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At least 19 recordsLinked to original sources
PubMed1976

Comparative serum prednisone and prednisolone concentrations following prednisone or prednisolone administration to beagle dogs.

The relative serum prednisone and prednisolone concentrations were determined following the administration of prednisone or prednisolone as 5-mg tablets to male beagle dogs. Serum prednisone concentrations were significantly greater following prednisone administration than they were following prednisolone administration. Serum prednisolone concentrations were significantly greater following treatment with prednisolone than with prednisone. The combined prednisone and prednisolone areas under the serum concentration-time curves were similar for the two treatments.

Animals↗
PubMed1979

Studies comparing the metabolic clearance rate of 11 beta,17,21-trihydroxypregn-1,4-diene-3,20-dione (prednisolone) after oral 17,21-dihydroxypregn-1,4-diene-3,11,20-trione and intravenous prednisolone.

The MCR of prednisolone (11 beta,17,21-trihydroxypregn-1,4-diene-3,20-dione) and the absorption of prednisone (17,21-dihydroxypregn 1,4-diene-3,11,20-trione) were studied in five normal subjects and four patients. Plasma and urinary prednisolone were measured by a competitive radioassay. The MCR was determined after iv administration of 30 mg nonisotopic prednisolone using one-compartment (MCR1) and two-compartment (MCR2) analyses. These values were compared with the MCR determined after oral administration of nonisotopic prednisone (MCR0). MCR1 and MCR2 were closely correlated, indicating the applicability of first order kinetics to the study of prednisolone metabolism. In subjects with normal gastrointestinal function, MCR0 was consistently lower than MCR2 (mean MCR2 = 0.175 liters/h.kg; MCR0 = 0.145 liters/h.kg). In two patients with steroid malabsorption, the MCR0 was significantly greater than MCR2. Knowledge of the expected relationship between MCR0 and MCR2 allowed quantitation of the degree of malabsorption. With or without impaired absorption, the absorptive process was essentially complete by the time of the peak plasma concentration. Estrogen therapy lowered the MCR0, and high prednisone dose increased the MCR0. Those effects and the effects of iv prednisolone administration on the MCR are explained by the effects of plasma protein binding of prednisolone. These studies demonstrate the usefulness of the oral MCR determination in the evaluation of steroid absorption and metabolism.

Administration, Oral↗
PubMed1979

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 prednisolone tablets. This gross day-to-day variation occurred irrespective of the dosage used. Breakfast given before prednisolone tended to reduce the rate of absorption of the drug, the effect being quantitatively most pronounced with large doses. Haemodialysis had no apparent effect on the elimination of prednisolone from plasma. Such erratic blood concentrations of prednisolone as observed in these patients, possibly resulting from variable absorption, may be potentially hazardous. Hence use of enteric-coated tablets in renal transplant recipients should be viewed with caution.

Adolescent↗
PubMed1978

The effects on polymorphonuclear leucocyte function of prednisolone and azathioprine in vivo and prednisolone, azathioprine and 6-mercaptopurine in vitro.

The effects of prednisolone azathioprine and 6-mercaptopurine on polymorphonuclear neutrophil chemotaxis, phagocytosis, and killing of Staphylococcus aureus and Candida albicans have been studied. In twenty patients with a functioning kidney graft, taking both azathioprine 2.5 mg/kg/day and prednisolone (mean dose 0.59 mg/kg/day; range 0.30-1.0 mg/kg/day), the polymorphonuclear function did not significantly differ from that in either twenty-two normal or eighteen uraemic controls. Addition of prednisolone, 1.2 X 10(-5) M, azathioprine, 2.1 X 10(-5) M, and 6-mercaptopurine, 2.1 X 10(-5) M, using each drug alone, to normal human polymorphonuclear cells in vitro did not significantly alter their function. It is concluded that prednisolone and azathioprine together in vivo and that both these drugs and 6-mercaptopurine singly in vitro have no significant deleterious effect on polymorphonuclear function and do not contribute, in this way, to the increased susceptibility of patients receiving these drugs to infection.

Adolescent↗
PubMed1977

[Treatment of idiopathic fibrosing alveolitis. Therapeutic experiences with azathioprine-prednisolone and D-penicillamine-prednisolone combination therapy].

Lung function data during three different therapies for idiopathic fibrosing alveolitis are presented. Corticosteroid monotherapyis without effect. A combination of prednisolone and azathioprin improves vital capacity by more than 15% in half of cases. Under this treatment the resting PO2 improves in a third of patients. No improvement in PO2 under exercise is observable in any patient. Combined therapy with D-penicillamine and prednisolone improves vital capacity and PO2 both at rest and under exercise; this therapy thus appears to be superior to the other two. The effectiveness of D-penicillamine-prednisolone therapy can be enhanced by adding azathioprin, as has been found in a pilot study thus far covering 4 patients.

Adult↗
PubMed1979

Plasma prednisolone levels and adrenocortical responsiveness after administration of prednisolone-21-phosphate as a retention enema.

Plasma prednisolone levels have been measured by radioimmunoassay after oral and rectal administration to healthy volunteers and to patients with idiopathic proctocolitis. The amount of prednisolone absorbed from a 20 mg retention enema given to patients with proctocolitis was about 44% of that absorbed from the same dose orally administered. Adrenocortical response to synthetic ACTH in patients receiving prolonged rectal therapy was either normal, or only slightly impaired, and this may be related to the pattern of steroid absorption rather than to the total amount absorbed.

Adolescent↗
PubMed1978

Prednisone or prednisolone for the treatment of chronic active hepatitis? A comparison of plasma availability.

1 The plasma availability of prednisolone after oral doses of prednisolone and its precursor, prednisone, were compared in ten normal controls and twenty-five patients with chronic active hepatitis by estimation of the area under the plasma concentration--time curve for the drug (AUC). 2 In controls, values for AUC were significantly more variable after prednisone than prednisolone, and two subjects showed markedly inefficient conversion of prednisone to prednisolone. In patients, variability was similarly wide after both preparations, but overall bioavailability after both prednisone and prednisolone was similar to that found in controls, although three patients showed subnormal values after both preparations, possibly as a result of impaired intestinal absorption. 3 Patients with biochemical and histological evidence of active hepatocellular necrosis showed evidence of impaired activation of prednisone, but this was compensated for by a decreased rate of elimination of prednisolone from the plasma. 4 It is concluded that plasma prednisolone levels will be more predictable after prednisolone than after prednisone in subjects without hepatic dysfunction. In the presence of liver disease, because of the marked variability in plasma prednisolone levels after either drug, estimation of these could be of value in those patients whose disease cannot be controlled by normal maintenance doses.

Adult↗
PubMed1977

Prednisolone bioavailability in the dog.

With a fasted dog as an animal model, the bioavailability and pharmacokinetics of prednisolone were studied following rapid intravenous injection and oral dosing of a prednisolone sodium phosphate solution and also following oral doses of prednisolone as tablets and a slurry. Hydrolysis of the phosphate ester to prednisolone in the body is extremely rapid and complete, thus permitting accurate calculation of the distribution volume of prednisolone. Enteral absorption of prednisolone from a slurry is superior to that from prednisolone tablets and from a prednisolone sodium phosphate solution. Reduced absorption from tablets, compared to the slurry, is probably due to tablet disintegration characteristics; reduced absorption from the solution is probably due to poor membrane permeability of the ionized drug. Information obtained from a single animal may indicate the need for expanded studies in humans.

Administration, Oral↗
PubMed1979

Short-term effects of prednisolone on neuromuscular transmission in normal rats and those with experimental autoimmune myasthenia gravis.

Electrophysiological investigations of the effects of bath-applied prednisolone at the neuromuscular junction were performed in muscles from normal rats and rats with experimental autoimmune myasthenia gravis (EAMG). In muscles from both groups, prednisolone reversible and significantly depressed the amplitudes of minature end-plate potentials (MEPPs), end-plate potentials (EPPs) and indirectly elicited action potentials (APs) without affecting resting membrane potentials. Prednisolone also caused a significant reduction in EPP rise time to peak and half-decay time while markedly increasing MEPP frequency and AP rise time to peak and duration. These effects were shown to be dose-dependent. The percentage decrease in amplitude after prednisolone perfusion was similar for EPPs and MEPPs, indicating that the depressive effect of prednisolone at the junction is postsynaptic. In all of the parameters studied, the percentage effect of prednisolone was the same in EAMG and normal preparations. No stimulus-linked repetitive EPPs or APs were observed after prednisolone. It is concluded that prednisolone has a depressive effect on neuromuscular transmission, but that this occurs only at high concentrations of the drug which are not achieved during the treatment of myasthenia gravis.

Action Potentials↗
PubMed1979

Effects on induction of tyrosine aminotransferase in fetal mouse liver in vitro of prednisolone, insulin and thyroxine.

The hormonal requirements for formation of tyrosine aminotransferase (EC 2.6.1.5) in fetal mouse liver were investigated in organ culture using chemically defined medium. The hormones tested were insulin, thyroxine and prednisolone. Prednisolone alone resulted in a two-fold increase in tyrosine amino-transferase activity in explanted liver in hormone-free medium on day 6, and its effect was dose dependent, but neither insulin nor thyroxine alone induced the enzyme. Addition of prednisolone plus thyroxine and prednisolone plus insulin increased the enzyme activity 1.4- and 1.3-fold, respectively, over that of explants with prednisolone alone. These three hormones together had the greatest effect, causing induction of 1.5-fold more activity than that with prednisolone plus insulin or plus thyroxine. The three hormones were not all needed continuously during the culture period: prednisolone and insulin were required during the early part of cultivation and thyroxine during the later part. The effects of these hormones were blocked by actinomycin D or puromycin, suggesting that these hormones increase de novo synthesis of tyrosine aminotransferase. Phase-contrast microscopy showed that prednisolone stimulated liver epithelial cell outgrowth, probably acting with insulin.

Animals↗
PubMed1975

Effect of prednisolone and salicyclic acid on ionic fluxes across the human stomach.

We compared ionic fluxes across human gastric mucosa after instillation of test solutions of isotonic hydrochloric acid alone or containing salicylic acid, or prednisolone or both. Prednisolone produced no alteration in fluxes of H+ and Na+ ions compared with controls. Salicyclic acid induced a significant net loss of H+ ions and gain of Na+ ions indicating alteration of the gastric mucosal barrier. Combined salicyclic acid plus prednisolone produced no increase in permeability of gastric mucosa to H+ and Na+ ions or to salicylic acid itself. Prednisolone was not appreciably absorbed from the stomach while salicylic acid was well absorbed. Combination of salicylic acid and prednisolone did not increase absorption of either drug. Neither salicylic acid nor prednisolone solutions alone or combined caused an increase in pepsin output over that due to 160 mM HCl. Salicylic acid resulted in a significant fall in potential difference compared to control while prednisolone produced no change in the one subject studied. In acute studies in man prednisolone is not absorbed from the stomach, does not itself affect the gastric mucosal barrier nor pepsin output nor does it enhance the absorption of or effect of salicylic acid on gastric ionic fluxes or pepsin output.

Absorption↗
PubMed1979

The effect of prednisolone on neuromuscular transmission in the rat diaphragm.

Prednisolone, in concentrations of 0.004--0.032 mmol/l, increased the amplitude of the miniature end-plate potentials (MEPPs). A maximum increase to 134% of the control values was seen at 0.016 mmol/l. At higher prednisolone concentrations the MEPP amplitude gradually decreased to reach 77% of the control value at 0.62 mmol/l. The MEPP frequency was increased to twice the control value at 0.62 mmol/l. The quantal content of the end-plate potential (EPP), however, was not influenced by prednisolone. The response to iontophoretically applied acetylcholine was diminished, especially at 0.62 mmol/l prednisolone. Prednisolone, therefore, caused presynaptic effects as was shown by an increase in unitary MEPP amplitude and by a considerable number of giant MEPPs, which at increasing prednisolone concentrations was antagonized increasingly by a postsynaptic depressant effect. These results also provide an explanation for the adverse effects of prednisolone on the end-plate potential and on neuromuscular transmission.

Acetylcholine↗
PubMed1979

High-pressure liquid chromatographic evaluation of aqueous vehicles for preparation of prednisolone and prednisone liquid dosage forms.

A high-pressure liquid chromatographic method was developed that separates prednisolone from prednisone, prednisone from methylprednisolone succinate sodium, and hydrocortisone from hydrocortisone acetate or cortisone acetate. The common liquid dosage preservatives methylparaben, propylparaben, and sodium benzoate do not interfere with quantitative prednisolone, prednisone, and hydrocortisone determinations. The method was used to study prednisolone and prednisone stability in five aqueous vehicles (water, citrate buffer USP, 50% glycerin, 50% sorbitol, and 50% sucrose) containing 10% (v/v) ethanol. Prednisone crystallized out in all vehicles except glycerin, in which it appeared to be stable for at least 92 days. Prednisolone did not crystallize in any vehicle but decomposed quickly in citrate buffer. Sorbitol and glycerin appeared to be the best vehicles for prednisolone. The developed method was applied successfully to the quantitative determinations of prednisolone, prednisone, and hydrocortisone in commercial tablets.

Chromatography, High Pressure Liquid↗
PubMed1978

Controlled trial prednisolone in acute polyneuropathy.

In a multicentre, randomised trial of prednisolone in acute polyneuropathy of undetermined aetiology (Guillain-Barré syndrome), 21 patients were treated with prednisolone (60 mg daily for one week, 40 mg daily for four days, and then 30 mg daily for three days) and 19 did not have steroid treatment. Patients were graded on a six-point scale by one of two neurologists who had no knowledge of the treatment schedule. Reassessment at one, three, and twelve months consistently showed greater improvement in the control than the prednisolone group but the only statistically significant result was in the improvement at three months among patients entered to the trial within a week of onset of illness. The 6 control patients had improved by 2.5 +/- 0.43 grades by three months from entry to the trial whereas the 10 prednisolone patients had only improved by 0.9 +/- 0.46 grades (P less than 0.05). There was 1 death related to the polyneuropathy in each group, and 1 suicide in a control patient during convalescence. 6 prednisolone patients were left with considerable disability compared with 1 control patient. There were 3 relapses in the prednisolone group, but none in the control group. The results indicate that steroid treatment is not beneficial and can be detrimental in acute neuropathy of undetermined aetiology.

Acute Disease↗
PubMed1979

The effect of food and tablet formulation on plasma prednisolone levels following administration of enteric-coated tablets.

1 Plasma prednisolone levels have been compared following the administration of enteric-coated prednisolone to fasted and non-fasted subjects. The effect on plasma levels of altering the formulation of the enteric-coating has also been studied. 2 The presence of food in the stomach at the time of administration does not affect the absorption of enteric-coated prednisolone tablets. 3 There was considerable inter-subject variation in plasma prednisolone levels after administration of shellac based enteric-coated tablets. However, plasma levels were more consistent when a preparation whose formulation was based upon cellulose acetate phthalate (CAP) was given. 4 It is concluded that the pattern of absorption and plasma prednisolone levels depend on the formulation of the enteric coating. The bioavailability of the CAP based preparation is similar to that of plain prednisolone.

Adult↗
PubMed1977

Immunosuppressive properties of sera and urine dialysates from kidney-graft recipients treated with azathioprine, prednisolone, and niridazole.

Niridazole, an antischistosomal agent, was given to renal transplant recipients in addition to azathioprine and prednisolone, as there is experimental evidence that this combination of drugs is highly immunosuppressive. Sera obtained from kidney-graft recipients during the first two weeks after transplantation were examined for their ability to inhibit the one-way mixed lymphocyte reaction (MLR). Sera from seven patients receiving azathioprine, prednisolone, and niridazole (triple-drug treatment), five patients receiving azathioprine and prednisolone, and two other patients treated with niridazole alone for schistosomiasis produced MLR inhibition by comparison with pretreatment (control) sera.A mean of 78% inhibition was observed with sera taken after one day's treatment with the three-drug combination, whereas this level of in-vitro immunosuppression occurred only after eight days of treatment with azathioprine and prednisolone. Niridazole alone produced an effect similar to azathioprine and prednisolone. Concentrated dialysate of urine from a patient receiving triple-drug treatment not only inhibited the MLR but also significantly prolonged the survival of heterotopic heart allografts in rats, whereas dialysate from the same patient after niridazole had been stopped gave less MLR inhibition and failed to prolong heart allograft survival.Since niridazole thus increased the in-vitro and in-vivo immunosuppressive action of azathioprine and prednisolone, we suggest that this triple-drug combination might be useful for preventing early acute kidney graft rejection.

Azathioprine↗