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American Journal of Veterinary Research Feb 1985Tritium-labeled prednisolone sodium succinate was administered IV to 4 healthy, awake, nonsplenectomized dogs. The concentration of prednisolone and its metabolites in...
Tritium-labeled prednisolone sodium succinate was administered IV to 4 healthy, awake, nonsplenectomized dogs. The concentration of prednisolone and its metabolites in the plasma were measured for 10 hours. Forty-one percent of the blood volume of these dogs was removed, and plasma prednisolone was measured again. The data before and after hemorrhage were fitted to a 2-compartment open model. From plasma profiles, a rapid distributional phase, followed by a slower phase, was observed in control and shock groups. Volume of the central compartment of prednisolone before and after hemorrhage was 165 ml/kg of body weight and 110 ml/kg, respectively; and the difference was significant (P less than 0.05). The rate of total body clearance of prednisolone before and after hemorrhage was 3.96 ml/min/kg and 2.53 ml/min/kg, respectively; the difference was significant. The mean plasma half-lives for prednisolone sodium succinate and its metabolites, before and after hemorrhage, were 166 and 197 minutes, respectively; the difference was not significant. The mean half-life data indicated that prednisolone sodium succinate may be repeated in a patient 2.5 to 3 hours after onset of treatment if signs of hypovolemic shock reappear.
Topics: Animals; Dog Diseases; Dogs; Female; Injections, Intravenous; Male; Prednisolone; Shock
PubMed: 3994116
DOI: No ID Found -
Postgraduate Medical Journal Jun 1979Malabsorption of prednisolone administered as enteric coated tablets was suspected following therapeutic failure in an asthmatic. This was investigated by cortisol...
Malabsorption of prednisolone administered as enteric coated tablets was suspected following therapeutic failure in an asthmatic. This was investigated by cortisol estimation and a Synacthen test and substantiated by the demonstration of abnormally low absorption of prednisolone from these tablets which nevertheless were normally absorbed by a volunteer. The absorption of prednisolone from conventional tablets in this patient was normal.
Topics: Asthma; Female; Humans; Intestinal Absorption; Middle Aged; Prednisolone; Tablets, Enteric-Coated
PubMed: 482191
DOI: 10.1136/pgmj.55.644.421 -
Journal of the American Veterinary... Mar 2012To compare the effects of 2 preoperative anti-inflammatory regimens on intraocular inflammation following phacoemulsification. (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVE
To compare the effects of 2 preoperative anti-inflammatory regimens on intraocular inflammation following phacoemulsification.
DESIGN
Randomized controlled trial
ANIMALS
21 dogs with immature cataracts.
PROCEDURES
All dogs had cataract surgery via phacoemulsification, and most received prosthetic intraocular lenses. Dogs were randomly divided into 2 groups. Group A dogs were treated topically with prednisolone acetate for 7 days prior to surgery, whereas prednisolone acetate treatment commenced the evening prior to surgery in group B dogs. Postoperative care was identical for both groups. Blood-aqueous barrier breakdown was quantified by use of anterior chamber fluorophotometry, with fluorescein entry into the anterior chamber measured 2 and 9 days after surgery compared with baseline scans obtained prior to surgery. Ophthalmic examinations were performed before surgery and 1 day, 9 days, 3 weeks, 7 weeks, 3 months, and 6 months after surgery. A subjective inflammation score was established at each examination. Intraocular pressures were measured 4 and 8 hours after surgery and at each follow-up examination.
RESULTS
There was no difference in the extent of blood-aqueous barrier disruption between the groups at 2 or 9 days after surgery. Subjective inflammation scores were also similar at most time points. Dogs in group A developed postoperative ocular hypertension at a higher frequency (60%) than did those in group B (18%).
CONCLUSIONS AND CLINICAL RELEVANCE
In dogs that underwent cataract surgery via phacoemulsification, a full week of topical prednisolone acetate treatment prior to surgery did not decrease postoperative inflammation, compared with commencement of topical prednisolone acetate treatment the evening prior to surgery, and was associated with a greater incidence of postoperative ocular hypertension.
Topics: Administration, Topical; Animals; Anti-Inflammatory Agents; Cataract; Dog Diseases; Dogs; Drug Administration Schedule; Female; Male; Ocular Hypertension; Phacoemulsification; Prednisolone
PubMed: 22332625
DOI: 10.2460/javma.240.5.563 -
Der Nervenarzt Dec 1998Tics-disorders are hyperkinetic movement disorders which manifest in childhood or early adolescence and ameliorate in later adulthood. We report on two patients with a...
Tics-disorders are hyperkinetic movement disorders which manifest in childhood or early adolescence and ameliorate in later adulthood. We report on two patients with a basically subclinical tic-disorder (age of 53 and 68 years). During the therapy of polymyalgia rheumatica and endocrine orbitopathy in Graves disease with prednisolone the tics exacerbated and were therefore diagnosed and treated for the first time. Possible causes for the exacerbation of the tics during the therapy with glucocorticosteroids are discussed in the context of the dopamine hypothesis of tics.
Topics: Aged; Akathisia, Drug-Induced; Anti-Inflammatory Agents; Dose-Response Relationship, Drug; Female; Graves Disease; Humans; Middle Aged; Polymyalgia Rheumatica; Prednisolone; Tic Disorders; Tourette Syndrome
PubMed: 9888149
DOI: 10.1007/s001150050390 -
The Journal of Rheumatology Feb 1988Methylprednisolone pulse therapy is often used in patients with severe rheumatoid arthritis (RA). To compare clinical and pharmacokinetic variables of methylprednisolone... (Comparative Study)
Comparative Study
Methylprednisolone pulse therapy is often used in patients with severe rheumatoid arthritis (RA). To compare clinical and pharmacokinetic variables of methylprednisolone and oral prednisolone in patients with RA, a controlled crossover study was carried out. Pharmacokinetic variables for methylprednisolone were Vd of 69.9 l, t1/2 of 2.96 h, total plasma clearance of 17.5 l/h. Pharmacokinetic variables for prednisolone were Vd of 47.5 l, t1/2 of 3.08 h and total plasma clearance of 11.3 l/h. During the elimination phase, a secondary rise in methylprednisolone concentration occurred which may be related to enterohepatic circulation. Clinical response to both prednisolone and methylprednisolone was short-lived with neither lasting more than 6 weeks.
Topics: Arthritis, Rheumatoid; Female; Humans; Male; Methylprednisolone; Osmolar Concentration; Prednisolone; Time Factors
PubMed: 3361533
DOI: No ID Found -
Wiener Klinische Wochenschrift Apr 1987The influence of high-dose prednisolone on extravascular lung water (EVLW) was studied in a randomized trial in patients with noncardiac pulmonary edema. The patients... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
The influence of high-dose prednisolone on extravascular lung water (EVLW) was studied in a randomized trial in patients with noncardiac pulmonary edema. The patients were treated every 6 hours for 48 hours with 2 g of prednisolone-hemisuccinate or placebo. In the prednisolone-group (n = 7) EVLW decreased from 16.4 +/- 6.2 before to 11.8 +/- 5.1 ml/kg after treatment (p less than 0.05). Additionally alveolar-arterial oxygen gradient (AaDO2/FiO2), pulmonary vascular resistance and heart rate decreased, while arterial oxygen tension (PaO2/FiO2) and mean arterial pressure increased (p less than 0.05). In the placebo-group (n = 7) EVLW increased slightly from 17.5 +/- 3.1 before to 19.3 +/- 10.3 ml/kg after treatment. Additionally all other parameters did not change significantly in this group. Although no statistical significant difference was found between the two groups of treatment, a decrease in EVLW was observed in all prednisolone-treated patients, whereas a pronounced increase in EVLW was found in 3 placebo-treated patients. Probably, those patients would have benefited from high-dose prednisolone treatment. High-dose prednisolone reduced EVLW and improved hemodynamics and gas exchange in patients with noncardiac pulmonary edema, whereas placebo did not achieve comparable effects. Therefore, high-dose prednisolone appears beneficial in noncardiac pulmonary edema in respect of EVLW, hemodynamics, and gas exchange.
Topics: Adult; Aged; Aged, 80 and over; Capillary Permeability; Dose-Response Relationship, Drug; Extracellular Space; Female; Hemodynamics; Humans; Male; Middle Aged; Prednisolone; Pulmonary Edema; Pulmonary Gas Exchange
PubMed: 3590805
DOI: No ID Found -
Revue Medicale Suisse Oct 2020Uveitis is an inflammation of the eye, resulting from infection or inflammation and is sometimes related to rheumatic and other auto-immune diseases. The condition is... (Review)
Review
Uveitis is an inflammation of the eye, resulting from infection or inflammation and is sometimes related to rheumatic and other auto-immune diseases. The condition is classified according to the anatomical site of inflammation: anterior, intermediate, posterior or panuveitis. Uveitis may result in a significant loss of visual acuity, that may however be avoided by controlling the inflammation. Anterior uveitis is the only form that responds to topical therapies (prednisolone acetate and mydriatics). The other forms of inflammatory and non-infectious uveitis often require treatment with systemic corticosteroids, followed by immunosuppressive or biological therapies, which requires close collaboration between the different medical sub-specialties.
Topics: Humans; Internal Medicine; Mydriatics; Prednisolone; Uveitis
PubMed: 33112521
DOI: No ID Found -
Journal of Enzyme Inhibition and... Dec 2016Drug target interactions (DTIs) are crucial in pharmacology and drug discovery. Presently, experimental determination of compound-protein interactions remains...
Drug target interactions (DTIs) are crucial in pharmacology and drug discovery. Presently, experimental determination of compound-protein interactions remains challenging because of funding investment and difficulties of purifying proteins. In this study, we proposed two in silico models based on support vector machine (SVM) and random forest (RF), using 1589 molecular descriptors and 1080 protein descriptors in 9948 ligand-protein pairs to predict DTIs that were quantified by Ki values. The cross-validation coefficient of determination of 0.6079 for SVM and 0.6267 for RF were obtained, respectively. In addition, the two-dimensional (2D) autocorrelation, topological charge indices and three-dimensional (3D)-MoRSE descriptors of compounds, the autocorrelation descriptors and the amphiphilic pseudo-amino acid composition of protein are found most important for Ki predictions. These models provide a new opportunity for the prediction of ligand-receptor interactions that will facilitate the target discovery and toxicity evaluation in drug development.
Topics: Ligands; Prednisolone; Protein Binding; Support Vector Machine
PubMed: 26888050
DOI: 10.3109/14756366.2016.1144594 -
Endocrinologia Japonica Jun 1990We investigated the pharmacokinetics of prednisolone (PSL) in six healthy men, with or without glycyrrhizin (GL), to confirm whether GL influences the metabolism of PSL...
We investigated the pharmacokinetics of prednisolone (PSL) in six healthy men, with or without glycyrrhizin (GL), to confirm whether GL influences the metabolism of PSL in humans. Each subject received an intravenous administration of 0.096 mg/kg of prednisolone hemisuccinate (PSL-HS, equivalent to 0.075 mg/kg of PSL), with or without 200 mg of GL. Blood samples were taken from a peripheral vein at 5, 10, 15, 30 and 45 min, and 1, 1.5, 2, 3, 4, 6, 8, 10, 12 and 24 h after PSL-HS infusion. The concentration of total PSL in the plasma was analyzed by high-performance liquid chromatography, and the free PSL was measured by an isocolloidosmolar equilibrium dialysis method. The pharmacokinetic parameters of PSL were determined, using noncompartmental analysis. GL was found to increase significantly the concentration of total PSL at 6, 8 h, and of free PSL at 4, 6, and 8 h after PSL-HS infusion. GL was also found to modify the pharmacokinetics of PSL. After the administration of GL, the area under the curve (AUC) increased, total plasma clearance (CL) decreased, and the mean residence time (MRT) was prolonged. However, only those of AUC, CL, and MRT of free PSL were significantly different. The volume of distribution at a steady-state (Vdss) of both total and free PSL showed no evident change. This suggests that GL increases the plasma PSL concentrations by inhibiting the metabolism of PSL and that it potentiates pharmacological effects of PSL.
Topics: Adult; Chromatography, High Pressure Liquid; Dialysis; Drug Interactions; Glycyrrhetinic Acid; Glycyrrhizic Acid; Humans; Male; Metabolic Clearance Rate; Prednisolone
PubMed: 2253583
DOI: 10.1507/endocrj1954.37.331 -
Steroids Dec 2013A six step transformation of prednisolone to 17α,21-dihydroxy-9β,11β-epoxy-16α-amethylpregna-1,4-diene-3,20-dione 21-acetate has been achieved in 13% unoptimised...
A six step transformation of prednisolone to 17α,21-dihydroxy-9β,11β-epoxy-16α-amethylpregna-1,4-diene-3,20-dione 21-acetate has been achieved in 13% unoptimised yield. Novel conditions for effecting a Mattox rearrangement and double dehydration of prednisolone were identified. Enhanced knowledge on the oxidation of silyl Δ(19,20)-enol ethers and structural factors that impact the success of the oxidation are also presented.
Topics: Glucocorticoids; Oxidation-Reduction; Prednisolone
PubMed: 24075969
DOI: 10.1016/j.steroids.2013.09.008