Clinical Pharmacokinetics of Prednisone and Prednisolone

@article{Pickup1979ClinicalPO,
  title={Clinical Pharmacokinetics of Prednisone and Prednisolone},
  author={M. E. Pickup},
  journal={Clinical Pharmacokinetics},
  year={1979},
  volume={4},
  pages={111-128}
}
  • M. Pickup
  • Published 1 March 1979
  • Medicine, Biology
  • Clinical Pharmacokinetics
SummaryPrednisone and prednisolone are used in a wide variety of diseases. The two compounds are metabolically interconvertible; prednisolone is assumed to be the pharmacologically active species.Prednisone and prednisolone plasma concentrations are commonly determined by either radioimmunoassay or competitive protein binding techniques. No relationship has been demonstrated between prednisolone plasma concentration (unbound or total concentration) and clinical response; alternate day dosage… 

Clinical Pharmacokinetics of Prednisone and Prednisolone

TLDR
The investigations performed so far have revealed that the dose-dependent pharmacokinetics partly explain the clinical observation that an alternate-day regimen with prednisone yields fewer biological effects.

Pharmacokinetics of prednisolone after high doses of prednisolone hemisuccinate.

TLDR
It is concluded that prednisolone shows doubled non-linear pharmacokinetics with higher total body clearance in the medium dose range than in the low and high dose range and volume of distribution changes accordingly, but overall elimination rate remains remarkably constant.

Prednisone and prednisolone bioavailability in renal transplant patients.

TLDR
The results from this study indicate that both of the oral preparations tested provide similar bioavailability of active prednisolone and the conversion of prednisone to prednislone occurs rapidly.

Pharmacokinetics of Methylprednisolone and Prednisolone After Single and Multiple Oral Administration

TLDR
After multiple administration, prednisolone showed significant time‐dependent pharmacokinetics with increased un bound clearance and increased unbound volume of distribution.

Dose-dependent pharmacokinetics of prednisolone in normal and adrenalectomized rats

TLDR
Prednisolone plasma protein binding was nonlinear due to saturation of transcortin binding, but changes in pharmacokinetic parameters were not related to the nonlinear plasma binding, and were more likely caused by saturation of elimination pathways and tissue binding sites.

Corticosteroid Pharmacokinetics in Liver Disease

TLDR
Patients with liver disease and hypoalbuminaemia are more likely to suffer major side effects of prednisone as a consequence of decreased protein binding and delayed clearance of Prednisolone, so dosage should be reduced in accordance with serum albumin concentration.

A Pharmacokinetic/Pharmacodynamic Approach to Predict Total Prednisolone Concentrations in Human Plasma

TLDR
The combination of nonlinear protein binding, cortisol circadian rhythm, and cortisol suppression could account for the nonlinearity of total prednisolone and the combination of pharmacokinetic models for free prednisone and prednislone, and the linear release rate model for cortisol suppression were combined to predict total predisonsolone concentrations in plasma.

Pharmacokinetics of prednisolone in children with the nephrotic syndrome

TLDR
Routine measurements of prednisolone kinetics do not help when assessing the treatment of children with INS, and no correlation was found between the values of pharmacokinetic parameters and criteria of clinical effectiveness.

Prednisolone pharmacokinetics and protein-binding in patients with portosystemic shunt.

TLDR
Reduction of the prednisolone dose is therefore not indicated in patients with portosystemic shunt and chronic liver disease, even in the presence of hypoalbuminemia.
...

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TLDR
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