Drug metabolism

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  • In a certain sense, the field of drug metabolism (DM) is standing still. More specifically, the basic experiment of drug metabolism (i.e., administering a new drug to an animal or human and determining the structures, amounts, and disposition of the metabolites) has changed very little over a period of decades. Remarkably, the experimental design and resulting data set from a typical absorption, distribution, metabolism, and excretion (ADME) study conducted today would be instantly recognized and understood by DM scientists from 50 years ago.

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  • Recent advances in mass spectrometry have rendered it an attractive and versatile tool in industrial and academic research laboratories. As a part of this rapid growth, a considerable body of literature has been devoted to the application of mass spectrometry in clinical studies. In concert with separation techniques such as liquid chromatography, mass spectrometry allows the rapid characterization and quantitative determination of a large array of molecules in complex mixtures.

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  • (BQ) Part 1 book "Essentials of pharmaceutical chemistry" has contents: Chemistry of acids and bases, partition coefficient and biopharmacy, partition coefficient and biopharmacy, stereochemistry, drug metabolism.

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  • (BQ) Part 1 book "Medical pharmacology at a glance" presents the following contents: Principles of drug action, drug absorption, distribution and excretion, drug metabolism, local anaesthetics, autonomic nervous system, autonomic drugs acting at cholinergic synapses, drugs acting on the sympathetic system, ocular pharmacology,... and other contents.

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  • Tuyển tập báo cáo các nghiên cứu khoa học quốc tế ngành hóa học dành cho các bạn yêu hóa học tham khảo đề tài: Molecular and macromolecular alterations of recombinant adenoviral vectors do not resolve changes in hepatic drug metabolism during infection

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  • Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Critical Care giúp cho các bạn có thêm kiến thức về ngành y học đề tài: Clinical review: Drug metabolism and nonrenal clearance in acute kidney injury...

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  • Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Critical Care giúp cho các bạn có thêm kiến thức về ngành y học đề tài: Drug metabolizing enzyme activities versus genetic variances for drug of clinical pharmacogenomic relevance...

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  • Five years have passed since the first edition of Principles of Clinical Pharmacology was published. The second edition remains focused on the principles underlying the clinical use and contemporary development of pharmaceuticals. However, recent advances in the areas of pharmacogenetics, membrane transport, and biotechnology and in our understanding of the pathways of drug metabolism, mechanisms of enzyme induction, and adverse drug reactions have warranted the preparation of this new edition.

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  • Introduction: Butyrophenone drugs including haloperidol are being widely used in the field of psychiatry. The acute butyrophenone poisoning incidents sometimes take place; in such cases, the analysis of a butyrophenone becomes necessary in forensic toxicology or clinical toxicology. Their analysis is being made by GC [1–4], GC/MS [5–6], HPLC [7–15] and LC/MS [16,17]. Six butyrophenones are now available as ethical drugs in Japan ( Fig. 2.1); the most typical ones are haloperidol and bromperidol, which most frequently cause poisoning incidents among butyrophenones.

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  • Introduction: Methanol (methyl alcohol) poisoning accidents take place most frequently by drinking it in mistake for ethanol. Methanol poisoning is not due to the effect of methanol itself, but due to toxicity of its metabolites. Methanol is rapidly absorbed into human body through the airway mucous membranes, digestive tract mucous membranes or the skin; it is metabolized into formaldehyde (formalin, HCHO) and then formic acid (HCOOH) by the actions of alcohol dehydrogenase and aldehyde dehydrogenase, respectively.

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  • The sixth edition of Modern Pharmacology With Clinical Applications continues our commitment to enlisting experts in pharmacology to provide a textbook that is up-to-date and comprehensive. Designed to be used during a single semester, the book focuses on the clinical application of drugs within a context of the major principles of pharmacology. It is meant to serve students in medicine, osteopathy, dentistry, pharmacy, and advanced nursing, as well as undergraduate students.

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  • Introduction: As coumarin rodenticides, warfarin, coumatetralyl, coumafuryl, coumachlor and bromadiolone are commercially available in Japan. The coumarin rodenticides do not show direct anticoagulant action causing bleeding, but inhibit the metabolic cycle of vitamin K; the inhibition causes the interference with protein biosynthesis of vitamin K-dependent coagulant factors (II, VII, IX and X factors) in the liver, which are very important for the blood coagulation system. The lowered coagulant factors cause the bleeding deaths of the rodents [1].

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  • Compared with hydrophilic drugs not undergoing transport, lipophilic drugs are more rapidly taken up from the blood into hepatocytes and more readily gain access to mixed-function oxidases embedded in sER membranes. For instance, a drug having lipophilicity by virtue of an aromatic substituent (phenyl ring) (B) can be hydroxylated and, thus, become more hydrophilic (Phase I reaction, p. 34). Besides oxidases, sER also contains reductases and glucuronyl transferases. The latter conjugate glucuronic acid with hydroxyl, carboxyl, amine, and amide groups (p.

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  • Antibacterial Drugs can be classified according to their respective primary mode of action (color tone in 2 and 3). When bacterial growth remains unaffected by an antibacterial drug, bacterial resistance is present. This may occur because of certain metabolic characteristics that confer a natural insensitivity to the drug on a particular strain of bacteria (natural resistance). Depending on whether a drug affects only a few or numerous types of bacteria, the terms narrow-spectrum (e.g., penicillin G) or broad-spectrum (e.g., tetracyclines) antibiotic are applied.

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  • Introduction: There are a number of compounds, such as morphine and codeine, which are classified into the opium alkaloids (opiates). They are being used as ethical drugs of narcotic analgesics and antitussives; 1 % powder of codeine or dihydrocodeine is commonly included in over-the-counter drugs of antitussives. Figure 3.1 shows metabolic pathways of morphine, heroin and codeine. Since morphine and codeine are finally excreted into urine in the conjugated forms with glucuronic acid [1–3], it is necessary to hydrolyze the conjugated forms of these compounds before GC/MS analysis.

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  • Introduction: Pyrethroids are the general term for insecticide pyrethrins and their analogs (cinerins and jasmolins) being included in the flowers of pyrethrum or chrysanthemum. Trace concentrations of pyrethroids exert rapid toxic effects on insects, but are rapidly metabolized for detoxification in warm-blooded animals; they are insecticides with very high safety for humans. On the basis of clarification of chemical structures of the effective components of the pyrethrum, many of new synthetic pyrethroids were developed.

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  • Introduction: Ethylene glycol is being widely used as solvents, lubricants and surfactants in industries; for daily necessities, it is being used as a component of cold-reserving materials and of nonfreezing coolants of automobiles. There were cases of accidental and suicidal ingestion of such fluids [1–3]. As toxic actions of ethylene glycol, suppression of central nervous system activities similar to that of alcohol and metabolic acidosis caused by glycolic acid produced from ethylene glycol can be mentioned.

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  • Constitutively expressed human cytochrome P450 2D6 (CYP2D6; EC 1.14.14.1) is responsible for the metabolism of approximately 25% of drugs in common clinical use. It is widely accepted that CYP2D6 is localized in the endoplasmic reticulum of cells; however, we have identified this enzyme in the mitochondria of human liver samples and found that extensive inter-individual variability exists with respect to the level of the mitochondrial enzyme.

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  • Great efficiencies have been achieved in the drug discovery process as a result of technological advances in target identification, high-throughput screening, high-throughput organic synthesis, just-in-time in vitro ADME (absorption, distribution, metabolism, and excretion), and early pharmacokinetic screening of drug leads. These advances, spanning target selection all the way through to clinical candidate selection, have placed greater and greater demands on the analytical community to develop robust high-throughput methods.

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  • Pharmacokinetics (t1/2) and the apparent volume of distribution Vapp (p. 28) by the equation: Vapp t1/2 = In 2 x –––– Cltot The smaller the volume of distribution or the larger the total clearance, the shorter is the half-life. In the case of drugs renally eliminated in unchanged form, the half-life of elimination can be calculated from the cumulative excretion in urine; the final total amount eliminated corresponds to the amount absorbed.

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