Identification

Name
Prednisolone phosphate
Accession Number
DB14631
Description

Prednisolone phosphate is a glucocorticoid similar to cortisol used for its anti-inflammatory, immunosuppressive, anti-neoplastic, and vasoconstrictive effects.2

Prednisolone phosphate was granted FDA Approval on 19 December 1973.8

Type
Small Molecule
Groups
Approved, Vet approved
Structure
Thumb
Weight
Average: 440.429
Monoisotopic: 440.160004892
Chemical Formula
C21H29O8P
Synonyms
  • Prednisolone 21-(dihydrogen phosphate)
  • Prednisolone 21-monophosphate
  • Prednisolone 21-phosphate

Pharmacology

Indication

Prednisolone phosphate is indication to a number of conditions including treat allergic states, dermatologic diseases, edematous states, endocrine disorders, gastrointestinal diseases, hematologic disorders, neoplastic diseases, nervous system, ophthalmic diseases, respiratory diseases, rheumatic disorders.6,7

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.2 Prednisolone has a short duration of action as the half life is 2-4 hours.5,6 Corticosteroids have a wide therapeutic window as patients make require doses that are multiples of what the body naturally produces.2 Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.2

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.2 Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.2

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-10.2

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.2 High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.2

TargetActionsOrganism
UGlucocorticoid receptor
agonist
Humans
UAnnexin A1
ligand
Humans
Absorption

A 30mg prednisolone oral solution reaches a Cmax of 461.33±77.94ng/mL with an AUC of 2426.1±360.0ng*h/mL.7 A 30mg prednisolone orally disintegrating tablet reaches a Cmax of 420.91±78.28ng/mL with an AUC of 2408.1±361.5ng*h/mL.7

Volume of distribution

The volume of distribution of prednisolone phosphate has been reported as 0.22-0.7L/kg.7

Protein binding

Prednisolone is 70-90% protein bound in plasma.6 Prednisolone typically binds to albumin and corticosteroid binding globulin.3,4

Metabolism

Prednisolone phosphate undergoes ester hydrolysis to prednisolone.1 After this step, the drug undergoes the normal metabolism of prednisolone.

Route of elimination

Prednisolone is predominantly eliminated in the urine as sulfate and glucuronide conjugate metabolites.6

Half-life

The half life of prednisolone is 2-4 hours.6

Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

Data regarding acute overdose is not readily available.6 However, patients experiencing chronic overdose may present with mental symptoms, moon face, abnormal fat deposits, and fluid retention.6 Acute oral overdose may be treated with immediate gastric lavage or emesis followed by symptomatic and supportive treatment.6 Chronic overdosage can be managed by temporary dose reduction or alternate day treatment.6

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
AbirateroneThe metabolism of Abiraterone can be increased when combined with Prednisolone phosphate.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Prednisolone phosphate.
AcarboseThe risk or severity of hyperglycemia can be increased when Prednisolone phosphate is combined with Acarbose.
AceclofenacThe risk or severity of gastrointestinal irritation can be increased when Prednisolone phosphate is combined with Aceclofenac.
AcemetacinThe risk or severity of gastrointestinal irritation can be increased when Prednisolone phosphate is combined with Acemetacin.
AcenocoumarolPrednisolone phosphate may increase the anticoagulant activities of Acenocoumarol.
AcetohexamideThe risk or severity of hyperglycemia can be increased when Prednisolone phosphate is combined with Acetohexamide.
AcetyldigitoxinThe risk or severity of adverse effects can be increased when Prednisolone phosphate is combined with Acetyldigitoxin.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Prednisolone phosphate is combined with Acetylsalicylic acid.
Adenovirus type 7 vaccine liveThe therapeutic efficacy of Adenovirus type 7 vaccine live can be decreased when used in combination with Prednisolone phosphate.
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
  • Take with food. Food reduces GI irritation.

Products

Product Ingredients
IngredientUNIICASInChI Key
Prednisolone sodium phosphateIV021NXA9J125-02-0VJZLQIPZNBPASX-OJJGEMKLSA-L
Product Images
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Inflamase Forte Oph Soln 1%LiquidOphthalmicIolab Pharmaceuticals1988-12-311996-09-09Canada flag
Inflamase Forte Ophthalmic Solution 1%SolutionOphthalmicNovartis Ophthalmics Novartis Pharmaceuticals (Canada) Inc1996-08-202004-07-13Canada flag
Inflamase MildLiquidOphthalmicNovartis Ophthalmics Novartis Pharmaceuticals (Canada) Inc1995-12-312002-07-04Canada flag
Inflamase Oph Soln 0.125%LiquidOphthalmicIolab Pharmaceuticals1988-12-311996-09-09Canada flag
Minims Prednisolone Sodium Phosphate 0.5%Solution / dropsOphthalmicValeant Canada Lp Valeant Canada S.E.C.1995-12-31Not applicableCanada flag
Orapred ODTTablet, orally disintegrating15 mg/1OralConcordia Pharmaceuticals Inc.2006-06-01Not applicableUS flag
Orapred ODTTablet, orally disintegrating30 mg/1OralShionogi2006-06-012015-08-31US flag59630 0702 48 nlmimage10 1e1b8f7c
Orapred ODTTablet, orally disintegrating10 mg/1OralConcordia Pharmaceuticals Inc.2006-06-01Not applicableUS flag
Orapred ODTTablet, orally disintegrating30 mg/1OralConcordia Pharmaceuticals Inc.2006-06-01Not applicableUS flag
Orapred ODTTablet, orally disintegrating10 mg/1OralShionogi2006-06-012015-03-31US 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.

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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
MillipredSolution10 mg/5mLOralLaser Pharmaceuticals Llc2009-07-012017-07-03US flag
MillipredSolution10 mg/5mLOralCerecor, Inc.2014-03-012018-05-31US flag
OrapredSolution15 mg/5mLOralShionogi2000-12-142015-10-31US flag
PediapredSolution5 mg/5mLOralRoyal Pharmaceuticals2003-03-262018-03-16US flag
PMS-prednisolone Sodium Phosphate Ophthalmic Solution ForteSolutionOphthalmicPharmascience Inc1992-12-31Not applicableCanada flag
Prednisolone Sodium PhosphateSolution15 mg/5mLOralPreferred Pharmaceuticals, Inc.2020-06-01Not applicableUS flag
Prednisolone Sodium PhosphateSolution15 mg/5mLOralUnit Dose Services2005-04-25Not applicableUS flag
Prednisolone Sodium PhosphateSolution10 mg/5mLOralEdenbridge Pharmaceuticals Llc2016-12-21Not applicableUS flag
Prednisolone Sodium PhosphateSolution15 mg/5mLOralLohxa2005-04-25Not applicableUS flag
Prednisolone Sodium PhosphateSolution15 mg/5mLOralPhysicians Total Care, Inc.2005-03-03Not 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
Sulfacetamide Sodium and Prednisolone Sodium PhosphatePrednisolone sodium phosphate (2.5 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)SolutionOphthalmicSandoz Inc2004-03-092018-07-31US flag
Sulfacetamide Sodium and Prednisolone Sodium PhosphatePrednisolone sodium phosphate (2.3 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)Solution / dropsOphthalmicRpk Pharmaceuticals, Inc.1995-12-29Not applicableUS flag
Sulfacetamide Sodium and Prednisolone Sodium PhosphatePrednisolone sodium phosphate (2.3 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)Solution / dropsOphthalmicBausch & Lomb Incoporated1995-12-29Not applicableUS flag
Sulfacetamide Sodium and Prednisolone Sodium PhosphatePrednisolone sodium phosphate (2.3 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)Solution / dropsOphthalmicRemedy Repack2016-06-072016-06-08US flag
Sulfacetamide Sodium and Prednisolone Sodium PhosphatePrednisolone sodium phosphate (2.3 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)Solution / dropsOphthalmicREMEDYREPACK INC.2015-01-202018-09-27US flag
Sulfacetamide Sodium and Prednisolone Sodium PhosphatePrednisolone sodium phosphate (2.3 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)Solution / dropsOphthalmicNucare Pharmaceuticals,inc.1995-12-29Not applicableUS flag
Sulfacetamide Sodium and Prednisolone Sodium PhosphatePrednisolone sodium phosphate (2.3 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)Solution / dropsOphthalmicREMEDYREPACK INC.2020-01-30Not applicableUS flag
Sulfacetamide Sodium and Prednisolone Sodium PhosphatePrednisolone sodium phosphate (2.5 mg/1mL) + Sulfacetamide sodium (100 mg/1mL)SolutionOphthalmicRebel Distributors1995-12-29Not applicableUS flag
VasocidinPrednisolone sodium phosphate (2.5 mg/1.0mL) + Sulfacetamide sodium (100.0 mg/1.0mL)SolutionOphthalmicNovartis Ophthalmics1988-08-262010-10-07US flag
Vasocidin Ophthalmic SolutionPrednisolone sodium phosphate (2.5 mg) + Sulfacetamide sodium (100 mg)LiquidOphthalmicIolab Pharmaceuticals1992-12-311996-09-09Canada flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Pred Phos - BromPrednisolone sodium phosphate (10 mg/1mL) + Bromfenac sodium (0.75 mg/1mL)Solution / dropsOphthalmicImprimis Njof, Llc2018-07-02Not applicableUS flag
Pred Phos - GatiPrednisolone sodium phosphate (10 mg/1mL) + Gatifloxacin sesquihydrate (5 mg/1mL)Solution / dropsOphthalmicImprimis Njof, Llc2018-07-022019-07-01US flag
Pred Phos-Gati-BromPrednisolone sodium phosphate (10 mg/1mL) + Bromfenac (0.75 mg/1mL) + Gatifloxacin sesquihydrate (5 mg/1mL)Solution / dropsOphthalmicImprimis Njof, Llc2018-07-022019-07-01US flag

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 / Glycerone phosphates / Monoalkyl phosphates / Tertiary alcohols / Alpha-hydroxy ketones / Secondary alcohols
show 4 more
Substituents
11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / Alcohol / Aliphatic homopolycyclic compound / Alkyl phosphate / Alpha-hydroxy ketone
show 18 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
Not Available

Chemical Identifiers

UNII
752SY38R6C
CAS number
302-25-0
InChI Key
JDOZJEUDSLGTLU-VWUMJDOOSA-N
InChI
InChI=1S/C21H29O8P/c1-19-7-5-13(22)9-12(19)3-4-14-15-6-8-21(25,17(24)11-29-30(26,27)28)20(15,2)10-16(23)18(14)19/h5,7,9,14-16,18,23,25H,3-4,6,8,10-11H2,1-2H3,(H2,26,27,28)/t14-,15-,16-,18+,19-,20-,21-/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-oxoethoxy}phosphonic acid
SMILES

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. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [PubMed:30285357]
  3. 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]
  4. Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [PubMed:23300763]
  5. 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]
  6. FDA Approved Drug Products: Pediapred Prednisolons Sodium Phosphate Oral Solution [Link]
  7. FDA Approved Drug Products: Orapred Prednisolone Sodium Phosphate Orally Disintegrating Tablets [Link]
  8. FDA Approved Drug Products: Inflamase Prednisolone Sodium Phosphate Ophthalmic Drops (Discontinued) [Link]
ChemSpider
65064
ChEBI
145705
ChEMBL
CHEMBL1201231
ZINC
ZINC000004097473
Wikipedia
Prednisolone_sodium_phosphate
AHFS Codes
  • 52:08.00 — Anti-inflammatory Agents
  • 52:08.08 — Corticosteroids

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentCorneal Transplant / Grafting, Corneal / Keratoplasty, Lamellar / Transplantation, Cornea / Transplantation, Corneal1
4TerminatedTreatmentAsthma / Status Asthmaticus / Wheezing1
4TerminatedTreatmentImmune Reconstitution Inflammatory Syndrome / Progressive Multifocal Leukoencephalopathy1
3CompletedPreventionAcute Urinary Tract Infection / Urinary Tract Infection1
3Unknown StatusTreatmentKeratitis, Herpetic / Ocular Herpes Simplex1
2Active Not RecruitingSupportive CareMalignant Tumor of Breast / Neoplasm of the Breast / Oral Mucositis / Stomatitis1
2CompletedTreatmentMalignant Lymphomas1
2RecruitingTreatmentAcanthamoeba Keratitis1
2TerminatedNot AvailableAcute Exacerbation of Remitting Relapsing Multiple Sclerosis / Clinically Isolated Syndrome (CIS)1
2TerminatedTreatmentHemangiomas1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Solution / dropsAuricular (otic)1 %
SolutionOphthalmic
LiquidOphthalmic
SolutionOral300 mg
SolutionOral10 mg/5mL
Solution / dropsOphthalmic
SolutionConjunctival; Ophthalmic1.2 mg
Tablet, orally disintegratingOral10 mg/1
Tablet, orally disintegratingOral30 mg/1
Tablet, orally disintegratingOral15 mg/1
SolutionOral0.1 g
SolutionOral15 mg/5mL
SolutionOral5 mg/5mL
Solution / dropsOphthalmic10 mg/1mL
SolutionOral25 mg/5mL
Liquid; solution / dropsOphthalmic
SolutionOphthalmic
Solution / dropsOphthalmic
LiquidOphthalmic
SolutionOral20 mg/5mL
Syrup
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US6221392No2001-04-242018-04-09US flag
US6024981No2000-02-152018-04-09US flag
US6740341No2004-05-252019-11-24US 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
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.432 mg/mLALOGPS
logP0.92ALOGPS
logP1.15ChemAxon
logS-3ALOGPS
pKa (Strongest Acidic)1.18ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge-2ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area141.36 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity109.37 m3·mol-1ChemAxon
Polarizability43.42 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
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. 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]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Ligand
General Function
Structural molecule activity
Specific Function
Plays important roles in the innate immune response as effector of glucocorticoid-mediated responses and regulator of the inflammatory process. Has anti-inflammatory activity (PubMed:8425544). Play...
Gene Name
ANXA1
Uniprot ID
P04083
Uniprot Name
Annexin A1
Molecular Weight
38713.855 Da
References
  1. Serres M, Viac J, Comera C, Schmitt D: Expression of annexin I in freshly isolated human epidermal cells and in cultured keratinocytes. Arch Dermatol Res. 1994;286(5):268-72. [PubMed:8060156]

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. Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [PubMed:20482443]
  2. 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]
  3. 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]
  4. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxygen binding
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 oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [PubMed:20482443]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
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...

Components:
References
  1. Roberts JK, Moore CD, Romero EG, Ward RM, Yost GS, Reilly CA: Regulation of CYP3A genes by glucocorticoids in human lung cells. F1000Res. 2013 Aug 13;2:173. doi: 10.12688/f1000research.2-173.v2. eCollection 2013. [PubMed:24555085]
  2. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxygen binding
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 oxidizes a variety of structurally un...
Gene Name
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
Catalyzes the conversion of cortisol to the inactive metabolite cortisone. Modulates intracellular glucocorticoid levels, thus protecting the nonselective mineralocorticoid receptor from occupation...
Gene Name
HSD11B2
Uniprot ID
P80365
Uniprot Name
Corticosteroid 11-beta-dehydrogenase isozyme 2
Molecular Weight
44126.06 Da
References
  1. Diederich S, Eigendorff E, Burkhardt P, Quinkler M, Bumke-Vogt C, Rochel M, Seidelmann D, Esperling P, Oelkers W, Bahr V: 11beta-hydroxysteroid dehydrogenase types 1 and 2: an important pharmacokinetic determinant for the activity of synthetic mineralo- and glucocorticoids. J Clin Endocrinol Metab. 2002 Dec;87(12):5695-701. doi: 10.1210/jc.2002-020970. [PubMed:12466373]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
11-beta-hydroxysteroid dehydrogenase [nad(p)] activity
Specific Function
Catalyzes reversibly the conversion of cortisol to the inactive metabolite cortisone. Catalyzes reversibly the conversion of 7-ketocholesterol to 7-beta-hydroxycholesterol. In intact cells, the rea...
Gene Name
HSD11B1
Uniprot ID
P28845
Uniprot Name
Corticosteroid 11-beta-dehydrogenase isozyme 1
Molecular Weight
32400.665 Da
References
  1. Diederich S, Eigendorff E, Burkhardt P, Quinkler M, Bumke-Vogt C, Rochel M, Seidelmann D, Esperling P, Oelkers W, Bahr V: 11beta-hydroxysteroid dehydrogenase types 1 and 2: an important pharmacokinetic determinant for the activity of synthetic mineralo- and glucocorticoids. J Clin Endocrinol Metab. 2002 Dec;87(12):5695-701. doi: 10.1210/jc.2002-020970. [PubMed:12466373]

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. Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [PubMed:23300763]
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
Inducer
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. 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]
  2. Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [PubMed:19953504]

Drug created on September 01, 2018 08:40 / Updated on September 27, 2020 08:17

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