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Identification
NameMethylprednisolone
Accession NumberDB00959  (APRD00342)
TypeSmall Molecule
GroupsApproved
Description

A prednisolone derivative with similar anti-inflammatory action. [PubChem]

Structure
Thumb
Synonyms
SynonymLanguageCode
(6alpha,11beta)-11,17,21-Trihydroxy-6-methylpregna-1,4-diene-3,20-dioneNot AvailableNot Available
(6α,11β)-11,17,21-trihydroxy-6-methylpregna-1,4-diene-3,20-dioneNot AvailableNot Available
1-dehydro-6alpha-MethylhydrocortisoneNot AvailableNot Available
1-dehydro-6α-methylhydrocortisoneNot AvailableNot Available
6alpha-Methyl-11beta,17alpha,21-triol-1,4-pregnadiene-3,20-dioneNot AvailableNot Available
delta(1)-6alpha-MethylhydrocortisoneNot AvailableNot Available
MedrateNot AvailableNot Available
MedrolNot AvailableNot Available
MedroneNot AvailableNot Available
MethylprednisolonNot AvailableNot Available
MethylprednisoloneNot AvailableNot Available
MethylprednisolonumLatinINN
MetilprednisolonaSpanishINN
SolometNot AvailableNot Available
UrbasonNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Solu-medrolinjection, powder, for solution500 mg/mLintramuscular; intravenousPharmacia and Upjohn Company1959-04-02Not AvailableUs
Solu-medrolinjection, powder, for solution1 g/mLintramuscular; intravenousPharmacia and Upjohn Company1959-04-02Not AvailableUs
Medroltablet2 mgoralPharmacia and Upjohn Company2013-09-20Not AvailableUs
Medroltablet8 mgoralPharmacia and Upjohn Company1957-10-24Not AvailableUs
Solu-medrolinjection, powder, for solution40 mg/mLintramuscular; intravenousPharmacia and Upjohn Company1959-04-02Not AvailableUs
Solu-medrolinjection, powder, for solution40 mg/mLintramuscular; intravenousPharmacia and Upjohn Company1959-04-02Not AvailableUs
Solu-medrolinjection, powder, for solution125 mg/mLintramuscular; intravenousPharmacia and Upjohn Company1959-04-02Not AvailableUs
Solu-medrolinjection, powder, for solution125 mg/mLintramuscular; intravenousPharmacia and Upjohn Company1959-04-02Not AvailableUs
Medroltablet2 mgoralPharmacia and Upjohn Company1957-10-24Not AvailableUs
Medroltablet4 mgoralPharmacia and Upjohn Company1957-10-24Not AvailableUs
Medroltablet16 mgoralPharmacia and Upjohn Company1957-10-24Not AvailableUs
Medroltablet32 mgoralPharmacia and Upjohn Company1957-10-24Not AvailableUs
Depo-medrolinjection, suspension20 mg/mLintralesional; intramuscular; intrasynovial; soft tissuePharmacia and Upjohn Company1959-05-28Not AvailableUs
Depo-medrolinjection, suspension40 mg/mLintralesional; intramuscular; intrasynovial; soft tissuePharmacia and Upjohn Company1959-05-28Not AvailableUs
Depo-medrolinjection, suspension40 mg/mLintralesional; intramuscular; intrasynovial; soft tissuePharmacia and Upjohn Company1959-05-28Not AvailableUs
Depo-medrolinjection, suspension80 mg/mLintralesional; intramuscular; intrasynovial; soft tissuePharmacia and Upjohn Company1959-05-28Not AvailableUs
Depo-medrolinjection, suspension80 mg/mLintralesional; intramuscular; intrasynovial; soft tissuePharmacia and Upjohn Company1959-05-28Not AvailableUs
Solu-medrolinjection, powder, for solution1 g/mLintramuscular; intravenousPharmacia and Upjohn Company1959-04-02Not AvailableUs
Solu-medrolinjection, powder, for solution500 mg/mLintramuscular; intravenousPharmacia and Upjohn Company1959-04-02Not AvailableUs
Solu-medrolkitPharmacia and Upjohn Company1959-04-02Not AvailableUs
Depo-medrolinjection, suspension40 mg/mLintra-articular; intralesional; intramuscular; soft tissuePharmacia and Upjohn Company1959-05-28Not AvailableUs
Depo-medrolinjection, suspension40 mg/mLintralesional; intramuscular; intrasynovial; soft tissuePharmacia and Upjohn Company1959-05-28Not AvailableUs
Depo-medrolinjection, suspension80 mg/mLintra-articular; intralesional; intramuscular; soft tissuePharmacia and Upjohn Company1959-05-28Not AvailableUs
Depo-medrolinjection, suspension80 mg/mLintralesional; intramuscular; intrasynovial; soft tissuePharmacia and Upjohn Company1959-05-28Not AvailableUs
Medroltablet4 mgoralStat Rx USA1957-10-24Not AvailableUs
Depo-medrolinjection, suspension40 mg/mLintralesional; intramuscular; intrasynovial; soft tissueRebel Distributors Corp1959-05-28Not AvailableUs
Medroltablet32 mgoralREMEDYREPACK INC.2011-10-11Not AvailableUs
Depo-medrolinjection, suspension40 mg/mLintramuscularREMEDYREPACK INC.2013-06-11Not AvailableUs
Solu-medrolpowder, for solution125 mg/mLintravenousREMEDYREPACK INC.2011-12-19Not AvailableUs
Depo-medrolinjection, suspension40 mgintramuscularREMEDYREPACK INC.2013-04-10Not AvailableUs
Medroltablet4 mgoralREMEDYREPACK INC.2013-02-19Not AvailableUs
Methylprednisolonetablet4 mgoralLake Erie Medical DBA Quality Care Products LLC2012-02-09Not AvailableUs
Medroltablet4 mgoralA S Medication Solutions Llc1957-10-24Not AvailableUs
Solu-medrolinjection, powder, for solution1 gintravenousREMEDYREPACK INC.2013-02-09Not AvailableUs
Solu-medrolinjection, powder, for solution40 mgintravenousREMEDYREPACK INC.2013-04-15Not AvailableUs
Solu-medrolinjection, powder, for solution40 mg/mLintramuscular; intravenousGeneral Injectables & Vaccines, Inc2010-04-01Not AvailableUs
Solu-medrolinjection, powder, for solution125 mg/mLintramuscular; intravenousGeneral Injectables & Vaccines, Inc2010-04-01Not AvailableUs
Solu-medrolinjection, powder, lyophilized, for solution40 mg/mLintramuscular; intravenousGeneral Injectables & Vaccines, Inc2010-09-01Not AvailableUs
Solu-medrolinjection, powder, lyophilized, for solution125 mg/2mLintramuscular; intravenousGeneral Injectables & Vaccines, Inc2010-09-01Not AvailableUs
Medroltablet4 mgoralA S Medication Solutions Llc1957-10-24Not AvailableUs
Solu-medrolinjection, powder, for solution125 mg/mLintramuscular; intravenousA S Medication Solutions Llc1959-04-02Not AvailableUs
Depo-medrolinjection, suspension80 mg/mLintralesional; intramuscular; intrasynovial; soft tissueDispensing Solutions, Inc.1959-05-28Not AvailableUs
Solu-medrolinjection, powder, for solution40 mg/mLintramuscular; intravenousCardinal Health1959-04-02Not AvailableUs
Solu-medrolinjection, powder, for solution125 mg/mLintramuscular; intravenousCardinal Health1959-04-02Not AvailableUs
Depo-medrolinjection, suspension40 mg/mLintra-articular; intralesional; intramuscular; soft tissueCardinal Health1959-05-28Not AvailableUs
Depo-medrolinjection, suspension80 mg/mLintra-articular; intralesional; intramuscular; soft tissueCardinal Health1959-05-28Not AvailableUs
Solu-medrolinjection, powder, for solution40 mg/mLintramuscular; intravenousCardinal Health1959-04-02Not AvailableUs
Solu-medrolinjection, powder, for solution40 mg/mLintramuscular; intravenousCardinal Health1959-04-02Not AvailableUs
Solu-medrolinjection, powder, for solution125 mg/mLintramuscular; intravenousCardinal Health1959-04-02Not AvailableUs
Solu-medrolinjection, powder, for solution125 mg/mLintramuscular; intravenousCardinal Health1959-04-02Not AvailableUs
Methylprednisolonetablet8 mgoralGreenstone LLC2013-03-25Not AvailableUs
Methylprednisolonetablet16 mgoralGreenstone LLC2013-03-25Not AvailableUs
Methylprednisolonetablet32 mgoralGreenstone LLC2013-03-25Not AvailableUs
Methylprednisolonetablet4 mgoralGreenstone LLC2011-10-11Not AvailableUs
Solu-medrolinjection, powder, for solution125 mg/mLintramuscular; intravenousUs Med Source, Llc2014-07-18Not AvailableUs
Depo-medrolinjection, suspension80 mg/mLintramuscularREMEDYREPACK INC.2014-09-12Not AvailableUs
Methylprednisolonetablet4 mgoralAltura Pharmaceuticals, Inc.2010-01-01Not AvailableUs
Methylprednisolonetablet4 mgoralKeltman Pharmaceuticals Inc.2007-09-14Not AvailableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Methylprednisolonetablet16 mgoralKAISER FOUNDATION HOSPITALS2012-09-12Not AvailableUs
A-methapredinjection, powder, lyophilized, for solution40 mg/mLintramuscular; intravenousHospira, Inc.2005-12-20Not AvailableUs
A-methapredinjection, powder, lyophilized, for solution125 mg/2mLintramuscular; intravenousHospira, Inc.2005-12-20Not AvailableUs
Methylprednisolonetablet4 mgoralQualitest Pharmaceuticals1998-12-22Not AvailableUs
Methylprednisolonetablet4 mgoralSandoz Inc1997-10-31Not AvailableUs
Methylprednisolonetablet4 mgoralSTAT Rx USA LLC1997-10-31Not AvailableUs
Methylprednisolonetablet4 mgoralRebel Distributors Corp.1997-10-31Not AvailableUs
Methylprednisolonetablet4 mgoralAidarex Pharmaceuticals LLC1997-10-31Not AvailableUs
Methylprednisolonetablet4 mgoralLake Erie Medical DBA Quality Care Products LLC1998-12-22Not AvailableUs
Methylprednisolonetablet4 mgoralSTAT Rx USA LLC1997-10-31Not AvailableUs
Methylprednisolonetablet4 mgoralREMEDYREPACK INC.2012-09-05Not AvailableUs
Methylprednisolonetablet4 mgoralREMEDYREPACK INC.2012-03-01Not AvailableUs
Methylprednisolonetablet4 mgoralREMEDYREPACK INC.2012-07-10Not AvailableUs
Methylprednisolonetablet4 mgoralUnit Dose Services1997-10-31Not AvailableUs
Methylprednisolonetablet4 mgoralBreckenridge Pharmaceutical, Inc.2003-11-07Not AvailableUs
Methylprednisolonetablet4 mgoralA S Medication Solutions Llc1998-12-22Not AvailableUs
Methylprednisolonetablet4 mgoralPhysicians Total Care, Inc.2009-10-15Not AvailableUs
Methylprednisolonetablet4 mgoralPhysicians Total Care, Inc.1994-11-29Not AvailableUs
Methylprednisolonetablet4 mgoralDispensing Solutions, Inc.1998-12-22Not AvailableUs
Methylprednisolonetablet4 mgoralClinical Solutions Wholesale1997-10-31Not AvailableUs
Methylprednisolonetablet4 mgoralJUBILANT CADISTA PHARMACEUTICALS, INC.1997-10-31Not AvailableUs
Methylprednisolonetablet8 mgoralJUBILANT CADISTA PHARMACEUTICALS, INC.1997-10-31Not AvailableUs
Methylprednisolonetablet16 mgoralJUBILANT CADISTA PHARMACEUTICALS, INC.1997-10-31Not AvailableUs
Methylprednisolonetablet32 mgoralJUBILANT CADISTA PHARMACEUTICALS, INC.1997-10-31Not AvailableUs
Methylprednisolonetablet4 mgoralDIRECT RX2014-01-01Not AvailableUs
Methylprednisolonetablet4 mgoralbryant ranch prepack1997-10-31Not AvailableUs
Methylprednisolonetablet4 mgoralBlue Point Laboratories2013-08-02Not AvailableUs
Methylprednisolonetablet4 mgoralAmerican Health Packaging2013-11-25Not AvailableUs
Methylprednisolonetablet4 mgoralPreferred Pharmaceuticals, Inc.2013-09-03Not AvailableUs
Methylprednisolonetablet4 mgoralPreferred Pharmaceuticals, Inc.2014-10-08Not AvailableUs
Over the Counter ProductsNot Available
International Brands
NameCompany
MedrateNot Available
MedroneNot Available
MeproloneNot Available
SolometNot Available
UrbasonNot Available
Brand mixtures
Brand NameIngredients
Depo-Medrol with LidocaineLidocaine Hydrochloride + Methylprednisolone Acetate
Medrol Acne LotionAluminum Chlorohydrate + Methylprednisolone Acetate + Sulfur
Methylprednisolone Sodium Succinate for InjectionMethylprednisolone + Water
Neo-MedrolMethylprednisolone Acetate + Neomycin Sulfate
Neo-Medrol Acne LotionAluminum Chlorohydrate + Methylprednisolone Acetate + Neomycin Sulfate + Sulfur
SaltsNot Available
Categories
CAS number83-43-2
WeightAverage: 374.4706
Monoisotopic: 374.20932407
Chemical FormulaC22H30O5
InChI KeyVHRSUDSXCMQTMA-PJHHCJLFSA-N
InChI
InChI=1S/C22H30O5/c1-12-8-14-15-5-7-22(27,18(26)11-23)21(15,3)10-17(25)19(14)20(2)6-4-13(24)9-16(12)20/h4,6,9,12,14-15,17,19,23,25,27H,5,7-8,10-11H2,1-3H3/t12-,14-,15-,17-,19+,20-,21-,22-/m0/s1
IUPAC Name
(1S,2R,8S,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,8,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
SMILES
[H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])C[C@H](C)C2=CC(=O)C=C[C@]12C
Mass SpecNot Available
Taxonomy
KingdomOrganic Compounds
SuperclassLipids
ClassSteroids and Steroid Derivatives
SubclassGluco/mineralocorticoids, Progestogins and Derivatives
Direct parentGluco/mineralocorticoids, Progestogins and Derivatives
Alternative parentsKetosteroids; Hydroxysteroids; Cyclohexanols; Tertiary Alcohols; Ketones; Cyclic Alcohols and Derivatives; Enolates; Polyamines; Primary Alcohols; Aldehydes
Substituents3-keto-steroid; 11-hydroxy-steroid; 17-hydroxy-steroid; 20-keto-steroid; cyclohexanol; tertiary alcohol; cyclic alcohol; secondary alcohol; ketone; primary alcohol; enolate; polyamine; alcohol; carbonyl group; aldehyde
Classification descriptionThis compound belongs to the gluco/mineralocorticoids, progestogins and derivatives. These are steroids whose structure is based on an hydroxylated prostane moiety.
Pharmacology
IndicationAdjunctive therapy for short-term administration in rheumatoid arthritis.
PharmacodynamicsMethylprednisolone and its derivatives, methylprednisolone sodium succinate and methylprednisolone acetate, are synthetic glucocorticoids used as antiinflammatory or immunosuppressive agents.
Mechanism of actionUnbound glucocorticoids cross cell membranes and bind with high affinity to specific cytoplasmic receptors, modifying transcription and protein synthesis. By this mechanism, glucocorticoids can inhibit leukocyte infiltration at the site of inflammation, interfere with mediators of inflammatory response, and suppress humoral immune responses. The antiinflammatory actions of corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
AbsorptionOral bioavailability 80-99%
Volume of distributionNot Available
Protein binding78%
Metabolism

Hepatic

Route of eliminationNot Available
Half life1-3 hours
ClearanceNot Available
ToxicityLD50=2000 mg/kg (orally in rat)
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 0.9911
Blood Brain Barrier + 0.9484
Caco-2 permeable - 0.6404
P-glycoprotein substrate Substrate 0.7812
P-glycoprotein inhibitor I Non-inhibitor 0.7489
P-glycoprotein inhibitor II Non-inhibitor 0.604
Renal organic cation transporter Non-inhibitor 0.769
CYP450 2C9 substrate Non-substrate 0.8415
CYP450 2D6 substrate Non-substrate 0.9115
CYP450 3A4 substrate Substrate 0.7582
CYP450 1A2 substrate Non-inhibitor 0.9473
CYP450 2C9 substrate Non-inhibitor 0.907
CYP450 2D6 substrate Non-inhibitor 0.9513
CYP450 2C19 substrate Non-inhibitor 0.9026
CYP450 3A4 substrate Non-inhibitor 0.8309
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9167
Ames test Non AMES toxic 0.9337
Carcinogenicity Non-carcinogens 0.9529
Biodegradation Not ready biodegradable 0.9492
Rat acute toxicity 2.0025 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.9459
hERG inhibition (predictor II) Non-inhibitor 0.5985
Pharmacoeconomics
Manufacturers
  • Pharmacia and upjohn co
  • Cadista pharmaceuticals inc
  • Duramed pharmaceuticals inc sub barr laboratories inc
  • Heather drug co inc
  • Par pharmaceutical inc
  • Sandoz inc
  • Vintage pharmaceuticals inc
  • Watson laboratories inc
  • Abbott laboratories hosp products div
  • Hemopharm usa corp
  • Hospira inc
  • Elkins sinn div ah robins co inc
  • Organon usa inc
  • Abraxis pharmaceutical products
  • App pharmaceuticals llc
  • Bedford laboratories
  • International medication systems ltd
  • Teva parenteral medicines inc
Packagers
Dosage forms
FormRouteStrength
Injection, powder, for solutionintramuscular; intravenous1 g/mL
Injection, powder, for solutionintramuscular; intravenous125 mg/mL
Injection, powder, for solutionintramuscular; intravenous40 mg/mL
Injection, powder, for solutionintramuscular; intravenous500 mg/mL
Injection, powder, for solutionintravenous1 g
Injection, powder, for solutionintravenous40 mg
Injection, powder, lyophilized, for solutionintramuscular; intravenous125 mg/2mL
Injection, powder, lyophilized, for solutionintramuscular; intravenous40 mg/mL
Injection, suspensionintra-articular; intralesional; intramuscular; soft tissue40 mg/mL
Injection, suspensionintra-articular; intralesional; intramuscular; soft tissue80 mg/mL
Injection, suspensionintralesional; intramuscular; intrasynovial; soft tissue20 mg/mL
Injection, suspensionintralesional; intramuscular; intrasynovial; soft tissue40 mg/mL
Injection, suspensionintralesional; intramuscular; intrasynovial; soft tissue80 mg/mL
Injection, suspensionintramuscular40 mg
Injection, suspensionintramuscular40 mg/mL
Injection, suspensionintramuscular80 mg/mL
Kit
Powder, for solutionintravenous125 mg/mL
Tabletoral16 mg
Tabletoral2 mg
Tabletoral32 mg
Tabletoral4 mg
Tabletoral8 mg
Prices
Unit descriptionCostUnit
Methylprednisolone powder96.25USDg
Methylprednisolone ac powdr40.09USDg
Methylprednisolone ss 1 gm vial31.2USDvial
Solu-medrol 1 gm vial24.43USDvial
Solu-medrol (pf) 500 mg vial20.9USDvial
MethylPREDNISolone (Pak) 21 4 mg tablet Disp Pack16.99USDdisp
Methylprednisolone 500 mg vial15.6USDvial
Solu-medrol 500 mg vial12.9USDvial
Depo-medrol 80 mg/ml vial11.67USDml
Methylprednisolone 125 mg vial10.0USDvial
Methylprednisolone 80 mg/ml vial9.12USDml
Depo-medrol 40 mg/ml vial6.41USDml
Solu-medrol (pf) 125 mg vial5.83USDvial
Methylprednisolone 40 mg/ml vial5.22USDml
Medrol 32 mg tablet5.13USDtablet
Methylprednisolone 32 mg tablet4.62USDtablet
Depo-medrol 20 mg/ml vial3.78USDml
Methylprednisolone 16 mg tablet3.17USDtablet
Methylprednisolone 40 mg vial3.0USDvial
A-methapred 40 mg vial2.36USDvial
Medrol 16 mg tablet2.28USDtablet
Medrol 8 mg tablet2.23USDtablet
Methylprednisolone 8 mg tablet1.74USDtablet
Methylprednisolone 4 mg tablet1.68USDtablet
Medrol 4 mg dosepak1.59USDeach
Medrol 4 mg tablet0.99USDtablet
Medrol 2 mg tablet0.84USDtablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
Statesolid
Experimental Properties
PropertyValueSource
melting point232.5 °CPhysProp
water solubility120 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP1.5Not Available
logS-2.99ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.109ALOGPS
logP2.06ALOGPS
logP1.56ChemAxon
logS-3.5ALOGPS
pKa (Strongest Acidic)12.58ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area94.83 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity103.04 m3·mol-1ChemAxon
Polarizability40.84 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Spectra
SpectraNot Available
References
Synthesis Reference

Klaus Annen, Karl Petzoldt, Henry Laurent, Rudolf Wiechert, Helmut Hofmeister, “Novel 6.alpha.-methylprednisolone derivatives, their preparation, and their use.” U.S. Patent US4587236, issued March, 1973.

US4587236
General Reference
  1. Sloka JS, Stefanelli M: The mechanism of action of methylprednisolone in the treatment of multiple sclerosis. Mult Scler. 2005 Aug;11(4):425-32. Pubmed
External Links
ResourceLink
KEGG DrugD00407
PubChem Compound6741
PubChem Substance46504885
ChemSpider6485
ChEBI6888
ChEMBLCHEMBL650
Therapeutic Targets DatabaseDAP001040
PharmGKBPA450466
RxListhttp://www.rxlist.com/cgi/generic/methprd.htm
Drugs.comhttp://www.drugs.com/methylprednisolone.html
WikipediaMethylprednisolone
ATC CodesNot Available
AHFS Codes
  • 68:04.00
PDB EntriesNot Available
FDA labelshow(244 KB)
MSDSshow(72.6 KB)
Interactions
Drug Interactions
Drug
Acetylsalicylic acidThe corticosteroid, methylprednisolone, may decrease the effect of the salicylate, acetylsalicylic acid.
AprepitantIncreases the effect and toxicity of methylprednisolone
ClarithromycinThe macrolide, clarithromycin, may increase the effect of corticosteroid, methylprednisolone.
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Methylprednisolone. Consider methylprednisolone dose titration and/or adjustments in patients receiving strong CYP3A4 inhibitors (eg, azole antifungals, protease inhibitors) and monitor for increased steroid related adverse effects.
ErythromycinThe macrolide, erythromycin, may increase the effect of corticosteroid, methylprednisolone.
FosphenytoinThe enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, methylprednisolone.
ItraconazoleThe imidazole, itraconazole, may increase the effect and toxicity of the corticosteroid, methylprednisolone.
KetoconazoleThe imidazole, ketoconazole, may increase the effect and toxicity of the corticosteroid, methylprednisolone.
MidodrineIncreased arterial pressure
PhenobarbitalThe barbiturate, phenobarbital, may decrease the effect of the corticosteroid, methylprednisolone.
PhenytoinThe enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, methylprednisolone.
PrimidoneThe barbiturate, primidone, may decrease the effect of the corticosteroid, methylprednisolone.
PyridostigmineThe corticosteroid, methylprednisolone, may decrease the effect of the anticholinesterase, pyridostigmine.
QuinupristinThis combination presents an increased risk of toxicity
RifampicinThe enzyme inducer, rifampin, may decrease the effect of the corticosteroid, methylprednisolone.
TacrineTacrine and Methylprednisolone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.
TacrolimusMethylprednisone may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Methylprednisone therapy is initiated, discontinued or altered.
TrastuzumabTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
VecuroniumVecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Methylprednisolone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
Food InteractionsNot Available

Targets

1. Glucocorticoid receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Glucocorticoid receptor P04150 Details

References:

  1. Owen HC, Miner JN, Ahmed SF, Farquharson C: The growth plate sparing effects of the selective glucocorticoid receptor modulator, AL-438. Mol Cell Endocrinol. 2007 Jan 29;264(1-2):164-70. Epub 2006 Dec 19. Pubmed
  2. Juruena MF, Cleare AJ, Papadopoulos AS, Poon L, Lightman S, Pariante CM: Different responses to dexamethasone and prednisolone in the same depressed patients. Psychopharmacology (Berl). 2006 Dec;189(2):225-35. Epub 2006 Oct 3. Pubmed
  3. Boivin MA, Ye D, Kennedy JC, Al-Sadi R, Shepela C, Ma TY: Mechanism of glucocorticoid regulation of the intestinal tight junction barrier. Am J Physiol Gastrointest Liver Physiol. 2007 Feb;292(2):G590-8. Epub 2006 Oct 26. Pubmed
  4. Quesnell RR, Han X, Schultz BD: Glucocorticoids stimulate ENaC upregulation in bovine mammary epithelium. Am J Physiol Cell Physiol. 2007 May;292(5):C1739-45. Epub 2007 Jan 24. Pubmed
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

Transporters

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. Oka A, Oda M, Saitoh H, Nakayama A, Takada M, Aungst BJ: Secretory transport of methylprednisolone possibly mediated by P-glycoprotein in Caco-2 cells. Biol Pharm Bull. 2002 Mar;25(3):393-6. Pubmed
  2. 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
  3. 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

Comments
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Drug created on June 13, 2005 07:24 / Updated on January 11, 2014 08:39