Identification

Name
Prednisolone acetate
Accession Number
DB15566
Description

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
Small Molecule
Groups
Approved, Vet approved
Structure
Thumb
Weight
Average: 402.4807
Monoisotopic: 402.204238692
Chemical Formula
C23H30O6
Synonyms
Not Available

Pharmacology

Indication

Prednisolone acetate is indicated as an anti-inflammatory or immunosuppressive agent for allergic, dermatologic, gastrointestinal, hematologic, ophthalmologic, nervous system, renal, respiratory, rheumatologic, or infectious conditions.5 Prednisolone acetate is also indicated in organ transplant patients, as well as endocrine or neoplastic conditions.5

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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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 action as the half life is 2-3 hours.5 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

Prednisolone acetate oral suspension given at a dose equivalent to 15mg prednisolone has a Cmax of 321.1ng/hr, a Tmaxof 1-2 hours, and an AUC of 1999.4ng*hr/mL.5 The absorption pharmacokinetics of prednisolone acetate are not significantly different from a comparable dose of prednisolone.5

Volume of distribution

The volume 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.1 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-3,11,30-trione (M-XVII), 20α-dihydro-prednisone (M-V), 6βhydroxy-prednisone (M-XII), 6α-hydroxy-prednisone (M-XIII), or 20β-dihydro-prednisone (M-IV).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 (M-XI), 20α-dihydro-prednisolone (M-III), 20β-dihydro-prednisolone (M-II), 6αhydroxy-prednisolone (M-VII), or 6βhydroxy-prednisolone(M-VI).2 6αhydroxy-prednisolone is metabolized to 6α,11β,17α,20β,21-pentahydroxypregnan-1,4-diene-3-one (M-X).2 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).2 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.2 These metabolites and their glucuronide conjugates are excreted predominantly in the urine.2,5

Hover over products below to view reaction partners

Route of elimination

Prednisolone acetate is predominantly excreted in the urine.5

Half-life

Oral prednisolone acetate has a plasma half life of 2-3 hours.5

Clearance

Data regarding the clearance of prednisolone acetate is not readily available.6,7,8

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

The oral LD50 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.5 Overdose of oral prednisolone acetate may be treated by gastric lavage or inducing vomiting if the overdose was recent, as well as supportive and symptomatic therapy.5 Chronic overdosage may be treated by dose reduction or treating patients on alternate days.5 An overdose by the ophthalmic route is not expected to cause problems.5

Affected organisms
  • Humans and other mammals
Pathways
Not Available
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 acetate can be increased when it is combined with Abametapir.
AcarboseThe risk or severity of hyperglycemia can be increased when Prednisolone acetate is combined with Acarbose.
AcetohexamideThe risk or severity of hyperglycemia can be increased when Prednisolone acetate is combined with Acetohexamide.
AcetyldigitoxinThe risk or severity of adverse effects can be increased when Prednisolone acetate is combined with Acetyldigitoxin.
Adenovirus type 7 vaccine liveThe therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Prednisolone acetate.
AlbiglutideThe risk or severity of hyperglycemia can be increased when Prednisolone acetate is combined with Albiglutide.
AlogliptinThe risk or severity of hyperglycemia can be increased when Prednisolone acetate is combined with Alogliptin.
AminoglutethimideThe therapeutic efficacy of Prednisolone acetate can be decreased when used in combination with Aminoglutethimide.
Anthrax immune globulin humanThe therapeutic efficacy of Anthrax immune globulin human can be decreased when used in combination with Prednisolone acetate.
Anthrax vaccineThe therapeutic efficacy of Anthrax vaccine can be decreased when used in combination with Prednisolone acetate.
Additional Data Available
  • Extended Description
    Extended Description

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

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  • Severity
    Severity

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

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  • Evidence Level
    Evidence Level

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

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  • Action
    Action

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

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Food Interactions
  • Avoid excessive or chronic alcohol consumption. Alcohol may cause gastric irritation.
  • Take with food. Food reduces gastrointestinal irritation.

Products

Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ak Tate Oph Sus 1%SuspensionOphthalmicSandoz Canada Incorporated1985-12-312008-08-07Canada
Diopred Suspension 1%SuspensionOphthalmicSandoz Canada Incorporated1994-12-31Not applicableCanada
EconopredSuspension10 mg/10mLOphthalmicPhysicians Total Care, Inc.1994-05-052011-05-31Us
EconopredSuspension1.25 mg/1OphthalmicALCON LABORATORIES, INC.2006-09-13Not applicableUs
EconopredSuspension10 mg/1mgOphthalmicAlcon, Inc.1973-07-102007-12-31Us
Flo-PredSuspension16.7 mg/5mLOralTaro Pharmaceuticals U.S.A., Inc.2008-01-17Not applicableUs
Flo-PredSuspension5 mg/5mLOralTaro Pharmaceuticals U.S.A., Inc.2008-07-072008-07-07Us
OmnipredSuspension10 mg/1mLOphthalmicALCON LABORATORIES, INC.2007-08-022007-08-02Us
OmnipredSuspension10 mg/1mLOphthalmicALCON LABORATORIES, INC.2007-11-062021-05-31Us
Pred ForteSuspension / drops10 mg/1mLOphthalmicPhysicians Total Care, Inc.1973-06-012012-06-30Us
Additional Data Available
  • Application Number
    Application Number

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

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  • Product Code
    Product Code

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

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Prednisolone AcetateSuspension10 mg/1mLOphthalmicPhysicians Total Care, Inc.2002-11-04Not applicableUs
Prednisolone AcetateSuspension / drops10 mg/1mLOphthalmicPacific Pharma, Inc.1997-08-19Not applicableUs
Prednisolone AcetateSuspension / drops10 mg/1mLOphthalmicA-S Medication Solutions1997-08-192017-10-31Us
Prednisolone AcetateSuspension / drops10 mg/1mLOphthalmicNucare Pharmaceuticals,inc.1997-08-192019-12-31Us
Prednisolone AcetateSuspension / drops10 mg/1mLOphthalmicClinical Solutions Wholsesale1994-12-152017-06-22Us
Prednisolone AcetateSuspension / drops10 mg/1mLOphthalmicH.J. Harkins Company1997-08-19Not applicableUs
Prednisolone AcetateSuspension / drops10 mg/1mLOphthalmicSandoz Inc1994-12-15Not applicableUs
Prednisolone AcetateSuspension / drops10 mg/1mLOphthalmicA-S Medication Solutions1994-12-152019-07-31Us
Prednisolone AcetateSuspension / drops10 mg/1OphthalmicRemedy Repack2013-02-062015-05-12Us
Prednisolone AcetateSuspension / drops10 mg/1mLOphthalmicNucare Pharmaceuticals,inc.1997-08-19Not applicableUs
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
BlephamidePrednisolone acetate (0.2 %) + Sulfacetamide sodium (10 %)Solution / dropsOphthalmicAllergan1989-12-31Not applicableCanada
BlephamidePrednisolone acetate (2 mg/1g) + Sulfacetamide sodium (100 mg/1g)OintmentOphthalmicA S Medication Solutions1987-01-01Not applicableUs
BlephamidePrednisolone acetate (2 mg/1g) + Sulfacetamide sodium (100 mg/1g)OintmentOphthalmicPhysicians Total Care, Inc.2012-03-04Not applicableUs
BlephamidePrednisolone acetate (2 mg/1g) + Sulfacetamide sodium (100 mg/1g)OintmentOphthalmicAllergan1987-01-01Not applicableUs
BlephamidePrednisolone acetate (2 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)Suspension / dropsOphthalmicA S Medication Solutions1961-10-01Not applicableUs
BlephamidePrednisolone acetate (2 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)Suspension / dropsOphthalmicPhysicians Total Care, Inc.1961-10-01Not applicableUs
BlephamidePrednisolone acetate (2 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)Suspension / dropsOphthalmicAllergan, Inc.1961-10-01Not applicableUs
Blephamide S.O.P.Prednisolone acetate (0.2 %) + Sulfacetamide sodium (10 %)OintmentOphthalmicAllergan1974-12-312019-07-15Canada
Dioptimyd OintmentPrednisolone acetate (5 mg) + Sulfacetamide sodium (100 mg)OintmentOphthalmic; TopicalPharma Stulln Inc.1994-12-312019-12-04Canada
Metimyd Oph SusPrednisolone acetate (5 mg) + Sulfacetamide sodium (100 mg)SuspensionOphthalmicSchering Plough1956-12-311999-07-22Canada
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Pred-BromPrednisolone acetate (10 mg/1mL) + Bromfenac (0.75 mg/1mL)Suspension / dropsOphthalmicImprimisRx NJ2018-02-01Not applicableUs
Pred-BromPrednisolone acetate (10 mg/1mL) + Bromfenac sodium (0.75 mg/1mL)Suspension / dropsOphthalmicImprimis Njof, Llc2018-01-05Not applicableUs
Pred-GatiPrednisolone acetate (10 mg/1mL) + Gatifloxacin hemihydrate (5 mg/1mL)SuspensionOphthalmicImprimisRx NJ2018-03-01Not applicableUs
Pred-GatiPrednisolone acetate (10 mg/1mL) + Gatifloxacin sesquihydrate (5 mg/1mL)Suspension / dropsOphthalmicImprimis Njof, Llc2018-01-052019-07-01Us
Pred-Gati-BromPrednisolone acetate (10 mg/1mL) + Bromfenac sodium (0.75 mg/1mL) + Gatifloxacin sesquihydrate (5 mg/1mL)Suspension / dropsOphthalmicImprimis Njof, Llc2018-01-122019-07-01Us
Pred-Gati-BromPrednisolone acetate (10 mg/1mL) + Bromfenac (0.75 mg/1mL) + Gatifloxacin hemihydrate (5 mg/1mL)Suspension / dropsOphthalmicImprimisRx NJ2018-01-01Not applicableUs
Pred-Gati-BromPrednisolone acetate (10 mg/1mL) + Bromfenac (0.75 mg/1mL) + Gatifloxacin sesquihydrate (5 mg/1mL)Suspension / dropsOphthalmicImprims Njof, Llc2018-01-052019-07-01Us
Prednisolone Acetate PFPrednisolone acetate (10 mg/1mL)Suspension / dropsOphthalmicImprimisRx NJ2018-01-01Not applicableUs

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class 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-1,4-steroids / 17-hydroxysteroids / 11-beta-hydroxysteroids / Delta-1,4-steroids / Alpha-acyloxy ketones / Tertiary alcohols / Alpha-hydroxy ketones / Secondary alcohols / Cyclic ketones
show 5 more
Substituents
11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / Alcohol / Aliphatic homopolycyclic compound / Alpha-acyloxy ketone / Alpha-hydroxy ketone
show 17 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
corticosteroid hormone (CHEBI:8380)

Chemical Identifiers

UNII
8B2807733D
CAS number
52-21-1
InChI Key
LRJOMUJRLNCICJ-JZYPGELDSA-N
InChI
InChI=1S/C23H30O6/c1-13(24)29-12-19(27)23(28)9-7-17-16-5-4-14-10-15(25)6-8-21(14,2)20(16)18(26)11-22(17,23)3/h6,8,10,16-18,20,26,28H,4-5,7,9,11-12H2,1-3H3/t16-,17-,18-,20+,21-,22-,23-/m0/s1
IUPAC Name
2-[(1R,3aS,3bS,9aR,9bS,10S,11aS)-1,10-dihydroxy-9a,11a-dimethyl-7-oxo-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-1-yl]-2-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

References

General References
  1. Musson DG, Bidgood AM, Olejnik O: Assay methodology for prednisolone, prednisolone acetate and prednisolone sodium phosphate in rabbit aqueous humor and ocular physiological solutions. J Chromatogr. 1991 Apr 19;565(1-2):89-102. doi: 10.1016/0378-4347(91)80373-k. [PubMed:1874907]
  2. 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]
  3. Doppenschmitt SA, Scheidel B, Harrison F, Surmann JP: Simultaneous determination of prednisolone, prednisolone acetate and hydrocortisone in human serum by high-performance liquid chromatography. J Chromatogr B Biomed Appl. 1995 Dec 15;674(2):237-46. doi: 10.1016/0378-4347(95)00317-7. [PubMed:8788152]
  4. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [PubMed:30285357]
  5. FDA Approved Drug Products: Prednisolone Acetate Oral Suspension [Link]
  6. FDA Approved Drug Products: Prednisolone Acetate Ophthalmic Suspension [Link]
  7. FDA Approved Drug Products: Prednisolone Acetate Ophthalmic Suspension 1% [Link]
  8. Greenstone LLC: Prednisolone Acetate Ophthalmic Suspension MSDS [Link]
KEGG Compound
C08180
PubChem Compound
5834
ChemSpider
5629
ChEBI
8380
ChEMBL
CHEMBL1152
ZINC
ZINC000003875348
Wikipedia
Prednisolone_acetate
AHFS Codes
  • 52:08.00 — Anti-inflammatory Agents
  • 52:08.08 — Corticosteroids

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingPreventionDry Eye Syndromes1
4Active Not RecruitingTreatmentCorneal Transplant / Grafting, Corneal / Keratoplasty, Lamellar / Transplantation, Cornea / Transplantation, Corneal1
4CompletedNot AvailableCataract Surgery1
4CompletedNot AvailableCataracts1
4CompletedNot AvailableMacula Thickening1
4CompletedPreventionCataracts2
4CompletedPreventionCorneal Edema / Fuchs' Dystrophy1
4CompletedTreatmentCataract Surgery1
4CompletedTreatmentCataracts1
4CompletedTreatmentCataracts / Corneal Edema / Retinal Structural Change, Deposit and Degeneration / Visual Acuity Reduced Transiently1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
OintmentOphthalmic
Solution / dropsOphthalmic
OintmentOphthalmic; Topical
SuspensionOphthalmic1.25 mg/1
SuspensionOphthalmic10 mg/1mg
SuspensionOphthalmic10 mg/10mL
SuspensionOral16.7 mg/5mL
SuspensionOral5 mg/5mL
SolutionOphthalmic
Suspension / dropsOphthalmic
Solution / dropsOphthalmic1 %
Solution / dropsOphthalmic0.12 %
Suspension / dropsOphthalmic1.2 mg/1mL
SuspensionOphthalmic
SuspensionOphthalmic10 mg/1mL
Suspension / dropsOphthalmic10 mg/1mL
Suspension / dropsOphthalmic10 mg/1
SuspensionOphthalmic
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US7799331No2010-09-212028-10-11Us
US6071523No2000-06-062018-06-03Us
US6399079No2002-06-042018-06-03Us
US5881926No1999-03-162016-03-16Us
US6656482No2003-12-022018-06-03Us
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)238ChemSpider
logP1.332ChemSpider
Predicted Properties
PropertyValueSource
Water Solubility0.0417 mg/mLALOGPS
logP2.17ALOGPS
logP1.71ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)12.61ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area100.9 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity107.64 m3·mol-1ChemAxon
Polarizability42.93 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
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-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-000i-0797000000-836ba07555e28d36300f
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00dj-2950000000-e2793b767fd6fd52b223

Targets

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. Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [PubMed:15634032]

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 October 23, 2019 15:18 / Updated on August 02, 2020 22:18

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