SEARCH · PubMed Health

Results for “PREDNISOLONE”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 19 recordsLinked to original sources

PubMed1992

An in vitro comparison of the permeability of prednisolone, prednisolone sodium phosphate, and prednisolone acetate across the NZW rabbit cornea.

Controversy and ambiguity in the literature concerning the corneal penetration of prednisolone acetate over Prednisolone Sodium phosphate in NZW rabbits has recently prompted comparative studies using specific chromatographic assays. In vitro, corneal penetration studies were performed using the Ussing Chambers to compare the permeability and flux of both esters and prednisolone at 0.5% using a reversed phase HPLC-UV assay. Chromatograms of samples from the receiver chambers show primarily the presence of prednisolone from both esters; only prednisolone phosphate penetrated the cornea intact. Flux measurements were similar for prednisolone and both salt forms in terms of the metabolite prednisolone. Permeability coefficient calculations give the relative comparison: prednisolone acetate greater than prednisolone greater than prednisolone sodium phosphate.

Animals↗

PubMed1991

Assay methodology for prednisolone, prednisolone acetate and prednisolone sodium phosphate in rabbit aqueous humor and ocular physiological solutions.

Prednisolone, prednisolone acetate and prednisolone sodium phosphate are glucocorticoids used for ocular, anti-inflammatory therapy. A reversed-phase high-performance liquid chromatographic assay using ultraviolet detection has been developed that affords baseline resolution of the above analytes in balanced salt solutions and rabbit aqueous humor. The drugs can be quantified at 0.025-0.05 micrograms/ml in the above matrices; 6 alpha-methylprednisolone is used as the internal standard. Both esters of prednisolone are vulnerable to chemical and enzymatic hydrolysis giving prednisolone. Analysis of aqueous humor samples shows prednisolone acetate penetrating/metabolizing primarily to prednisolone; prednisolone sodium phosphate penetrates the cornea giving the ester and alcohol.

Animals↗

PubMed2001

Comparison of suppressive potency between prednisolone and prednisolone sodium succinate against mitogen-induced blastogenesis of human peripheral blood mononuclear cells in-vitro.

Clinically, both prednisolone and prednisolone sodium succinate are widely used as immunosuppressive agents for the treatment of various allergic disorders. However, whether prednisolone sodium succinate itself has immunosuppressive or anti-inflammatory effects is unclear, and prednisolone sodium succinate may exhibit its efficacy only after hydrolytic conversion to prednisolone in-vivo. If this is the case, the impairment of prednisolone sodium succinate conversion to prednisolone in some clinical conditions may attenuate the efficacy of prednisolone sodium succinate. We therefore compared the pharmacological efficacy of prednisolone with that of prednisolone sodium succinate in-vitro using human peripheral blood mononuclear cells (PBMCs). PBMCs were obtained from 5 healthy subjects and 1 patient with pneumonia. The cells were incubated in the presence of concanavalin A and the cell growth was estimated by 3-(4,5-dimethyl thiazo-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. Both prednisolone and prednisolone sodium succinate dose-dependently suppressed PBMC blastogenesis. Mean (s.d.) prednisolone and prednisolone sodium succinate IC50 (concentration of drug that gave 50% inhibition of cell growth) values were 580.0 (1037.9) and 3237.1 (4627.3) nM, respectively. The ratio of prednisolone IC50/prednisolone sodium succinate IC50 ranged from 0.005 to 0.230. Thus, prednisolone sodium succinate potency was markedly lower than that of prednisolone. After incubation of PBMCs with 100 microM prednisolone sodium succinate, 22.7-42.9 microM prednisolone was liberated into the culture medium, as determined by HPLC. The ratio of prednisolone liberation from prednisolone sodium succinate was not affected by the presence of fetal bovine serum or PBMC, or both, in the culture medium. These results suggested that the PBMC-suppressive effects of prednisolone sodium succinate might be due, at least partially, to prednisolone liberated from prednisolone sodium succinate into the culture medium. Prednisolone sodium succinate can be converted to prednisolone in the absence of serum or PBMCs, but the ratio of this conversion was very slow (t(1/2) > 4 days). Therefore, impairment of the enzymatic conversion of prednisolone sodium succinate to prednisolone in some pathological conditions such as liver diseases may result in attenuation of the clinical efficacy of prednisolone sodium succinate.

Adult↗

PubMed1989

Randomised controlled trial comparing prednisolone alone with cyclophosphamide and low dose prednisolone in combination in cryptogenic fibrosing alveolitis.

In a randomised, controlled study alternate day prednisolone with an initial high dose phase ("prednisolone only series") has been compared with cyclophosphamide plus alternate day low dose prednisolone ("cyclophosphamide-prednisolone series") in 43 patients with previously untreated fibrosing alveolitis (five patients had received prednisolone in minimal dosage). In the prednisolone only series prednisolone 60 mg daily was given for one month and then reduced by 5 mg a week to 20 mg on alternate days or the minimum dose to maintain early improvement. Patients in the cyclophosphamide-prednisolone series received 100, 110, or 120 mg cyclophosphamide daily (depending on body weight) plus 20 mg prednisolone on alternate days. Treatment was continued indefinitely, or changed to the alternative regimen if the patient deteriorated, failed to improve, or developed drug toxicity. For response to treatment (as judged by change in breathlessness score, radiographic appearance, and lung function) patients were classified as improved, stable, or deteriorating. Deaths from cryptogenic fibrosing alveolitis were also analysed. Improvement had occurred at one or more assessments in seven of the 22 patients in the prednisolone only series and in five of the 21 patients in the cyclophosphamide-prednisolone series. At three years, however, only two of the 22 patients in the prednisolone only series were still improved and three stable, compared with one and seven of the 21 patients in the cyclophosphamide-prednisolone series (three of the seven had stopped treatment because of toxicity). Life table analysis suggested better survival in patients in the cyclophosphamide-prednisolone series but this was not significant. At three years 10 of 22 patients in the prednisolone only series had died compared with three of 21 patients in the cyclophosphamide-prednisolone series. With death or failure of first treatment regimen as outcome there was a significant advantage to the patients having cyclophosphamide-prednisolone. This advantage was explained in part by the better lung volumes in this group on admission. After allowance had been made for total lung capacity (TLC), no other factor was predictive of outcome. Analyses of subgroups according to TLC on admission showed that patients with a TLC below 60% predicted did badly and those with a TLC of 80% or more predicted did well with both regimens. Patients with an initial TLC of 60-79% predicted did better with the cyclophosphamide-prednisolone regimen. Side effects were uncommon in both series and those due to cyclophosphamide resolved when treatment was stopped. The combination of cyclophosphamide with prednisolone may be an alternative to prednisolone alone with an initial high dose phase. Many patients, however, failed to respond to either treatment.

Adult↗

PubMed1994

[Anti-inflammatory effect of a local combination therapy with diclofenac and prednisolone vs. indomethacin and prednisolone. A laser flare cell photometry study].

UNLABELLED: The nonsteroidal anti-inflammatory agent diclofenac (Voltaren) has recently become commercially available in form of 0.1% eyedrops (Voltaren ophtha). In the present study, we compared the anti-inflammatory effect of a topical combination therapy with diclofenac and prednisolone vs. indomethacin and prednisolone. PATIENTS AND METHOD: The FC-1000 laser flare-cell photometer (Kowa) was used to investigate 40 patients before and after cataract surgery with IOL implantation. This method allows quantitative in vivo determination of aqueous flare and aqueous particle concentration. The patients were randomly assigned to one of the following two treatment protocols: Protocol A: diclofenac 0.1% eyedrops and prednisolone 1% eyedrops (Inflanefran forte); protocol B: indomethacin 1% eyedrops (Chibro-Amuno 3) and prednisolone 1% eyedrops. One drop of either drug was administered 4 times per day to each patient. Treatment with nonsteroidal agents started on the day before surgery, whereas prednisolone treatment started immediately at the end of surgery. No parabulbar or oral steroids were administered. RESULTS: In group A (diclofenac and prednisolone), the flare (in photon counts/ms) increased from a preoperative value of 10 +/- 4.3 (mean +/- SD) to 36.7 +/- 19.3 on the 1st postoperative day. This value is significantly (P < 0.05) higher than in group B (indomethacin and prednisolone) on the 1st postoperative day: 27.4 +/- 9.4. The aqueous particle concentration on day 1 after surgery was also significantly (P < 0.01) higher under treatment with diclofenac and prednisolone than with indomethacin and prednisolone (44.3 vs 26.3 particles/0.075 mm3, respectively). On the 3rd postoperative day, the differences between the two treatment groups were no longer present. CONCLUSIONS: In the early postoperative period after cataract surgery, the anti-inflammatory effect of a topical combination therapy with diclofenac and prednisolone is weaker than that of indomethacin and prednisolone. However, this difference is no longer observed on day 3 after surgery, so that there is probably no major difference in clinical outcome between the two treatment protocols.

Aged↗

PubMed2005

Phase solubility and structure of the inclusion complexes of prednisolone and 6 alpha-methyl prednisolone with various cyclodextrins.

The purpose of this work was to study the inclusion binding interaction of two structurally related steroids, prednisolone and 6alpha-methyl prednisolone with a wide variety of cyclodextrins (CDs), both native (alpha-, beta- and gamma-CD) as well as modified (hydroxypropyl-, sulfobutyl ether-, glucosyl-, and maltosyl-beta-CD and sulfobutyl ether-gamma-CD), and to relate the binding constants to structural differences in the steroids. Phase-solubility diagrams of the steroids with various CDs were obtained. The stability constants (K1:1) revealed that beta-CD formed the strongest complex with prednisolone, followed by gamma-CD. With 6alpha-methyl prednisolone, the stability constants of both beta- and alpha-CD were considerably lower compared with prednisolone. In contrast, gamma-CD formed a stronger complex with 6alpha-methyl prednisolone compared with prednisolone. Derivatives of beta-CD gave slightly altered stability constants compared with native beta-CD. The structures of the complexes between the two guest molecules and native beta-CD were studied by nuclear magnetic resonance spectroscopy. This clearly showed that the introduction of the methyl group led to a different binding geometry of 6alpha-methyl prednisolone compared with prednisolone. Additionally, the nuclear magnetic resonance results indicate the presence of an additional, weaker binding site, which is less populated in prednisolone.

Cyclodextrins↗

PubMed1991

Prednisolone concentrations in cerebrospinal fluid after different prednisolone prodrugs.

The concentration-time curves of prednisolone in cerebrospinal fluid (CSF) and plasma were measured following an equimolar i.v. bolus dose of prednisolone phosphate (five patients) and prednisolone phthalate (four patients). Independent of the prodrug administered, the value of the AUC (0.360 min) in CSF was more than three times lower than the corresponding value in plasma. The AUCs of unbound prednisolone in plasma were higher after prednisolone phosphate, than after prednisolone phthalate (68.1 +/- 15.7 vs 19.0 +/- 5.2 micrograms ml-1 min, P less than 0.001). Similarly, the AUCs of prednisolone were higher in the CSF after prednisolone phosphate, than after prednisolone phthalate (17.6 +/- 2.8 vs 3.3 +/- 1.0 micrograms ml-1 min, P less than 0.0001). The results indicate that the concentrations of prednisolone in CSF are much lower than the unbound concentrations in plasma and that therapeutic inequivalence should be expected when the two prodrugs are given in equimolar doses.

Aged↗

PubMed2005

Comparative study of prednisolone alone and prednisolone plus fusidic acid in the treatment of children with steroid-responsive nephrotic syndrome.

BACKGROUND: There are several reports in the literature indicating that fusidic acid owns functions similar to those of cyclosporin. As cyclosporin has effectively been used in frequently relapsing steroid-responsive nephrotic syndrome we carried out this study to determine whether fusidic acid used along with prednisolone diminishes rate of steroid-responsive nephrotic syndrome relapses in children. PATIENTS AND METHODS: The patients were randomly allocated to receive either prednisolone alone or prednisolone plus fusidic acid for two months in standard doses. In the cases of relapses the treatment was changed to the comparative treatment method. Altogether 18 children (12 boys and 6 girls) aged 1.3 to 13.2 years entered the study. Thirteen of them were treated by either method on different occasions, four patients were treated with prednisolone only, and one child was treated with prednisolone plus fusidic acid only. Thus, there were 17 evaluable treatment courses with prednisolone alone and 14 courses with prednisolone plus fusidic acid. The patients were followed-up as long as the remission lasted. RESULTS: There was prompt and complete response under the influence of both treatment methods. However, relapses occurred in all the patients irrespective of the mode of treatment. Mean duration of remissions did not differ significantly between the study groups (17.8+/-20.4 weeks in the prednisolone group and 18.3+/-23.9 weeks in the prednisolone plus fusidic acid group; p>0.05). There were no statistically significant differences in laboratory parameters reflecting therapeutic efficacy in the comparative treatment groups, too. CONCLUSION: Thus, it was not revealed any remission-sustaining efficacy of fusidic acid used in standard doses for two months along with prednisolone in children with frequently relapsing steroid-responsive nephrotic syndrome.

Adolescent↗

PubMed1985

Prednisolone succinate and prednisolone acetate in cattle: pharmacokinetics and action on the adrenal gland.

The pharmacokinetics of prednisolone were studied in a group of 6 cows given prednisolone 21-sodium succinate IV and IM (600 micrograms/kg of body weight expressed as prednisolone alcohol) and prednisolone acetate IM (600 micrograms/kg of body weight expressed as prednisolone alcohol). After IV administration of prednisolone 21-sodium succinate, the half-life of elimination was 3.6 +/- 1.177 hours. After IM administration of prednisolone 21-sodium succinate, absorption was rapid and complete. After IM administration of prednisolone acetate, absorption was very slow with an absorption half-life of 48 hours, but was still complete. Basal plasma hydrocortisone was about 7.5 ng/ml. After IV and IM administration of prednisolone 21-sodium succinate, plasma hydrocortisone returned to normal values within 48 hours. In contrast, after IM administration of prednisolone acetate, a long adrenal suppression lasting from 4 to 6 weeks was observed.

Adrenal Glands↗

PubMed1980

Separation of serum prednisolone and prednisolone-21-hemisuccinate by extraction and their concurrent determination by radioimmunoassay.

We describe a simple, sensitive, and reliable radioimmunoassay for prednisolone and prednisolone-21-hemisuccinate in serum. The antiserum produced in rabbits to prednisolone-21-hemisuccinate/bovine serum albumin was specific for prednisolone and prednisolone-21-hemisuccinate. A simple dichloromethane extraction permitted the separation of prednisolone from prednisolone-21-hemisuccinate in the serum samples. Interference by cortisol, although not insignificant, is minimized in this assay. We used the method to measure prednisolone and prednisolone-21-hemisuccinate concentrations after a bolus injection of prednisolone-21-hemisuccinate into human beings and mice.

Animals↗

PubMed1987

[Pharmacokinetics and pharmacodynamics of prednisolone following extremely high dosage as prednisolone hemisuccinate].

Plasma levels of prednisolone and prednisolone hemisuccinate of volunteers were measured with HPLC following i.v. injections of 1200 and 75 mg of prednisolone, given as the water-soluble hemisuccinate ester. The hemisuccinate ester is hydrolyzed relatively quickly with a plasma half-life between 18 and 25 min, and the resulting prednisolone has a plasma half-life of 3.5-3.7 h. The dose dependency of the pharmacokinetic parameters indicates a partial saturation of the metabolizing enzymes as consequence of the application of the high dose of prednisolone. In saliva no hemisuccinate could be detected. The prednisolone saliva concentration corresponds with those of non-protein-bound prednisolone in plasma measured at the same time. Only minor quantities of intact ester (1-8%) or intact prednisolone (2-4%) are excreted in urine. Following the application of 1200 mg prednisolone the endogenous cortisol level is partially suppressed only 24 h after the i.v. injection; 48 h later the difference from the basis value is not statistically significant. Leukocytosis and granulocytosis are at maximum 24 h after the injection of the high dose, and after 48 h normal values are observed. Lymphocytes and monocytes fall below normal levels for a longer time after 1200 mg compared to 75 mg, the minimum is between 4 and 8 h. Glucose levels are enhanced dose-dependently. They are normalized even after the extremely high dose at 24 h. Sodium, potassium, calcium, plasma proteins, urea, creatinine, hematocrit and hemoglobin showed no significant differences within 48 h following the injections.

Adult↗

PubMed2001

[Permeability of the round window membrane for prednisolone-21-hydrogen succinate. Prednisolone content of the perilymph after local administration vs. systemic injection].

BACKGROUND AND OBJECTIVE: Prednisolone is the drug of first choice for the treatment of cochleovestibular disorders, such as sudden hearing loss. Because of the known side effects, the efficient drug levels to be achieved within inner ear fluids are limited by intravenous administration. The aim of the study was to determine the concentration in the perilymph of prednisolone-21-hydrogen succinate applied into the round window niche in comparison to the concentration after intraperitoneal application. METHODS: Application of prednisolone-21-hydrogen succinate (5 mg in 0.1 ml) on the round window membrane was performed after sedation under microscopic view directly into the round window niche of the guinea pig. In order to compare the results, perilymph samples after systemic application of 60 mg/kg body weight prednisolone were used. The time between application and taking specimens of perilymph from the cochlea varied. Specimens of perilymph were obtained after 15, 20, 80, 180, 330, and 960 min (10 specimens in each group, n = 60) by dissecting the cochlea and opening the apex cochleae. Levels of prednisolone-21-hydrogen succinate in perilymph were measured by isocratic high-pressure liquid chromatography (HPLC). RESULTS: The highest levels of prednisolone-21-hydrogen succinate were found after 180 min: 952.3 mg/l (95% confidence interval: 382.7). After 960 min the level was 18.72 mg/l (95% confidence interval: 16.9). In the group with systemic application, the levels measured were below 14.71 mg/l (95% confidence interval: 7.05). CONCLUSION: The results demonstrate that high levels of prednisolone-21-hydrogen succinate in perilymph are achievable by local application of a single dose into the round window niche. After application of 5 mg, the levels of prednisolone are measurable up to 16 h.

Administration, Topical↗

PubMed2000

21-NO-prednisolone is a novel nitric oxide-releasing derivative of prednisolone with enhanced anti-inflammatory properties.

1. Anti-inflammatory effects of a novel derivative of the glucocorticoid prednisolone were investigated. NCX-1015 (prednisolone 21-[(4'-nitrooxymethyl)benzoate]) incubation in human platelet-rich plasma produced a time (0 - 60 min) and concentration (3 - 300 microM) dependent release of nitrite, that was mirrored by accumulation of cyclic guanosine monophosphate in the human platelets. Intraperitoneal injection of NCX-1015 to mice (up to 27.7 micromol kg(-1)) produced nitrite accumulation in the peritoneal cavity maximal at 60 min. 2. NCX-1015 dose-dependently induced the steroid sensitive cell surface marker CD163 in human peripheral blood mononuclear cells (PBMCs). NCX-1015 was more potent than prednisolone in inducing CD163. Similarly, lipopolysaccharide induced interleukin-1 beta release from these cells was inhibited by NCX-1015 with higher potency than prednisolone. 3. In the zymosan peritonitis model, NCX-1015 was more active than prednisolone in suppressing neutrophil extravasation (ED(50) of 5.5 and 25.8 micromol kg(-1), respectively), nitrite accumulation (ED(50) of 1.38 and 22.2 micromol kg(-1), respectively) and release of the chemokine KC (ED(50) of 5.5 and 27.7 micromol kg(-1), respectively) as determined at the 4 h time-point. No differences were measured for the levels of interleukin-1 beta or prostaglandin E(2). NCX-1015 administered orally was also found to be equally active. Co-administration of the nitric oxide donors NOC-18 ((z)-1-[(2-aminoethyl)-N-(2-aminoethyl)amino] diazen-1-ium-1, 2-diolate; 7.9 micromol kg(-1)) or sodium nitroprusside (13.8 micromol kg(-1)) with prednisolone resulted in an additive anti-migratory action. 4. In a chronic model of granulomatous tissue inflammation, administration of NCX-1015 (13.9 micromol kg(-1)) from day 1 (i.e. after induction of inflammation) was more effective than prednisolone in reducing the granuloma dry weight, and this was associated to a lower anti-angiogenic effect. 5. In conclusion we show that NCX-1015 is more potent than prednisolone in controlling several, though not all, parameters of acute and chronic inflammation, and propose that this effect may be due to a co-operation between the steroid moiety and nitric oxide or related species released in biological fluids. Whereas this aspect needs to be further clarified, we propose NCX-1015 as the first member of a novel class of anti-inflammatory compounds, the nitro-steroids.

Administration, Oral↗

PubMed1988

Comparison of three immunosuppressive regimens in cadaver renal transplantation: long-term cyclosporine, short-term cyclosporine followed by azathioprine and prednisolone, and azathioprine and prednisolone without cyclosporine.

We conducted a randomized trial in seven Australian hospitals of the efficacy and safety of three immunosuppressive regimens after first transplantation of a cadaver kidney: long-term cyclosporine, short-term (three months) cyclosporine followed by azathioprine and prednisolone, and azathioprine and prednisolone without cyclosporine. Patients assigned to long-term cyclosporine (n = 138) or short-term cyclosporine followed by azathioprine and prednisolone (n = 141) had similar actuarial 12-month survival (98.4 vs. 96.4 percent) and graft survival (83.9 vs. 82.1 percent). Patients assigned to receive only azathioprine and prednisolone (n = 138), with optional use of antithymocyte globulin, had a significantly poorer survival rate (91.3 percent, P = 0.015) because of deaths from cardiac causes and infection, but their graft survival of 76.0 percent (P = 0.31) did not differ significantly from that of either group receiving cyclosporine. After the switch from cyclosporine to azathioprine and prednisolone, 15 percent of patients had reversible rejection episodes, but the frequency of rejection and graft loss did not differ from that in the long-term cyclosporine group. After the change to azathioprine and prednisolone, serum creatinine levels declined in nearly all patients, so that after three months they were comparable to those in the group receiving azathioprine and prednisolone only, and significantly lower than those in the group receiving long-term cyclosporine therapy (P less than 0.003). We conclude that the two cyclosporine regimens result in comparable patient and graft survival, but that changing to azathioprine and prednisolone at three months improves graft function.

Adult↗

PubMed2004

The distinct alterations produced in cardiovascular functions by prednisolone and nitro-prednisolone (NCX-1015) in the rat highlight a causal role for endothelin-1.

Daily administration of prednisolone, but not the derivative NCX-1015 (or prednisolone 21-[4'-nitrooxymethyl]benzoate), to rats resulted in a time- and dose-dependent increase in mean arterial blood pressure (MABP), significant after 1 week for the dose of 6.9 micromol/kg i.p. (n = 10; P < 0.05), and 3 weeks for the lower dose of 1.38 micromol/kg. A similar dichotomy of behavior was observed with respect to myocardial contractility and renal vascular resistance, in either case augmented by 3-week treatment with prednisolone but not NCX-1015. In contrast, both NCX-1015 and prednisolone reduced plasma levels of corticosterone in a dose- (dose range of 0.69-6.9 micromol/kg i.p.) and time-dependent (1-3 weeks) manner. Similar profiles were obtained for plasma nitrate values, although they were increased selectively after NCX-1015 administration. In contrast, prednisolone, but not NCX-1015, augmented plasma endothelin 1 (ET-1) with a profile that mirrored the changes observed in MABP and renal blood flow. Supply in the drinking water of the ET-1 receptor type A (ETA) antagonist FR139317 [(R-2-[(R)-2-[(S)-2-[[1-(hexahydro-1H-azepinyl)]-carbonyl]amino-4-methylpentanoyl]-amino-3-(2-pyridil)propionic] or mixed ETA/B, but not of selective ETB, antagonists prevented the changes produced by a 21-day treatment with prednisolone. In conclusion, this study indicates 1) a lack of occurrence of cardiovascular alterations by nitro-releasing derivative of prednisolone (NCX-1015), and 2) a functional link between prednisolone effects and the endogenous endothelin-1 system.

Animals↗

PubMed1986

Measurements of prednisolone and some of its metabolites, in urine of patients after orthotopic liver transplantation, as a means of monitoring prednisolone absorption.

In patients who had undergone orthotopic liver transplantation, malabsorption of prednisolone or increased metabolism of prednisolone was suspected. In order to rule out this possibility, urinary prednisolone, and some of its metabolites, viz prednisone and 6 beta-hydroxyprednisolone, were determined by means of a gas chromatographic assay. To evaluate this assay aliquots of a pooled urine from several of our patients were analysed in multiplicate (n = 10). Mean prednisone, prednisolone and 6 beta-hydroxyprednisolone concentrations of 1.9 mg/l, 6.3 mg/l and 4.1 mg/l, respectively, were found with the following respective day-to-day coefficients of variation: 12.3%, 5.2% and 5.3%. Amounts of prednisolone metabolites excreted in the urine of these patients were correlated with the ingested daily dose of prednisolone. It was concluded that overall absorption of prednisolone in these patients was adequate and not influenced by shortage of bile acids in the gastro-intestinal tract, or by steatorrhoea, both caused by external bile drainage. In addition there was no evidence for increased metabolism of prednisolone.

Adolescent↗

PubMed1993

Azathioprine combined with prednisolone or monotherapy with prednisolone in active Crohn's disease.

BACKGROUND: The role of azathioprine (AZA) in the treatment of active Crohn's disease (CD) is still controversial. This study examined whether AZA combined with standard prednisolone therapy improved the therapeutic outcome compared with monotherapy with prednisolone. METHODS: Forty-two patients with a Crohn's Disease Activity Index (CDAI) of > 150 were randomized into two groups. Both received 60 mg of prednisolone daily in a tapering regimen to a maintenance dose of 10 mg. In addition, group 1 received 2.5 mg AZA/kg body wt and group 2 received a placebo over the whole study period of 4 months. RESULTS: At the end of the trial, 16 of 21 patients (76%) in group 1 were in remission (CDAI < 150), compared with 8 of 21 (38%) in group 2 (P = 0.03). The CDAI in group 1 dropped from 290 +/- 97 (SD) to 72 +/- 84 and from 285 +/- 110 to 155 +/- 105 in group 2. The differences between activity indices in groups 1 and 2 became statistically significant after 8 weeks. The average prednisolone dose per day was 20.9 mg in group 1 and 26.7 mg in group 2 (P = 0.02). No major side effects were observed in this study. CONCLUSION: The combination of prednisolone and AZA was superior to the treatment with prednisolone alone in active CD. Patients receiving AZA showed remission more frequently, more quickly, and with lower doses of prednisolone.

Adolescent↗

PubMed1991

Comparative corneal penetration of prednisolone sodium phosphate and prednisolone acetate in NZW rabbits.

Comparative corneal penetration studies in the literature with prednisolone sodium phosphate solution and prednisolone acetate suspension administered to rabbit eyes give conflicting results concerning the greater bioavailability of prednisolone acetate. A recent in vitro penetration study shows similar fluxes for both salt forms in terms of prednisolone, quantified by a specific HPLC assay. An in vivo comparison has been conducted in NZW rabbit eyes and shows similar bioavailability for both drugs. Prednisolone sodium phosphate, prednisolone acetate and the primary metabolite prednisolone are quantified by a specific HPLC assay in aqueous humor.

Animals↗