Stereochemical Aspects of Drug Action and Disposition

Michel F. Eichelbaum, Bernard Testa, Andrew Somogyi (Herausgeber)

Buch | Softcover

XXV, 442 Seiten

2012 | 1. Softcover reprint of the original 1st ed. 2003
Springer Berlin (Verlag)
978-3-642-62575-6 (ISBN)

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State-of-the-Art Chirality Stereochemistry in general and chirality in particular have long been recog nized as major structural factors influencing pharmacological activity and pharmacokinetic behavior. For more than a century, relevant information in these fields has been accumulating at an accelerating pace, leading to rationalizations, concepts and theories of increasing breadth and depth. Frequently, fundamental advances in stereochemical aspects of molecular pharmacology, drug disposition and pharmacochemistry have been translated into corresponding progress in clinical pharmacology and pharmacotherapy. There have been exceptions, however, since some extrapolations from the biochemical and in vitro situations to the in vivo human situation have proven premature. This notion resulted in the now appeased, but far from closed, debate regarding racemic versus enantiopure drugs, which saw some pro ponents state that "in many cases, only one isomer contributes to the thera peutic action while the other, the 'isomeric ballast', only contributes to the side effects and toxicity" (ARIENS 1986,1989,1992). Other authors, in contrast, have cautioned against hasty generalizations and advocated a more pragmatic, case by-case and evidence-based view (CALDWELL 1995; DE CAMP 1989; SZELENYI et al. 1998; TESTA 1991; TESTA and TRAGER 1990; TESTA et al. 1993).

Chemical Aspects.- 1 Recent Developments in Asymmetric Organic Synthesis: Principles and Examples.- 2 Stereoselective Separations: Recent Advances in Capillary Electrophoresis and High-Performance Liquid Chromatography.- 3 Stereochemical Issues in Bioactive Natural Products.- 4 Drug Racemization and Its Significance in Pharmaceutical Research.- 5 Physical Properties and Crystal Structures of Chiral Drugs.- Experimental Pharmacology.- 6 Chiral Recognition in Biochemical Pharmacology: An Overview.- 7 Enantioselectivity in Drug-Receptor Interactions.- 8 Mechanisms of Stereoselective Binding to Functional Proteins.- 9 Stereoselective Drug-Channel Interactions.- 10 Stereoselective Bioactivation and Bioinactivation - Toxicological Aspects.- Drug Absorption, Distribution, Metabolism, Elimination.- 11 Intestinal Drug Transport: Stereochemical Aspects.- 12 Enantioselective Plasma and Tissue Binding.- 13 Stereoselective Drug Metabolism and Drug Interactions.- 14 Metabolic Chiral Inversion of 2-Arylpropionic Acids.- 15 Stereoselective Renal Elimination.- Implications for Drug Development and Therapy.- 16 Regulatory Requirements for the Development of Chirally Active Drugs.- 17 Improving Clinical Risk/Benefit Through Stereochemistry.

Erscheint lt. Verlag	21.10.2012
Reihe/Serie	Handbook of Experimental Pharmacology
Zusatzinfo	XXV, 442 p.
Verlagsort	Berlin
Sprache	englisch
Maße	155 x 235 mm
Gewicht	708 g
Themenwelt	Medizin / Pharmazie ► Medizinische Fachgebiete ► Pharmakologie / Pharmakotherapie
	Medizin / Pharmazie ► Pharmazie ► PTA / PKA
	Naturwissenschaften ► Biologie ► Biochemie
Schlagworte	Absorption • Chemistry • Drug • drug development • Drug disposition and action • Drug research • Drug toxicity • Metabolism • natural product • organic synthesis • pharmacology • Protein • receptor • Research • Stereochemie • stereochemistry • synthesis • Toxicology • Toxizität
ISBN-10	3-642-62575-4 / 3642625754
ISBN-13	978-3-642-62575-6 / 9783642625756
Zustand	Neuware