 80 questions will have to be answered. Each question carries one mark. 2. No provision of negative marking. 3. Total 07 short answer questions (to be answered maximum in 75 words) out of which any 04 Questions will have to be answe ...
introduction to drug discovery
introduction to drug discovery

... the early 1990's it was believed that combinatorial chemistry would revolutionize the drug discovery industry. Ten years later the route from design and synthesis of compound libraries to identification of lead structures is still long and costly. Synthesis of an almost unlimited number of organic c ...
TEMSIS
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The Use of Ontologies in Drug Discovery
The Use of Ontologies in Drug Discovery

... are created using Protégé as the ontology development tool, but are exported from this environment into a relational database, for use in information retrieval. Because of the dynamic nature of the language used in the life sciences, automated methods for updating the ontologies and synonyms knowled ...
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Drug design



Drug design, sometimes referred to as rational drug design or simply rational design, is the inventive process of finding new medications based on the knowledge of a biological target. The drug is most commonly an organic small molecule that activates or inhibits the function of a biomolecule such as a protein, which in turn results in a therapeutic benefit to the patient. In the most basic sense, drug design involves the design of molecules that are complementary in shape and charge to the biomolecular target with which they interact and therefore will bind to it. Drug design frequently but not necessarily relies on computer modeling techniques. This type of modeling is often referred to as computer-aided drug design. Finally, drug design that relies on the knowledge of the three-dimensional structure of the biomolecular target is known as structure-based drug design. In addition to small molecules, biopharmaceuticals and especially therapeutic antibodies are an increasingly important class of drugs and computational methods for improving the affinity, selectivity, and stability of these protein-based therapeutics have also been developed.The phrase ""drug design"" is to some extent a misnomer. A more accurate term is ligand design (i.e., design of a molecule that will bind tightly to its target). Although design techniques for prediction of binding affinity are reasonably successful, there are many other properties, such as bioavailability, metabolic half-life, side effects, etc., that first must be optimized before a ligand can become a safe and efficacious drug. These other characteristics are often difficult to predict with rational design techniques. Nevertheless, due to high attrition rates, especially during clinical phases of drug development, more attention is being focused early in the drug design process on selecting candidate drugs whose physicochemical properties are predicted to result in fewer complications during development and hence more likely to lead to an approved, marketed drug. Furthermore, in vitro experiments complemented with computation methods are increasingly used in early drug discovery to select compounds with more favorable ADME (absorption, distribution, metabolism, and excretion) and toxicological profiles.
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