Revision as of 12:16, 16 February 2012 editBeetstra (talk | contribs)Edit filter managers, Administrators172,111 edits Saving copy of the {{drugbox}} taken from revid 477123740 of page Prednisolone for the Chem/Drugbox validation project (updated: 'DrugBank'). |
Latest revision as of 14:16, 12 January 2025 edit Arthurfragoso (talk | contribs)Extended confirmed users, Template editors4,591 edits dark mode fix |
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{{Short description|Corticosteroid medication}} |
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{{ambox | text = This page contains a copy of the infobox ({{tl|drugbox}}) taken from revid of page ] with values updated to verified values.}} |
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{{Distinguish|Prednisone}} |
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{{Drugbox |
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{{Use dmy dates|date=March 2020}} |
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{{Infobox drug |
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| Watchedfields = changed |
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| verifiedrevid = 464213513 |
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| verifiedrevid = 477172058 |
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| IUPAC_name = (11β)-11,17,21-trihydroxypregna-1,4-diene-3,20-dione |
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| image = Prednisolone-2D-skeletal.svg |
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| image = Prednisolone-2D-skeletal.svg |
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| image_class = skin-invert-image |
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| image2 = Prednisolone-3D-balls.png |
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| width = |
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| alt = |
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<!--Clinical data--> |
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| image2 = Prednisolone-from-xtal-3D-bs-17.png |
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| tradename = |
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| image_class2 = bg-transparent |
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| width2 = |
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| alt2 = |
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| caption = <!-- Clinical data --> |
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| pronounce = |
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| tradename = Orapred, PediaPred, Millipred, others |
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| Drugs.com = {{drugs.com|monograph|prednisolone}} |
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| Drugs.com = {{drugs.com|monograph|prednisolone}} |
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| MedlinePlus = a682794 |
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| MedlinePlus = a615042 |
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| DailyMedID = Prednisolone |
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| pregnancy_AU = A |
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| pregnancy_AU = A |
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| pregnancy_AU_comment = <ref name="Drugs.com pregnancy">{{cite web | title=Prednisolone Use During Pregnancy | website=Drugs | date=16 January 2000 | url=https://www.drugs.com/pregnancy/prednisolone.html | access-date=9 March 2020 | archive-date=21 December 2016 | archive-url=https://web.archive.org/web/20161221002545/https://www.drugs.com/pregnancy/prednisolone.html | url-status=live }}</ref> |
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| pregnancy_US = C |
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| pregnancy_category = |
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| routes_of_administration = ], ], ], ] |
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| class = ] |
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| ATCvet = |
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| ATC_prefix = A07 |
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| ATC_suffix = EA01 |
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| ATC_supplemental = {{ATC|A01|AC04}}, {{ATC|C05|AA04}}, {{ATC|D07|AA03}}, {{ATC|D07|XA02}}, {{ATC|H02|AB06}}, {{ATC |R01|AD02}}, {{ATC|S01|BA04}}, {{ATC|S01|CB02}}, {{ATC|S02|BA03}}, {{ATC|S03|BA02}}, {{ATC|D07|CA03}}, {{ATC|S01|CA02}}, {{ATC |S02|CA01}}, {{ATC|S03|CA02}}, {{ATC|D07|BA01}}, {{ATC|S01|BB02}}, {{ATC|V03|AB05}}, {{ATC|A01|AC54}}, {{ATC |R01|AD52}}, {{ATCvet|A01|AC04}} |
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<!-- Legal status -->| legal_AU = <!-- S2, S3, S4, S5, S6, S7, S8, S9 or Unscheduled--> |
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| legal_AU_comment = |
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| legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F--> |
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| legal_BR_comment = |
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| legal_CA = <!-- OTC, Rx-only, Schedule I, II, III, IV, V, VI, VII, VIII --> |
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| legal_CA_comment = |
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| legal_DE = <!-- Anlage I, II, III or Unscheduled--> |
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| legal_DE_comment = |
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| legal_NZ = <!-- Class A, B, C --> |
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| legal_NZ_comment = |
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| legal_UK = POM |
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| legal_UK = POM |
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| legal_UK_comment = |
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| legal_US = Rx-only |
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| legal_US = Rx-only |
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| legal_US_comment = |
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| legal_UN = <!-- N I, II, III, IV / P I, II, III, IV--> |
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| legal_UN_comment = |
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| legal_status = Rx-only |
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<!--Pharmacokinetic data--> |
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<!-- Pharmacokinetic data -->| bioavailability = |
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| protein_bound = |
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| elimination_half-life = 2-3 hours |
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| metabolism = |
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| excretion = Prednisolone is excreted via urine |
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| metabolites = |
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| onset = |
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| elimination_half-life = 2–3.5 hours<ref name="pmid378499">{{cite journal | vauthors = Pickup ME | title = Clinical pharmacokinetics of prednisone and prednisolone | journal = Clinical Pharmacokinetics | volume = 4 | issue = 2 | pages = 111–28 | date = 1979 | pmid = 378499 | doi = 10.2165/00003088-197904020-00004 | s2cid = 12218704 }}</ref><ref name= "pmid6861855">{{cite journal | vauthors = Bergrem H, Grøttum P, Rugstad HE | title = Pharmacokinetics and protein binding of prednisolone after oral and intravenous administration | journal = European Journal of Clinical Pharmacology | volume = 24 | issue = 3 | pages = 415–9 | date = 1983 | pmid = 6861855 | doi = 10.1007/BF00610064| s2cid = 33189235 }}</ref><ref name= "pmid30083083">{{cite journal | vauthors = Bashar T, Apu MN, Mostaid MS, Islam MS, Hasnat A | title = Pharmacokinetics and Bioavailability Study of a Prednisolone Tablet as a Single Oral Dose in Bangladeshi Healthy Volunteers | journal = Dose-response | volume = 16 | issue = 3 | date = 2018 | pmid = 30083083 | pmc = 6073839 | doi = 10.1177/1559325818783932}}</ref> |
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| duration_of_action = |
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| excretion = ] |
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<!--Identifiers--> |
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<!-- Identifiers -->| CAS_number_Ref = {{cascite|correct|??}} |
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| CASNo_Ref = {{cascite|correct|CAS}} |
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| CAS_number_Ref = {{cascite|correct|??}} |
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| CAS_number = 50-24-8 |
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| CAS_number = 50-24-8 |
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| ATC_prefix = A07 |
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| CAS_supplemental = |
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| ATC_suffix = EA01 |
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| ATC_supplemental = {{ATC|C05|AA04}}, {{ATC|D07|AA03}}, {{ATC|H02|AB06}}, {{ATC|R01|AD02}}, {{ATC|S01|BA04}}, {{ATC|S01|CB02}}, {{ATC|S02|BA03}}, {{ATC|S03|BA02}} |
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| PubChem = 5755 |
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| PubChem = 5755 |
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| IUPHAR_ligand = 2866 |
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| DrugBank_Ref = {{drugbankcite|changed|drugbank}} |
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| DrugBank_Ref = {{drugbankcite|correct|drugbank}} |
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| DrugBank = DB00860 |
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| DrugBank = DB00860 |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEMBL_Ref = {{ebicite|correct|EBI}} |
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| ChEMBL = 131 |
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| ChEMBL = 131 |
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| NIAID_ChemDB = |
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| PDB_ligand = |
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| synonyms = 11,17-Dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydrocyclopentaphenanthren-3-one |
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<!-- Chemical and physical data -->| IUPAC_name = (11β)-11,17,21-Trihydroxypregna-1,4-diene-3,20-dione |
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<!--Chemical data--> |
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| C=21 | H=28 | O=5 |
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| chemical_formula = |
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| C = 21 |
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| molecular_weight = 360.444 g/mol |
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| H = 28 |
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| smiles = O=C\1\C=C/4(/C(=C/1)CC24(O)C3((O)(C(=O)CO)CC23)C)C |
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| O = 5 |
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| InChI = 1/C21H28O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h5,7,9,14-16,18,22,24,26H,3-4,6,8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1 |
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| SMILES = O=C\1\C=C/4(/C(=C/1)CC24(O)C3((O)(C(=O)CO)CC23)C)C |
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| InChIKey = OIGNJSKKLXVSLS-VWUMJDOOBF |
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| Jmol = |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChI = 1S/C21H28O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h5,7,9,14-16,18,22,24,26H,3-4,6,8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1 |
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| StdInChI = 1S/C21H28O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h5,7,9,14-16,18,22,24,26H,3-4,6,8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1 |
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| StdInChI_comment = |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} |
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| StdInChIKey = OIGNJSKKLXVSLS-VWUMJDOOSA-N |
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| StdInChIKey = OIGNJSKKLXVSLS-VWUMJDOOSA-N |
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| density = |
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| synonyms = <small>11,17-dihydroxy-17- (2-hydroxyacetyl)- 10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17- dodecahydrocyclopenta phenanthren-3-one</small> |
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| density_notes = |
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}} |
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}} |
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<!-- Definition and medical uses --> |
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'''Prednisolone''' is a ], a ] used to treat certain types of ], ], ], and ]s, ] and skin conditions.<ref name="WHO2008">{{cite book | title = WHO Model Formulary 2008 | year = 2009 | isbn = 978-924154765-9 | veditors = Stuart MC, Kouimtzi M, Hill SR | hdl = 10665/44053 | publisher = World Health Organization |pages= 53–54 }}</ref><ref name="AHFS2016" /> Some of these conditions include ], ], ], ], eye inflammation, ], ], and ].<ref name=AHFS2016/> It can be taken ], ], used ] as a skin cream, or as ].<ref name="Orapred ODT label" /><ref name="Omnipred label" /><ref name=AHFS2016 /> It differs from the similarly named ] in having a ] at the 11th carbon instead of a ]. |
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<!-- Side effects and mechanism --> |
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Common side effects with short-term use include ], difficulty concentrating, ], ], and ].<ref name="WHO2008" /> More severe side effects include psychiatric problems, which may occur in about 5% of people.<ref name="ER2014">{{cite web|title=Pevanti 10mg Tablets – Summary of Product Characteristics (SPC) – (eMC)|url=https://www.medicines.org.uk/emc/medicine/30014 |date= 1 December 2014 |website= Medicines | place = ] |access-date=13 December 2016|url-status=live|archive-url= https://web.archive.org/web/20161220175357/https://www.medicines.org.uk/emc/medicine/30014 |archive-date=20 December 2016}}</ref> Common side effects with long-term use include ], ], ], and easy ].<ref name=AHFS2016/> While short-term use in the later part of ] is safe, long-term use or use in early pregnancy is occasionally associated with harm to the baby.<ref name="Drugs.com pregnancy" /> It is a ] made from ] (]).<ref name=Kim2016/> |
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<!-- History, society and culture --> |
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Prednisolone was discovered and approved for medical use in 1955.<ref name=Kim2016>{{cite book | vauthors = Kim KW, Roh JK, Wee HJ, Kim C |title=Cancer Drug Discovery: Science and History |date=2016 |publisher=Springer |isbn=978-940240844-7 |page= 169 |url=https://books.google.com/books?id=BR9_DQAAQBAJ&pg=PA169 |url-status=live|archive-url= https://web.archive.org/web/20170910174620/https://books.google.com/books?id=BR9_DQAAQBAJ&pg=PA169 |archive-date= 2017-09-10 }}</ref> It is on the ].<ref name="WHO23rd">{{cite book | vauthors = ((World Health Organization)) | title = The selection and use of essential medicines 2023: web annex A: World Health Organization model list of essential medicines: 23rd list (2023) | year = 2023 | hdl = 10665/371090 | author-link = World Health Organization | publisher = World Health Organization | location = Geneva | id = WHO/MHP/HPS/EML/2023.02 | hdl-access=free }}</ref> It is available as a ].<ref name=AHFS2016>{{cite web |title= Prednisolone |url=https://www.drugs.com/monograph/prednisolone.html |publisher= The American Society of Health-System Pharmacists |access-date=8 December 2016|url-status=live|archive-url=https://web.archive.org/web/20161223131831/https://www.drugs.com/monograph/prednisolone.html|archive-date= 23 December 2016}}</ref> In 2022, it was the 136th most commonly prescribed medication in the United States, with more than 4{{nbsp}}million prescriptions.<ref>{{cite web | title=The Top 300 of 2022 | url=https://clincalc.com/DrugStats/Top300Drugs.aspx | website=ClinCalc | access-date=30 August 2024 | archive-date=30 August 2024 | archive-url=https://web.archive.org/web/20240830202410/https://clincalc.com/DrugStats/Top300Drugs.aspx | url-status=live }}</ref><ref>{{cite web | title = Prednisolone Drug Usage Statistics, United States, 2013 - 2022 | website = ClinCalc | url = https://clincalc.com/DrugStats/Drugs/Prednisolone | access-date = 30 August 2024 }}</ref> |
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==Medical uses== |
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When used in low doses, ] serve as an ]. At higher doses, they are considered as ].<ref name=":6" /> Corticosteroids inhibit the ] response to a variety of inciting agents and, it is presumed, delay or slow healing.<ref>{{cite journal |vauthors=Schwiebert LM, Beck LA, Stellato C, Bickel CA, Bochner BS, Schleimer RP, Schwiebert LA |date=January 1996 |title=Glucocorticosteroid inhibition of cytokine production: relevance to antiallergic actions |journal=The Journal of Allergy and Clinical Immunology |volume=97 |issue=1 Pt 2 |pages=143–52 |doi=10.1016/s0091-6749(96)80214-4 |pmid=8568145 |s2cid=27261595 |doi-access=free}}</ref> They inhibit ], ] deposition, capillary dilation, ] migration, capillary proliferation, ] proliferation, deposition of ], and ] formation associated with inflammation.<ref>{{cite journal |vauthors=Lee SH |date=November 2015 |title=Mechanisms of Glucocorticoid Action in Chronic Rhinosinusitis |journal=Allergy, Asthma & Immunology Research |volume=7 |issue=6 |pages=534–7 |doi=10.4168/aair.2015.7.6.534 |pmc=4605925 |pmid=26333699}}</ref> |
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===Systemic use=== |
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Prednisolone is a ] drug with predominant ] and low ] activity, making it useful for the treatment of a wide range of ] and ] conditions<ref>{{cite journal | vauthors = Czock D, Keller F, Rasche FM, Häussler U | title = Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids | journal = Clinical Pharmacokinetics | volume = 44 | issue = 1 | pages = 61–98 | year = 2005 | pmid = 15634032 | doi = 10.2165/00003088-200544010-00003 | s2cid = 24458998 }}</ref> such as ],<ref>{{cite journal | vauthors = Fiel SB, Vincken W | title = Systemic corticosteroid therapy for acute asthma exacerbations | journal = The Journal of Asthma | volume = 43 | issue = 5 | pages = 321–31 | date = Jun 2006 | pmid = 16801135 | doi = 10.1080/02770900600567163 | s2cid = 24656857 }}</ref> ], ], ], ],<ref name="Angie">{{cite journal | vauthors = Spickett G |title=Urticaria and angioedema |journal=J R Coll Physicians Edinb |date=2014 |volume=44 |issue=1 |pages=50–4 | doi = 10.4997/JRCPE.2014.112|doi-broken-date=1 December 2024 |pmid=24995449 |doi-access=free }}</ref> ],<ref name="Angie"/> ], ], ], ], ], ],<ref>{{cite journal | vauthors = Thrower BW | title = Relapse management in multiple sclerosis | journal = The Neurologist | volume = 15 | issue = 1 | pages = 1–5 | date = January 2009 | pmid = 19131851 | doi = 10.1097/NRL.0b013e31817acf1a | s2cid = 10687818 }}</ref> ], ], ], ],<ref>{{cite journal | vauthors = Lambrou GI, Vlahopoulos S, Papathanasiou C, Papanikolaou M, Karpusas M, Zoumakis E, Tzortzatou-Stathopoulou F | title = Prednisolone exerts late mitogenic and biphasic effects on resistant acute lymphoblastic leukemia cells: Relation to early gene expression | journal = Leukemia Research | volume = 33 | issue = 12 | pages = 1684–95 | date = December 2009 | pmid = 19450877 | doi = 10.1016/j.leukres.2009.04.018 }}</ref> ], ],<ref>{{cite journal | vauthors = Miura M, Tamame T, Naganuma T, Chinen S, Matsuoka M, Ohki H | title = Steroid pulse therapy for Kawasaki disease unresponsive to additional immunoglobulin therapy | journal = Paediatrics & Child Health | volume = 16 | issue = 8 | pages = 479–84 | date = October 2011 | pmid = 23024586 | pmc = 3202387 | doi = 10.1093/pch/16.8.479 }}</ref> ],<ref name="Orapred ODT label" /> ],<ref>{{Cite web |title= Prednisolone 5mg Tablets - Summary of Product Characteristics (SmPC) - (emc) |url= https://www.medicines.org.uk/emc/product/2427/smpc |access-date= 2022-11-27 |website= Medicines |place= UK |archive-date= 27 November 2022 |archive-url= https://web.archive.org/web/20221127163015/https://www.medicines.org.uk/emc/product/2427/smpc |url-status= live }}</ref> and ].<ref>{{cite journal | vauthors = Gera K, Gupta N, Ahuja A, Shah A | title = Acute alveolar sarcoidosis presenting with hypoxaemic respiratory failure | journal = BMJ Case Reports | volume = 2014 | date = April 2014 | pages = bcr2013202247 | pmid = 24789154 | pmc = 4024548 | doi = 10.1136/bcr-2013-202247 }}</ref> |
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Prednisolone can also be used for ] ranging from ] to ] reactions.<ref name="Millipred label">{{cite web | title=Millipred- prednisolone tablet | website=DailyMed | publisher=NIH | date=8 April 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=863ad743-eec0-46f0-beba-c1556384c636 | access-date=9 March 2020 | archive-date=9 March 2020 | archive-url=https://web.archive.org/web/20200309183826/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=863ad743-eec0-46f0-beba-c1556384c636 | url-status=live }}</ref> |
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Prednisolone can also be used as an ] for ].<ref name="Orapred ODT label" /><ref>{{cite journal | vauthors = Vethe NT, Midtvedt K, Asberg A, Amundsen R, Bergan S | title = | journal = Tidsskrift for den Norske Laegeforening | volume = 131 | issue = 20 | pages = 2000–3 | date = October 2011 | pmid = 22016125 | doi = 10.4045/tidsskr.11.0138 | doi-access = free }}</ref> |
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Prednisolone in lower doses can be used in cases of adrenal insufficiency due to ].<ref>{{cite journal | vauthors = Husebye ES, Allolio B, Arlt W, Badenhoop K, Bensing S, Betterle C, Falorni A, Gan EH, Hulting AL, Kasperlik-Zaluska A, Kämpe O, Løvås K, Meyer G, Pearce SH | title = Consensus statement on the diagnosis, treatment and follow-up of patients with primary adrenal insufficiency | journal = Journal of Internal Medicine | volume = 275 | issue = 2 | pages = 104–15 | date = February 2014 | pmid = 24330030 | doi = 10.1111/joim.12162 | s2cid = 206117017 | doi-access = free }}</ref><ref>{{cite book | title = AMA Department of Drugs: AMA Drug Evaluations | edition = 6th | publisher = American Medical Association | location = Chicago, IL | date = 1986 }}</ref> |
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===Topical use=== |
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'''Ophthalmology'''] |
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Topical prednisolone is mainly used in the ] pathway as ]s in numerous eye conditions,<ref name=":0">{{Cite web |title=Prednisolone (ophthalmic): Drug information |url=https://www.uptodate.com/contents/prednisone-drug-information }}</ref> including ]l injuries caused by ], ], and alien objects, ] of the ]s, mild to moderate non-infectious ], disorders of the ], ] or ], ocular inflammation caused by operation and ].<ref name=":1a">{{Cite web |title=Goodman & Gilman's: The Pharmacological Basis of Therapeutics, 13e > Ocular Pharmacy |url=https://login.eproxy.lib.hku.hk/login?qurl=https%3A%2F%2Faccesspharmacy.mhmedical.com%2FViewLarge.aspx%3Ffigid%3D194557123 |access-date=2022-03-16 |website=AccessPharmacy |archive-date=16 March 2022 |archive-url=https://web.archive.org/web/20220316194007/https://login.eproxy.lib.hku.hk/login?qurl=https%3A%2F%2Faccesspharmacy.mhmedical.com%2FViewLarge.aspx%3Ffigid%3D194557123 |url-status=live }}</ref><ref name=":2">{{Cite web |title=Prednisolone (Ophthalmic Route) Side Effects |publisher=Mayo Clinic |url=https://www.mayoclinic.org/drugs-supplements/prednisolone-ophthalmic-route/side-effects/drg-20406320?p=1 |access-date=2022-03-16 |archive-date=25 February 2023 |archive-url=https://web.archive.org/web/20230225143952/https://www.mayoclinic.org/drugs-supplements/prednisolone-ophthalmic-route/side-effects/drg-20406320?p=1 |url-status=live }}</ref> Some side effects include ], ], eye discomfort, impaired recovery of injured site, scarring of the ], ], and ].<ref name=":2" /> However, their prevalence is not known. |
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Prednisolone eye drops are contraindicated in individuals who develop ] reactions against prednisolone,<ref name=":0" /> or individuals with the current conditions, such as ] of the eye, ] affecting the eye, raised ], and ] caused by ].<ref name=":8">{{Cite web |title=Common and Rare Side Effects for prednisolone acetate ophthalmic (eye) |url=https://www.webmd.com/drugs/2/drug-13561/prednisolone-acetate-ophthalmic-eye/details/list-contraindications |access-date=2022-03-16 |website=www.webmd.com |archive-date=21 May 2022 |archive-url=https://web.archive.org/web/20220521081538/https://www.webmd.com/drugs/2/drug-13561/prednisolone-acetate-ophthalmic-eye/details/list-contraindications |url-status=live }}</ref> |
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Prednisolone acetate ophthalmic suspension (eye drops) is prepared as a sterile ophthalmic suspension and used to reduce swelling, ], ], and ] affecting the eye.<ref name="Pred Forte label">{{cite web | title=Pred Forte- prednisolone acetate suspension/ drops | website=DailyMed | date=19 July 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=00a5aa88-e361-4ea7-8922-530c738b726e | access-date=9 March 2020 | archive-date=9 March 2020 | archive-url=https://web.archive.org/web/20200309184003/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=00a5aa88-e361-4ea7-8922-530c738b726e | url-status=live }}</ref><ref name="Omnipred label">{{cite web | title=Omnipred- prednisolone acetate suspension | website=DailyMed | date=9 September 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4bbb4356-b4b3-4497-a3a3-8f4b65d326fe | access-date=9 March 2020 | archive-date=13 May 2021 | archive-url=https://web.archive.org/web/20210513121834/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4bbb4356-b4b3-4497-a3a3-8f4b65d326fe | url-status=live }}</ref><ref name="Pred Mild label">{{cite web | title=Pred Mild- prednisolone acetate suspension/ drops | website=DailyMed | date=19 July 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4fcce64a-94ea-4031-ad5a-c4eddc73a910 | access-date=9 March 2020 | archive-date=9 March 2020 | archive-url=https://web.archive.org/web/20200309184016/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4fcce64a-94ea-4031-ad5a-c4eddc73a910 | url-status=live }}</ref> It has been explored as a treatment option for bacterial ].<ref name="Herretes">{{cite journal | vauthors = Herretes S, Wang X, Reyes JM | title = Topical corticosteroids as adjunctive therapy for bacterial keratitis | journal = The Cochrane Database of Systematic Reviews | issue = 10 | pages = CD005430 | date = October 2014 | volume = 2014 | pmid = 25321340 | pmc = 4269217 | doi = 10.1002/14651858.CD005430.pub3 }}</ref> |
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Prednisolone eye drops are used in ] caused by ] and ], marginal ], ], ], which is an infection of the eye involving the ], ], ], inflammation of the eye after ], and ] injuries caused by ], ], ], or penetration of foreign objects.<ref name=":1a" /> It is also used in the prevention of ],<ref>{{cite journal | vauthors = Arslan N, Tepe D, Taştan E, Demirci M, Caydere M, Ustun H, Oguz H | title = Evaluation of the effectiveness of topical ciprofloxacin and prednisolone in the prevention of myringosclerosis | journal = European Archives of Oto-Rhino-Laryngology | volume = 269 | issue = 11 | pages = 2335–2341 | date = November 2012 | pmid = 22197890 | doi = 10.1007/s00405-011-1889-z | s2cid = 23472925 }}</ref> ].<ref>{{cite journal | vauthors = Wilhelmus KR, Gee L, Hauck WW, Kurinij N, Dawson CR, Jones DB, Barron BA, Kaufman HE, Sugar J, Hyndiuk RA, Laibson PR, Stulting RD, Asbell PA | display-authors = 6 | title = Herpetic Eye Disease Study: A Controlled Trial of Topical Corticosteroids for Herpes Simplex Stromal Keratitis | journal = Ophthalmology | volume = 127 | issue = 4S | pages = S5–S18 | date = April 2020 | pmid = 32200827 | doi = 10.1016/j.ophtha.2020.01.037 | s2cid = 214616647 }}</ref> Topical prednisolone can also be used after procedures such as Laser Peripheral Iridotomy for patients with primary ] suspects (PACS) to control inflammations.<ref>{{cite journal | vauthors = Gayam K, Ramulu PY, Rengaraj V, Srinivasan K | title = Safety and Efficacy of 0.1% Nepafenac versus 1% Prednisolone Acetate Eye Drops after Laser Peripheral Iridotomy: A Prospective, Randomized Trial | journal = Ophthalmology. Glaucoma | volume = 3 | issue = 3 | pages = 174–180 | date = 2020-02-29 | pmid = 32672612 | doi = 10.1016/j.ogla.2020.02.006 | s2cid = 90234022 }}</ref> |
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'''Ear drops''' |
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In addition, topical prednisolone can also be administered as ]s.<ref name=":10">{{Cite web |title=BNF: Prednisolone, Medicine Forms |url=https://login.eproxy.lib.hku.hk/login?qurl=https%3A%2F%2Fwww.medicinescomplete.com%2F |access-date=2022-04-14 |website=Medicines Complete |archive-date=16 March 2022 |archive-url=https://web.archive.org/web/20220316194910/https://login.eproxy.lib.hku.hk/login?qurl=https%3A%2F%2Fwww.medicinescomplete.com%2F |url-status=live }}</ref> |
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{| class="wikitable" |
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|+Examples of topical prednisolone Products |
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!Eye drops |
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!Ear drops |
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|Prednisolone sodium phosphate ophthalmic solution<ref name=":0" /> |
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| rowspan="4" |Prednisolone sodium phosphate 0.5% eye/ ear drops<ref name=":10" /> |
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|Pred forte ophthalmic suspension (prednisolone acetate ophthalmic suspension)<ref name="Pred Forte label" /> |
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|Suspension (prednisolone mild ophthalmic)<ref name=":0" /> |
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|Suspension (prednisolone acetate ophthalmic)<ref name=":0" /> |
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==Adverse effects== |
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Adverse reactions from the use of prednisolone include:<ref name="Flo-Pred label" /><ref name="Orapred ODT label" /> |
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* ], ], ], and ] |
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* ] |
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* ] events |
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* ] effects including reddening of the face, bruising/skin discoloration, impaired wound healing, ], ], ], and abnormal hair growth |
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* ]; patients with ] may need increased ] or diabetic therapies |
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* ] |
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* Lower response to hormones, especially during stressful instances such as surgery or illness |
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* Change in electrolytes: rise in ], increased sodium and low potassium, leading to ] |
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* ] system effects: swelling of the stomach lining, reversible increase in liver enzymes, and risk of ] |
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* Muscular and skeletal abnormalities, such as muscle weakness/muscle loss, ] (see ]), long bone fractures, tendon rupture, and back fractures |
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* Neurological effects, including involuntary movements (]s), ], and ] |
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* ] behavioral and emotional disturbances<ref name="Pediapred label" /> with ] being one of the most common cognitive symptoms, especially with oral use.<ref name=":MayoOral">{{Cite news|url= https://www.mayoclinic.org/drugs-supplements/prednisolone-oral-route/side-effects/drg-20075189|title= Prednisolone (Oral Route) |publisher=Mayo Clinic|access-date=1 August 2023}}</ref> |
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* ] and ] (in some pathologic conditions).<ref>{{cite journal | vauthors = ReMine SG, McIlrath DC | title = Bowel perforation in steroid-treated patients | journal = Annals of Surgery | volume = 192 | issue = 4 | pages = 581–6 | year = 1980 | pmid = 7425698 | pmc = 1347010 | doi = 10.1097/00000658-198010000-00016 }}</ref><ref>{{cite journal | vauthors = Cervin A, Andersson M | title = Intranasal steroids and septum perforation--an overlooked complication? A description of the course of events and a discussion of the causes | journal = Rhinology | volume = 36 | issue = 3 | pages = 128–32 | date = September 1998 | pmid = 9830677 }}</ref> |
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Discontinuing prednisolone after long-term or high-dose use can lead to ].<ref name="Pediapred label" /> |
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===Pregnancy and breastfeeding=== |
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Although there are no major human studies of prednisolone use in pregnant women, studies in several animals show that it may cause birth defects including increased likelihood of ]. |
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Prednisolone is found in the breast milk of mothers taking prednisolone.<ref name="Pediapred label">{{cite web | title=Pediapred- prednisolone sodium phosphate solution | website=DailyMed | date=29 January 2020 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1b996564-a777-4d37-ae00-b6a5ffc5e596 | access-date=9 March 2020 | archive-date=9 May 2021 | archive-url=https://web.archive.org/web/20210509192922/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1b996564-a777-4d37-ae00-b6a5ffc5e596 | url-status=live }}</ref> |
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=== Local adverse effects in the eye === |
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] |
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When used topically on the eye, the following are potential side effects: |
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* ]s: Extended usage of corticosteroids may cause clouding at the back of the lens, also known as posterior subcapsular cataract. This type of cataract reduces the path of light from reaching the eye, which interferes with a person's reading vision. Consumption of prednisolone eye drops post-surgery may also retard the healing process.<ref name=":0" /> |
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* ]l thinning: When corticosteroids are used in the long term, corneal and ]l thinning is also one of its consequences. When not ceased, thinning may ultimately lead to perforation of the cornea.<ref name=":0" /> |
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* ]: Elongated use of corticosteroids has a chance of causing a raised intraocular pressure (IOP), injuring the optic nerve, and weakening visual awareness. Corticosteroids should be used cautiously in patients with concomitant conditions of glaucoma. Doctors track patients' IOP if they are using corticosteroid eye drops for more than 103 days.<ref name=":0" /> |
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==Pharmacology== |
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===Pharmacodynamics=== |
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As a ], the lipophilic structure of prednisolone allows for easy passage through the cell membrane where it then binds to its respective ] (GCR) located in the cytoplasm. Upon binding, the formation of the GC/GCR complex causes dissociation of ] from the glucocorticoid receptor enabling the GC/GCR complex to translocate inside the nucleus.<ref name=":11">{{Cite web | vauthors = Goldstein BG, Goldstein AO | date = 13 September 2022 | veditors = Dellavalle RP, Levy ML, Corona R |title=Topical corticosteroids: Use and adverse effects |url=https://www.uptodate.com/contents/topical-corticosteroids-use-and-adverse-effects }}</ref> This process occurs within 20 minutes of binding. Once inside the nucleus, the ] GC/GCR complex binds to specific DNA binding sites known as glucocorticoid response elements (GREs) resulting in gene expression or inhibition. Complex binding to positive GREs leads to the synthesis of anti-inflammatory proteins while binding to negative GREs blocks the ] of inflammatory genes.<ref>{{cite journal | vauthors = Stahn C, Löwenberg M, Hommes DW, Buttgereit F | title = Molecular mechanisms of glucocorticoid action and selective glucocorticoid receptor agonists | journal = Molecular and Cellular Endocrinology | volume = 275 | issue = 1–2 | pages = 71–78 | date = September 2007 | pmid = 17630118 | doi = 10.1016/j.mce.2007.05.019 | url = https://hal.archives-ouvertes.fr/hal-00531935/file/PEER_stage2_10.1016%252Fj.mce.2007.05.019.pdf | access-date = 27 June 2019 | url-status = live | s2cid = 4121936 | archive-url = https://web.archive.org/web/20200928224448/https://hal.archives-ouvertes.fr/hal-00531935/file/PEER_stage2_10.1016%252Fj.mce.2007.05.019.pdf | archive-date = 28 September 2020 }}</ref> They inhibit the release of signals that promote inflammation such as ], ], ], and stimulate anti-inflammatory signals such as the ] gene.<ref name=":7">{{cite journal | vauthors = Schijvens AM, Ter Heine R, de Wildt SN, Schreuder MF | title = Pharmacology and pharmacogenetics of prednisone and prednisolone in patients with nephrotic syndrome | journal = Pediatric Nephrology | volume = 34 | issue = 3 | pages = 389–403 | date = March 2019 | pmid = 29549463 | pmc = 6349812 | doi = 10.1007/s00467-018-3929-z }}</ref><ref name=":6">{{Cite web |title=Prednisolone phosphate |url=https://go.drugbank.com/drugs/DB14631 |access-date=2022-03-16 |website=go.drugbank.com |archive-date=25 February 2023 |archive-url=https://web.archive.org/web/20230225143952/https://go.drugbank.com/drugs/DB14631 |url-status=live }}</ref> All of them will collectively cause a sequence of events, including the inhibition of ] synthesis and additional inflammatory mediators. ]s also inhibit ] ] and ]. As well as ], which in turn lessens ] derivative genesis.<ref>{{Cite web |title=Prednisolone acetate |url=https://go.drugbank.com/drugs/DB15566 |access-date=2022-03-16 |website=go.drugbank.com |archive-date=25 February 2023 |archive-url=https://web.archive.org/web/20230225143951/https://go.drugbank.com/drugs/DB15566 |url-status=live }}</ref> |
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===Pharmacokinetics=== |
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Prednisolone has a relatively short ], ranging 2–4 hours. It also has a large ], considering the dosage required to produce a therapeutic effect is a few times higher than what the body naturally produces.<ref name=":6" /> |
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Prednisolone is 70–90% ], it binds to ]s such as ].<ref name=":6" /> |
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Both prednisolone ] and prednisolone ] go through ] ] in the body to form prednisolone. It subsequently undergoes the usual ] of prednisolone. Concomitant use of prednisolone and strong ] inhibitors such as ] is shown to cause a rise in plasma prednisolone concentrations by about 50% owing to a diminished ].<ref name=":7" /> |
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Prednisolone predominantly undergoes ] elimination and is excreted in the ] as ] and metabolites of ] conjugate.<ref name=":6" /> |
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===Prednisone=== |
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] is a ] that is activated in the liver. When it enters the body, prednisone is triggered by the liver and body chemicals to turn into its active form, prednisolone.<ref>{{Cite web |url=https://www.goodrx.com/classes/corticosteroids/prednisolone-vs-prednisone |title=What's the Difference Between Prednisolone and Prednisone? |access-date=27 November 2022 |archive-date=10 October 2022 |archive-url=https://web.archive.org/web/20221010171640/https://www.goodrx.com/classes/corticosteroids/prednisolone-vs-prednisone |url-status=live }}</ref> |
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==Chemistry== |
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Prednisolone is a ] ] ] closely related to its cognate ], having identical structure save for two fewer hydrogens near C<sub>11</sub>. It is also known as '''δ<sup>1</sup>-cortisol''', '''δ<sup>1</sup>-hydrocortisone''', '''1,2-dehydrocortisol''', or '''1,2-dehydrohydrocortisone''', as well as '''11β,17α,21-trihydroxypregna-1,4-diene-3,20-dione'''.<ref name="Elks2014">{{cite book | vauthors = Elks J |title=The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies |url=https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA1011 |date=14 November 2014|publisher=Springer|isbn=978-1-4757-2085-3|pages=1011–1012|url-status=live|archive-url=https://web.archive.org/web/20170910174620/https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA1011|archive-date=10 September 2017}}</ref><ref name="IndexNominum2000">{{cite book|title=Index Nominum 2000: International Drug Directory|url=https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA869|date=January 2000|publisher=Taylor & Francis|isbn=978-3-88763-075-1|pages=869–|url-status=live|archive-url=https://web.archive.org/web/20170910174620/https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA869|archive-date=2017-09-10}}</ref> |
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== Interactions == |
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Co-administration of prednisolone eye drops with ophthalmic ] (NSAIDs) may perhaps exacerbate its effects, causing unwanted side effects such as toxicity.{{clarify|date=November 2024}} The wound healing process may also be hindered.<ref>{{Cite web |title=Prednisolone (Ophthalmic Route) |url=https://www.mayoclinic.org/drugs-supplements/prednisolone-ophthalmic-route/side-effects/drg-20406320?p=1 |publisher=Mayo Foundation for Medical Education and Research}}</ref> |
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Drug interactions of prednisolone include other ]s like ] or ], ]s like ], ]s like ] or ], or NSAIDs such as ], ], or ].<ref>{{Cite web |title=Prednisolone Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing - WebMD |url=https://www.webmd.com/drugs/2/drug-6307-2333/prednisolone-oral/prednisolone-liquid-oral/details |access-date=2024-02-29 |website=www.webmd.com |language=en}}</ref> |
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== Contraindications == |
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{{Empty section|date=October 2023}} |
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== Special populations == |
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=== Children === |
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Prolonged use of prednisolone eye drops in children may lead to raised intraocular pressure. While this phenomenon is dose-dependent, it is shown to have a greater effect, especially in children under 6 years of age.<ref name=":0" /> |
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=== Pregnancy and breastfeeding === |
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Research on animal reproduction has indicated that there is a trace of ] when doses are reduced by 10 times the human recommended dose.<ref name=":9">{{Cite web |title=Prednisolone ophthalmic Use During Pregnancy |url=https://www.drugs.com/pregnancy/prednisolone-ophthalmic.html |access-date=2022-03-16 |website=Drugs.com |language=en |archive-date=25 February 2023 |archive-url=https://web.archive.org/web/20230225143952/https://www.drugs.com/pregnancy/prednisolone-ophthalmic.html |url-status=live }}</ref> There is no sufficient information on human pregnancy at this moment. Use is only recommended when the potential benefits outweigh the potential risks for the pregnant mother and the fetus.<ref name=":9" /> |
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Prednisolone when delivered systemically can be found in the mother's breast milk, however, there is no data provided for the extent of prednisolone found in the system after administering eye drops.<ref name=":0" /><ref name=":9" /> However, the presence of corticosteroids is recorded when they are administered systemically, and it could affect the fetus' growth.<ref name=":9" /> Therefore, the use of prednisolone during breastfeeding is not advocated.<ref name=":9" /> |
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==Society and culture== |
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===Dosage forms=== |
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Prednisolone is supplied as oral liquid, oral suspension, oral syrup, oral tablet, and oral disintegrating tablet. It may be a generic medication or supplied as brands Flo-Pred (prednisolone acetate oral suspension),<ref name="Flo-Pred label">{{cite web | title=Flo-Pred- prednisolone acetate suspension | website=DailyMed | date=28 February 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=980b3c11-a502-4235-bbff-af83a17ebcdf | access-date=9 March 2020 | archive-date=9 May 2021 | archive-url=https://web.archive.org/web/20210509192923/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=980b3c11-a502-4235-bbff-af83a17ebcdf | url-status=live }}</ref> Millipred (oral tablets),<ref name="Millipred label" /> Orapred (prednisolone sodium phosphate oral dissolving tablets),<ref name="Orapred ODT label">{{cite web | title=Orapred ODT- prednisolone sodium phosphate tablet, orally disintegrating | website=DailyMed | date=11 September 2019 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1e379543-c4cf-4e72-953b-db15b7f0c2a1 | access-date=9 March 2020 | archive-date=12 May 2021 | archive-url=https://web.archive.org/web/20210512151422/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=1e379543-c4cf-4e72-953b-db15b7f0c2a1 | url-status=live }}</ref> Pediapred (] oral solution),<ref name="Pediapred label" /> Veripred 20, Prelone, Hydeltra-T.B.A., Hydeltrasol, Key-Pred, Cotolone, Predicort, Medicort, Predcor, Bubbli-Pred, Omnipred (prednisolone acetate ophthalmic suspension),<ref name="Omnipred label" /> Pred Mild,<ref name="Pred Mild label" /> Pred Forte,<ref name="Pred Forte label" /> and others.<ref>{{cite web | title=Prednisolone: Uses, Dosage, Side Effects, Warnings | website=Drugs.com | date=6 July 2022 | url=https://www.drugs.com/prednisolone.html}}</ref> |
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===Athletics=== |
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As a glucocorticosteroid, unauthorized or ad hoc use of prednisolone during competition via oral, intravenous, intramuscular, or rectal routes is banned under ] (WADA) anti-doping rules.<ref name=":1">{{Cite web |title=Prohibited List |url=https://www.wada-ama.org/sites/default/files/wada_2020_english_prohibited_list_0.pdf |date=January 2020 | publisher=] |url-status=live |archive-url=https://web.archive.org/web/20200309181458/https://www.wada-ama.org/sites/default/files/wada_2020_english_prohibited_list_0.pdf |archive-date=2020-03-09 }}</ref> |
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==Veterinary uses== |
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Prednisolone is used in the treatment of inflammatory and allergic conditions in cats, dogs, horses, small mammals such as ], birds, and reptiles.<ref name=":3">{{Cite web |title=PrednisoLONE Acetate Ophthalmic Suspension |url=https://www.vetrxdirect.com/product/view/prednisolone-eye-drops-for-dogs-and-cats-rx |access-date=2022-03-16 |website=www.vetrxdirect.com |language=en |archive-date=25 February 2023 |archive-url=https://web.archive.org/web/20230225143952/https://www.vetrxdirect.com/product/view/prednisolone-eye-drops-for-dogs-and-cats-rx |url-status=live }}</ref><ref name=":4">{{Cite web |title=Prednisolone Acetate Ophthalmic for Veterinary Use |url=https://www.wedgewoodpharmacy.com/learning-center/professional-monographs/prednisolone-acetate-ophthalmic-for-veterinary-use.html |access-date=2022-03-16 |website=www.wedgewoodpharmacy.com |archive-date=4 July 2022 |archive-url=https://web.archive.org/web/20220704051059/https://www.wedgewoodpharmacy.com/learning-center/professional-monographs/prednisolone-acetate-ophthalmic-for-veterinary-use.html |url-status=live }}</ref> Its usage in treating inflammation, immune-mediated disease, ], and ] is often considered ] use. Many drugs are commonly prescribed for off-label use in ]."<ref name="vcarg">{{cite news |vauthors=Gollakner R |title=Prednisolone/Prednisone |url=https://vcahospitals.com/know-your-pet/prednisoloneprednisone |access-date=3 July 2021 |publisher=VCA Hospitals |archive-date=21 June 2021 |archive-url=https://web.archive.org/web/20210621213643/https://vcahospitals.com/know-your-pet/prednisoloneprednisone |url-status=live }}</ref> Studies in ruminating species, such as ], have shown that oral administration of the drug is associated with a reduced ] compared to intravenous administration; however, levels that are therapeutic in other species can be achieved with oral administration in alpacas.<ref>{{cite journal | vauthors = Videla R, Sommardahl C, Smith J, Schaefer DM, Cox S | title = Pharmacokinetics of Orally Administered Prednisolone in Alpacas | journal = Frontiers in Veterinary Science | volume = 8 | pages = 745890 | year = 2021 | pmid = 34746285 | pmc = 8569471 | doi = 10.3389/fvets.2021.745890 | doi-access = free }}</ref> |
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It is used in a broad spectrum of diseases, for example, inflammation of scleral tissues, cornea, and conjunctiva in dogs.<ref name=":3" /> In horses, prednisolone acetate suspensions are priorly used to treat inflammation in the middle layer of the eye, also known as ] and ] (ERU), which is the leading cause of visual impairment in horses.<ref name=":4" /> Prednisolone acetate eye drops are not to be used in other animals such as birds.<ref name=":3" /> |
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Prednisolone acetate eye drops are also prescribed to dogs and cats to lessen swelling, ], burning, and pain sensations after surgeries of the eye.<ref name=":3" /> |
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Cats with conjunctivitis usually are required to avoid using ophthalmic preparations of ]s and its derivatives. The most typical infections are caused by ].<ref name=":4" /> |
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==References== |
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{{Reflist}} |
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==External links== |
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* {{cite web | title=Prednisolone Ophthalmic | website=MedlinePlus | url=https://medlineplus.gov/druginfo/meds/a682794.html }} |
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* {{cite patent |country=US |number=2837464 |status=patent |title=Process for production of dienes by corynebacteria |pubdate= 1958-06-03 |gdate=1958-06-03 |fdate=1955-01-11 |pridate=1955-01-11 |invent1=Arthur Nobile |assign1=Schering Corp |url=https://worldwide.espacenet.com/publicationDetails/biblio?II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=19580603&CC=US&NR=2837464A&KC=A}} |
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| title = ] |
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| titlestyle = background:#ccccff |
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| list1 = |
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{{Glucocorticoid receptor modulators}} |
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{{Mineralocorticoid receptor modulators}} |
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{{Xenobiotic-sensing receptor modulators}} |
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}} |
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{{Portal bar | Medicine}} |
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] |
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] |
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] |
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] |
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] |
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] |
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] |
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] |
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] |