Drug Metabolism and Pharmacokinetics Quick Guide

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S.C. Khojasteh, H. Wong, C.E.C.A. Hop Drug Metabolism and Pharmacokinetics Quick Guide ▶ Covers aspects of drug assessment at drug discovery and development stages ▶ Explores topics in pharmacokinetics, absorption, metabolism, enzyme kinetics, drug transporters, drug interactions, drug-like properties, assays and in silico calculations ▶ Includes tables on physiological parameters, chemical structure, nomenclature, and moieties leading to bioactivation Drug Metabolism and Pharmacokinetics Quick Guide is intended for broad readership of those interested in the discipline of drug metabolism and pharmacokinetics who work in drug discovery coming from the various disciplines, a background such as of medicinal chemistry, pharmacology, drug metabolism and pharmacokinetics, bioanalysis, clinical sciences, biochemistry, pharmaceutics or toxicology. 2011, XIII, 214 p. This guide provides, for the first time, a completely integrated look at multiple aspects of absorption, distribution, metabolism, and excretion (ADME) science in a summary format that is clear, concise and self-explanatory. Printed book This book will be used and referenced frequently as it provides detailed figures and tables Softcover for data interpretation. Also included are brief yet relevant factoids that bring a real-world ▶ 89,99 € | £79.99 | $109.99 dimension to the discussion of drug metabolism and pharmacokinetics. ▶ *96,29 € (D) | 98,99 € (A) | CHF 106.50 Key topics covered: eBook Available from your bookstore or 1. Pharmacokinetics ▶ springer.com/shop 2. Drug metabolizing enzymes MyCopy 3. Oral absorption Printed eBook for just ▶ € | $ 24.99 4. Transporters ▶ springer.com/mycopy 5. Metabolism-based drug interactions 6. Biotransformation and bioactivation 7. Prediction of human pharmacokinetics 8. Order online at springer.com ▶ or for the Americas call (toll free) 1-800-SPRINGER ▶ or email us at: [email protected]. ▶ For outside the Americas call +49 (0) 6221-345-4301 ▶ or email us at: [email protected]. The first € price and the £ and $ price are net prices, subject to local VAT. Prices indicated with * include VAT for books; the €(D) includes 7% for Germany, the €(A) includes 10% for Austria. Prices indicated with ** include VAT for electronic products; 19% for Germany, 20% for Austria. All prices exclusive of carriage charges. Prices and other details are subject to change without notice. All errors and omissions excepted..

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1: Clinical Pharmacokinetics 1
1: CLINICAL PHARMACOKINETICS 1 General overview: clinical pharmacokinetics, 2 Pharmacokinetics, 4 Drug clearance (CL), 6 Volume of distribution (Vd), 8 The half-life (t½), 10 Oral availability (F), 12 Protein binding (PB), 14 pH and pharmacokinetics, 16 1 Clinical pharmacokinetics General overview General overview: clinical pharmacokinetics 1 The ultimate aim of drug therapy is to achieve effi cacy without toxicity. This involves achieving a plasma concentration (Cp) within the ‘therapeutic window’, i.e. above the min- imal effective concentration (MEC), but below the minimal toxic concentration (MTC). Clinical pharmacokinetics is about all the factors that determine variability in the Cp and its time-course. The various factors are dealt with in subsequent chapters. Ideal therapeutics: effi cacy without toxicity Minimum Toxic Concentration (MTC) Ideal dosing Minimum Effective Concentration (MEC) Drug concentration Time The graph shows a continuous IV infusion at steady state, where the dose-rate is exactly appropriate for the patient’s clearance (CL). Inappropriate dosing Dosing too high in relation to the patient’s CL – toxicity likely Minimum Toxic Concentration (MTC) Minimum Effective Concentration (MEC) Dosing too low in relation to the Drug concentration patient’s CL – drug may be ineffective Time Some reasons for variation in CL Low CL High CL Normal variation Normal variation Renal impairment Increased renal blood fl ow Genetic poor metabolism Genetic hypermetabolism Liver impairment Enzyme induction Enzyme inhibition Old age/neonate 2 General overview Clinical Pharmacokinetics Pharmacokinetic factors determining ideal therapeutics If immediate effect is needed, a loading dose (LD) must be given to achieve a desired 1 concentration. The LD is determined by the volume of distribution (Vd).
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