What Is Prednisolone Acetate Used For

Prednisolone acetate

Summary

Prednisolone acetate is a glucocorticoid used to treat a broad variety of endocrine, inflammatory, and immune conditions equally well as for palliation of neoplastic conditions.

Make Names

Blephamide, Econopred Plus, Flo-pred, Pred Forte, Pred Mild, Pred-Chiliad

Generic Name

Prednisolone acetate

DrugBank Accretion Number

DB15566

Background

Prednisolone acetate is a prednisolone molecule bound to an acetate functional group by an ester bond.⁵

Prednisolone acetate was granted FDA approval in 1955.⁵

Type

Pocket-sized Molecule

Groups

Canonical, Vet approved

Construction

Weight: Boilerplate: 402.4807
Monoisotopic: 402.204238692
Chemical Formula: C₂₃H₃₀O_vi

Synonyms

Prednisolone acetate

Indication

Prednisolone acetate is indicated every bit an anti-inflammatory or immunosuppressive agent for allergic, dermatologic, gastrointestinal, hematologic, ophthalmologic, nervous organization, renal, respiratory, rheumatologic, or infectious conditions.^v Prednisolone acetate is also indicated in organ transplant patients, as well every bit endocrine or neoplastic conditions.^v

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Associated Atmospheric condition

Inflammation

Inflammatory Conditions

Ocular Infections, Irritations and Inflammations

Ocular Inflammation

Transplanted Organ Rejection

Contraindications & Blackbox Warnings

Avoid life-threatening adverse drug events

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Pharmacodynamics

Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals.⁴ Prednisolone acetate has a short duration of activeness as the half life is 2-3 hours.⁵ Corticosteroids accept a wide therapeutic window as patients make crave doses that are multiples of what the torso naturally produces.^iv Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal centrality suppression and increased susceptibility to infections.^four

Mechanism of activity

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

Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acrid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes similar interleukin-ten.^four

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

Target Actions Organism

AGlucocorticoid receptor
agonist
Humans

Absorption

Target	Actions	Organism
AGlucocorticoid receptor	agonist	Humans

Prednisolone acetate oral pause given at a dose equivalent to 15mg prednisolone has a C_max of 321.1ng/hr, a T_maxof i-ii hours, and an AUC of 1999.4ng*hr/mL.^v The assimilation pharmacokinetics of prednisolone acetate are non significantly different from a comparable dose of prednisolone.^v

Book of distribution

The book of distribution of the active metabolite, prednisolone, is 0.22/0.7L/kg.⁵

Protein binding

The active metabolite, prednisolone, is 70-90% protein bound in plasma.⁵

Metabolism

Prednisolone acetate undergoes ester hydrolysis to prednisolone.^one After this step, the drug undergoes the normal metabolism of prednisolone.

Prednisolone can be reversibly metabolized to prednisone which is then metabolized to 17α,21-dihydroxy-pregnan-1,4,6-trien-3,xi,30-trione (One thousand-XVII), 20α-dihydro-prednisone (Grand-V), 6βhydroxy-prednisone (M-XII), 6α-hydroxy-prednisone (1000-13), or 20β-dihydro-prednisone (One thousand-Four).² 20β-dihydro-prednisone is metabolized to 17α,20ξ,21-trihydroxy-5ξ-pregn-1-en-3,11-dione(M-Xviii).² Prednisolone is metabolized to Δ6-prednisolone (Yard-Xi), 20α-dihydro-prednisolone (M-Three), 20β-dihydro-prednisolone (1000-II), 6αhydroxy-prednisolone (One thousand-Vii), or 6βhydroxy-prednisolone(M-VI).² 6αhydroxy-prednisolone is metabolized to 6α,11β,17α,20β,21-pentahydroxypregnan-i,4-diene-iii-one (M-X).^two 6βhydroxy-prednisolone is metabolized to 6β,11β,17α,20β,21-pentahydroxypregnan-1,4-diene-3-i (Chiliad-VIII), 6β,11β,17α,20α,21-pentahydroxypregnan-1,iv-diene-3-one (M-Ix), and 6β,11β,17α,21-tetrahydroxy-5ξ-pregn-ane-en-iii,20-dione (K-14).² MVIII is metabolized to 6β,11β,17α,20β,21-pentahydroxy-5ξ-pregn-1-en-3-one (M-XV) and so to MXIV, while MIX is metabolized to 6β,11β,17α,20α,21-pentahydroxy-5ξ-pregn-1-en-iii-one (M-XVI) and then to MXIV.^two These metabolites and their glucuronide conjugates are excreted predominantly in the urine.^2,five

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Route of elimination

Prednisolone acetate is predominantly excreted in the urine.^five

Half-life

Oral prednisolone acetate has a plasma half life of ii-3 hours.⁵

Clearance

Data regarding the clearance of prednisolone acetate is non readily available.^6,7,8

Adverse Effects

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Toxicity

The oral LD_fifty of prednisolone acetate in mice is 1680 mg/kg.⁸ Patients experiencing an overdose of oral prednisolone acetate may experience an increased severity in the adverse effects of corticosteroids.^v Overdose of oral prednisolone acetate may be treated by gastric lavage or inducing vomiting if the overdose was recent, too equally supportive and symptomatic therapy.⁵ Chronic overdosage may be treated by dose reduction or treating patients on alternate days.^v An overdose by the ophthalmic route is not expected to cause problems.⁵

Pathways

Non Available

Pharmacogenomic Effects/ADRs

Not Available

Drug Interactions

This information should non exist 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 hateful no interactions exist.

Drug	Interaction
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Abametapir	The serum concentration of Prednisolone acetate tin can be increased when information technology is combined with Abametapir.
Abemaciclib	The metabolism of Abemaciclib can be increased when combined with Prednisolone acetate.
Acalabrutinib	The metabolism of Acalabrutinib tin can be increased when combined with Prednisolone acetate.
Acarbose	The take chances or severity of hyperglycemia tin be increased when Prednisolone acetate is combined with Acarbose.
Aceclofenac	The risk or severity of gastrointestinal irritation can be increased when Prednisolone acetate is combined with Aceclofenac.
Acemetacin	The risk or severity of gastrointestinal irritation can be increased when Prednisolone acetate is combined with Acemetacin.
Acenocoumarol	Prednisolone acetate may increase the anticoagulant activities of Acenocoumarol.
Acetohexamide	The take chances or severity of hyperglycemia can be increased when Prednisolone acetate is combined with Acetohexamide.
Acetyldigitoxin	The risk or severity of adverse effects tin be increased when Prednisolone acetate is combined with Acetyldigitoxin.
Acetylsalicylic acid	The risk or severity of gastrointestinal irritation tin can be increased when Prednisolone acetate is combined with Acetylsalicylic acid.

Food Interactions

Avoid excessive or chronic booze consumption. Alcohol may cause gastric irritation.

Accept with food. Nutrient reduces gastrointestinal irritation.

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dosage, class, labeller, route of assistants, and marketing flow.

Admission drug production data from over 10 global regions.

Brand Proper name Prescription Products

Proper noun	Dosage	Strength	Road	Labeller	Marketing Outset	Marketing Terminate
Ak Tate Oph Sus 1%	Suspension	1 %	Ophthalmic	Sandoz Canada Incorporated	1985-12-31	2008-08-07
Diopred Suspension 1%	Suspension	one %	Ophthalmic	Sandoz Canada Incorporated	1994-12-31	Non applicable
Econopred	Break	x mg/1mg	Ophthalmic	ALCON LABORATORIES, INC.	1973-07-x	2007-12-31
Econopred	Suspension	1.25 mg/1	Ophthalmic	ALCON LABORATORIES, INC.	2006-09-13	Not applicable
Econopred	Pause	10 mg/10mL	Ophthalmic	Physicians Total Intendance, Inc.	1994-05-05	2011-05-31
Flo-Pred	Break	16.7 mg/5mL	Oral	Taro Pharmaceuticals U.South.A., Inc.	2008-01-17	Not applicable
Flo-Pred	Break	v mg/5mL	Oral	Taro Pharmaceuticals U.S.A., Inc.	2008-07-07	2008-07-07
Omnipred	Break	10 mg/1mL	Ophthalmic	ALCON LABORATORIES, INC.	2007-08-02	2007-08-02
Omnipred	Suspension	10 mg/1mL	Ophthalmic	ALCON LABORATORIES, INC.	2007-11-06	2021-05-31
Pred Forte	Solution / drops	ane %	Ophthalmic	Allergan	1974-12-31	Not applicable

Generic Prescription Products

Proper name	Dosage	Strength	Route	Labeller	Marketing Beginning	Marketing Finish
Prednisolone Acetate	Suspension / drops	x mg/1mL	Ophthalmic	A-South Medication Solutions	1994-12-15	Not applicative
Prednisolone Acetate	Intermission	10 mg/1mL	Ophthalmic	Physicians Total Care, Inc.	2002-11-04	Not applicable
Prednisolone Acetate	Interruption / drops	x mg/1mL	Ophthalmic	A-Southward Medication Solutions	1997-08-19	Not applicative
Prednisolone Acetate	Intermission / drops	10 mg/1mL	Ophthalmic	Pacific Pharma, Inc.	1997-08-19	Not applicable
Prednisolone Acetate	Suspension / drops	10 mg/1mL	Ophthalmic	A-Southward Medication Solutions	1994-12-15	Not applicable
Prednisolone Acetate	Intermission / drops	10 mg/1mL	Ophthalmic	Clinical Solutions Wholesale	1994-12-15	2017-06-22
Prednisolone Acetate	Suspension / drops	ten mg/1mL	Ophthalmic	A-Due south Medication Solutions	1997-08-19	Not applicable
Prednisolone Acetate	Suspension / drops	10 mg/1mL	Ophthalmic	H.J. Harkins Company, Inc.	1997-08-19	Not applicable
Prednisolone Acetate	Suspension / drops	ten mg/1mL	Ophthalmic	Nucare Pharmaceuticals,inc.	1997-08-19	Not applicative
Prednisolone Acetate	Break / drops	10 mg/1mL	Ophthalmic	Sandoz Inc	1994-12-15	Not applicable

Mixture Products

Name	Ingredients	Dosage	Road	Labeller	Marketing Showtime	Marketing End
Blephamide	Prednisolone acetate (2 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)	Interruption / drops	Ophthalmic	Physicians Total Care, Inc.	1961-x-01	Not applicable
Blephamide	Prednisolone acetate (ii mg/1g) + Sulfacetamide sodium (100 mg/1g)	Ointment	Ophthalmic	A-S Medication Solutions LLC	1987-01-01	Non applicative
Blephamide	Prednisolone acetate (0.2 %) + Sulfacetamide sodium (x %)	Solution / drops	Ophthalmic	Allergan	1989-12-31	2022-01-21
Blephamide	Prednisolone acetate (2 mg/1g) + Sulfacetamide sodium (100 mg/1g)	Ointment	Ophthalmic	Physicians Full Care, Inc.	2012-03-04	Not applicable
Blephamide	Prednisolone acetate (2 mg/1g) + Sulfacetamide sodium (100 mg/1g)	Ointment	Ophthalmic	Allergan, Inc.	1987-01-01	Not applicable
Blephamide	Prednisolone acetate (2 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)	Suspension / drops	Ophthalmic	Allergan, Inc.	1961-ten-01	Not applicative
Blephamide	Prednisolone acetate (2 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)	Pause / drops	Ophthalmic	A-Due south Medication Solutions LLC	1961-10-01	Not applicable
BLEPHAMIDE % 0,ii + % x GÖZ DAMLASI, SÜSPANSİYON, 5 ML	Prednisolone acetate (2 mg) + Sulfacetamide sodium (100 mg)	Intermission / drops	Ophthalmic	ALLERGAN İLAÇLARI TİC. A.Ş.	2020-08-14	Non applicative
Blephamide Southward.O.P.	Prednisolone acetate (0.2 %) + Sulfacetamide sodium (10 %)	Ointment	Ophthalmic	Allergan	1974-12-31	2019-07-15
CARTEOF®	Prednisolone acetate (10 mg) + Gatifloxacin (3 mg)	Break	Ophthalmic	LABORATORIOS SYNTHESIS Southward.A.S.	2015-07-28	Not applicable

Unapproved/Other Products

Name	Ingredients	Dosage	Road	Labeller	Marketing Outset	Marketing Finish
Ixoba M	Prednisolone acetate (10 mg/1mL) + Ketorolac tromethamine (5 mg/1mL) + Moxifloxacin hydrochloride monohydrate (five mg/1mL)	Kit	Ophthalmic	Brisk Pharmaceuticals, Inc.	2021-08-26	Not applicable
Pred-Brom	Prednisolone acetate (10 mg/1mL) + Bromfenac (0.75 mg/1mL)	Suspension / drops	Ophthalmic	ImprimisRx NJ	2018-02-01	Non applicable
Pred-Brom	Prednisolone acetate (10 mg/1mL) + Bromfenac sodium (0.75 mg/1mL)	Suspension / drops	Ophthalmic	Imprimis Njof, Llc	2018-01-05	Not applicable
Pred-Gati	Prednisolone acetate (10 mg/1mL) + Gatifloxacin hemihydrate (5 mg/1mL)	Suspension	Ophthalmic	ImprimisRx NJ	2018-03-01	Not applicative
Pred-Gati	Prednisolone acetate (10 mg/1mL) + Gatifloxacin sesquihydrate (5 mg/1mL)	Suspension / drops	Ophthalmic	Imprimis Njof, Llc	2018-01-05	2019-07-01
Pred-Gati-Brom	Prednisolone acetate (10 mg/1mL) + Bromfenac (0.75 mg/1mL) + Gatifloxacin sesquihydrate (5 mg/1mL)	Break / drops	Ophthalmic	Imprims Njof, Llc	2018-01-05	2019-07-01
Pred-Gati-Brom	Prednisolone acetate (x mg/1mL) + Bromfenac sodium (0.75 mg/1mL) + Gatifloxacin sesquihydrate (5 mg/1mL)	Suspension / drops	Ophthalmic	Imprimis Njof, Llc	2018-01-12	2019-07-01
Pred-Gati-Brom	Prednisolone acetate (10 mg/1mL) + Bromfenac (0.75 mg/1mL) + Gatifloxacin hemihydrate (v mg/1mL)	Pause / drops	Ophthalmic	ImprimisRx NJ	2018-01-01	Not applicable
Prednisolone Acetate PF	Prednisolone acetate (10 mg/1mL)	Suspension / drops	Ophthalmic	ImprimisRx NJ	2018-01-01	Non applicative

Drug Categories

Adrenal Cortex Hormones

Anti-Inflammatory Agents

Corticosteroids

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

Fused-Ring Compounds

P-glycoprotein substrates

Pregnadienes

Pregnadienetriols

Pregnanes

Prodrugs

Steroids

Chemic TaxonomyProvided by Classyfire

Description: This chemical compound belongs to the form of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety.
Kingdom: Organic compounds
Super Class: Lipids and lipid-like molecules
Class: Steroids and steroid derivatives
Sub Class: Pregnane steroids
Direct Parent: Gluco/mineralocorticoids, progestogins and derivatives
Alternative Parents: 20-oxosteroids / 3-oxo delta-1,four-steroids / 17-hydroxysteroids / 11-beta-hydroxysteroids / Delta-1,4-steroids / Blastoff-acyloxy ketones / 3rd alcohols / Alpha-hydroxy ketones / Secondary alcohols / Cyclic ketones / Cyclic alcohols and derivatives / Carboxylic acid esters / Monocarboxylic acids and derivatives / Organic oxides / Hydrocarbon derivatives evidence five more than
Substituents: xi-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / twenty-oxosteroid / three-oxo-delta-1,4-steroid / iii-oxosteroid / Booze / Aliphatic homopolycyclic compound / Alpha-acyloxy ketone / Alpha-hydroxy ketone / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester / Circadian alcohol / Cyclic ketone / Delta-1,4-steroid / Hydrocarbon derivative / Hydroxysteroid / Ketone / Monocarboxylic acrid or derivatives / Organic oxide / Organic oxygen compound / Organooxygen compound / Oxosteroid / Progestogin-skeleton / Secondary alcohol / Third alcohol show 17 more than
Molecular Framework: Aliphatic homopolycyclic compounds
External Descriptors: corticosteroid hormone (CHEBI:8380)

Affected organisms

Humans and other mammals

UNII: 8B2807733D
CAS number: 52-21-1
InChI Key: LRJOMUJRLNCICJ-JZYPGELDSA-Northward
InChI: InChI=1S/C23H30O6/c1-13(24)29-12-nineteen(27)23(28)9-7-17-sixteen-5-iv-xiv-10-15(25)half-dozen-8-21(fourteen,ii)xx(16)18(26)11-22(17,23)three/h6,8,10,16-xviii,20,26,28H,4-five,7,9,11-12H2,i-3H3/t16-,17-,18-,20+,21-,22-,23-/m0/s1
IUPAC Proper noun: 2-[(1R,3aS,3bS,9aR,9bS,10S,11aS)-i,ten-dihydroxy-9a,11a-dimethyl-7-oxo-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-ane-yl]-ii-oxoethyl acetate
SMILES: [H][C@@]12CC[C@](O)(C(=O)COC(C)=O)[C@@]1(C)C[C@]([H])(O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)C=C[C@]12C

General References

Musson DG, Bidgood AM, Olejnik O: Assay methodology for prednisolone, prednisolone acetate and prednisolone sodium phosphate in rabbit aqueous sense of humor and ocular physiological solutions. J Chromatogr. 1991 April 19;565(1-ii):89-102. doi: 10.1016/0378-4347(91)80373-g. [Article]
Matabosch X, Pozo OJ, Perez-Mana C, Papaseit E, Segura J, Ventura R: Detection and characterization of prednisolone metabolites in human urine past LC-MS/MS. J Mass Spectrom. 2015 Mar;50(3):633-42. doi: 10.1002/jms.3571. [Commodity]
Doppenschmitt SA, Scheidel B, Harrison F, Surmann JP: Simultaneous conclusion of prednisolone, prednisolone acetate and hydrocortisone in homo serum past high-operation liquid chromatography. J Chromatogr B Biomed Appl. 1995 December xv;674(2):237-46. doi: x.1016/0378-4347(95)00317-7. [Article]
Yasir Thou, Sonthalia Due south: Corticosteroid Adverse Effects . [Article]
FDA Approved Drug Products: Prednisolone Acetate Oral Suspension [Link]
FDA Approved Drug Products: Prednisolone Acetate Ophthalmic Suspension [Link]
FDA Approved Drug Products: Prednisolone Acetate Ophthalmic Interruption ane% [Link]
Greenstone LLC: Prednisolone Acetate Ophthalmic Intermission MSDS [Link]

External Links

KEGG Compound: C08180
PubChem Compound: 5834
ChemSpider: 5629
ChEBI: 8380
ChEMBL: CHEMBL1152
ZINC: ZINC000003875348
Wikipedia: Prednisolone_acetate

Clinical Trials

Phase	Condition	Purpose	Weather	Count
4	Active Not Recruiting	Supportive Care	Collagen Crosslinking / Keratoconus, Unstable / Postoperative pain	ane
4	Agile Not Recruiting	Handling	Corneal Transplant / Grafting, Corneal / Keratoplasty, Lamellar / Transplantation, Cornea / Transplantation, Corneal	1
four	Completed	Not Available	Cataract Surgery	i
4	Completed	Not Available	Cataracts	1
4	Completed	Not Available	Macula Thickening	1
four	Completed	Prevention	Cataracts	2
iv	Completed	Prevention	Corneal Edema / Fuchs' Dystrophy	one
4	Completed	Prevention	Dry out Eye Syndrome (DES)	1
4	Completed	Treatment	Allergic Conjunctivitis (Air-conditioning)	1
4	Completed	Treatment	Cataract Surgery	1

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Ointment	Ophthalmic
Solution / drops	Ophthalmic
Suspension	Conjunctival; Ophthalmic
Interruption	Conjunctival; Ophthalmic	5 mg
Ointment	Ophthalmic; Topical
Suspension	Ophthalmic	one.25 mg/1
Interruption	Ophthalmic	10 mg/1mg
Interruption	Ophthalmic	10 mg/10mL
Break	Ophthalmic	1 %
Suspension	Oral	16.7 mg/5mL
Intermission	Oral	v mg/5mL
Kit	Ophthalmic
Injection	Intra-articular; Intramuscular
Solution	Ophthalmic
Suspension / drops	Ophthalmic
Solution / drops	Ophthalmic	1 %
Solution	Ophthalmic	10 mg/ml
Solution / drops	Ophthalmic	0.12 %
Interruption / drops	Ophthalmic	1.2 mg/1mL
Suspension	Ophthalmic
Pause	Ophthalmic	ane.2 mg
Suspension / drops	Ophthalmic
Suspension	Ophthalmic	10 mg/1mL
Suspension / drops	Ophthalmic	x mg/1mL
Interruption / drops	Ophthalmic	10 mg/ane
Injection	Intra-articular; Intramuscular	25 mg/ml
Injection, suspension	Intramuscular
Suspension	Conjunctival; Ophthalmic	10 mg
Suspension	Ophthalmic	10 mg
Interruption	Ophthalmic	0.12 %
Suspension	Ophthalmic	1.two mg
Solution / drops	Ophthalmic
Solution, gel forming / drops	Intraocular	0.5 thousand
Suspension	Intraocular; Ophthalmic
Liquid	Ophthalmic	10 mg/1ml

Prices

Non Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
US7799331	No	2010-09-21	2028-10-eleven
US6071523	No	2000-06-06	2018-06-03
US6399079	No	2002-06-04	2018-06-03
US5881926	No	1999-03-16	2016-03-16
US6656482	No	2003-12-02	2018-06-03

Land

Solid

Experimental Properties

Belongings	Value	Source
melting point (°C)	238	ChemSpider
logP	ane.332	ChemSpider

Predicted Properties

Property	Value	Source
H2o Solubility	0.0417 mg/mL	ALOGPS
logP	two.17	ALOGPS
logP	one.71	ChemAxon
logS	-iv	ALOGPS
pKa (Strongest Acidic)	12.61	ChemAxon
pKa (Strongest Basic)	-2.9	ChemAxon
Physiological Charge	0	ChemAxon
Hydrogen Acceptor Count	5	ChemAxon
Hydrogen Donor Count	2	ChemAxon
Polar Expanse	100.9 Å²	ChemAxon
Rotatable Bond Count	4	ChemAxon
Refractivity	107.64 chiliad^three·mol^-one	ChemAxon
Polarizability	42.93 Åⁱⁱⁱ	ChemAxon
Number of Rings	4	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yep	ChemAxon
Ghose Filter	Yes	ChemAxon
Veber'southward Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET Features

Not Available

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Non Bachelor
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Bachelor
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	Not Bachelor
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	Not Available
MS/MS Spectrum - , positive	LC-MS/MS	splash10-000i-0797000000-836ba07555e28d36300f
MS/MS Spectrum - , positive	LC-MS/MS	splash10-00dj-2950000000-e2793b767fd6fd52b223

Targets

Build, predict & validate automobile-learning models

Apply our structured and evidence-based datasets to unlock new
insights and advance drug research.

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Kind

Protein

Organism

Humans

Pharmacological activeness

Yes

Actions

Agonist

General Function

Zinc ion binding

Specific Function

Receptor for glucocorticoids (GC). Has a dual style of action: equally a transcription cistron that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modula...

Gene Proper noun

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-vii. 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

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 send pathway. It performs a variety of oxidation react...
Factor 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. Clan between consecration of CYP3A4 and expression of glucocorticoid receptor. Biol Pharm Bull. 2003 Apr;26(4):510-7. doi: 10.1248/bpb.26.510. [Commodity]
Pichard 50, Fabre I, Daujat Thou, 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 man hepatocytes. Mol Pharmacol. 1992 Jun;41(vi):1047-55. [Commodity]
Litt J. (2016). Litt's Drug eruption & reaction manual (22nd ed.). CRC Press LLc.

Carriers

Kind: Poly peptide
Organism: Humans
Pharmacological activity: Unknown
Actions: Folder

General Function: Steroid binding
Specific Role: Major transport protein for glucocorticoids and progestins in the blood of near 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 at that place? Nat Rev Drug Discov. 2006 Dec;v(12):993-6. [Commodity]
Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;v(ten):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 February;thirteen(2):245-nine. [Article]
Ko HC, Almon RR, Jusko WJ: Effect of corticosteroid binding globulin on the pharmacokinetics of prednisolone in rats. Pharm Res. 1995 Jun;12(six):902-iv. [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 January;23(1):47-53. [Article]
Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-v. [Commodity]

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Deportment: Binder

General Function: Toxic substance bounden
Specific Office: 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 Proper name: Serum albumin
Molecular Weight: 69365.94 Da

References

Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(ane):61-98. doi: 10.2165/00003088-200544010-00003. [Article]

Transporters

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Inhibitor

General Function: Sodium-contained organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent transport of organic anions such equally sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Proper noun: 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(three):891-6. [Article]

Kind: Protein
Organism: Humans
Pharmacological action: Unknown
Actions: Substrate

General Function: Xenobiotic-transporting atpase activity
Specific Function: Free energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Factor Proper noun: ABCB1
Uniprot ID: P08183
Uniprot Name: Multidrug resistance protein 1
Molecular Weight: 141477.255 Da

References

Troutman Doc, Thakker DR: Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell civilisation 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 Pow: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res. 2003 Nov;20(11):1794-803. [Commodity]

Drug created at October 23, 2019 21:18 / Updated at May 07, 2022 13:55