Methylprednisolone

Identification

Summary

Methylprednisolone is a corticosteroid used to treat inflammation or immune reactions across a variety of organ systems, endocrine conditions, and neoplastic diseases.

Brand Names
Depo-medrol, Depo-medrol With Lidocaine, Hybrisil, Medrol, Medroloan Suik, Readysharp-p40, Readysharp-p80
Generic Name
Methylprednisolone
DrugBank Accession Number
DB00959
Background

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
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

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Adjunct therapy in management ofAcute gouty arthritis•••••••••••••••••••••• ••••••
Management ofAcute leukemia••••••••••••••••••••••••••
Used in combination to treatAcute tendonitisCombination Product in combination with: Lidocaine (DB00281)•••••••••••••••••••••• ••••••••••
Treatment ofAllergic conjunctivitis (ac)••••••••••••••••••
Treatment ofAllergic corneal marginal ulcers••••••••••••••••••
Associated Therapies
Contraindications & Blackbox Warnings
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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

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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
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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

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.
AbemaciclibThe metabolism of Abemaciclib 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.
Food Interactions
  • Avoid alcohol.
  • Take with food. Food reduces GI irritation.

Products

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dosage, form, labeller, route of administration, and marketing period.
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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, suspension20 mg/1mLIntralesional; Intramuscular; Intrasynovial; Soft tissuePharmacia & Upjohn Company LLC1959-05-28Not applicableUS flag
Depo-medrolInjection, suspension40 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissueA-S Medication Solutions1959-05-28Not applicableUS flag
Depo-MedrolInjection, suspension40 mg/1mLIntralesional; Intramuscular; Intrasynovial; Soft tissueRebel Distributors1959-05-28Not applicableUS flag
Depo-MedrolInjection, suspension40 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissueREMEDYREPACK INC.2017-05-10Not applicableUS flag
Depo-MedrolInjection, suspension80 mg/1mLIntra-articular; Intralesional; Intramuscular; Soft tissueAsclemed Usa, Inc.1959-05-28Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
medPREDkit PlusKit4 mg/1OralMedarbor Llc2018-01-242018-02-20US flag
Methylpred DPTablet4 mg/1OralDirect_Rx2019-06-26Not applicableUS flag
MethylprednisoloneTablet4 mg/1OralMajor Pharmaceuticals2018-05-01Not applicableUS flag
MethylprednisoloneTablet4 mg/1OralAdvanced Rx Pharmacy of Tennessee, LLC2023-01-11Not applicableUS flag
MethylprednisoloneTablet4 mg/1OralOAKRUM PHARMA, LLC2019-11-122024-01-31US flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Depo-medrol With LidocaineMethylprednisolone acetate (40 mg / mL) + Lidocaine hydrochloride (10 mg / mL)SuspensionIntra-articular; Intrabursal; Intrasynovial; PeriarticularPfizer Canada Ulc1973-12-31Not applicableCanada flag
Lido-mp40Methylprednisolone acetate (40 mg/1mL) + Lidocaine hydrochloride (10 mg/1mL)KitInfiltrationBurke Therapeutics, LLC2015-06-182015-09-14US flag
LIDODEPOMEDROLMethylprednisolone acetate (40 MG/ML) + Lidocaine hydrochloride (10 MG/ML)Injection, suspensionParenteralPfizer Italia S.R.L.2014-11-13Not applicableItaly flag
LIDODEPOMEDROLMethylprednisolone acetate (40 MG/ML) + Lidocaine hydrochloride (10 MG/ML)Injection, suspensionParenteralPfizer Italia S.R.L.2014-11-13Not applicableItaly flag
LIDODEPOMEDROLMethylprednisolone acetate (40 MG/ML) + Lidocaine hydrochloride (10 MG/ML)Injection, suspensionParenteralPfizer Italia S.R.L.2014-11-13Not applicableItaly flag
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) + Sodium chloride (9 mg/1mL) + Water (1 mL/1mL)KitIntra-articular; Intralesional; Intramuscular; Soft tissue; TopicalAsclemed Usa, Inc.2014-07-25Not applicableUS flag
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) + Sodium chloride (9 mg/1mL) + Water (1 mL/1mL)KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; TopicalAdvanced Rx Pharmacy of Tennessee, LLC2023-07-31Not applicableUS flag
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) + Sodium chloride (9 mg/1mL) + Water (1 mL/1mL)KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; TopicalAdvanced Rx Pharmacy of Tennessee, LLC2023-07-31Not applicableUS flag
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) + Sodium chloride (9 mg/1mL) + Water (1 mL/1mL)KitIntra-articular; Intralesional; Intramuscular; Soft tissue; TopicalAsclemed Usa, Inc.2014-08-01Not applicableUS flag
Dyural 80-LMMethylprednisolone 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; TopicalAdvanced Rx Pharmacy of Tennessee, LLC2023-07-31Not applicableUS flag

Categories

ATC Codes
D07AA01 — MethylprednisoloneD10AA02 — MethylprednisoloneH02AB04 — MethylprednisoloneH02BX01 — Methylprednisolone, combinationsD07CA02 — Methylprednisolone and antibioticsS03CA07 — Methylprednisolone and antiinfectivesS01CA08 — Methylprednisolone and antiinfectives
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)
Affected organisms
  • Humans and other mammals

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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  5. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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
FDA label
Download (244 KB)
MSDS
Download (72.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentAllergic Rhinitis (AR) / Allergy to Tree Pollen / Seasonal Allergic Rhinitis1
4Active Not RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19) / Corticosteroids1
4Active Not RecruitingTreatmentKidney Transplantation1
4Active Not RecruitingTreatmentThyroid Associated Ophthalmopathy1
4CompletedNot AvailableHealthy Volunteers (HV)1

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
Cream
CreamCutaneous0.1 %
Ointment0.1 %
SolutionTopical1 %
Emulsion
Injection, powder, for solutionIntramuscular; Intravenous
InjectionIntralesional; Intramuscular
Injection, suspensionIntra-articular40 MG/ML
Injection, suspensionIntra-articular; Intramuscular40 mg/mL
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
SuspensionIntramuscular40.000 mg
SuspensionIntra-articular; Intralesional; Intramuscular; Intrasynovial20 mg / mL
SuspensionIntra-articular; Intralesional; Intramuscular; Intrasynovial80 mg / mL
SuspensionIntra-articular; Intralesional; Intramuscular; Rectal40 mg
SuspensionIntra-articular; Intralesional; Intramuscular; Intrasynovial40 mg / mL
Suspension40 mg/ml
SuspensionIntramuscular40 mg
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Intrasynovial
SuspensionIntra-articular; Intrabursal; Intrasynovial; Periarticular
KitIntra-articular; Intralesional; Intramuscular; Soft tissue; Topical
KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; Topical
KitEpidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical
SolutionIntramuscular500.000 mg
Pill
SuspensionParenteral40.000 mg
GelTopical10 mg/1g
Injection, powder, for solution
SolutionIntravenous500.000 mg
KitInfiltration
Injection, suspensionParenteral
Injection, powder, for solution120 MG/2ML
Injection, powder, for solution40 MG/2ML
Injection, powder, for solutionIntramuscular; Intravenous20 MG/2ML
Injection, powder, for solutionIntravenous500 MG
Injection, powder, for solution; injection, powder, lyophilized, for solution500 mg
KitOral
KitOral4 mg/1
TabletOral2 MG
TabletOral2 mg/1
TabletOral32 mg/1
CreamTopical2.5 mg / g
Ointment
Tablet, film coatedOral4 MG
TabletOral
Tablet, film coatedOral
TabletOral32 MG
TabletOral16 mg/1
TabletOral4 mg/1
TabletOral8 mg/1
Injection, suspensionIntra-arterial; Intralesional; Intramuscular; Soft tissue80 mg/1mL
Injection, suspensionIntra-articular; Intralesional; Intrameningeal; Soft tissue40 mg/1mL
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Intrasynovial; Soft tissue40 mg/1mL
Injection, suspensionIntra-articular; Intralesional; Intramuscular; Intrasynovial; Soft tissue80 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 tissue40 mg / mL
SuspensionIntra-articular; Intramuscular; Intrasynovial; Soft tissue80 mg / mL
Injection, powder, lyophilized, for solutionIntravenous500 mg
Powder, for solutionIntramuscular; Intravenous
Injection, powder, for solutionIntramuscular80 MG/1.5ML
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous500 mg
Emulsion1 MG/G
Injection, powder, for solutionParenteral1000 MG
Injection, powder, for solutionParenteral125 MG
Injection, powder, for solutionParenteral40 MG
Injection, powder, for solutionParenteral500 MG
TabletOral40 MG
KitInfiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical
CreamTopical
LotionTopical
LotionTopical100 mg/ml
Injection, suspension; kit; solutionIntra-articular; Intralesional; Intramuscular; Soft tissue; Topical
Injection, solution; injection, suspension; kit; solutionEpidural; Infiltration; Intra-articular; Intracaudal; Intralesional; Intramuscular; Intravenous; Perineural; Soft tissue; Topical
KitEpidural; Infiltration; Intramuscular; Intrasynovial; Soft tissue; Topical
KitInfiltration; Soft tissue; Topical
KitEpidural; Infiltration; Intracaudal
Tablet, coatedOral16 mg
Tablet, coatedOral4 mg
SolutionIntramuscular125.000 mg
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous20 mg
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous250 mg
Injection, powder, lyophilized, for solutionIntramuscular; Intravenous40 mg
SolutionParenteral500.000 mg
KitEpidural; Infiltration
TabletOral8 MG
SolutionTopical
Suspension80.000 mg
SolutionIntravenous500.000 mg
Tablet, extended release4 MG
Tablet, extended release8 MG
InjectionIntramuscular; Intravenous20 mg/ml
Injection, powder, for solutionIntravenous
Injection, powder, for solutionIntramuscular; Intravenous16 mg
Injection, powder, for solutionIntramuscular; Intravenous250 mg
Injection, powder, for solutionIntramuscular; Intravenous31.56 mg
Suspension40 mg/1ml
TabletOral16 mg
TabletOral4 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-MSsplash10-0a5c-4897000000-e8a5119b3469a050dd85
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-0bti-0896000000-86854a3fa2cb3c3bde0b
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-0a4r-0796000000-b0070da713077c3f7975
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSsplash10-01p9-3950000000-b938f656c358e1e42bb5
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
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-0a4r-0009000000-4709bd1de703e931926f
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-0009000000-dba0932242812862f053
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-0a71-0679000000-36589a7b6be5f751a9cb
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0006-1009000000-ff2c814b789dd2674714
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0005-1149000000-c49dfdcf868f31a3e9d2
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0pdr-0941000000-88ee982d36052c93bd85
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-196.1549557
predicted
DarkChem Lite v0.1.0
[M-H]-195.7159557
predicted
DarkChem Lite v0.1.0
[M-H]-196.1608557
predicted
DarkChem Lite v0.1.0
[M-H]-192.73662
predicted
DeepCCS 1.0 (2019)
[M+H]+196.3829557
predicted
DarkChem Lite v0.1.0
[M+H]+197.1977557
predicted
DarkChem Lite v0.1.0
[M+H]+197.7216557
predicted
DarkChem Lite v0.1.0
[M+H]+194.63203
predicted
DeepCCS 1.0 (2019)
[M+Na]+196.9138557
predicted
DarkChem Lite v0.1.0
[M+Na]+196.9147557
predicted
DarkChem Lite v0.1.0
[M+Na]+200.84096
predicted
DeepCCS 1.0 (2019)

Targets

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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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
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. [Article]

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. [Article]
  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. [Article]
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. [Article]
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]

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. [Article]

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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]

Drug created at June 13, 2005 13:24 / Updated at March 18, 2024 16:48