Literature DB >> 6533294

Prediction of the volumes of distribution of basic drugs in humans based on data from animals.

Y Sawada, M Hanano, Y Sugiyama, H Harashima, T Iga.   

Abstract

The apparent volume of distribution-after distribution equilibrium and the ratio of distributive tissue volume to the unbound fraction in the tissue (VT/fuT) of 10 weak basic drugs, i.e., chlorpromazine, imipramine, propranolol, disopyramide, lidocaine, quinidine, meperidine, pentazocine, chlorpheniramine, and methacyclin were compared in animal species and humans. In these two parameters, a statistically significant correlation between animals and humans was obtained, when the parameters were plotted on a log-log scale. The correlation coefficient between VT/fuT was significantly higher than that between the apparent volumes of distribution (p less than 0.05). In general, there was little difference between VT/fuT of various basic drugs in animals and that in humans. Prediction of the apparent volume of distribution in humans using animal data of VT/fuT, plasma unbound fraction, blood volume, and blood-to-plasma concentration ratio in humans was successful for most of drugs studied.

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Year:  1984        PMID: 6533294     DOI: 10.1007/bf01059554

Source DB:  PubMed          Journal:  J Pharmacokinet Biopharm        ISSN: 0090-466X


  45 in total

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4.  Pharmacokinetics and steady-state myocardial uptake of disopyramide in the dog.

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Journal:  Drug Metab Dispos       Date:  1978 May-Jun       Impact factor: 3.922

5.  Role of concentration-dependent plasma protein binding in disopyramide disposition.

Authors:  P J Meffin; E W Robert; R A Winkle; S Harapat; F A Peters; D C Harrison
Journal:  J Pharmacokinet Biopharm       Date:  1979-02

6.  Disopyramide binding to serum protein in man and animals.

Authors:  J J Lima; D B Haughey
Journal:  Drug Metab Dispos       Date:  1981 Nov-Dec       Impact factor: 3.922

7.  Effect of sulfaphenazole on tolbutamide distribution in rabbits: analysis of interspecies differences in tissue distribution of tolbutamide.

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Journal:  J Pharm Sci       Date:  1984-05       Impact factor: 3.534

8.  Concentration-time effects of quinidine disposition kinetics in rhesus monkeys.

Authors:  C T Ueda; B Ballard; M Rowland
Journal:  J Pharmacol Exp Ther       Date:  1977-03       Impact factor: 4.030

9.  Binding of tricyclic antidepressants and perazine to human plasma. Methodology and findings in normals.

Authors:  M Brinkschulte; U Breyer-Pfaff
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10.  Methadone binding to orosomucoid (alpha 1-acid glycoprotein): determinant of free fraction in plasma.

Authors:  M K Romach; K M Piafsky; J G Abel; V Khouw; E M Sellers
Journal:  Clin Pharmacol Ther       Date:  1981-02       Impact factor: 6.875

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  24 in total

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6.  Interethnic scaling of fraction unbound of a drug in plasma and volume of distribution: an analysis of extrapolation from Caucasians to Chinese.

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8.  Prediction of ACNU plasma concentration-time profiles in humans by animal scale-up.

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9.  The role of permeability in drug ADME/PK, interactions and toxicity--presentation of a permeability-based classification system (PCS) for prediction of ADME/PK in humans.

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10.  Modelling and PBPK simulation in drug discovery.

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