Literature DB >> 6092093

Stereochemistry, a basis for sophisticated nonsense in pharmacokinetics and clinical pharmacology.

E J Ariëns.   

Abstract

The significance of stereochemistry in therapeutic action is outlined and elucidated. Often only one isomer is therapeutically active, but this does not mean that the other is really inactive. It may very well contribute to the side-effects. The therapeutically non-active isomer in a racemate should be regarded as an impurity (50% or more). It is emphasized how in clinical pharmacology, and particularly in pharmacokinetics, neglect of stereoselectivity in action leads to the performance of expensive "highly sophisticated scientific nonsense". This also holds true in the development and marketing of new drugs as exemplified by various "pseudo-hybrid" drugs now reaching the clinic.

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Year:  1984        PMID: 6092093     DOI: 10.1007/bf00541922

Source DB:  PubMed          Journal:  Eur J Clin Pharmacol        ISSN: 0031-6970            Impact factor:   2.953


  29 in total

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Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1973       Impact factor: 3.000

4.  A study of the excitatory effects of barbiturates.

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Journal:  J Pharmacol Exp Ther       Date:  1970-12       Impact factor: 4.030

5.  Cholinergic and anticholinergic drugs, do they act on common receptors?

Authors:  E J Ariens; A M Simonis
Journal:  Ann N Y Acad Sci       Date:  1967-10-31       Impact factor: 5.691

Review 6.  Fixed combination drug therapy.

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Journal:  Drugs       Date:  1982-06       Impact factor: 9.546

7.  Pharmacology of ketamine isomers in surgical patients.

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Journal:  Anesthesiology       Date:  1980-03       Impact factor: 7.892

8.  Enhancement of uricosuric properties of indacrinone by manipulation of the enantiomer ratio.

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Journal:  Clin Pharmacol Ther       Date:  1981-03       Impact factor: 6.875

9.  alpha 2-Adrenergic agonist and antagonist activity of the respective (-)-and (+)-enantiomers of 6-ethyl-9-oxaergoline (EOE).

Authors:  V J Lotti; D A Taylor
Journal:  Eur J Pharmacol       Date:  1982-11-19       Impact factor: 4.432

10.  Pharmacological appraisal of fixed-dose combination medicines: discussion paper.

Authors:  E S Snell
Journal:  J R Soc Med       Date:  1982-06       Impact factor: 18.000

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  73 in total

Review 1.  Stereoselectivity in clinical pharmacokinetics and drug development.

Authors:  D B Campbell
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1990 Apr-Jun       Impact factor: 2.441

2.  A moment invariant for evaluating the chirality of three-dimensional objects.

Authors:  Johan Hattne; Victor S Lamzin
Journal:  J R Soc Interface       Date:  2010-08-04       Impact factor: 4.118

Review 3.  Enantioselective pharmacodynamics and pharmacokinetics of chiral non-steroidal anti-inflammatory drugs.

Authors:  A M Evans
Journal:  Eur J Clin Pharmacol       Date:  1992       Impact factor: 2.953

4.  Design guidelines for an electron diffractometer for structural chemistry and structural biology.

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Journal:  Acta Crystallogr D Struct Biol       Date:  2019-04-08       Impact factor: 7.652

5.  Racemic therapeutics--ethical and regulatory aspects.

Authors:  E J Ariëns
Journal:  Eur J Clin Pharmacol       Date:  1991       Impact factor: 2.953

Review 6.  Clinical pharmacology through the looking glass: reflections on the racemate vs enantiomer debate.

Authors:  M S Lennard
Journal:  Br J Clin Pharmacol       Date:  1991-06       Impact factor: 4.335

Review 7.  Stereoselectivity in pharmacokinetics: a general theory.

Authors:  R H Levy; A V Boddy
Journal:  Pharm Res       Date:  1991-05       Impact factor: 4.200

8.  Effect of chirality on cellular uptake, imaging and photodynamic therapy of photosensitizers derived from chlorophyll-a.

Authors:  Avinash Srivatsan; Paula Pera; Penny Joshi; Yanfang Wang; Joseph R Missert; Erin C Tracy; Walter A Tabaczynski; Rutao Yao; Munawwar Sajjad; Heinz Baumann; Ravindra K Pandey
Journal:  Bioorg Med Chem       Date:  2015-04-09       Impact factor: 3.641

Review 9.  The relevance of pharmacokinetics in the development of biotechnology products.

Authors:  S Toon
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1996 Apr-Jun       Impact factor: 2.441

10.  Stereoselective dissolution of propranolol hydrochloride from hydroxypropyl methylcellulose matrices.

Authors:  S P Duddu; M Vakilynejad; F Jamali; D J Grant
Journal:  Pharm Res       Date:  1993-11       Impact factor: 4.200

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