Pharmacokinetics and protein binding of prednisolone after oral and intravenous administration

  title={Pharmacokinetics and protein binding of prednisolone after oral and intravenous administration},
  author={Harald Bergrem and Per Gr{\o}ttum and Hans Erik Rugstad},
  journal={European Journal of Clinical Pharmacology},
SummaryThe pharmacokinetics of prednisolone after oral and intravenous administration of 10 and 20 mg have been studied. Serum protein binding of prednisolone was also measured after the i.v. injections. The bioavailability after oral administration was 84.5% after 10 mg and 77.6% after 20 mg (p>0.05). Dose dependent pharmacokinetics were found, the VDss and Clt being significantly larger (p<0.01) after 20 mg i.v. than after 10 mg i.v. The protein binding of prednisolone in all subjects was non… 

Altered prednisolone pharmacokinetics in patients treated with rifampicin.

The dosage should be adjusted accordingly if prednisolone and rifampicin are prescribed concomitantly because of the marked reduction in total and especially free prednisOLone.

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This study comprehensively elucidates the complexities of prednisolone pharmacokinetics and demonstrates how plasma concentration-time profiles of total or free prednisOLone can be utilized for evaluation of predisonsolone Pharmacodynamics.

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It is suggested that the development and persistency of some cushingoid features may be related to a decreased total body clearance of prednisolone, which, in turn, may be influenced by impaired renal function.

Intra-individual consistency of prednisolone kinetics during long-term prednisone treatment

The results indicate considerable intra-individual consistency of prednisolone kinetics if other conditions are not changed, and no association was found between the prednisone dose rate, patient age or mean endogenous plasma hydrocortisone level and prednisolin clearance/kg.

Biowaiver monographs for immediate release solid oral dosage forms: prednisolone.

Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing prednisolone are

Population Pharmacokinetics of Prednisolone in Relation to Clinical Outcome in Children With Nephrotic Syndrome

Evidence is provided for the possibility of prednisolone drug monitoring through salivary measurements in children with nephrotic syndrome and this may be of particular usefulness in pediatric patients.

Effect of betamethasone on airway obstruction and bronchial response to salbutamol in prednisolone resistant asthma.

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Pharmacokinetics of intravenous and oral prednisolone.

It was concluded that over the dose range investigated, non-linear pharmacokinetic behaviour had not been demonstrated in this group of normal volunteers.

Dose dependent pharmacokinetics of prednisone and prednisolone in man

It is indicated that the pharmacokinetic parameters of protein-free and transcortin-free prednisolone were relatively constant with dose and that protein binding does not fully explain their apparent nonlinear distribution and disposition.

Dose dependent pharmacokinetics of prednisolone

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.

Dose‐dependent pharmacokinetics of prednisone and prednisolone in man

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).

Clinical Pharmacokinetics of Prednisone and Prednisolone

  • M. Pickup
  • Medicine, Biology
    Clinical pharmacokinetics
  • 1979
No relationship has been demonstrated between prednisolone plasma concentration (unbound or total concentration) and clinical response; alternate day dosage regimens with fluctuating plasma concentrations being considered generally to be as effective with less side effects than a daily dosage regimen.

Dose‐dependent prednisolone kinetics

Since it has been demonstrated that bioavailability, serum protein binding, prednisone‐prednisolone interconversion, and t½β remained constant over this dosage range, the altered Vd may account for the nonlinear relationship between AUC and dose.

Effectiveness of prednisolone during phenytoin therapy

The effects of diphenylhydantoin (DPH) on the clearance of prednisolone from plasma, its bioavailability, and its biologic effectiveness were studied in 5 persons before and after daily DPH therapy

Plasma protein binding of prednisolone in normal volunteers and arthritic patients

An in vitro assessment of the binding following the addition of prednisolone, prednisone, and hydrocortisone to the plasmas obtained from the subjects showed significant differences in the percentage of predisonsolone bound, but the differences observed were regarded as clinically insignificant.

Pharmacokinetics of prednisolone and endogenous hydrocortisone levels in cushingoid and non-cushingoid patients

The data suggest that endogenous hydrocortisone production is not as suppressed in patients with visible cushingoids signs as in noncushingoid patients, and that there is no significant difference in the pharmacokinetics of exogenous glucocorticoids between patients with and without cushingoid side effects.

Variation in plasma prednisolone concentrations in renal transplant recipients given enteric-coated prednisolone.

Renal transplant recipients receiving intermittent haemodialysis and kept under normal ward conditions showed appreciable differences in plasma prednisolone concentrations after therapeutic doses of enteric-coated prednisols, the effect being quantitatively most pronounced with large doses.