Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults

@article{Szefler2004MethylprednisoloneVP,
  title={Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults},
  author={S. Szefler and W. Ebling and J. Georgitis and W. Jusko},
  journal={European Journal of Clinical Pharmacology},
  year={2004},
  volume={30},
  pages={323-329}
}
SummaryThe disposition and plasma binding of methylprednisolone were examined in seven normal volunteers following the administration of 5, 20 and 40 mg of intravenous methylprednisolone sodium succinate. Methylprednisolone exhibits linear plasma protein binding averaging 77%. The mean plasma methylprednisolone clearance of 337 ml·h−1. kg−1 was independent of dose. The steroid appears to moderately distribute into tissue spaces with a mean volume of distribution of 1.41·kg−1. Methylprednisolone… Expand
Methylprednisolone achieves greater concentrations in the lung than prednisolone. A pharmacokinetic analysis.
TLDR
Although the clearance of the two drugs are not significantly different, methylprednisolone appears to have a slower clearance than prednisolones, and plasma glucocorticoid concentrations became significantly different in the two groups by 90 min (p less than 0.05). Expand
Troleandomycin effects on methylprednisolone and methylprednisone interconversion and disposition in the rabbit
SummaryA study of the effects of troleandomycin (TAO) on the disposition of intravenous methylprednisolone in rabbits was performed in order to develop an animal model to further evaluate theExpand
High dose oral methylprednisolone in patients with rheumatoid arthritis: pharmacokinetics and clinical response
TLDR
Oral administration of methylprednisolone in patients requiring high-dose pulse steroid therapy is convenient and avoids the discomfort and inconvenience associated with i.v. administration. Expand
Comparative Pharmacokinetics of Methylprednisolone Phosphate and Hemisuccinate in High Doses
TLDR
The results indicate that methylprednisolone phosphate results in a faster and more efficient conversion to its active form, methylpredisonsolone, than methylprednesolone hemisuccinate. Expand
Pharmacokinetic/Pharmacodynamic Evaluation of Deflazacort in Comparison to Methylprednisolone and Prednisolone
TLDR
The PK-PD-model was suitable to describe time course and magnitude of the observed effects and results were consistent with reported values for glucocorticoid receptor binding affinities for the investigated compounds. Expand
Methylprednisolone Exposure in Pediatric Renal Transplant Patients
TLDR
GBA might provide a complementary tool for monitoring GC exposure but further studies are needed, as no correlation of MP‐AUC or GBA was found with blood glucose or serum lipid concentrations, glomerular filtration rate, bone mineral density or graft histology. Expand
Pharmacokinetics and Pharmacodynamics of Systemically Administered Glucocorticoids
TLDR
Simulations with a pharmacokinetic/pharmacodynamic model using T helper cell counts and endogenous Cortisol as biomarkers for the effects of methylprednisolone suggest that the clinical efficacy of low-dose glucocorticoid regimens might be increased with twice-daily glucocORTicoid administration. Expand
Immunosuppressant pharmacodynamics on peripheral-blood mononuclear cells from patients with ulcerative colitis.
TLDR
The results showed that large individual deviations in PBMC response to the drugs were observed in UC, and UC patients exhibiting low PBMC sensitivity to prednisolone required a high predisonsolone amount as well as long period of prednisOLone administration for treatment. Expand
Focus on radioiodine-131 biokinetics: the influence of methylprednisolone on intratherapeutic effective half-life of 131I during radioiodine therapy of Graves’ disease
TLDR
Co-medication with methylprednisolone in patients with GO may be preferred to avoid an intratherapeutic decrease of EHL by accompanying protective glucocorticoides. Expand
Glucocorticoids in the treatment of rheumatic diseases: an update on the mechanisms of action.
TLDR
Recent insights relating to signaling, transcription processes, and gene expression as induced, inhibited, and/or modified by the interaction of GCs with their cytosolic receptors are reported, as well as relationships between dosages and plasma levels. Expand
...
1
2
3
4
...

References

SHOWING 1-10 OF 39 REFERENCES
Disposition of pulse dose methylprednisolone in adult and paediatric patients with the nephrotic syndrome
TLDR
The limited variability of the pharmacokinetics of methylprednisolone suggests that tissue sensitivity may be a more important indicator of drug dosage needs in nephrotic syndrome. Expand
Dose‐dependent pharmacokinetics of prednisone and prednisolone in man
TLDR
The apparent clearance values indicate that the dose-dependent effect occurs following oral administration of prednisone, and are in good agreement with those reported by Pickup & others (1977). Expand
Dose dependent pharmacokinetics of prednisolone
TLDR
It is proposed that changes in pharmacokinetic parameters may be associated with non-linear binding of the steroid to plasma proteins and prolongation of the plasma half-life and increase in the volume of distribution and plasma clearance of prednisolone. Expand
Methylprednisolone disposition in rabbits. Analysis, prodrug conversion, reversible metabolism, and comparison with man.
TLDR
The rabbit is a useful animal model for further assessing mechanisms of drug- or disease-steroid interactions which occur in man and the occurrence of reversible metabolism produces an apparent clearance which is about 71% of the value of the real elimination clearance for both steroids. Expand
Kinetics and interconversion of prednisolone and prednisone studied with new radioimmunogassays.
TLDR
The data indicate that prednisone is extensively metabolized to prednisolone before it clears the splanchnic circulation and the formationprednisone by oxidation of the 11-hydorxyl group of prednislone appears to occur mainly in peripheral tissues. Expand
PREDNISONE AND METHYLPREDNISOLONE DISPOSITION IN THE LUNG
TLDR
Methylprednisolone is better able than prednisone to penetrate lung acini and could not be detected in the BAL fluid in 3 patients; the overall correlation between blood and BAL fluid for all patients was r = 0.5. Expand
Prednisone or prednisolone for the treatment of chronic active hepatitis? A comparison of plasma availability.
TLDR
It is concluded that plasma prednisolone levels will be more predictable after prednisone than afterprednisone in subjects without hepatic dysfunction, and estimation of these could be of value in patients whose disease cannot be controlled by normal maintenance doses. Expand
Decreased clearance of prednisolone, a factor in the development of corticosteroid side effects.
TLDR
The data suggest that patients who develop side effects linked to steroid side effects, hirsutism and facial and truncal obesity, correlated with a slow rate of prednisolone catabolism. Expand
Prednisolone clearance at steady state in man.
TLDR
The results indicate that prednisolone exhibits dose- and concentration-dependent kinetics and that the great majority of the change in kinetics may be attributed to saturable protein binding of predisonsolone. Expand
Analysis of cortisol, methylprednisolone, and methylprednisolone hemisuccinate. Absence of effects of troleandomycin on ester hydrolysis.
A sensitive, selective, and reproducible high-performance liquid chromatographic assay for the simultaneous measurement of cortisol and methylprednisolone using dexamethasone as the internal standardExpand
...
1
2
3
4
...