Methylprednisolone
Identification
- Name
- Methylprednisolone
- Accession Number
- DB00959 (APRD00342)
- Type
- Small Molecule
- Groups
- Approved, Vet approved
- Description
A prednisolone derivative with similar anti-inflammatory action.
- Structure
- 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
- Product Ingredients
Ingredient UNII CAS InChI Key Methylprednisolone acetate 43502P7F0P 53-36-1 PLBHSZGDDKCEHR-LFYFAGGJSA-N - Product Images
- Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Depo-Medrol Injection, suspension 80 mg/1mL Intra-articular; Intralesional; Intramuscular; Soft tissue Physicians Total Care, Inc. 2007-02-06 2012-06-30 US Depo-Medrol Injection, suspension 40 mg/1mL Intra-articular; Intralesional; Intramuscular; Soft tissue Cardinal Health 1959-05-28 Not applicable US Depo-Medrol Injection, suspension 80 mg/1mL Intra-articular; Intralesional; Intramuscular; Soft tissue Pharmacia and Upjohn Company LLC 1959-05-28 Not applicable US Depo-Medrol Injection, suspension 40 mg/1mL Intralesional; Intramuscular; Intrasynovial; Soft tissue Rebel Distributors 1959-05-28 Not applicable US Depo-Medrol Injection, suspension 80 mg/1mL Intralesional; Intramuscular; Intrasynovial; Soft tissue Remedy Repack 2014-09-11 Not applicable US Depo-Medrol Injection, suspension 40 mg/1mL Intra-articular; Intralesional; Intramuscular; Soft tissue Remedy Repack 2017-05-10 Not applicable US Depo-Medrol Injection, suspension 40 mg/1mL Intra-articular; Intralesional; Intramuscular; Soft tissue Physicians Total Care, Inc. 2005-05-03 2012-06-30 US Depo-Medrol Injection, suspension 40 mg/1mL Intralesional; Intramuscular; Intrasynovial; Soft tissue Remedy Repack 2018-03-29 Not applicable US Depo-Medrol Injection, suspension 80 mg/1mL Intralesional; Intramuscular; Intrasynovial; Soft tissue Pharmacia and Upjohn Company LLC 1959-05-28 Not applicable US Depo-Medrol Injection, suspension 40 mg/1mL Intralesional; Intramuscular; Intrasynovial; Soft tissue A-S Medication Solutions 1959-05-28 Not applicable US - Generic Prescription Products
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Depo-medrol With Lidocaine Methylprednisolone acetate (40 mg) + Lidocaine hydrochloride (10 mg) Solution Intra-articular; Intrabursal Pfizer 1973-12-31 Not applicable Canada Lido-mp40 Methylprednisolone acetate (40 mg/1mL) + Lidocaine hydrochloride (10 mg/1mL) Kit Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue Burke Therapeutics, LLC 2015-06-18 2015-09-14 US medPREDkit Methylprednisolone (4 mg/1) + Omeprazole (20 mg/1) + Sodium bicarbonate (1100 mg/1) Kit Medarbor Llc 2017-12-25 2018-01-15 US Medrol Acne Lotion Methylprednisolone acetate (2.5 mg) + Aluminum chlorohydrate (100 mg) + Octasulfur (50 mg) Lotion Topical Pfizer 1973-12-31 2014-04-04 Canada Methylprednisolone Sodium Succinate for Injection, USP Methylprednisolone (1 g) + Water (20 ml) Powder, for solution Intramuscular; Intravenous Hospira, Inc. 1998-03-12 Not applicable Canada Methylprednisolone Sodium Succinate for Injection, USP Methylprednisolone (500 mg) + Water (10 ml) Powder, for solution Intramuscular; Intravenous Hospira, Inc. 1998-03-12 Not applicable Canada Multi-Specialty Kit Methylprednisolone acetate (40 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) Kit Proficient Rx LP 2014-02-06 Not applicable US Neo-medrol Methylprednisolone acetate (2.5 mg) + Neomycin sulfate (5 mg) Cream Topical Pfizer 1960-12-31 2006-08-02 Canada Neo-medrol Acne Lotion Methylprednisolone acetate (2.5 mg) + Aluminum chlorohydrate (100 mg) + Neomycin sulfate (2.5 mg) + Octasulfur (50 mg) Lotion Topical Pfizer 1965-12-31 Not applicable Canada P-Care D40 Methylprednisolone acetate (40 mg/1mL) + Isopropyl alcohol (0.7 mL/1mL) + Povidone-iodine (10 mg/1mL) Kit RX PHARMA-PACK, INC. 2017-06-16 Not applicable US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Dyural 40 Kit Methylprednisolone acetate (40 mg/1mL) + Bupivacaine hydrochloride monohydrate (2.5 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL) Kit Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; Topical Asclemed Usa, Inc. 2014-07-25 Not applicable US Dyural 80 Kit Methylprednisolone acetate (80 mg/1mL) + Bupivacaine hydrochloride monohydrate (2.5 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL) Kit Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; Topical Asclemed Usa, Inc. 2014-08-01 Not applicable US Dyural L Kit Methylprednisolone acetate (40 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL) Kit Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical Asclemed Usa, Inc. 2014-08-15 Not applicable US Dyural LM Kit Methylprednisolone acetate (40 mg/1mL) + Bupivacaine hydrochloride monohydrate (2.5 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) + Povidone-iodine (10 mg/1mL) Kit Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical Asclemed Usa, Inc. 2014-08-21 Not applicable US Hybrisil Methylprednisolone acetate (10 mg/1g) Gel Topical BioZone Laboratories, Inc. 2010-05-05 Not applicable US Medroloan II SUIK Methylprednisolone acetate (40 mg/1mL) Injection, suspension Intra-articular; Intralesional; Intramuscular; Soft tissue Asclemed Usa, Inc. 2016-06-29 Not applicable US Medroloan SUIK Methylprednisolone acetate (40 mg/1mL) Injection, suspension Intra-articular; Intralesional; Intramuscular; Soft tissue Asclemed Usa, Inc. 2016-06-29 Not applicable US Multi-Specialty Kit Methylprednisolone acetate (40 mg/1mL) + Isopropyl alcohol (70 mL/100mL) + Lidocaine hydrochloride (10 mg/1mL) Kit Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical Asclemed Usa, Inc. 2014-02-06 Not applicable US Physicians EZ Use M-pred Methylprednisolone acetate (40 mg/1mL) + Bupivacaine hydrochloride monohydrate (5 mg/1mL) + Povidone-iodine (10 mg/1g) Kit Epidural; Infiltration; Intramuscular; Intrasynovial; Soft tissue; Topical Asclemed Usa, Inc. 2013-05-30 Not applicable US - International/Other Brands
- Medrate / Medrol / Medrone / Meprolone / Solomet / Urbason
- Categories
- Adrenal Cortex Hormones
- Adrenals
- Anti-Acne Preparations
- Anti-Acne Preparations for Topical Use
- Anti-Inflammatory Agents
- Antiemetics
- Antineoplastic Agents
- Autonomic Agents
- Central Nervous System Agents
- Corticosteroid Hormone Receptor Agonists
- Corticosteroids
- Corticosteroids for Systemic Use
- Corticosteroids for Systemic Use, Plain
- Corticosteroids, Dermatological Preparations
- Corticosteroids, Weak (Group I)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inducers
- Dermatologicals
- Gastrointestinal Agents
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hyperglycemia-Associated Agents
- Immunosuppressive Agents
- Neuroprotective Agents
- Ophthalmologicals
- P-glycoprotein/ABCB1 Substrates
- Peripheral Nervous System Agents
- Prednisolone
- Pregnadienes
- Pregnadienetriols
- Pregnanes
- Protective Agents
- Sensory Organs
- Steroids
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- UNII
- X4W7ZR7023
- CAS number
- 83-43-2
- Weight
- Average: 374.4706
Monoisotopic: 374.20932407 - Chemical Formula
- C22H30O5
- 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
Pharmacology
- Indication
Adjunctive therapy for short-term administration in rheumatoid arthritis.
- Associated Conditions
- Acne Rosacea
- Acute Gouty Arthritis
- Adrenal cortical hypofunctions
- Adrenocortical Hyperfunction
- Ankylosing Spondylitis (AS)
- Anterior Segment Inflammation
- Aspiration Pneumonitis
- Asthma Bronchial
- Atopic Dermatitis (AD)
- Berylliosis
- Bullous dermatitis herpetiformis
- Bursitis
- Choroiditis
- Congenital Adrenal Hyperplasia (CAH)
- Congenital Hypoplastic Anemia
- Conjunctivitis, Seasonal Allergic
- Corneal Inflammation
- Cushing's Syndrome
- Dermatitis, Contact
- Drug hypersensitivity reaction
- Epicondylitis
- Erythroblastopenia
- Hypercalcemia
- Idiopathic Thrombocytopenic Purpura (ITP)
- Inflammatory Reaction
- Iridocyclitis
- Iritis
- Leukemia, Acute
- Loeffler's syndrome
- Malignant Lymphomas
- Mycosis Fungoides (MF)
- Ophthalmia, Sympathetic
- Optic Neuritis
- Pemphigus
- Perennial Allergic Rhinitis (PAR)
- Post-traumatic Osteoarthritis
- Regional Enteritis
- Rheumatoid Arthritis
- Rheumatoid Arthritis, Juvenile
- Sarcoidosis
- Seasonal Allergic Rhinitis (SAR)
- Secondary thrombocytopenia
- Serum Sickness
- Severe Seborrheic Dermatitis
- Stevens Johnson Syndrome
- Synovitis
- Systemic Lupus Erythematosus (SLE)
- Trichinosis
- Tuberculosis Infection
- Tuberculosis Meningitis
- Ulcerative Colitis (UC)
- Uveitis
- Acquired immune hemolytic anemia
- Acute nonspecific tenosynovitis
- Acute rheumatic carditis
- Diffuse posterior uveitis
- Exfoliative erythroderma
- Non-suppurative Thyroiditis
- Severe Psoriasis
- Varicella-zoster virus acute retinal necrosis
- Pharmacodynamics
Methylprednisolone and its derivatives, methylprednisolone sodium succinate and methylprednisolone acetate, are synthetic glucocorticoids used as antiinflammatory or immunosuppressive agents.
- Mechanism of action
Unbound 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.
Target Actions Organism AGlucocorticoid receptor agonistHumans - Absorption
Oral bioavailability 80-99%
- Volume of distribution
- Not Available
- Protein binding
78%
- Metabolism
Hepatic
- Route of elimination
- Not Available
- Half life
1-3 hours
- Clearance
- Not Available
- Toxicity
LD50=2000 mg/kg (orally in rat)
- Affected organisms
- Humans and other mammals
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction (R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Methylprednisolone. (S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Methylprednisolone. 1-Testosterone The risk or severity of edema formation can be increased when 1-Testosterone is combined with Methylprednisolone. 1,10-Phenanthroline The therapeutic efficacy of 1,10-Phenanthroline can be decreased when used in combination with Methylprednisolone. 16-Bromoepiandrosterone The risk or severity of edema formation can be increased when 16-Bromoepiandrosterone is combined with Methylprednisolone. 19-norandrostenedione The risk or severity of edema formation can be increased when 19-norandrostenedione is combined with Methylprednisolone. 1alpha-Hydroxyvitamin D5 The therapeutic efficacy of 1alpha-Hydroxyvitamin D5 can be decreased when used in combination with Methylprednisolone. 2-Methoxyethanol The risk or severity of adverse effects can be increased when Methylprednisolone is combined with 2-Methoxyethanol. 2,4-thiazolidinedione The therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Methylprednisolone. 3,5-diiodothyropropionic acid The metabolism of 3,5-diiodothyropropionic acid can be increased when combined with Methylprednisolone. - Food Interactions
- Not 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 References
- 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:16042225]
- External Links
- Human Metabolome Database
- HMDB0015094
- KEGG Drug
- D00407
- PubChem Compound
- 6741
- PubChem Substance
- 46504885
- BindingDB
- 50103616
- ChEBI
- 6888
- ChEMBL
- CHEMBL650
- Therapeutic Targets Database
- DAP001040
- PharmGKB
- PA450466
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Methylprednisolone
- ATC Codes
- D10AA02 — Methylprednisolone
- D10AA — Corticosteroids, combinations for treatment of acne
- D10A — ANTI-ACNE PREPARATIONS FOR TOPICAL USE
- D10 — ANTI-ACNE PREPARATIONS
- D — DERMATOLOGICALS
- H02AB — Glucocorticoids
- H02A — CORTICOSTEROIDS FOR SYSTEMIC USE, PLAIN
- H02 — CORTICOSTEROIDS FOR SYSTEMIC USE
- H — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
- H02BX — Corticosteroids for systemic use, combinations
- H02B — CORTICOSTEROIDS FOR SYSTEMIC USE, COMBINATIONS
- H02 — CORTICOSTEROIDS FOR SYSTEMIC USE
- H — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
- D07CA — Corticosteroids, weak, combinations with antibiotics
- D07C — CORTICOSTEROIDS, COMBINATIONS WITH ANTIBIOTICS
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- S01CA — Corticosteroids and antiinfectives in combination
- S01C — ANTIINFLAMMATORY AGENTS AND ANTIINFECTIVES IN COMBINATION
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- 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
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
Form Route Strength Injection, suspension Intralesional; Intramuscular; Intrasynovial; Soft tissue 20 mg/1mL Injection, suspension Intralesional; Intramuscular; Intrasynovial; Soft tissue 40 mg/1mL Injection, suspension Intralesional; Intramuscular; Intrasynovial; Soft tissue 80 mg/1mL Suspension Intra-articular; Intralesional; Intramuscular; Intrasynovial 20 mg Suspension Intra-articular; Intralesional; Intramuscular; Intrasynovial 80 mg Suspension Intra-articular; Intralesional; Intramuscular; Intrasynovial 40 mg Solution Intra-articular; Intrabursal Kit Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Intravenous; Soft tissue; Subcutaneous; Topical Kit Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical Gel Topical 10 mg/1g Kit Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue Kit 4 mg/1 Tablet Oral 2 mg/1 Tablet Oral 32 mg/1 Tablet Oral 16 mg Tablet Oral 4 mg Cream Topical 2.5 mg Tablet Oral 16 mg/1 Tablet Oral 4 mg/1 Tablet Oral 8 mg/1 Injection, suspension Intra-articular; Intralesional; Intramuscular; Parenteral; Soft tissue 40 mg/1mL Injection, suspension Intra-articular; Intralesional; Intramuscular; Parenteral; Soft tissue 80 mg/1mL Injection, suspension Intra-articular; Intralesional; Intramuscular; Soft tissue 40 mg/1mL Injection, suspension Intra-articular; Intralesional; Intramuscular; Soft tissue 80 mg/1mL Injection, suspension Intramuscular; Intrasynovial; Soft tissue 40 mg/1mL Suspension Intra-articular; Intramuscular; Intrasynovial; Soft tissue 40 mg Suspension Intra-articular; Intramuscular; Intrasynovial; Soft tissue 80 mg Powder, for solution Intramuscular; Intravenous 1 g Powder, for solution Intramuscular; Intravenous 125 mg Powder, for solution Intramuscular; Intravenous 40 mg Powder, for solution Intramuscular; Intravenous 5 g Powder, for solution Intramuscular; Intravenous 500 mg Powder, for solution Intramuscular; Intravenous Kit Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue; Topical Cream Topical Lotion Topical Kit Kit Epidural; Infiltration; Intramuscular; Intrasynovial; Soft tissue; Topical Kit Infiltration; Soft tissue; Topical Kit Epidural; Infiltration; Intracaudal Kit Epidural; Infiltration; Intra-articular; Intralesional; Intramuscular; Soft tissue Kit; powder Intramuscular; Intravenous 1 g Kit; powder Intramuscular; Intravenous 125 mg Kit; powder Intramuscular; Intravenous 40 mg Kit; powder Intramuscular; Intravenous 500 mg Kit; powder, for solution Intramuscular; Intravenous 1 g Kit; powder, for solution Intramuscular; Intravenous 125 mg Kit; powder, for solution Intramuscular; Intravenous 40 mg Kit; powder, for solution Intramuscular; Intravenous 500 mg - Prices
Unit description Cost Unit Methylprednisolone powder 96.25USD g Methylprednisolone ac powdr 40.09USD g Methylprednisolone ss 1 gm vial 31.2USD vial Solu-medrol 1 gm vial 24.43USD vial Solu-medrol (pf) 500 mg vial 20.9USD vial MethylPREDNISolone (Pak) 21 4 mg tablet Disp Pack 16.99USD disp Methylprednisolone 500 mg vial 15.6USD vial Solu-medrol 500 mg vial 12.9USD vial Depo-medrol 80 mg/ml vial 11.67USD ml Methylprednisolone 125 mg vial 10.0USD vial Methylprednisolone 80 mg/ml vial 9.12USD ml Depo-medrol 40 mg/ml vial 6.41USD ml Solu-medrol (pf) 125 mg vial 5.83USD vial Methylprednisolone 40 mg/ml vial 5.22USD ml Medrol 32 mg tablet 5.13USD tablet Methylprednisolone 32 mg tablet 4.62USD tablet Depo-medrol 20 mg/ml vial 3.78USD ml Methylprednisolone 16 mg tablet 3.17USD tablet Methylprednisolone 40 mg vial 3.0USD vial A-methapred 40 mg vial 2.36USD vial Medrol 16 mg tablet 2.28USD tablet Medrol 8 mg tablet 2.23USD tablet Methylprednisolone 8 mg tablet 1.74USD tablet Methylprednisolone 4 mg tablet 1.68USD tablet Medrol 4 mg dosepak 1.59USD each Medrol 4 mg tablet 0.99USD tablet Medrol 2 mg tablet 0.84USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 232.5 °C PhysProp water solubility 120 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992) logP 1.5 Not Available logS -2.99 ADME Research, USCD - Predicted Properties
Property Value Source Water Solubility 0.109 mg/mL ALOGPS logP 2.06 ALOGPS logP 1.56 ChemAxon logS -3.5 ALOGPS pKa (Strongest Acidic) 12.59 ChemAxon pKa (Strongest Basic) -2.9 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 5 ChemAxon Hydrogen Donor Count 3 ChemAxon Polar Surface Area 94.83 Å2 ChemAxon Rotatable Bond Count 2 ChemAxon Refractivity 103.04 m3·mol-1 ChemAxon Polarizability 40.77 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - 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 inhibitor Non-inhibitor 0.907 CYP450 2D6 inhibitor Non-inhibitor 0.9513 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor 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
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Taxonomy
- 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
- Progestogin-skeleton / 21-hydroxysteroid / 20-oxosteroid / Pregnane-skeleton / 3-oxo-delta-1,4-steroid / 3-oxosteroid / Oxosteroid / 11-beta-hydroxysteroid / 11-hydroxysteroid / 17-hydroxysteroid show 15 more
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- 6-methylprednisolone (CHEBI:6888) / C21 steroids (gluco/mineralocorticoids, progestogins) and derivatives (LMST02030178)
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
- 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]
- 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]
- 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]
- 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]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- 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
- 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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
- Litt J. (2016). Litt's Drug eruption & reaction manual (22nd ed.). CRC Press LLc.
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- 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]
- 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]
- Yates CR, Chang C, Kearbey JD, Yasuda K, Schuetz EG, Miller DD, Dalton JT, Swaan PW: Structural determinants of P-glycoprotein-mediated transport of glucocorticoids. Pharm Res. 2003 Nov;20(11):1794-803. [PubMed:14661924]
Drug created on June 13, 2005 07:24 / Updated on February 18, 2019 20:24