Identification

Name
Methylprednisolone
Accession Number
DB00959
Description

Methylprednisolone is a prednisolone derivative glucocorticoid with higher potency than prednisone.9 It was first described in the literature in the late 1950s.9,10

Methylprednisolone was granted FDA approval on 24 October 1957.12 In the outbreak of COVID-19, low dose methylprednisolone-based therapy was successful in treating COVID-19-associated pneumonia in one patient with long-term immunosuppression.11 The efficacy of methylprednisolone in novel coronavirus pneumonia is being investigated further in clinical trials.15

Type
Small Molecule
Groups
Approved, Vet approved
Structure
Thumb
Weight
Average: 374.4706
Monoisotopic: 374.20932407
Chemical Formula
C22H30O5
Synonyms
  • (6α,11β)-11,17,21-trihydroxy-6-methylpregna-1,4-diene-3,20-dione
  • 1-dehydro-6α-methylhydrocortisone
  • 6α-methyl-11β,17α,21-triol-1,4-pregnadiene-3,20-dione
  • delta(1)-6alpha-Methylhydrocortisone
  • Methylprednisolon
  • Methylprednisolone
  • Methylprednisolonum
  • Metilprednisolona
External IDs
  • J3.872E
  • NSC-19987

Pharmacology

Indication

Oral and intramuscular methylprednisolone are indicated for a number of endocrine, rheumatic, collagen, dermatologic, allergic, ophthalmic, respiratory, hematologic, neoplastic, edematous, gastrointestinal, nervous system, and other disorders.12,13 Intra-articular and soft tissue injections are indicated for short term treatment of acute gouty arthritis, acute and subactute bursitis, acute nonspecific tenosynovitis, epicondylitis, rheumatoid arthritis, and synovitis of osteoarthritis.13 Intralesional injections are indicated for alopecia areata, discoid lupus erythematosus, keloids, lichen planus, lichen simplex chronicus and psoriatic plaques, necrobiosis lipoidica diabeticorum, and localized hypertrophic infiltrated inflammatory lesions of granuloma annulare.13

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Corticosteroids bind to the glucocorticoid receptor, inhibiting pro-inflammatory signals, and promoting anti-inflammatory signals.5 Corticosteroids have a wide therapeutic window as patients may require doses that are multiples of what the body naturally produces.5 Patients taking corticosteroids should be counselled regarding the risk of hypothalamic-pituitary-adrenal axis suppression and increased susceptibility to infections.5

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.5 Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.5

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-10.5

Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.5 High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.5

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Humans
UAnnexin A1
agonist
Humans
Absorption

Oral methylprednisolone has 89.9% the bioavailability of oral methylprednisolone acetate, while rectal methylprednisolone has 14.2% the bioavailability.6 Intravitreal methylprednisolone has a Tmax of 2.5h.7 Approximately 1/10 of an oral or IV dose of methylprednisolone will reach the vitreous humor.7 Further data regarding the absorption of methylprednisolone are not readily available.12,13

Volume of distribution

The average volume of distribution of methylprednisolone is 1.38L/kg.1

Protein binding

Methylprednisolone is 76.8% protein bound in plasma and does not significantly bind to corticosteroid binding protein.1 Methylprednisolone is bound to human serum albumin in plasma.2

Metabolism

The metabolism of methylprednisolone is thought to be mostly mediated by 11beta-hydroxysteroid dehydrogenases and 20-ketosteroid reductases.1

Hover over products below to view reaction partners

Route of elimination

Methylprednisolone and its metabolites have been collected in urine in humans.3 A study in dogs showed 25-31% elimination in urine and 44-52% elimination in feces.4

Half-life

Methylprednisolone has a half life of 2.3h.1,6

Clearance

The average plasma clearance of methylprednisolone is 336mL/h/kg.1

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

The oral LD50 in rats is >4g/kg.14 The intraperitoneal LD50 in mice is 2292mg/kg and in rats is 100mg/kg.14

Data regarding acute overdoses of glucocorticoids are rare.12,13 Chronic high doses of glucocorticoids can lead to the development of cataract, glaucoma, hypertension, water retention, hyperlipidemia, peptic ulcer, pancreatitis, myopathy, osteoporosis, mood changes, psychosis, dermal atrophy, allergy, acne, hypertrichosis, immune suppression, decreased resistance to infection, moon face, hyperglycemia, hypocalcemia, hypophosphatemia, metabolic acidosis, growth suppression, and secondary adrenal insufficiency.8 Treat acute overdoses with symptomatic and supportive therapy, while chronic overdoses will require temporarily reduced dosages.8,13

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 Methylprednisolone can be increased when it is combined with Abametapir.
AbataceptThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Abatacept.
AbirateroneThe metabolism of Abiraterone can be increased when combined with Methylprednisolone.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Methylprednisolone.
AcarboseThe risk or severity of hyperglycemia can be increased when Methylprednisolone is combined with Acarbose.
AceclofenacThe risk or severity of gastrointestinal irritation can be increased when Methylprednisolone is combined with Aceclofenac.
AcemetacinThe risk or severity of gastrointestinal irritation can be increased when Methylprednisolone is combined with Acemetacin.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Methylprednisolone.
AcetohexamideThe risk or severity of hyperglycemia can be increased when Methylprednisolone is combined with Acetohexamide.
AcetyldigitoxinThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Acetyldigitoxin.
Additional Data Available
  • Extended Description
    Extended Description

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

    Learn more
  • Severity
    Severity

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

    Learn more
  • Evidence Level
    Evidence Level

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

    Learn more
  • Action
    Action

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

    Learn more
Food Interactions
  • Avoid alcohol.
  • Take with food. Food reduces GI irritation.

Products

Product Ingredients
IngredientUNIICASInChI Key
Methylprednisolone acetate43502P7F0P53-36-1PLBHSZGDDKCEHR-LFYFAGGJSA-N
Product Images
International/Other Brands
Medrate / Medrone / Meprolone / Solomet / Urbason
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Depo-MedrolInjection, suspension80 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissuePhysicians Total Care, Inc.2007-02-062012-06-30Us
Depo-MedrolInjection, suspension40 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissueRemedy Repack2016-06-152017-02-24Us
Depo-MedrolInjection, suspension80 mg/1mLIntralesional; Intramuscular; Intrasynovial; Soft tissuePharmacia and Upjohn Company LLC1959-05-28Not applicableUs
Depo-MedrolInjection, suspension80 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissuePharmacia and Upjohn Company LLC1959-05-28Not applicableUs
Depo-MedrolInjection, suspension80 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissueAsclemed Usa, Inc.1959-05-28Not applicableUs
Depo-MedrolInjection, suspension40 mg/1mLIntralesional; Intramuscular; Intrasynovial; Soft tissueA-S Medication Solutions1959-05-28Not applicableUs
Depo-MedrolInjection, suspension40 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissueREMEDYREPACK INC.2017-05-10Not applicableUs
Depo-MedrolInjection, suspension40 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissueA-S Medication Solutions1959-05-282019-06-30Us
Depo-MedrolInjection, suspension40 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissueCardinal Health1959-05-282017-05-31Us
Depo-MedrolInjection, suspension40 mg/1mLIntralesional; Intramuscular; Intrasynovial; Soft tissueRebel Distributors1959-05-28Not 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
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
medPREDkit PlusKit4 mg/1OralMedarbor Llc2018-01-242018-02-20Us
Methylpred DPTablet4 mg/1OralDirect_Rx2019-06-26Not applicableUs
MethylPREDNISoloneTablet4 mg/1OralPar Pharmaceutical1998-12-22Not applicableUs0603 459320180913 8702 17704ci
MethylprednisoloneTablet4 mg/1OralEpic Pharma,LLC2018-05-14Not applicableUs
MethylprednisoloneTablet8 mg/1OralZydus Pharmaceuticals (USA) Inc.2018-05-01Not applicableUs
MethylprednisoloneTablet4 mg/1OralSandoz Inc1997-10-31Not applicableUs0781 502220180907 15195 14sfmji
MethylprednisoloneTablet4 mg/1OralBarr Laboratories1990-09-302012-07-31Us
MethylprednisoloneTablet4 mg/1OralCadila Healthcare Limited2018-05-01Not applicableUs
MethylprednisoloneTablet4 mg/1OralA-S Medication Solutions2018-05-01Not applicableUs
MethylPREDNISoloneTablet4 mg/1OralMc Kesson Packaging Services A Buisness Unit Of Mc Kesson Corporation2007-08-212012-06-30Us
Additional Data Available
  • Application Number
    Application Number

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

    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
Depo-medrol With LidocaineMethylprednisolone acetate (40 mg) + Lidocaine hydrochloride (10 mg)SuspensionIntra-articular; IntrabursalPfizer Canada Ulc1973-12-31Not applicableCanada
Lido-mp40Methylprednisolone acetate (40 mg/1mL) + Lidocaine hydrochloride (10 mg/1mL)KitInfiltrationBurke Therapeutics, LLC2015-06-182015-09-14Us
medPREDkitMethylprednisolone (4 mg/1) + Omeprazole (20 mg/1) + Sodium bicarbonate (1100 mg/1)KitOralMedarbor Llc2017-12-252018-01-15Us
Medrol Acne LotionMethylprednisolone acetate (2.5 mg) + Aluminum chlorohydrate (100 mg) + Octasulfur (50 mg)LotionTopicalPfizer Canada Ulc1973-12-312014-04-04Canada
Methylprednisolone Sodium Succinate for Injection, USPMethylprednisolone (1 g) + Water (20 ml)Powder, for solutionIntramuscular; IntravenousHospira Healthcare Ulc1998-03-122019-04-05Canada
Methylprednisolone Sodium Succinate for Injection, USPMethylprednisolone (500 mg) + Water (10 ml)Powder, for solutionIntramuscular; IntravenousHospira Healthcare Ulc1998-03-122019-04-05Canada
Multi-Specialty KitMethylprednisolone acetate (40 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL)KitInfiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; TopicalProficient Rx LP2014-02-06Not applicableUs
Neo-medrolMethylprednisolone acetate (2.5 mg) + Neomycin sulfate (5 mg)CreamTopicalPfizer Canada Ulc1960-12-312006-08-02Canada
Neo-medrol Acne LotionMethylprednisolone acetate (2.5 mg) + Aluminum chlorohydrate (100 mg) + Neomycin sulfate (2.5 mg) + Octasulfur (50 mg)LotionTopicalPfizer Canada Ulc1965-12-31Not applicableCanada
P-Care D40Methylprednisolone acetate (40 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL) + Povidone-iodine (10 mg/1mL)Intra-articular; Intralesional; Intramuscular; Soft tissue; TopicalRX PHARMA-PACK, INC.2017-06-16Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Dyural 40 KitMethylprednisolone acetate (40 mg/1mL) + Bupivacaine hydrochloride (2.5 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; TopicalAsclemed Usa, Inc.2014-07-25Not applicableUs
Dyural 80 KitMethylprednisolone acetate (80 mg/1mL) + Bupivacaine hydrochloride (2.5 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; TopicalAsclemed Usa, Inc.2014-08-01Not applicableUs
Dyural L KitMethylprednisolone acetate (40 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitInfiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; TopicalAsclemed Usa, Inc.2014-08-15Not applicableUs
Dyural LM KitMethylprednisolone acetate (40 mg/1mL) + Bupivacaine hydrochloride (2.5 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL)KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; TopicalAsclemed Usa, Inc.2014-08-21Not applicableUs
HybrisilMethylprednisolone acetate (10 mg/1g)GelTopicalBioZone Laboratories, Inc.2010-05-05Not applicableUs
Medroloan II SUIKMethylprednisolone acetate (40 mg/1mL)Injection, suspensionIntra-articular; Intralesional; Intramuscular; Soft tissueAsclemed Usa, Inc.2016-06-29Not applicableUs
Medroloan SUIKMethylprednisolone acetate (40 mg/1mL)Injection, suspensionIntra-articular; Intralesional; Intramuscular; Soft tissueAsclemed Usa, Inc.2016-06-29Not applicableUs
Multi-Specialty KitMethylprednisolone acetate (40 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL)KitTopicalAsclemed Usa, Inc.2014-02-06Not applicableUs
Physicians EZ Use M-predMethylprednisolone acetate (40 mg/1mL) + Bupivacaine hydrochloride (5 mg/1mL) + Povidone-iodine (10 mg/1g)KitTopicalAsclemed Usa, Inc.2013-05-30Not applicableUs

Categories

ATC Codes
D10AA02 — MethylprednisoloneH02AB04 — MethylprednisoloneH02BX01 — Methylprednisolone, combinationsD07CA02 — Methylprednisolone and antibioticsS01CA08 — Methylprednisolone and antiinfectivesD07AA01 — Methylprednisolone
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Hydroxysteroids
Direct Parent
21-hydroxysteroids
Alternative Parents
Gluco/mineralocorticoids, progestogins and derivatives / 20-oxosteroids / 3-oxo delta-1,4-steroids / 17-hydroxysteroids / 11-beta-hydroxysteroids / Delta-1,4-steroids / Tertiary alcohols / Alpha-hydroxy ketones / Secondary alcohols / Cyclic ketones
show 4 more
Substituents
11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid / 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / Alcohol / Aliphatic homopolycyclic compound / Alpha-hydroxy ketone
show 15 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
6-methylprednisolone (CHEBI:6888) / C21 steroids (gluco/mineralocorticoids, progestogins) and derivatives (LMST02030178)

Chemical Identifiers

UNII
X4W7ZR7023
CAS number
83-43-2
InChI Key
VHRSUDSXCMQTMA-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
(1R,3aS,3bS,5S,9aR,9bS,10S,11aS)-1,10-dihydroxy-1-(2-hydroxyacetyl)-5,9a,11a-trimethyl-1H,2H,3H,3aH,3bH,4H,5H,7H,9aH,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-one
SMILES
[H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])C[C@H](C)C2=CC(=O)C=C[C@]12C

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 References
  1. Szefler SJ, Ebling WF, Georgitis JW, Jusko WJ: Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults. Eur J Clin Pharmacol. 1986;30(3):323-9. doi: 10.1007/bf00541537. [PubMed:3732369]
  2. Abboud R, Akil M, Charcosset C, Greige-Gerges H: Interaction of glucocorticoids and progesterone derivatives with human serum albumin. Chem Phys Lipids. 2017 Oct;207(Pt B):271-278. doi: 10.1016/j.chemphyslip.2017.04.007. Epub 2017 Apr 21. [PubMed:28435101]
  3. Matabosch X, Pozo OJ, Monfort N, Perez-Mana C, Farre M, Marcos J, Segura J, Ventura R: Urinary profile of methylprednisolone and its metabolites after oral and topical administrations. J Steroid Biochem Mol Biol. 2013 Nov;138:214-21. doi: 10.1016/j.jsbmb.2013.05.019. Epub 2013 Jun 20. [PubMed:23792784]
  4. BUHLER DR, THOMAS RC Jr, SCHLAGEL CA: ABSORPTION, METABOLISM AND EXCRETION OF 6-ALPHA-METHYL-PREDNISOLONE-3H,21-ACETATE FOLLOWING ORAL AND INTRAMUSCULAR ADMINISTRATIONS IN THE DOG. Endocrinology. 1965 May;76:852-64. doi: 10.1210/endo-76-5-852. [PubMed:14294877]
  5. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [PubMed:30285357]
  6. Garg DC, Wagner JG, Sakmar E, Weidler DJ, Albert KS: Rectal and oral absorption of methylprednisolone acetate. Clin Pharmacol Ther. 1979 Aug;26(2):232-9. doi: 10.1002/cpt1979262232. [PubMed:455892]
  7. Behar-Cohen FF, Gauthier S, El Aouni A, Chapon P, Parel JM, Renard G, Chauvaud D: Methylprednisolone concentrations in the vitreous and the serum after pulse therapy. Retina. 2001;21(1):48-53. doi: 10.1097/00006982-200102000-00008. [PubMed:11217929]
  8. Ciriaco M, Ventrice P, Russo G, Scicchitano M, Mazzitello G, Scicchitano F, Russo E: Corticosteroid-related central nervous system side effects. J Pharmacol Pharmacother. 2013 Dec;4(Suppl 1):S94-8. doi: 10.4103/0976-500X.120975. [PubMed:24347992]
  9. FEINBERG SM, FEINBERG AR, PRUZANSKY J, FISHERMAN EW: Methylprednisolone (medrol), a potent new anti-inflammatory steroid; therapeutic results in allergic diseases. J Am Med Assoc. 1957 Nov 23;165(12):1560-2. doi: 10.1001/jama.1957.72980300006009b. [PubMed:13475063]
  10. BOLAND EW, LIDDLE GW: Metabolic and antirheumatic activities of 6-methylprednisolone (medrol). Ann Rheum Dis. 1957 Sep;16(3):297-306. doi: 10.1136/ard.16.3.297. [PubMed:13470731]
  11. Zhu L, Xu X, Ma K, Yang J, Guan H, Chen S, Chen Z, Chen G: Successful recovery of COVID-19 pneumonia in a renal transplant recipient with long-term immunosuppression. Am J Transplant. 2020 Mar 17. doi: 10.1111/ajt.15869. [PubMed:32181990]
  12. FDA Approved Drug Products: Medrol Methylprednisolone Oral Tablets [Link]
  13. FDA Approved Drug Products: Depo-Medrol Methylprednisolone Acetate Injection [Link]
  14. Cayman Chemicals: Methylprednisolone MSDS [Link]
  15. Efficacy and Safety of Corticosteroids in COVID-19 [Link]
Human Metabolome Database
HMDB0015094
KEGG Drug
D00407
PubChem Compound
6741
PubChem Substance
46504885
ChemSpider
6485
BindingDB
50103616
RxNav
6902
ChEBI
6888
ChEMBL
CHEMBL650
ZINC
ZINC000003875560
Therapeutic Targets Database
DAP001040
PharmGKB
PA450466
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Methylprednisolone
AHFS Codes
  • 68:04.00 — Adrenals
  • 84:06.00 — Anti-inflammatory Agents
FDA label
Download (244 KB)
MSDS
Download (72.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentAdvanced Follicular Lymphoma1
4Active Not RecruitingTreatmentKidney Transplant Patients1
4Active Not RecruitingTreatmentPlantar fascial fibromatosis1
4CompletedNot AvailableHealthy Volunteers1
4CompletedNot AvailableRelapsing Remitting Multiple Sclerosis (RRMS)1
4CompletedBasic ScienceRheumatoid Arthritis1
4CompletedPreventionAdrenocortical Deficiency / Hemodynamics Instability1
4CompletedPreventionAutoimmune Adrenocortical Failure1
4CompletedPreventionChronic Migraine / Migraine1
4CompletedPreventionDelirium - Postoperative / Postoperative Delirium / Stress, Physiological1

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
  • Advanced Pharmaceutical Services Inc.
  • Aidarex Pharmacuticals LLC
  • Amerisource Health Services Corp.
  • Apotheca Inc.
  • APP Pharmaceuticals
  • A-S Medication Solutions LLC
  • Barr Pharmaceuticals
  • Bedford Labs
  • Breckenridge Pharmaceuticals
  • Bryant Ranch Prepack
  • C.O. Truxton Inc.
  • Cadista Pharmaceuticals Inc.
  • Cardinal Health
  • Carlisle Laboratories Inc.
  • Clint Pharmaceutical Inc.
  • DAVA Pharmaceuticals
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • DRX Pharmaceuticals
  • General Injectables and Vaccines Inc.
  • Greenstone LLC
  • H.J. Harkins Co. Inc.
  • Hemofarm AD
  • Hospira Inc.
  • Innoviant Pharmacy Inc.
  • Keltman Pharmaceuticals Inc.
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Medisca Inc.
  • Merrell Pharmaceuticals Inc.
  • Neuman Distributors Inc.
  • Nucare Pharmaceuticals Inc.
  • Palmetto Pharmaceuticals Inc.
  • Par Pharmaceuticals
  • Patheon Inc.
  • PD-Rx Pharmaceuticals Inc.
  • Pfizer Inc.
  • Pharmacia Inc.
  • Pharmedix
  • Physician Partners Ltd.
  • Physicians Total Care Inc.
  • Prasco Labs
  • Preferred Pharmaceuticals Inc.
  • Prescript Pharmaceuticals
  • Qualitest
  • Rebel Distributors Corp.
  • Redpharm Drug
  • San Jose Surgical Supply Inc.
  • Sandhills Packaging Inc.
  • Sandoz
  • Schein Pharmaceutical Inc.
  • Sicor Pharmaceuticals
  • Southwood Pharmaceuticals
  • Spectrum Pharmaceuticals
  • Stat Rx Usa
  • Vintage Pharmaceuticals Inc.
Dosage Forms
FormRouteStrength
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Soft tissue40 mg/1mL
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Soft tissue80 mg/1mL
Injection, suspensionIntralesional; Intramuscular; Intrasynovial; Soft tissue20 mg/1mL
Injection, suspensionIntralesional; Intramuscular; Intrasynovial; Soft tissue40 mg/1mL
Injection, suspensionIntralesional; Intramuscular; Intrasynovial; Soft tissue80 mg/1mL
SuspensionIntra-articular; Intralesional; Intramuscular; Intrasynovial
SuspensionIntra-articular; Intrabursal
KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; Topical
KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical
GelTopical10 mg/1g
KitInfiltration
Tablet16 MG
Tablet4 MG
Tablet8 MG
KitOral
KitOral4 mg/1
TabletOral2 mg/1
TabletOral32 mg/1
TabletOral
CreamTopical
Tablet32 MG
TabletOral16 mg/1
TabletOral4 mg/1
TabletOral8 mg/1
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Intrasynovial; Soft tissue40 mg/1mL
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Parenteral; Soft tissue40 mg/1mL
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Parenteral; Soft tissue80 mg/1mL
Injection, suspensionIntrabronchial; Intralesional; Intramuscular; Parenteral; Soft tissue80 mg/1mL
Injection, suspensionIntramuscular; Intrasynovial; Soft tissue40 mg/1mL
SuspensionIntra-articular; Intramuscular; Intrasynovial; Soft tissue
Powder, for solutionIntramuscular; Intravenous
Powder, for solutionIntramuscular; Intravenous
Tablet40 MG
KitInfiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical
CreamTopical
LotionTopical
KitEpidural; Infiltration; Intramuscular; Intrasynovial; Soft tissue; Topical
KitTopical
KitEpidural; Infiltration
Kit; powderIntramuscular; Intravenous1 g
Kit; powderIntramuscular; Intravenous125 mg
Kit; powderIntramuscular; Intravenous40 mg
Kit; powderIntramuscular; Intravenous500 mg
Kit; powder, for solutionIntramuscular; Intravenous1 g
Kit; powder, for solutionIntramuscular; Intravenous125 mg
Kit; powder, for solutionIntramuscular; Intravenous40 mg
Kit; powder, for solutionIntramuscular; Intravenous500 mg
Prices
Unit descriptionCostUnit
Methylprednisolone powder96.25USD g
Methylprednisolone ac powdr40.09USD g
Methylprednisolone ss 1 gm vial31.2USD vial
Solu-medrol 1 gm vial24.43USD vial
Solu-medrol (pf) 500 mg vial20.9USD vial
MethylPREDNISolone (Pak) 21 4 mg tablet Disp Pack16.99USD disp
Methylprednisolone 500 mg vial15.6USD vial
Solu-medrol 500 mg vial12.9USD vial
Depo-medrol 80 mg/ml vial11.67USD ml
Methylprednisolone 125 mg vial10.0USD vial
Methylprednisolone 80 mg/ml vial9.12USD ml
Depo-medrol 40 mg/ml vial6.41USD ml
Solu-medrol (pf) 125 mg vial5.83USD vial
Methylprednisolone 40 mg/ml vial5.22USD ml
Medrol 32 mg tablet5.13USD tablet
Methylprednisolone 32 mg tablet4.62USD tablet
Depo-medrol 20 mg/ml vial3.78USD ml
Methylprednisolone 16 mg tablet3.17USD tablet
Methylprednisolone 40 mg vial3.0USD vial
A-methapred 40 mg vial2.36USD vial
Medrol 16 mg tablet2.28USD tablet
Medrol 8 mg tablet2.23USD tablet
Methylprednisolone 8 mg tablet1.74USD tablet
Methylprednisolone 4 mg tablet1.68USD tablet
Medrol 4 mg dosepak1.59USD each
Medrol 4 mg tablet0.99USD tablet
Medrol 2 mg tablet0.84USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)232.5 °CPhysProp
water solubility120 mg/L (at 25 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP1.525ChemSpider
logS-2.99ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.109 mg/mLALOGPS
logP2.06ALOGPS
logP1.56ChemAxon
logS-3.5ALOGPS
pKa (Strongest Acidic)12.59ChemAxon
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
Polarizability40.77 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9911
Blood Brain Barrier+0.9484
Caco-2 permeable-0.6404
P-glycoprotein substrateSubstrate0.7812
P-glycoprotein inhibitor INon-inhibitor0.7489
P-glycoprotein inhibitor IINon-inhibitor0.604
Renal organic cation transporterNon-inhibitor0.769
CYP450 2C9 substrateNon-substrate0.8415
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7582
CYP450 1A2 substrateNon-inhibitor0.9473
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorNon-inhibitor0.9513
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9167
Ames testNon AMES toxic0.9337
CarcinogenicityNon-carcinogens0.9529
BiodegradationNot ready biodegradable0.9492
Rat acute toxicity2.0025 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9459
hERG inhibition (predictor II)Non-inhibitor0.5985
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
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
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0a6r-0019000000-3a4955cf7cc34e1e8d0f
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-0k9i-0696000000-003c4527b983cf71aefd
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-01p9-0980000000-e5097669b38e84057a0f
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-01p9-0960000000-ef914702163187cc80af
LC-MS/MS Spectrum - LC-ESI-QTOF , positiveLC-MS/MSsplash10-06y9-0940000000-54b01b6c04c68be3f1b3
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0009000000-3fe2869617af3697e2ed
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0009000000-8ad4f169606968256614
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0f79-0895000000-29d1cbf49bb2b32c5a98
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01p9-0940000000-baa402ac94c228229ea2
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01p9-0910000000-5cf9fb219d798a9316f4
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4r-0910000000-a2d2af7f573229dc3147
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0006-2900000000-a01d5bfe926dc48e6e4c
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0019000000-11519ee9583104c00505
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0gw0-0974000000-af5d4ebce055ce6efb23
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01p9-0960000000-22e2342fcec2bf1cd833
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-01p9-0920000000-63759535c53af1efb13f
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0c09-1900000000-a48c07db31cf27cf0381
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-05tp-2900000000-b802f5e17b69cd6c707f
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-0009000000-0e0cc8bfc7721357c5cf
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0bti-0896000000-86854a3fa2cb3c3bde0b
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4r-0796000000-b0070da713077c3f7975
MS/MS Spectrum - , positiveLC-MS/MSsplash10-01p9-3950000000-b938f656c358e1e42bb5

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. 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:17182172]
  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:17016711]
  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:17068119]
  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:17251323]
  5. 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
Agonist
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 group
Organism
Humans and other mammals
Pharmacological action
Unknown
Actions
Substrate
General Function
Trans-1,2-dihydrobenzene-1,2-diol dehydrogenase activity
Specific Function
Converts progesterone to its inactive form, 20-alpha-dihydroxyprogesterone (20-alpha-OHP). In the liver and intestine, may have a role in the transport of bile. May have a role in monitoring the in...

Components:
References
  1. Malatkova P, Wsol V: Carbonyl reduction pathways in drug metabolism. Drug Metab Rev. 2014 Feb;46(1):96-123. doi: 10.3109/03602532.2013.853078. Epub 2013 Oct 31. [PubMed:24171394]
  2. Szefler SJ, Ebling WF, Georgitis JW, Jusko WJ: Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults. Eur J Clin Pharmacol. 1986;30(3):323-9. doi: 10.1007/bf00541537. [PubMed:3732369]
Kind
Protein group
Organism
Humans and other mammals
Pharmacological action
Unknown
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...

Components:
References
  1. Szefler SJ, Ebling WF, Georgitis JW, Jusko WJ: Methylprednisolone versus prednisolone pharmacokinetics in relation to dose in adults. Eur J Clin Pharmacol. 1986;30(3):323-9. doi: 10.1007/bf00541537. [PubMed:3732369]
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. Lee SJ, Jusko WJ, Salaita CG, Calis KA, Jann MW, Spratlin VE, Goldstein JA, Hon YY: Reduced methylprednisolone clearance causing prolonged pharmacodynamics in a healthy subject was not associated with CYP3A5*3 allele or a change in diet composition. J Clin Pharmacol. 2006 May;46(5):515-26. doi: 10.1177/0091270006287588. [PubMed:16638735]
  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]
  5. Litt J. (2016). Litt's Drug eruption & reaction manual (22nd ed.). CRC Press LLc.
Kind
Protein group
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...

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
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
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]

Carriers

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. Abboud R, Akil M, Charcosset C, Greige-Gerges H: Interaction of glucocorticoids and progesterone derivatives with human serum albumin. Chem Phys Lipids. 2017 Oct;207(Pt B):271-278. doi: 10.1016/j.chemphyslip.2017.04.007. Epub 2017 Apr 21. [PubMed:28435101]

Transporters

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. 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:11913542]
  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:12948019]
  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:14661924]
  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]
  5. Tomita M, Watanabe A, Fujinaga I, Yamakawa T, Hayashi M: Nonlinear absorption of methylprednisolone by absorptive and secretory transporters. Int J Pharm. 2010 Mar 15;387(1-2):1-6. doi: 10.1016/j.ijpharm.2009.10.042. Epub 2009 Oct 31. [PubMed:19883743]

Drug created on June 13, 2005 07:24 / Updated on August 09, 2020 06:16

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates
Covid drug repurpose