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  • 1
    Electronic Resource
    Electronic Resource
    Binding of amobarbital, pentobarbital and diphenylhydantoin to blood cells and plasma proteins in healthy volunteers and uraemic patients (1975)
    Springer
    European journal of clinical pharmacology 8 (1975), S. 445-453 
    Details
    ISSN: 1432-1041
    Keywords: Amobarbital ; pentobarbital ; diphenylhydantoin ; protein binding ; erythrocytes ; uraemia
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary By equilibrium dialysis of human plasma it has been shown that the binding of pentobarbital and diphenylhydantoin to plasma proteins is decreased in uraemic patients (46 and 74 per cent bound, respectively) compared to healthy volunteers (61 and 88 per cent bound). The degree of binding of pentobarbital was significantly correlated with that of diphenylhydantoin and amobarbital, which suggests similarity of their binding sites. Appreciable proportions of the drugs were found in blood cells both in healthy and uraemic subjects. As expected, the distribution of drugs in whole blood was different in the uraemics from healthy subjects, because of the decreased plasma protein binding and the lowered red cell count in uraemia. Analysis of the data showed that the ratio between the concentrations in blood cells and plasma water in uraemic patients was not significantly different from that in healthy subjects.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00562320
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Distribution of pentobarbital and diphenylhydantoin between plasma and cells in blood: Effect of salicylic acid, temperature and total drug concentration (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 37-42 
    Details
    ISSN: 1432-1041
    Keywords: Pentobarbital ; diphenylhydantoin ; salicyclic acid ; protein binding ; erythrocytes ; cell equilibration ; temperature effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The binding of pentobarbital, diphenylhydantoin and salicylic acid to cells in blood was found to be independent of total drug concentration within therapeutic levels. Salicylic acid displaced pentobarbital and diphenylhydantoin from plasma protein binding sites, but high levels of salicylic acid had no effect on the distribution of the other two drugs to washed blood cells. Thus, in whole blood the presence of salicylic acid decreased the fraction of pentobarbital or diphenylhydantoin bound to plasma protiens and increased the fraction of the drug in plasma water and in blood cells. Diphenylhydantoin was shown not to be bound irreversibly to blood cells and equilibration in between the inside and outside of the cells was found to be rapid (within 5 min), even at high concentrations. Binding to washed blood cells was the same at 37°C and 25°C, in contrast to plasma protein binding. It is pointed out that these effects may cause certain analytical errors, resulting in changes in plasma concentration if plasma is separated at a low temperature.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561786
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Pethidine binding to blood cells and plasma proteins in old and young subjects (1982)
    Springer
    European journal of clinical pharmacology 23 (1982), S. 457-461 
    Details
    ISSN: 1432-1041
    Keywords: geriatrics ; pethidine ; drug disposition in blood ; erythrocytes ; age effect ; plasma protein binding ; red cell binding ; intracellular concentration
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The distribution of3H-pethidine in whole blood was compared in old (63–86 years;n=11) and young (19–25 years,n=12) subjects using equilibrium dialysis. The plasma protein binding was 52.7±3.3% (mean ± SD) in the old subjects and 51.8±3.1% in the young; the difference was not statistically significant. Studies on isolated plasma protein fractions showed that the main pethidine-binding protein wasα 1-acid glycoprotein. Accordingly, the degree of pethidine binding is likely to be affected by inflammatory disease rather than by age. The distribution of pethidine to blood cells showed no age-related difference; the ratio between whole blood and plasma concentrations was 0.99 in old and 0.98 in young subjects. In whole blood from old and young subjects, 43% and 41% of pethidine was present in erythrocytes, 27% and 26% in plasma water whereas 30% and 29% was bound to plasma proteins. The mean ratio between pethidine in cells and plasma water (2.01) indicates binding of the drug in or on the blood cells. These in vitro results do not support the previous theory that a decrease in intracellular pethidine distribution in old age was the reason for the reported higher plasma levels. A slower elimination rate remains the most likely explanation for the increased plasma concentration of pethidine in old patients.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00605998
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    Paper (German National Licenses)
    Fulltext
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