Identification

Name
Prednisolone
Accession Number
DB00860
Description

Prednisolone is a glucocorticoid similar to cortisol used for its anti-inflammatory, immunosuppressive, anti-neoplastic, and vasoconstrictive effects.4

Prednisolone was granted FDA approval on 21 June 1955.6

Type
Small Molecule
Groups
Approved, Vet approved
Structure
Thumb
Weight
Average: 360.444
Monoisotopic: 360.193674006
Chemical Formula
C21H28O5
Synonyms
  • (11β)-11,17,21-trihydroxypregna-1,4-diene-3,20-dione
  • 1,4-pregnadiene-11β,17α,21-triol-3,20-dione
  • 1,4-pregnadiene-3,20-dione-11β,17α,21-triol
  • 3,20-dioxo-11β,17α,21-trihydroxy-1,4-pregnadiene
  • delta-dehydrocortisol
  • delta-dehydrohydrocortisone
  • delta-hydrocortisone
  • delta(1)-Dehydrocortisol
  • delta(1)-Dehydrohydrocortisone
  • delta(1)-Hydrocortisone
  • Hydroretrocortine
  • Metacortandralone
  • PRDL
  • Prednisolona
  • Prednisolone
  • Prednisolonum
External IDs
  • NSC-9120
  • NSC-9900

Pharmacology

Indication

Prednisolone is indicated to treat endocrine, rheumatic, and hematologic disorders; collagen, dermatologic, ophthalmic, respiratory, and gastrointestinal diseases; allergic and edematous states; and other conditions like tuberculous meningitis.7

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals.4 Prednisolone has a short duration of action as the half life is 2.1-3.5 hours.1 Corticosteroids have a wide therapeutic window as patients make require doses that are multiples of what the body naturally produces.4 Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.4

Mechanism of action

The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation.4 Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.4

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.4

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.4 High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.4

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Humans
Absorption

Oral prednisolone reaches a Cmax of 113-1343ng/mL with a Tmax of 1.0-2.6 hours.1 Oral prednisolone is approximately 70% bioavailable.2

Volume of distribution

A 0.15mg/kg dose of prednisolone has a volume of distribution of 29.3L, while a 0.30mg/kg dose has a volume of distribution of 44.2L.1

Protein binding

Prednisolone's protein binding is highly variable, ranging from 65-91% in healthy patients.1

Metabolism

Prednisolone can be reversibly metabolized to prednisone which is then metabolized to 17α,21-dihydroxy-pregnan-1,4,6-trien-3,11,30-trione (M-XVII), 20α-dihydro-prednisone (M-V), 6βhydroxy-prednisone (M-XII), 6α-hydroxy-prednisone (M-XIII), or 20β-dihydro-prednisone (M-IV).3 20β-dihydro-prednisone is metabolized to 17α,20ξ,21-trihydroxy-5ξ-pregn-1-en-3,11-dione(M-XVIII).3 Prednisolone is metabolized to Δ6-prednisolone (M-XI), 20α-dihydro-prednisolone (M-III), 20β-dihydro-prednisolone (M-II), 6αhydroxy-prednisolone (M-VII), or 6βhydroxy-prednisolone(M-VI).3 6αhydroxy-prednisolone is metabolized to 6α,11β,17α,20β,21-pentahydroxypregnan-1,4-diene-3-one (M-X).3 6βhydroxy-prednisolone is metabolized to 6β,11β,17α,20β,21-pentahydroxypregnan-1,4-diene-3-one (M-VIII), 6β,11β,17α,20α,21-pentahydroxypregnan-1,4-diene-3-one (M-IX), and 6β,11β,17α,21-tetrahydroxy-5ξ-pregn-1-en-3,20-dione (M-XIV).3 MVIII is metabolized to 6β,11β,17α,20β,21-pentahydroxy-5ξ-pregn-1-en-3-one (M-XV) and then to MXIV, while MIX is metabolized to 6β,11β,17α,20α,21-pentahydroxy-5ξ-pregn-1-en-3-one (M-XVI) and then to MXIV.3 These metabolites and their glucuronide conjugates are excreted predominantly in the urine.3

Hover over products below to view reaction partners

Route of elimination

Prednisolone is over 98% eliminated in urine.1

Half-life

Prednisolone has a plasma half life of 2.1-3.5 hours.1 This half life is shorter in children and longer in those with liver disease.1

Clearance

A 0.15mg/kg dose of prednisolone has a clearance of 0.09L/kg/h, while a 0.30mg/kg dose has a clearance of 0.12L/kg/h.1

Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

The intraperitoneal LD50 in rats is 2g/kg and 65mg/kg in mice.8 The subcutaneous LD50 in rats is 147mg/kg and >3500mg/kg in mice.8 The oral LD50 in mice is 1680mg/kg.8 In humans, the oral TDLO in men is 9mg/kg/2W and in women is 14mg/kg/13D.8

Patients experiencing an overdose of prednisolone may present with gastrointestinal disturbances, insomnia, and restlessness.5 Overdose of oral prednisolone may be treated by gastric lavage or inducing vomiting if the overdose was recent, as well as supportive and symptomatic therapy.9 Chronic overdosage may be treated by dose reduction or treating patients on alternate days.9 An overdose by the ophthalmic route is not expected to cause problems.9

Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Prednisone Action PathwayDrug action
Prednisolone Action PathwayDrug action
Prednisone Metabolism PathwayDrug metabolism
Prednisolone Metabolism PathwayDrug metabolism
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Prednisolone can be increased when it is combined with Abametapir.
AbataceptThe risk or severity of adverse effects can be increased when Prednisolone is combined with Abatacept.
AbirateroneThe metabolism of Abiraterone can be increased when combined with Prednisolone.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Prednisolone.
AcarboseThe risk or severity of hyperglycemia can be increased when Prednisolone is combined with Acarbose.
AceclofenacThe risk or severity of gastrointestinal irritation can be increased when Prednisolone is combined with Aceclofenac.
AcemetacinThe risk or severity of gastrointestinal irritation can be increased when Prednisolone is combined with Acemetacin.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Prednisolone.
AcetohexamideThe risk or severity of hyperglycemia can be increased when Prednisolone is combined with Acetohexamide.
AcetyldigitoxinThe risk or severity of adverse effects can be increased when Prednisolone is combined with Acetyldigitoxin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
  • Avoid alcohol.
  • Take with food. Food reduces irritation.

Products

Product Images
International/Other Brands
Ak-Pred / Decortin H / Delta-Cortef / Deltacortril / Hydeltra / Hydeltra-TBA / Hydeltrasol / Inflamase / Key-Pred / Klismacort / Meticortelone / Panafcortelone / Predonine / Prelone / Solone / Sterolone / Ultracortenol
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
PediapredSolution5 mgOralSanofi Aventis1998-09-23Not applicableCanada flag
Pediapred - Liq 6.7mg/5mlLiquidOralFisons1995-12-311998-08-12Canada flag
PrednisoLONESyrup15 mg/5mLOralVintage Pharmaceuticals, LLC2007-12-132007-12-13US flag
PrednisoloneSyrup5 mg/5OralKV Pharmaceuticals2007-01-09Not applicableUS flag
PrednisoloneTablet5 mg/1OralWatson Pharmaceuticals2007-03-31Not applicableUS flag
PrednisoLONESolution15 mg/5mLOralPharmaceutical Associates, Inc.2007-08-09Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
MillipredTablet5 mg/5mgOralLaser Pharmaceuticals Llc2008-10-012017-07-03US flag16477 0505 01 nlmimage10 851b42ca
MillipredTablet5 mg/1OralCerecor, Inc.2014-03-01Not applicableUS flag
Novo-prednisolone 5mgTabletOralNovopharm Limited1967-12-312005-08-10Canada flag
PMS-prednisoloneSolutionOralPharmascience Inc2002-03-19Not applicableCanada flag
PrednisoloneSyrup15 mg/5mLOralApotex Corporation2005-08-252005-08-26US flag
PrednisoloneSolution15 mg/5mLOralbryant ranch prepack2003-02-27Not applicableUS flag
PrednisoloneSolution15 mg/5mLOralA-S Medication Solutions2003-02-27Not applicableUS flag
PrednisoloneSolution15 mg/5mLOralHi Tech Pharmacal Co., Inc.2003-02-27Not applicableUS flag
PrednisoloneSolution15 mg/5mLOralStat Rx USA2003-02-27Not applicableUS flag
PrednisoloneSyrup5 mg/5mLOralPhysicians Total Care, Inc.2003-02-28Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
CambisonPrednisolone (4 mg/1g) + Neomycin sulfate (3 mg/1g)OintmentTopicalOASIS TRADING2018-11-15Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
CambisonPrednisolone (4 mg/1g) + Neomycin sulfate (3 mg/1g)OintmentTopicalOASIS TRADING2018-11-15Not applicableUS flag

Categories

ATC Codes
D07AA03 — PrednisoloneS01CA02 — Prednisolone and antiinfectivesD07XA02 — PrednisoloneA01AC54 — Prednisolone, combinationsR01AD02 — PrednisoloneS01BB02 — Prednisolone and mydriaticsR01AD52 — Prednisolone, combinationsS01CB02 — PrednisoloneV03AB05 — Prednisolone and promethazineS03BA02 — PrednisoloneD07BA01 — Prednisolone and antisepticsD07CA03 — Prednisolone and antibioticsS01BA04 — PrednisoloneS02BA03 — PrednisoloneA07EA01 — PrednisoloneH02AB06 — PrednisoloneS02CA01 — Prednisolone and antiinfectivesC05AA04 — PrednisoloneS03CA02 — Prednisolone and antiinfectives
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Hydroxysteroids
Direct Parent
21-hydroxysteroids
Alternative Parents
Gluco/mineralocorticoids, progestogins and derivatives / 20-oxosteroids / 3-oxo delta-1,4-steroids / 17-hydroxysteroids / 11-beta-hydroxysteroids / Delta-1,4-steroids / Tertiary alcohols / Alpha-hydroxy ketones / Secondary alcohols / Cyclic ketones
show 4 more
Substituents
11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / Alcohol / Aliphatic homopolycyclic compound / Alpha-hydroxy ketone
show 15 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
11beta-hydroxy steroid, 17alpha-hydroxy steroid, glucocorticoid, 20-oxo steroid, 3-oxo-Delta(1),Delta(4)-steroid, 21-hydroxy steroid (CHEBI:8378) / Pregnane and derivatives [Fig] (C07369) / C21 steroids (gluco/mineralocorticoids, progestogins) and derivatives (LMST02030179)

Chemical Identifiers

UNII
9PHQ9Y1OLM
CAS number
50-24-8
InChI Key
OIGNJSKKLXVSLS-VWUMJDOOSA-N
InChI
InChI=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
IUPAC Name
(1R,3aS,3bS,9aR,9bS,10S,11aS)-1,10-dihydroxy-1-(2-hydroxyacetyl)-9a,11a-dimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
SMILES

References

Synthesis Reference

Gunther Bellmann, "Process for producing a sterile prednisolone gel." U.S. Patent US5811417, issued September 22, 1998.

US5811417
General References
  1. Pickup ME: Clinical pharmacokinetics of prednisone and prednisolone. Clin Pharmacokinet. 1979 Mar-Apr;4(2):111-28. doi: 10.2165/00003088-197904020-00004. [PubMed:378499]
  2. Ferry JJ, Horvath AM, Bekersky I, Heath EC, Ryan CF, Colburn WA: Relative and absolute bioavailability of prednisone and prednisolone after separate oral and intravenous doses. J Clin Pharmacol. 1988 Jan;28(1):81-7. doi: 10.1002/j.1552-4604.1988.tb03105.x. [PubMed:3350994]
  3. Matabosch X, Pozo OJ, Perez-Mana C, Papaseit E, Segura J, Ventura R: Detection and characterization of prednisolone metabolites in human urine by LC-MS/MS. J Mass Spectrom. 2015 Mar;50(3):633-42. doi: 10.1002/jms.3571. [PubMed:25800201]
  4. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [PubMed:30285357]
  5. Robinson J, McKenzie C, MacLeod D: Paediatric dosing errors with oral prednisolone mixture. Aust Prescr. 2016 Oct;39(5):176. doi: 10.18773/austprescr.2016.062. Epub 2016 Oct 1. [PubMed:27789930]
  6. FDA Approved Drug Products: Delta-Cortef Prednisolone Oral Tablets (Discontinued) [Link]
  7. FDA Approved Drug Products: Prednisolone Oral Syrup [Link]
  8. Cayman Chemicals: Prednisolone MSDS [Link]
  9. FDA Approved Drug Products: Prednisolone Acetate Oral Suspension [Link]
  10. FDA Approved Drug Products: Prednisolone Acetate Ophthalmic Suspension [Link]
  11. FDA Approved Drug Products: Orapred Prednisolone Sodium Phosphate Orally Disintegrating Tablets [Link]
  12. FDA Approved Drug Products: Pediapred Prednisolons Sodium Phosphate Oral Solution [Link]
Human Metabolome Database
HMDB0014998
KEGG Drug
D00472
KEGG Compound
C07369
PubChem Compound
5755
PubChem Substance
46504847
ChemSpider
5552
BindingDB
19190
RxNav
8638
ChEBI
8378
ChEMBL
CHEMBL131
ZINC
ZINC000003833821
Therapeutic Targets Database
DAP000419
PharmGKB
PA451096
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Prednisolone
AHFS Codes
  • 68:04.00 — Adrenals
FDA label
Download (101 KB)
MSDS
Download (72.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentAdvanced Follicular Lymphoma1
4Active Not RecruitingTreatmentAnti-Neutrophil Cytoplasmic Antibody-Associated Vasculitis / Granulomatosis With Polyangiitis / Microscopic Polyangiitis1
4Active Not RecruitingTreatmentCrohn's Disease (CD)1
4Active Not RecruitingTreatmentFunction of Renal Transplant1
4Active Not RecruitingTreatmentMalignant Lymphomas1
4Active Not RecruitingTreatmentProstate Cancer1
4Active Not RecruitingTreatmentRheumatoid Arthritis3
4Active Not RecruitingTreatmentSeasonal Allergic Rhinitis (SAR)1
4CompletedDiagnosticCoughing1
4CompletedOtherAsthma2

Pharmacoeconomics

Manufacturers
  • Pharmacia and upjohn co
  • Akorn inc
  • Sandoz canada inc
  • Teva parenteral medicines inc
  • Watson laboratories inc
  • Bel mar laboratories inc
  • Schering corp sub schering plough corp
  • Alpharma uspd inc
  • Apotex inc richmond hill
  • Hi tech pharmacal co inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Kv pharmaceutical co
  • Pharmaceutical assoc inc div beach products
  • Teva pharmaceuticals usa
  • Vintage pharmaceuticals llc
  • We pharmaceuticals inc
  • Wockhardt eu operations (swiss) ag
  • Muro pharmaceutical inc
  • Teva pharmaceuticals usa inc
  • Halsey drug co inc
  • Ferndale laboratories inc
  • Barr laboratories inc
  • Cm bundy co
  • Elkins sinn div ah robins co inc
  • Everylife
  • John j ferrante
  • Heather drug co inc
  • Impax laboratories inc
  • Inwood laboratories inc sub forest laboratories inc
  • Lannett co inc
  • Marshall pharmacal corp
  • Panray corp sub ormont drug and chemical co inc
  • L perrigo co
  • Phoenix laboratories inc
  • Purepac pharmaceutical co
  • Private formulations inc
  • Roxane laboratories inc
  • Sandoz inc
  • Sperti drug products inc
  • Superpharm corp
  • Tablicaps inc
  • Udl laboratories inc
  • Valeant pharmaceuticals international
  • Vitarine pharmaceuticals inc
  • West ward pharmaceutical corp
  • Whiteworth towne paulsen inc
  • Pfizer laboratories div pfizer inc
  • Central pharmaceuticals inc
  • Alcon laboratories inc
  • Allergan pharmaceutical
  • Taro pharmaceuticals usa inc
  • Merck and co inc
  • Novartis pharmaceuticals corp
  • Pharmafair inc
  • Alcon universal ltd
  • Bausch and lomb pharmaceuticals inc
  • Sola barnes hind
  • Shionogi pharma inc
  • Ucb inc
  • Amneal pharmaceuticals
  • Paddock laboratories inc
  • Pharmaceutical assoc inc
Packagers
  • Adamis Laboratories
  • Aidarex Pharmacuticals LLC
  • Akorn Inc.
  • Alcon Laboratories
  • Allergan Inc.
  • Amend
  • Amneal Pharmaceuticals
  • A-S Medication Solutions LLC
  • Atlantic Biologicals Corporation
  • Bausch & Lomb Inc.
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • BioMarin Pharmaceuticals Inc.
  • Blansett Pharmacal Co. Inc.
  • Bryant Ranch Prepack
  • C.O. Truxton Inc.
  • Cardinal Health
  • Carlisle Laboratories Inc.
  • Cima Laboratories Inc.
  • Clint Pharmaceutical Inc.
  • Consolidated Midland Corp.
  • Darby Dental Supply Co. Inc.
  • Dexo LLC
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Ethex Corp.
  • Falcon Pharmaceuticals Ltd.
  • Hawthorn Pharmaceuticals
  • Hi Tech Pharmacal Co. Inc.
  • Keene Pharmaceuticals Inc.
  • KV Pharmaceutical Co.
  • Lake Erie Medical and Surgical Supply
  • Laser Pharmaceuticals
  • Lunsco Inc.
  • Lyne Laboratories Inc.
  • Major Pharmaceuticals
  • Marpac
  • Martica Enterprises Inc.
  • Martin Surgical Supply
  • Medisca Inc.
  • Merit Pharmaceuticals
  • MWI Veterinary Supply Co.
  • National Pharmaceuticals
  • Novartis AG
  • Ocusoft
  • OMJ Pharmaceuticals
  • Pacific Pharma Lp
  • Paddock Labs
  • Palmetto Pharmaceuticals Inc.
  • Pfizer Inc.
  • Pharmaceutical Association
  • Pharmacia Inc.
  • Pharmedix
  • Physicians Total Care Inc.
  • Preferred Pharmaceuticals Inc.
  • Prescript Pharmaceuticals
  • Primedics Laboratories
  • Qualitest
  • Rebel Distributors Corp.
  • San Jose Surgical Supply Inc.
  • Sandoz
  • Sciele Pharma Inc.
  • Shionogi Pharma Inc.
  • Stat Rx Usa
  • Taro Pharmaceuticals USA
  • Teva Pharmaceutical Industries Ltd.
  • UCB Pharma
  • Upstate Pharma LLC
  • Vedco Inc.
  • Vintage Pharmaceuticals Inc.
  • Wa Butler Co.
  • Watson Pharmaceuticals
  • Wockhardt Ltd.
Dosage Forms
FormRouteStrength
OintmentTopical
Tablet10 MG
Tablet1 MG
Tablet20 MG
Tablet50 MG
Tablet5 MG
Tablet
TabletOral10 MG
TabletOral2.5 MG
TabletOral20 MG
CreamTopical
TabletOral50 mg
TabletOral5 mg/5mg
Solution / dropsOphthalmic0.125 %
TabletOral
SolutionOral5 mg
LiquidOral
SolutionOral
Injection, suspensionParenteral10 MG
Injection, suspensionParenteral25 MG
Injection, suspensionParenteral50 MG
Tablet2 MG
CreamTopical0.25 %
SolutionOral15 mg/5mL
SyrupOral15 mg/5mL
SyrupOral5 mg/5mL
SyrupOral5 mg/5
TabletOral5 mg/1
Cream0.125 %
Ointment0.125 %
Syrup
Cream50 g
TabletOral5 mg
Prices
Unit descriptionCostUnit
Orapred ODT 48 15 mg Dispersible Tablet Box289.42USD box
Pred Forte 1% Suspension 15ml Bottle97.79USD bottle
PrednisoLONE Sodium Phosphate 1% Solution 10ml Bottle72.82USD bottle
Pred Forte 1% Suspension 10ml Bottle68.06USD bottle
Econopred Plus 1% Suspension 10ml Bottle63.44USD bottle
Solu-Medrol Act-O-Vial 1 g/vial61.25USD vial
Solu-Medrol 1 g/vial60.04USD vial
Pediapred 6.7 mg/5ml Solution 120ml Bottle57.77USD bottle
Pred Mild 0.12% Suspension 10ml Bottle44.33USD bottle
Econopred Plus 1% Suspension 5ml Bottle40.99USD bottle
Solu-Medrol Act-O-Vial 500 mg/vial39.96USD vial
Medrol (Pak) 21 4 mg tablet Disp Pack39.3USD disp
Solu-Medrol 500 mg/vial39.17USD vial
Pred Forte 1% Suspension 5ml Bottle37.12USD bottle
Prednisolone sod ph powder36.11USD g
PrednisoLONE Acetate 1% Suspension 15ml Bottle35.46USD bottle
PrednisoLONE Sodium Phosphate 1% Solution 15ml Bottle34.41USD bottle
Pred Mild 0.12% Suspension 5ml Bottle33.98USD bottle
Methylprednisolone Sod Succin. 1 g/vial32.47USD vial
Solu-medrol 1 gm vial24.43USD vial
PrednisoLONE Acetate 1% Suspension 10ml Bottle24.02USD bottle
Solu-medrol (pf) 500 mg vial20.9USD vial
PrednisoLONE Sodium Phosphate 1% Solution 5ml Bottle19.99USD bottle
Methylprednisolone Sod Succin. 500 mg/vial19.48USD vial
PrednisoLONE Acetate 1% Suspension 5ml Bottle15.99USD bottle
Solu-Medrol Act-O-Vial 125 mg/vial15.94USD vial
Solu-medrol 500 mg vial12.9USD vial
Depo-medrol 80 mg/ml vial11.67USD ml
Depo-Medrol 80 mg/ml11.51USD ml
Pred forte 1% eye drops10.32USD ml
Methylprednisolone Acetate 80 mg/ml9.01USD ml
Methylprednisolone Sod Succin. 125 mg/vial8.9USD vial
Depo-Medrol (Preserved) 80 mg/ml8.89USD ml
Orapred odt 30 mg tablet8.34USD tablet
Orapred odt 15 mg tablet7.97USD tablet
Methylprednisolone Acetate (P) 80 mg/ml6.97USD ml
Omnipred 1% eye drops6.78USD ml
Solu-Medrol Act-O-Vial 40 mg/vial6.72USD vial
Depo-medrol 40 mg/ml vial6.41USD ml
Depo-Medrol 40 mg/ml6.01USD ml
Pred Forte 1 % Suspension5.95USD ml
Solu-medrol (pf) 125 mg vial5.83USD vial
Depo-Medrol (Preserved) 40 mg/ml5.75USD ml
Prednisolone ac 1% eye drop5.75USD ml
Prednisol 1% eye drops5.69USD ml
Pred mild 0.12% eye drops5.14USD ml
Medrol 32 mg tablet5.13USD tablet
Methylprednisolone Acetate 40 mg/ml4.71USD ml
Methylprednisolone Acetate (P) 40 mg/ml4.5USD ml
Econopred plus 1% eye drops3.93USD ml
Orapred odt 10 mg tablet3.89USD tablet
Depo-medrol 20 mg/ml vial3.78USD ml
Methylprednisolone Sod Succin. 40 mg/vial3.77USD vial
Prednisolone sod 1% eye drops3.7USD ml
Medrol 16 mg tablet3.5USD tablet
Prednisolone acetate powder3.36USD g
Prednisolone powder3.36USD g
Depo-Medrol 20 mg/ml2.63USD ml
Medrol 8 mg tablet2.3USD tablet
Ratio-Prednisolone 1 % Suspension2.03USD ml
Sandoz Prednisolone Acetate 1 % Suspension2.03USD ml
Pred Mild 0.12 % Suspension2.02USD ml
Medrol 4 mg tablet1.69USD tablet
Medrol 4 mg dosepak1.59USD each
Sandoz Prednisolone Acetate 0.12 % Suspension1.33USD ml
Millipred dp 5 mg dose pack tablet1.18USD tablet
Medrol 2 mg tablet0.84USD tablet
Orapred 15 mg/5 ml solution0.74USD ml
Millipred 5 mg tablet0.59USD tablet
Prelone 15 mg/5 ml syrup0.54USD ml
Prelone 15 mg/5ml Syrup0.47USD ml
PrednisoLONE Sodium Phosphate 15 mg/5ml Solution0.33USD ml
PrednisoLONE Sodium Phosphate 5 mg/5ml Solution0.23USD ml
Prednisolone 5 mg tablet0.14USD tablet
Pediapred 1 mg/ml Liquid0.14USD ml
Pms-Prednisolone 1 mg/ml Liquid0.07USD ml
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Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5178878No1993-01-122010-01-12US flag
US6221392No2001-04-242018-04-09US flag
US6024981No2000-02-152018-04-09US flag
US6740341No2004-05-252019-11-24US flag
US7799331No2010-09-212028-10-11US flag
US6071523No2000-06-062018-06-03US flag
US6399079No2002-06-042018-06-03US flag
US5881926No1999-03-162016-03-16US flag
US6656482No2003-12-022018-06-03US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)235 °CPhysProp
water solubility223 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP1.62HANSCH,C ET AL. (1995)
logS-3.21ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.239 mg/mLALOGPS
logP1.66ALOGPS
logP1.27ChemAxon
logS-3.2ALOGPS
pKa (Strongest Acidic)12.59ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area94.83 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity98.49 m3·mol-1ChemAxon
Polarizability38.69 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9918
Blood Brain Barrier+0.9383
Caco-2 permeable-0.5096
P-glycoprotein substrateSubstrate0.7861
P-glycoprotein inhibitor INon-inhibitor0.7847
P-glycoprotein inhibitor IINon-inhibitor0.8383
Renal organic cation transporterNon-inhibitor0.7463
CYP450 2C9 substrateNon-substrate0.8496
CYP450 2D6 substrateNon-substrate0.9138
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9406
CYP450 2C9 inhibitorNon-inhibitor0.9072
CYP450 2D6 inhibitorNon-inhibitor0.9418
CYP450 2C19 inhibitorNon-inhibitor0.9253
CYP450 3A4 inhibitorNon-inhibitor0.8902
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9095
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.9597
BiodegradationNot ready biodegradable0.925
Rat acute toxicity1.8914 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.95
hERG inhibition (predictor II)Non-inhibitor0.584
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-00di-1910000000-2f59b266e7257ff0e7ad
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0006-0019000000-34782b355045c38d0504
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-002f-0009000000-4a00ac3c2f4930e108cc
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0005-0689000000-b0eaba9949ae34d0e571
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00dj-0900000000-0a92fbafb31c0170151c
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00dj-0900000000-856481c7f4d3a6d1ac63
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00dj-0900000000-813955b7791f046a3a67
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00di-0900000000-c70a1009bba6e4f3a2c8
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0006-0009000000-e4bce0d078573494d8cd
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-006w-0905000000-94eb00e6ffa4c56ac51b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00dj-0900000000-7797dc6be351391cf57a
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00dj-0900000000-d156992d517e46c9575d
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00r2-0910000000-598b90f7f0f7ba4e13eb
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-00di-0900000000-eed30fed077e1dfffd3b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-002f-0009000000-0af4f657def15fe9274e
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03di-1920000000-5811b59a6f57222762d7
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-06xw-2910000000-84fec77617e1b7a1648b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03dl-0596000000-e0abadaf09054d046b08
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-03xu-0595000000-4f8d30df506ea649fc04
MS/MS Spectrum - , positiveLC-MS/MSsplash10-006x-1986000000-d088900fa4c56b9ff51d
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0159-0900000000-01f9c0e6f14839685506

Targets

Details
1. Glucocorticoid receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...
Gene Name
NR3C1
Uniprot ID
P04150
Uniprot Name
Glucocorticoid receptor
Molecular Weight
85658.57 Da
References
  1. Ikonomidis I, Tzortzis S, Lekakis J, Paraskevaidis I, Andreadou I, Nikolaou M, Kaplanoglou T, Katsimbri P, Skarantavos G, Soucacos P, Kremastinos DT: Lowering interleukin-1 activity with anakinra improves myocardial deformation in rheumatoid arthritis. Heart. 2009 Sep;95(18):1502-7. doi: 10.1136/hrt.2009.168971. Epub 2009 May 28. [PubMed:19482847]
  2. Boudinot FD, D'Ambrosio R, Jusko WJ: Receptor-mediated pharmacodynamics of prednisolone in the rat. J Pharmacokinet Biopharm. 1986 Oct;14(5):469-93. [PubMed:2879901]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Usui T, Saitoh Y, Komada F: Induction of CYP3As in HepG2 cells by several drugs. Association between induction of CYP3A4 and expression of glucocorticoid receptor. Biol Pharm Bull. 2003 Apr;26(4):510-7. doi: 10.1248/bpb.26.510. [PubMed:12673034]
  2. Pichard L, Fabre I, Daujat M, Domergue J, Joyeux H, Maurel P: Effect of corticosteroids on the expression of cytochromes P450 and on cyclosporin A oxidase activity in primary cultures of human hepatocytes. Mol Pharmacol. 1992 Jun;41(6):1047-55. [PubMed:1614409]
  3. Litt J. (2016). Litt's Drug eruption & reaction manual (22nd ed.). CRC Press LLc.

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Steroid binding
Specific Function
Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species.
Gene Name
SERPINA6
Uniprot ID
P08185
Uniprot Name
Corticosteroid-binding globulin
Molecular Weight
45140.49 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Frey BM, Frey FJ: Estimation of transcortin concentration by measurements of plasma protein-binding of prednisolone and by electroimmunodiffusion. Br J Clin Pharmacol. 1982 Feb;13(2):245-9. [PubMed:6800390]
  4. Ko HC, Almon RR, Jusko WJ: Effect of corticosteroid binding globulin on the pharmacokinetics of prednisolone in rats. Pharm Res. 1995 Jun;12(6):902-4. [PubMed:7667198]
  5. Angeli A, Frajria R, De Paoli R, Fonzo D, Ceresa F: Diurnal variation of prednisolone binding to serum corticosteroid-binding globulin in man. Clin Pharmacol Ther. 1978 Jan;23(1):47-53. [PubMed:563315]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Pickup ME: Clinical pharmacokinetics of prednisone and prednisolone. Clin Pharmacokinet. 1979 Mar-Apr;4(2):111-28. doi: 10.2165/00003088-197904020-00004. [PubMed:378499]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
References
  1. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [PubMed:8786566]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Troutman MD, Thakker DR: Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharm Res. 2003 Aug;20(8):1210-24. [PubMed:12948019]
  2. Yates CR, Chang C, Kearbey JD, Yasuda K, Schuetz EG, Miller DD, Dalton JT, Swaan PW: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res. 2003 Nov;20(11):1794-803. [PubMed:14661924]

Drug created on June 13, 2005 07:24 / Updated on September 20, 2020 08:50

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