Prednisolone is a corticosteroid, a steroid hormone used to treat certain types of allergies, inflammatory conditions, autoimmune disorders, and cancers, electrolyte imbalances and skin conditions. Some of these conditions include adrenocortical insufficiency, high blood calcium, rheumatoid arthritis, dermatitis, eye inflammation, asthma, multiple sclerosis, and phimosis. It can be taken by mouth, injected into a vein, used topically as a skin cream, or as eye drops. It differs from the similarly named prednisone in having a hydroxyl at the 11th carbon instead of a ketone.
Common side effects with short-term use include nausea, difficulty concentrating, insomnia, increased appetite, and fatigue. More severe side effects include psychiatric problems, which may occur in about 5% of people. Common side effects with long-term use include bone loss, weakness, yeast infections, and easy bruising. While short-term use in the later part of pregnancy is safe, long-term use or use in early pregnancy is occasionally associated with harm to the baby. It is a glucocorticoid made from hydrocortisone (cortisol).
Prednisolone was discovered and approved for medical use in 1955. It is on the World Health Organization's List of Essential Medicines. It is available as a generic drug. In 2022, it was the 136th most commonly prescribed medication in the United States, with more than 4 million prescriptions.
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environmental contaminant
Any minor or unwanted substance introduced into the environment that can have undesired effects.
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adrenergic agent
Any agent that acts on an adrenergic receptor or affects the life cycle of an adrenergic transmitter.
immunosuppressive agent
An agent that suppresses immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-cells or by inhibiting the activation of helper cells. In addition, an immunosuppressive agent is a role played by a compound which is exhibited by a capability to diminish the extent and/or voracity of an immune response.
drug metabolite
xenobiotic
A xenobiotic (Greek, xenos "foreign"; bios "life") is a compound that is foreign to a living organism. Principal xenobiotics include: drugs, carcinogens and various compounds that have been introduced into the environment by artificial means.
hormone
Originally referring to an endogenous compound that is formed in specialized organ or group of cells and carried to another organ or group of cells, in the same organism, upon which it has a specific regulatory function, the term is now commonly used to include non-endogenous, semi-synthetic and fully synthetic analogues of such compounds.
(via steroid hormone )
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adrenergic agent
Any agent that acts on an adrenergic receptor or affects the life cycle of an adrenergic transmitter.
anti-inflammatory drug
A substance that reduces or suppresses inflammation.
antineoplastic agent
A substance that inhibits or prevents the proliferation of neoplasms.
immunosuppressive agent
An agent that suppresses immune function by one of several mechanisms of action. Classical cytotoxic immunosuppressants act by inhibiting DNA synthesis. Others may act through activation of T-cells or by inhibiting the activation of helper cells. In addition, an immunosuppressive agent is a role played by a compound which is exhibited by a capability to diminish the extent and/or voracity of an immune response.
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View more via ChEBI Ontology
11β,17,21-trihydroxypregna-1,4-diene-3,20-dione
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prednisolona
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ChemIDplus
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prednisolone
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ChemIDplus
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prednisolone
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WHO MedNet
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prednisolonum
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(11β)-11,17,21-trihydroxypregna-1,4-diene-3,20-dione
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ChEBI
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1,4-pregnadiene-11β,17α,21-triol-3,20-dione
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ChemIDplus
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1,4-pregnadiene-3,20-dione-11β,17α,21-triol
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ChemIDplus
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3,20-dioxo-11β,17α,21-trihydroxy-1,4-pregnadiene
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Δ1-dehydrocortisol
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Δ1-dehydrohydrocortisone
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Δ1-hydrocortisone
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hydroretrocortine
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ChemIDplus
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metacortandralone
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1354103
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Reaxys Registry Number
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Reaxys
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50-24-8
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CAS Registry Number
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KEGG COMPOUND
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50-24-8
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CAS Registry Number
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Haibel H, Fendler C, Listing J, Callhoff J, Braun J, Sieper J (2014) Efficacy of oral prednisolone in active ankylosing spondylitis: results of a double-blind, randomised, placebo-controlled short-term trial. Annals of the rheumatic diseases 73, 243-246 [PubMed:23625982] [show Abstract]
BackgroundThe efficacy of oral prednisolone in patients with active ankylosing spondylitis (AS) has not been studied to date.MethodsIn this double-blind, randomised, placebo-controlled trial, patients with AS with active disease despite taking non-steroidal antirheumatic drugs were randomised to three groups in which they were either treated with 20 mg (n=13) or 50 mg (n=12) of prednisolone, or placebo (n=14), administered orally every day for a total of 2 weeks. The primary endpoint was defined as a 50% improvement of the Bath AS Disease Activity Index (BASDAI) at week 2.ResultsThe primary endpoint was reached in 33% and 27% of the patients treated with 50 and 20 mg of prednisolone, respectively, versus only 8% on placebo (p=0.16 and p=0.30). However, the mean improvement of BASDAI score was significantly higher in the 50 mg prednisolone compared to the placebo group (2.39±0.5 vs 0.66±0.49, p=0.03), while there was only a small change in the 20 mg group (1.19±0.53; p=0.41). The results for other outcome parameters were similar.ConclusionsOral prednisolone 50 mg per day, but not low dose prednisolone, showed a short-term response that was significantly higher than placebo. The clinical significance and the duration of this effect warrant further study. | de Rijke E, Zoontjes PW, Samson D, Oostra S, Sterk SS, van Ginkel LA (2014) Investigation of the presence of prednisolone in bovine urine. Food additives & contaminants. Part A, Chemistry, analysis, control, exposure & risk assessment 31, 605-613 [PubMed:24392764] [show Abstract] Over the past two years low levels of prednisolone have been reported in bovine urine by a number of laboratories in European Union member states. Concentrations vary, but are reported to be below approximately 3 µg l(-1). Forty per cent of bovine urine samples from the Dutch national control plan had concentrations of prednisolone between 0.11 and 2.04 µg l(-1). In this study the mechanism of formation of prednisolone was investigated. In vitro conversion of cortisol by bacteria from faeces and soil, bovine liver enzymes and stability at elevated temperatures were studied. In vitro bovine liver S9 incubation experiments showed a significant 20% decrease of cortisol within 6 h, and formation of prednisolone was observed from 0.2 g l(-1) at t = 0 to 0.5 g l(-1) at t = 6. Under the influence of faeces, the stability of cortisol in urine is reduced and cortisol breaks down within 50 h. Prednisolone is formed up to 4 µg l(-1) at 70°C after 15 h. However, this decreases again to zero after 50 h. With soil bacteria, a slower decrease of cortisol was observed, but slightly higher overall formation of prednisolone, up to 7 µg l(-1) at 20°C. As opposed to incurred urine, in fortified urine incubated with faeces or soil bacteria no prednisolone was detected. This difference may be explained by the presence of natural corticosteroids in the incurred sample. With UPLC-QToF-MS experiments, in urine and water samples incubated with faeces, metabolites known from the literature could be (tentatively) identified as 20β-hydroxy-prednisolone, cortisol-21-sulfate, oxydianiline, tetrahydrocortisone-3-glucuronide and cortexolone, but for all compounds except 20β-hydroxy-prednisolone no standards were available for confirmation. Based on the results of this study and literature data, for regulatory purposes a threshold of 5 µg l(-1) for prednisolone in bovine urine is proposed. Findings of prednisolone in concentrations up to 5 µg l(-1) in bovine urine can, most likely, originate from other sources than illegal treatment with growth promoters. | Majid O, Akhlaghi F, Lee T, Holt DW, Trull A (2001) Simultaneous determination of plasma prednisolone, prednisone, and cortisol levels by high-performance liquid chromatography. Therapeutic drug monitoring 23, 163-168 [PubMed:11294518] [show Abstract] Recipients of organ transplants remain particularly dependent on prednisolone as part of their maintenance immunosuppression. Despite this, the pharmacokinetics of prednisolone have never been fully characterized in these patients, and consequently dosing remains empirical. Accurate monitoring of prednisolone, its primary metabolite prednisone, and endogenous cortisol suppression in such patients may provide a means of improving the clinical outcome by adjusting for variability in prednisolone pharmacokinetics and pharmacodynamics. Measurement of endogenous cortisol may provide an independent marker of prednisolone pharmacodynamics. A simple isocratic reverse-phase high-performance liquid chromatography procedure, using betamethasone as an internal standard, was developed to quantify plasma prednisolone, prednisone, and cortisol simultaneously. The steroids were extracted from 0.5 mL plasma with 3 mL (1:1 v/v) ethyl acetate/tert-methyl butyl ether and 0.1 mL phosphoric acid, washed in 0.1 mol/L NaOH before a final drying step and reconstitution in mobile phase for injection. Separation was achieved using a Supelcosil LC-18-DB, 150 x 4.6-mm, 5-microm particle size, reverse-phase column attached to a Newguard 15 x 3-mm, RP8 guard column maintained at 25 degreesC, with ultraviolet detector set at 254 nm. The mobile phase consisted of 16% isopropanol in water containing 0.1% trifluoroacetic acid, set at a flow rate of 1.2 mL/min. The assay was linear up to 1,002 microg/L for prednisolone, 982 microg/L for prednisone, and 545 microg/L for cortisol. Mean intra-assay and interassay imprecision levels were 6.0% and 7.2%, respectively, for prednisolone, 5.8% and 7.2% for prednisone, and 5.6% and 7.9% for cortisol. Intra-assay inaccuracy was <7% of nominal values for prednisolone, prednisone, and cortisol. The lower limit of quantification was 7 microg/L for prednisolone and prednisone and 10 microg/L for cortisol. Corticosteroid recoveries were 73%, 74%, and 90% for prednisolone, prednisone, and cortisol, respectively. The authors describe a robust, inexpensive, and simple method suitable for therapeutic drug monitoring or pharmacokinetic studies of prednisolone; it may also be used to measure the suppression of endogenous cortisol production. |
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