Measurement of plasma prednisolone in man.

Wilson, C. W. M.; Ssendagire, R; May, C S; Paterson, J. W.

doi:10.1111/j.1365-2125.1975.tb02778.x

Cited by 30 publications

(11 citation statements)

References 12 publications

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“…Thus, data obtained from oral dosing alone cannot distinguish between these two groups of patients. Similar magnitudes of variability were noted in peak prednisolone levels and prednisolone concentration-time profiles after oral prednisone or prednisolone was administered to patients with respiratory disease (11) and pediatric patients with various disease states (12). Bioavailability data in patients with kidney disease have been limited to studies in transplant patients.…”

Section: Discussionmentioning

confidence: 69%

Prednisolone Disposition in Cushingoid and Noncushingoid Kidney Transplant Patients*

Gambertoglio

Vincenti

Feduska

et al. 1980

The Journal of Clinical Endocrinology & Metabolism

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Little information is available on the disposition of prednisolone in kidney transplant patients and whether correlations exist between the pharmacokinetics and therapeutic or toxic effects of this drug. The present study was designed to determine the pharmacokinetics of prednisolone in six noncushingoid and six cushingoid transplant recipients. The elimination half-lives were not significantly different in the noncushingoid and cushingoid patients (2.3 vs. 3.3 h). However, other pharmacokinetic parameters were significantly lower in the cushingoid group: plasma clearance (147 vs. 82 ml/min) and volume of distribution (32 vs. 20 liters). In addition, the availability of prednisolone after oral prednisone administration was considerably variable (overall range, 27-108%) and was not significantly different between the two groups. Thus, in kidney transplant patients it appears that the plasma clearance and volume of distribution of prednisolone may distinguish between noncushingoid and cushingoid patients.

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Section: Discussionmentioning

confidence: 69%

Prednisolone Disposition in Cushingoid and Noncushingoid Kidney Transplant Patients*

Gambertoglio

Vincenti

Feduska

et al. 1980

The Journal of Clinical Endocrinology & Metabolism

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“…This could indicate first-pass metabolism after oral administration, poor absorption or a combination of the two. Wide variation in peak prednisolone concentration and A UC has been reported following oral dosage to normal and diseased subjects (Sandberg et al, 1970;Leclercq and Copinschi, 1974; Wilson et al, 1975;Davis et al, 1978;Petereit and Meikle, 1977). The wide interindividual variation is illustrated in figure 4; it is apparent after prednisone as well as prednisolone dosage and may also be a consequence of impaired drug absorption in some individuals (Davis et al, 1978), a factor which may well determine whether a given individual responds to therapy.…”

Section: Absorption and Bioavailabilitymentioning

confidence: 94%

Clinical Pharmacokinetics of Prednisone and Prednisolone

Pickup

1979

Clinical Pharmacokinetics

167

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Prednisone 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 regimens with fluctuating plasma concentrations being considered generally to be as effective with less side effects than a daily dosage regimen.Both drugs are rapidly absorbed after oral administration, reaching peak plasma concentrations after I to 3 hours. In general, plasma half-lives for prednisone are slightly longer (3.4 to 3.8h) than for prednisolone (2.1 to 3.5h). Either drug can be prescribed in most situations. On average, however, the bioavailability of prednisolone after oral prednisone is approximately 80 % of that after prednisolone. A wide intersubject variation in prednisolone concentration is evident after both drugs, which may suggest impaired drug absorption in some individuals. Prednisolone shows dose dependent pharmacokinetics; an increase in dose leading to an increase in volume of distribution and plasma clearance. This can be explained in terms of the non-linear binding of the drug to plasma proteins. The degree of binding will determine the distribution and clearance of free (i.e. pharmacologically active) drug. Reduced doses are recommended in patients with hypoalbuminaemia.Prednisolone pharmacokinetics are also dependent on age; the half-life being shorter in children. Liver disease prolongs the prednisolone half-life and, due to thefrequently associated hypoalbuminaemia, also increases the percentage of unbound drug. It has been recommended by some that prednisolone rather than prednisone is the drug of choice in active liver disease owing to the poor conversion of prednisone to prednisolone in some patients. However, the reduced plasma concentration of prednisolone in such patients is compensated for by delayed clearance. Thus, there is little advantage of one preparation over the other.

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“…The maximum plasma concentration (Cmax) and the time at which it was attained (tmax) appear in (Leclercq & Copinschi, 1974;Sullivan et al, 1974) or by studying patients already treated with steroids (Hulme, James & Rault, 1975). Alternatively the specificity of this type of assay can be improved by introducing a preliminary thin layer chromatographic step to separate prednisolone from other drugs and metabolites which might interfere with the subsequent protein binding assay (Wilson, Ssendagire, May & Paterson, 1975). This, however, also requires a tritiated prednisolone marker to be added to assess and compensate for extraction losses during the separation of prednisolone prior to elution.…”

Section: Plasma Level Profilesmentioning

confidence: 99%

Plasma prednisolone levels from enteric and non‐enteric coated tablets estimated by an original technique.

Morrison¹,

Bradbrook²,

Rogers³

1977

Brit J Clinical Pharma

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1 A quantitative thin layer chromatographic technique for the estimation of plasma prednisolone levels has been devised with a minimum level of estimation of 10 ng/ml. 2 A comparative study of the absorption of 5 and 10 mg prednisolone from enteric and non‐enteric coated tablets (5 mg) was carried out in healthy subjects. 3 Mean plasma half‐life and peak plasma concentrations obtained from the non‐ enteric coated preparation agree well with previous studies in normal subjects reported by other investigators using competitive protein binding or radioimmunoassay techniques. Intersubject variability in bioavailability was noted. 4 Enteric coating increased the lag time before prednisolone appeared in the blood but did not alter the bioavailability of prednisolone compared to the equivalent dose of the non‐enteric coated tablet.

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Measurement of plasma prednisolone in man.

Cited by 30 publications

References 12 publications

Prednisolone Disposition in Cushingoid and Noncushingoid Kidney Transplant Patients*

Prednisolone Disposition in Cushingoid and Noncushingoid Kidney Transplant Patients*

Clinical Pharmacokinetics of Prednisone and Prednisolone

Plasma prednisolone levels from enteric and non‐enteric coated tablets estimated by an original technique.

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