Prednisolone
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Identification
- Summary
Prednisolone is a glucocorticoid used to treat adrenocortical insufficiency, inflammatory conditions, and some cancers.
- Brand Names
- Millipred Dp 6 Day
- Generic Name
- Prednisolone
- DrugBank Accession Number
- DB00860
- Background
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
- 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
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Acne rosacea •••••••••••• •••••••••• Treatment of Acute gouty arthritis •••••••••••• Management of Acute leukemia •••••••••••• Management of Allergic bronchopulmonary aspergillosis •••••••••••• Management of Allergic conjunctivitis •••••••••••• - Contraindications & Blackbox Warnings
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- 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
Target Actions Organism AGlucocorticoid receptor agonistHumans - 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
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- 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
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- 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
- Pathways
Pathway Category Prednisone Action Pathway Drug action Prednisolone Action Pathway Drug action Prednisone Metabolism Pathway Drug metabolism Prednisolone Metabolism Pathway Drug 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Prednisolone can be increased when it is combined with Abametapir. Abatacept The risk or severity of adverse effects can be increased when Prednisolone is combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Prednisolone. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Prednisolone. Acarbose The risk or severity of hyperglycemia can be increased when Prednisolone is combined with Acarbose. - Food Interactions
- Avoid alcohol.
- Take with food. Food reduces irritation.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- 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
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Prednisolone Syrup 5 mg/5 Oral KV Pharmaceuticals 2007-01-09 Not applicable US Prednisolone Tablet 5 mg/1 Oral Watson Pharmaceuticals 2007-03-31 Not applicable US PrednisoLONE Solution 15 mg/5mL Oral Pharmaceutical Associates, Inc. 2007-08-09 Not applicable US PrednisoLONE Syrup 15 mg/5mL Oral Vintage Pharmaceuticals, LLC 2007-12-13 2007-12-13 US - Generic Prescription Products
- Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image เพรดนิคอร์ท Cream 0.5 %w/w Topical บริษัท ซีฟาม จำกัด จำกัด 2001-01-18 Not applicable Thailand - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Cambison Prednisolone (4 mg/1g) + Neomycin sulfate (3 mg/1g) Ointment Topical OASIS TRADING 2018-11-15 Not applicable US Delta - Hädensa - Zäpfchen Prednisolone (1 mg) + Carvasept (1 mg) + Ichthammol (4 mg) + Levomenthol (50 mg) Suppository Rectal Merz Pharma Austria Gmb H 1969-12-10 Not applicable Austria EXOPRED (OPHTHALMIC SUSPENSION) Prednisolone (10 MG/1ML) + Ofloxacin (3 MG/1ML) Suspension Ophthalmic บริษัท แอลเลอร์แกน (ประเทศไทย) จำกัด 2016-07-14 Not applicable Thailand OTIMISIN DAMLA, 10 ML Prednisolone (3.3 mg) + Tetracaine (22 mg) Solution / drops Auricular (otic) HÜSNÜ ARSAN İLAÇLARI A.Ş. 1989-07-19 Not applicable Turkey SOLONE EYE-EAR DROPS Prednisolone (2.6 MG/1ML) + Neomycin (4 MG/1ML) Liquid Auricular (otic); Ophthalmic บริษัท โรงงานเภสัชกรรมแอตแลนติค จำกัด 1987-07-23 2020-09-29 Thailand - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Cambison Prednisolone (4 mg/1g) + Neomycin sulfate (3 mg/1g) Ointment Topical OASIS TRADING 2018-11-15 Not applicable US PREDNI-POS %1 10 ML OFTALMIK SUSPANSIYON Prednisolone (1 %) Suspension Ophthalmic BİEM İLAÇ SAN. VE TİC. A.Ş. 2013-01-29 2020-12-09 Turkey
Categories
- ATC Codes
- D07AA03 — Prednisolone
- D07AA — Corticosteroids, weak (group I)
- D07A — CORTICOSTEROIDS, PLAIN
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- S01CA — Corticosteroids and antiinfectives in combination
- S01C — ANTIINFLAMMATORY AGENTS AND ANTIINFECTIVES IN COMBINATION
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- D07XA — Corticosteroids, weak, other combinations
- D07X — CORTICOSTEROIDS, OTHER COMBINATIONS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- A01AC — Corticosteroids for local oral treatment
- A01A — STOMATOLOGICAL PREPARATIONS
- A01 — STOMATOLOGICAL PREPARATIONS
- A — ALIMENTARY TRACT AND METABOLISM
- R01AD — Corticosteroids
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- L02BX — Other hormone antagonists and related agents
- L02B — HORMONE ANTAGONISTS AND RELATED AGENTS
- L02 — ENDOCRINE THERAPY
- L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
- S01BB — Corticosteroids and mydriatics in combination
- S01B — ANTIINFLAMMATORY AGENTS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- S01CB — Corticosteroids/antiinfectives/mydriatics in combination
- S01C — ANTIINFLAMMATORY AGENTS AND ANTIINFECTIVES IN COMBINATION
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- R01AD — Corticosteroids
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- V03AB — Antidotes
- V03A — ALL OTHER THERAPEUTIC PRODUCTS
- V03 — ALL OTHER THERAPEUTIC PRODUCTS
- V — VARIOUS
- S03BA — Corticosteroids
- S03B — CORTICOSTEROIDS
- S03 — OPHTHALMOLOGICAL AND OTOLOGICAL PREPARATIONS
- S — SENSORY ORGANS
- D07BA — Corticosteroids, weak, combinations with antiseptics
- D07B — CORTICOSTEROIDS, COMBINATIONS WITH ANTISEPTICS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- D07CA — Corticosteroids, weak, combinations with antibiotics
- D07C — CORTICOSTEROIDS, COMBINATIONS WITH ANTIBIOTICS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- S01BA — Corticosteroids, plain
- S01B — ANTIINFLAMMATORY AGENTS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- A01AC — Corticosteroids for local oral treatment
- A01A — STOMATOLOGICAL PREPARATIONS
- A01 — STOMATOLOGICAL PREPARATIONS
- A — ALIMENTARY TRACT AND METABOLISM
- A07EA — Corticosteroids acting locally
- A07E — INTESTINAL ANTIINFLAMMATORY AGENTS
- A07 — ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
- A — ALIMENTARY TRACT AND METABOLISM
- H02AB — Glucocorticoids
- H02A — CORTICOSTEROIDS FOR SYSTEMIC USE, PLAIN
- H02 — CORTICOSTEROIDS FOR SYSTEMIC USE
- H — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
- S02CA — Corticosteroids and antiinfectives in combination
- S02C — CORTICOSTEROIDS AND ANTIINFECTIVES IN COMBINATION
- S02 — OTOLOGICALS
- S — SENSORY ORGANS
- C05AA — Corticosteroids
- C05A — AGENTS FOR TREATMENT OF HEMORRHOIDS AND ANAL FISSURES FOR TOPICAL USE
- C05 — VASOPROTECTIVES
- C — CARDIOVASCULAR SYSTEM
- Drug Categories
- Adrenal Cortex Hormones
- Adrenals
- Agents for Treatment of Hemorrhoids and Anal Fissures for Topical Use
- Alimentary Tract and Metabolism
- Anti-Inflammatory Agents
- Antidiarrheals, Intestinal Antiinflammatory/antiinfective Agents
- Antidotes
- Antineoplastic Agents
- Antineoplastic Agents, Hormonal
- Antineoplastic and Immunomodulating Agents
- Corticosteroid Hormone Receptor Agonists
- Corticosteroids
- Corticosteroids Acting Locally
- Corticosteroids for Local Oral Treatment
- Corticosteroids for Systemic Use
- Corticosteroids for Systemic Use, Plain
- Corticosteroids, Dermatological Preparations
- Corticosteroids, Weak (Group I)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Dermatologicals
- Endocrine Therapy
- Fused-Ring Compounds
- Hormone Antagonists and Related Agents
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hyperglycemia-Associated Agents
- Immunosuppressive Agents
- Intestinal Antiinflammatory Agents
- Nasal Preparations
- Ophthalmological and Otological Preparations
- Ophthalmologicals
- Otologicals
- P-glycoprotein substrates
- Prednisolone and Prodrugs
- Pregnadienes
- Pregnadienetriols
- Pregnanes
- Sensory Organs
- Steroids
- Stomatological Preparations
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- Vasoprotectives
- 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)
- Affected organisms
- Humans and other mammals
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
- [H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
References
- Synthesis Reference
Gunther Bellmann, "Process for producing a sterile prednisolone gel." U.S. Patent US5811417, issued September 22, 1998.
US5811417- General References
- Pickup ME: Clinical pharmacokinetics of prednisone and prednisolone. Clin Pharmacokinet. 1979 Mar-Apr;4(2):111-28. doi: 10.2165/00003088-197904020-00004. [Article]
- 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. [Article]
- 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. [Article]
- Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
- 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. [Article]
- FDA Approved Drug Products: Delta-Cortef Prednisolone Oral Tablets (Discontinued) [Link]
- FDA Approved Drug Products: Prednisolone Oral Syrup [Link]
- Cayman Chemicals: Prednisolone MSDS [Link]
- FDA Approved Drug Products: Prednisolone Acetate Oral Suspension [Link]
- FDA Approved Drug Products: Prednisolone Acetate Ophthalmic Suspension [Link]
- FDA Approved Drug Products: Orapred Prednisolone Sodium Phosphate Orally Disintegrating Tablets [Link]
- FDA Approved Drug Products: Pediapred Prednisolons Sodium Phosphate Oral Solution [Link]
- EMA Approved Drug Products: Lynparza (olaparib) Oral Tablets (March 2023) [Link]
- External Links
- Human Metabolome Database
- HMDB0014998
- KEGG Drug
- D00472
- KEGG Compound
- C07369
- PubChem Compound
- 5755
- PubChem Substance
- 46504847
- ChemSpider
- 5552
- BindingDB
- 19190
- 8638
- ChEBI
- 8378
- ChEMBL
- CHEMBL131
- ZINC
- ZINC000003833821
- Therapeutic Targets Database
- DAP000419
- PharmGKB
- PA451096
- Guide to Pharmacology
- GtP Drug Page
- PDBe Ligand
- TUA
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Prednisolone
- PDB Entries
- 6w9k / 8cc1
- FDA label
- Download (101 KB)
- MSDS
- Download (72.6 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Anti-Neutrophil Cytoplasmic Antibody-Associated Vasculitis / Granulomatosis With Polyangiitis / Microscopic Polyangiitis (MPA) 1 4 Active Not Recruiting Treatment Asthma in Children 1 4 Active Not Recruiting Treatment Minimal Change Disease / Nephrotic Syndrome 1 4 Active Not Recruiting Treatment Rheumatoid Arthritis 1 4 Active Not Recruiting Treatment Sarcoidosis, Pulmonary 1
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
Form Route Strength Tablet Oral 25 mg Ointment Topical Cream Tablet Oral 10 MG Tablet Oral 20 MG Suppository Rectal Injection, powder, for solution Powder, for solution Suspension Ophthalmic Tablet Oral 2.5 MG Ointment Topical Cream Topical 0.4 % Injection Tablet Oral 50 mg Tablet Oral 5 mg/5mg Solution Oral 0.100 g Solution / drops Ophthalmic 0.125 % Solution / drops Auricular (otic); Ophthalmic 10 mg/ml Solution / drops Auricular (otic) Solution / drops Ophthalmic Ointment Ophthalmic 5.000 mg Injection, suspension Parenteral 10 MG Injection, suspension Parenteral 25 MG Suspension Ophthalmic 1 % Injection, suspension Parenteral 50 MG Solution Intra-articular; Intralesional; Intramuscular; Intravenous 25 mg Injection, suspension Parenteral 250 MG Tablet Oral 2 MG Cream Topical 0.25 % Solution Oral 15 mg/5mL Syrup Oral 15 mg/5mL Syrup Oral 5 mg/5mL Syrup Oral 5 mg/5 Tablet Oral 5 mg/1 Tablet Oral 1 mg Cream Topical 0.125 % Ointment Topical 0.125 % Tablet Oral Syrup Oral 3 mg/5ml Syrup Oral Syrup Oral 2.5 MG/5ML Cream Topical 50 g Solution / drops Oral Solution Oral Syrup Oral 10 mg/5ml Suspension Ophthalmic 25 mg/1ml Tablet Oral 5 mg Tablet, film coated 5 mg Tablet, coated Oral 5 mg Liquid Auricular (otic); Ophthalmic Capsule 5 mg Tablet, sugar coated Oral 5 mg Cream Topical 0.5 %w/w - Prices
Unit description Cost Unit Orapred ODT 48 15 mg Dispersible Tablet Box 289.42USD box Pred Forte 1% Suspension 15ml Bottle 97.79USD bottle PrednisoLONE Sodium Phosphate 1% Solution 10ml Bottle 72.82USD bottle Pred Forte 1% Suspension 10ml Bottle 68.06USD bottle Econopred Plus 1% Suspension 10ml Bottle 63.44USD bottle Solu-Medrol Act-O-Vial 1 g/vial 61.25USD vial Solu-Medrol 1 g/vial 60.04USD vial Pediapred 6.7 mg/5ml Solution 120ml Bottle 57.77USD bottle Pred Mild 0.12% Suspension 10ml Bottle 44.33USD bottle Econopred Plus 1% Suspension 5ml Bottle 40.99USD bottle Solu-Medrol Act-O-Vial 500 mg/vial 39.96USD vial Medrol (Pak) 21 4 mg tablet Disp Pack 39.3USD disp Solu-Medrol 500 mg/vial 39.17USD vial Pred Forte 1% Suspension 5ml Bottle 37.12USD bottle Prednisolone sod ph powder 36.11USD g PrednisoLONE Acetate 1% Suspension 15ml Bottle 35.46USD bottle PrednisoLONE Sodium Phosphate 1% Solution 15ml Bottle 34.41USD bottle Pred Mild 0.12% Suspension 5ml Bottle 33.98USD bottle Methylprednisolone Sod Succin. 1 g/vial 32.47USD vial Solu-medrol 1 gm vial 24.43USD vial PrednisoLONE Acetate 1% Suspension 10ml Bottle 24.02USD bottle Solu-medrol (pf) 500 mg vial 20.9USD vial PrednisoLONE Sodium Phosphate 1% Solution 5ml Bottle 19.99USD bottle Methylprednisolone Sod Succin. 500 mg/vial 19.48USD vial PrednisoLONE Acetate 1% Suspension 5ml Bottle 15.99USD bottle Solu-Medrol Act-O-Vial 125 mg/vial 15.94USD vial Solu-medrol 500 mg vial 12.9USD vial Depo-medrol 80 mg/ml vial 11.67USD ml Depo-Medrol 80 mg/ml 11.51USD ml Pred forte 1% eye drops 10.32USD ml Methylprednisolone Acetate 80 mg/ml 9.01USD ml Methylprednisolone Sod Succin. 125 mg/vial 8.9USD vial Depo-Medrol (Preserved) 80 mg/ml 8.89USD ml Orapred odt 30 mg tablet 8.34USD tablet Orapred odt 15 mg tablet 7.97USD tablet Methylprednisolone Acetate (P) 80 mg/ml 6.97USD ml Omnipred 1% eye drops 6.78USD ml Solu-Medrol Act-O-Vial 40 mg/vial 6.72USD vial Depo-medrol 40 mg/ml vial 6.41USD ml Depo-Medrol 40 mg/ml 6.01USD ml Pred Forte 1 % Suspension 5.95USD ml Solu-medrol (pf) 125 mg vial 5.83USD vial Depo-Medrol (Preserved) 40 mg/ml 5.75USD ml Prednisolone ac 1% eye drop 5.75USD ml Prednisol 1% eye drops 5.69USD ml Pred mild 0.12% eye drops 5.14USD ml Medrol 32 mg tablet 5.13USD tablet Methylprednisolone Acetate 40 mg/ml 4.71USD ml Methylprednisolone Acetate (P) 40 mg/ml 4.5USD ml Econopred plus 1% eye drops 3.93USD ml Orapred odt 10 mg tablet 3.89USD tablet Depo-medrol 20 mg/ml vial 3.78USD ml Methylprednisolone Sod Succin. 40 mg/vial 3.77USD vial Prednisolone sod 1% eye drops 3.7USD ml Medrol 16 mg tablet 3.5USD tablet Prednisolone acetate powder 3.36USD g Prednisolone powder 3.36USD g Depo-Medrol 20 mg/ml 2.63USD ml Medrol 8 mg tablet 2.3USD tablet Ratio-Prednisolone 1 % Suspension 2.03USD ml Sandoz Prednisolone Acetate 1 % Suspension 2.03USD ml Pred Mild 0.12 % Suspension 2.02USD ml Medrol 4 mg tablet 1.69USD tablet Medrol 4 mg dosepak 1.59USD each Sandoz Prednisolone Acetate 0.12 % Suspension 1.33USD ml Millipred dp 5 mg dose pack tablet 1.18USD tablet Medrol 2 mg tablet 0.84USD tablet Orapred 15 mg/5 ml solution 0.74USD ml Millipred 5 mg tablet 0.59USD tablet Prelone 15 mg/5 ml syrup 0.54USD ml Prelone 15 mg/5ml Syrup 0.47USD ml PrednisoLONE Sodium Phosphate 15 mg/5ml Solution 0.33USD ml PrednisoLONE Sodium Phosphate 5 mg/5ml Solution 0.23USD ml Prednisolone 5 mg tablet 0.14USD tablet Pediapred 1 mg/ml Liquid 0.14USD ml Pms-Prednisolone 1 mg/ml Liquid 0.07USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5178878 No 1993-01-12 2010-01-12 US US6221392 No 2001-04-24 2018-04-09 US US6024981 No 2000-02-15 2018-04-09 US US6740341 No 2004-05-25 2019-11-24 US US7799331 No 2010-09-21 2028-10-11 US US6071523 No 2000-06-06 2018-06-03 US US6399079 No 2002-06-04 2018-06-03 US US5881926 No 1999-03-16 2016-03-16 US US6656482 No 2003-12-02 2018-06-03 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 235 °C PhysProp water solubility 223 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 1.62 HANSCH,C ET AL. (1995) logS -3.21 ADME Research, USCD - Predicted Properties
Property Value Source Water Solubility 0.239 mg/mL ALOGPS logP 1.66 ALOGPS logP 1.27 Chemaxon logS -3.2 ALOGPS pKa (Strongest Acidic) 12.59 Chemaxon pKa (Strongest Basic) -2.9 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 5 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 94.83 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 98.49 m3·mol-1 Chemaxon Polarizability 38.69 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9918 Blood Brain Barrier + 0.9383 Caco-2 permeable - 0.5096 P-glycoprotein substrate Substrate 0.7861 P-glycoprotein inhibitor I Non-inhibitor 0.7847 P-glycoprotein inhibitor II Non-inhibitor 0.8383 Renal organic cation transporter Non-inhibitor 0.7463 CYP450 2C9 substrate Non-substrate 0.8496 CYP450 2D6 substrate Non-substrate 0.9138 CYP450 3A4 substrate Substrate 0.7407 CYP450 1A2 substrate Non-inhibitor 0.9406 CYP450 2C9 inhibitor Non-inhibitor 0.9072 CYP450 2D6 inhibitor Non-inhibitor 0.9418 CYP450 2C19 inhibitor Non-inhibitor 0.9253 CYP450 3A4 inhibitor Non-inhibitor 0.8902 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9095 Ames test Non AMES toxic 0.9132 Carcinogenicity Non-carcinogens 0.9597 Biodegradation Not ready biodegradable 0.925 Rat acute toxicity 1.8914 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.95 hERG inhibition (predictor II) Non-inhibitor 0.584
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 194.9290006 predictedDarkChem Lite v0.1.0 [M-H]- 194.5804006 predictedDarkChem Lite v0.1.0 [M-H]- 193.7266006 predictedDarkChem Lite v0.1.0 [M-H]- 186.31522 predictedDeepCCS 1.0 (2019) [M-H]- 194.9290006 predictedDarkChem Lite v0.1.0 [M-H]- 194.5804006 predictedDarkChem Lite v0.1.0 [M-H]- 193.7266006 predictedDarkChem Lite v0.1.0 [M-H]- 186.31522 predictedDeepCCS 1.0 (2019) [M+H]+ 196.6404006 predictedDarkChem Lite v0.1.0 [M+H]+ 194.5796006 predictedDarkChem Lite v0.1.0 [M+H]+ 194.5713006 predictedDarkChem Lite v0.1.0 [M+H]+ 188.21063 predictedDeepCCS 1.0 (2019) [M+H]+ 196.6404006 predictedDarkChem Lite v0.1.0 [M+H]+ 194.5796006 predictedDarkChem Lite v0.1.0 [M+H]+ 194.5713006 predictedDarkChem Lite v0.1.0 [M+H]+ 188.21063 predictedDeepCCS 1.0 (2019) [M+Na]+ 196.2325006 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.6212006 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.86131 predictedDeepCCS 1.0 (2019) [M+Na]+ 196.2325006 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.6212006 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.86131 predictedDeepCCS 1.0 (2019)
Targets
![](/assets/locked/DrugTargets2-1d1d534575da54e734c316d80c9fb35f8210c070dca913c026f8e58660e3e71a.png)
- 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
- 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. [Article]
- Boudinot FD, D'Ambrosio R, Jusko WJ: Receptor-mediated pharmacodynamics of prednisolone in the rat. J Pharmacokinet Biopharm. 1986 Oct;14(5):469-93. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- 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
- 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. [Article]
- 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. [Article]
- 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
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- 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
- Pickup ME: Clinical pharmacokinetics of prednisone and prednisolone. Clin Pharmacokinet. 1979 Mar-Apr;4(2):111-28. doi: 10.2165/00003088-197904020-00004. [Article]
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
- 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. [Article]
- 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
- 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. [Article]
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at June 05, 2024 03:45