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Results for “PREDNISOLONE, THERAPEUTIC”

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PubMed2006

Therapeutic drug monitoring of prednisolone after lung transplantation.

BACKGROUND: Despite well-known and serious potential side-effects of corticosteroid therapy, therapeutic drug monitoring (TDM) of prednisolone is rarely performed after lung transplantation (LTx). METHODS: We measured prednisolone exposure using a 6-hour area-under-the-curve (AUC) analysis in 52 LTx recipients (41 bilateral, 9 single and 2 heart-lung), who were 99 +/- 13 (mean +/- SEM) weeks (range 4 to 380) post-LTx. Fourteen of 52 had cystic fibrosis (CF), and 36 of 52 were on cyclosporine and 16 of 52 on tacrolimus. Prednisolone dose was 9.8 +/- 0.7 mg/day (range 1 to 20). RESULTS: Only 9 of 52 LTx patients had a prednisolone AUC within the previously reported reference range for healthy adult control subjects (170 to 260 nmol x hr/liter/milligram prednisolone). Six patients had values below and 37 above this range. Prednisolone AUC was higher in patients with CF compared with non-CF patients (511 +/- 82 vs 349 +/- 27 nmol x hr/liter/milligram, p < 0.02) and 70% of LTx recipients had measurable prednisolone levels at baseline (26.5 +/- 4.5 nmol/liter), unlike normal controls. CONCLUSIONS: LTx recipients show a wide inter-individual variation in prednisolone pharmacokinetics; therefore, many are overdosed on conventional protocols. Side-effects of corticosteroid therapy remain a major clinical problem after transplantation, justifying the use of prednisolone TDM to optimize dosing and minimize morbidity.

Area Under Curve↗
PubMed1985

Pharmacokinetics of 3 prednisolone prodrugs. Evidence of therapeutic inequivalence in renal transplant patients with rejection.

Renal allograft rejections are often treated with high doses of prednisone or prednisolone. The solubility of the biologically active prednisolone is poor. Therefore prednisolone is given i.v. as prednisolone disodium phosphate (prednisolone phosphate) or as prednisolone sodium tetrahydrophthalate (prednisolone phthalate). The time course of hydrolysis of high doses of these prodrugs and the reduction of high doses of oral prednisone into prednisolone has not been investigated. Therefore 10 patients treated for acute rejection were given, on 3 occasions, oral prednisone, i.v. prednisolone phosphate, or i.v. prednisolone phthalate in equimolar doses corresponding to 7 mg/kg of prednisolone. Blood samples were collected over a 24-hr period. Measurements were performed by high-performance liquid chromatography and equilibrium dialysis. The time to peak, the peak concentrations, and the area under the plasma-concentration-vs.-time curve (AUC) of prednisone and of unbound prednisolone were calculated. In all patients the hydrolysis of the prednisolone phosphate ester was faster than that of the prednisolone phthalate ester. The mean (+/- SD) peak concentrations of unbound prednisolone were higher after i.v. prednisolone phosphate (18.5 +/- 3.4 micrograms/ml) than after i.v. prednisolone phthalate (2.9 +/- 0.5 micrograms/ml) or after oral prednisone (3.1 +/- 0.8 micrograms/ml), (P less than 0.001). The mean AUCs of unbound prednisolone were 2324 +/- 683 micrograms/ml/min from prednisolone phosphate, 1209 +/- 324 micrograms/ml/min from prednisolone phthalate, and 1584 +/- 556 micrograms/ml/min from oral prednisone. The AUCs of prednisolone from i.v. prednisolone phosphate (P less than 0.001) or from oral prednisone (P less than 0.005) were higher than from i.v. prednisolone phthalate.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1976

[Characteristics of energy metabolism in different regions of the heart, liver and kidneys in myocardial infarct after administration of prednisolone].

The effect of therapeutic doses of Prednisolone (1 mg/kg) on the indices of energy metabolism in different regions of the heart, liver and kidneys was studied in 70 dogs within the initial 10 days after the ligation of the left coronary artery. The administration of such doses of Prednisolone was found to increase the respiration of the mytochondria and especially the binding of the inorganic phosphate in the zone of the infarction, to switch over from the poorly effective oxidation in the nondamaged area of the left ventricle to the one firmly conjugated with phosphorylation, to level the balance between the respiration and phosphorylation of the mytochondria in the right ventricle, liver and kidneys. The beneficial effect of Prednisolone upon the energy metabolism in the tissues during myocardial infarction manifested itself in growing depots of ATP and creatinephosphate in all regions of the heart. This effect of Prednisolone is most clearly expressed during the initial 5 days of its administration, and is less demonstrative when given for 10 days.

Animals↗
PubMed1993

Strength and endurance in the therapeutic evaluation of prednisolone-treated MDX mice.

The dystrophin-deficient, X-linked dystrophic mouse (mdx) was used to evaluate the efficacy of prednisolone treatment. A test protocol was used to take advantage of the quantifiable weakness and disability as well as molecular genetic defect shared with the X-linked Duchenne muscular dystrophy (DMD). Whole-body weakness and fatigue were determined by non-invasive force-transducer physiographic and variable-speed treadmill techniques, respectively. Other measurements included hind-limb muscle protein, calcium, and histomorphology. Subcutaneously-administered prednisolone elicited significant improvements in whole body strength throughout a two-month test period. Increases in strength were also accompanied by measurable increments in running endurance. In fact, prednisolone treatment appeared to protect mdx mice from the stressful effect of continuous running as determined by strength and muscle fiber diameter. Test results from this study support the limited therapeutic benefit observed previously in DMD patients treated with the glucocorticoid.

Animals↗
PubMed2002

Therapeutic effect of intraarterial prednisolone injection in severe intestinal Behçet's disease.

A 64-year-old woman with severe intestinal Behçet's disease who was unresponsive to conventional therapies, including intensive intravenous steroid injections, underwent intraarterial steroid injection therapy. After the infusion of prednisolone into the mesenteric arteries, her colon ulcers improved markedly, and the frequency of bloody stools decreased immediately. The present case suggests that intraarterial steroid injection therapy may be potentially useful in severe intestinal Behçet's disease.

Anti-Inflammatory Agents↗
PubMed1977

Indication and duration of the prednisolone therapy of chronic pulmonary sarcoidosis--a prognostic-therapeutic screening as a result of a controlled trial.

Report on a controlled therapeutic trial with prednisolone of chronic pulmonary sarcoidosis. The patients comprised three groups differing from the dose of prednisolone and the duration of the treatment. 194 clinically and histologically proven cases were completely treated. Two years after ending the treatment the relapse rates were about 20 to 30% in each group. This corresponds well with the rate of spontaneous regression. These results are an indicator that in most cases the underlying pathogenic process of immune deficiency is calming down during treatment and this leads to a possible change in therapeutic indication:--treating all patients for only one year, --taking into account that a relapse will occur in about one third of all cases,--avoiding supertreatment of the other two thirds with a not harmless and costly drug.

Chronic Disease↗
PubMed1985

Therapeutic benefits from a poorly absorbed prednisolone enema in distal colitis.

A double blind controlled trial has been conducted in 40 patients to compare the therapeutic effects of prednisolone metasulphobenzoate enemas with those of prednisolone-21-phosphate enemas. Both enemas brought about improvement in symptoms and sigmoidoscopic appearances in more than 70% of patients treated. The absorption of prednisolone from the metasulphobenzoate enema in three patients was less than from the 21-phosphate enema. In view of the low plasma prednisolone concentrations obtained, there are theoretical advantages in using a poorly absorbed enema to avoid the possibility of systemic steroid effects in patients requiring long term steroid treatment.

Adult↗