Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C24H32O6 |
Molecular Weight | 416.5073 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H]1C[C@H]2[C@@H]3CC[C@](O)(C(=O)COC(C)=O)[C@@]3(C)C[C@H](O)[C@@H]2[C@@]4(C)C=CC(=O)C=C14
InChI
InChIKey=PLBHSZGDDKCEHR-LFYFAGGJSA-N
InChI=1S/C24H32O6/c1-13-9-16-17-6-8-24(29,20(28)12-30-14(2)25)23(17,4)11-19(27)21(16)22(3)7-5-15(26)10-18(13)22/h5,7,10,13,16-17,19,21,27,29H,6,8-9,11-12H2,1-4H3/t13-,16-,17-,19-,21+,22-,23-,24-/m0/s1
Molecular Formula | C24H32O6 |
Molecular Weight | 416.5073 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.drugbank.ca/drugs/DB00959Curator's Comment: Description was created based on several sources, including https://www.drugs.com/pro/medrol.html
Sources: http://www.drugbank.ca/drugs/DB00959
Curator's Comment: Description was created based on several sources, including https://www.drugs.com/pro/medrol.html
Methylprednisolone is a prednisolone derivative with similar anti-inflammatory and immunosuppressive action. It is adjunctive therapy for short-term administration in rheumatoid arthritis. It is indicated in the following conditions: endocrine disorders, rheumatic disorders, collagen diseases, allergic states etc. Methylprednisolone is marketed in the USA and Canada under the brand names Medrol and Solu-Medrol. Methylprednisolone is a GR receptor agonist.
CNS Activity
Originator
Sources: http://adisinsight.springer.com/drugs/800003722
Curator's Comment: # Pfizer
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2034 Sources: http://www.drugbank.ca/drugs/DB00959 |
2.4 nM [EC50] | ||
Target ID: CHEMBL2034 Sources: http://www.ampoule.org.hk/pdf/advantan.pdf |
|||
Target ID: CHEMBL2111332 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15329590 |
1.07 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | MEDROL Approved UseINDICATIONS AND USAGE
MEDROL Tablets are indicated in the following conditions:
1. Endocrine Disorders
Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the first choice; synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy mineralocorticoid supplementation is of particular importance).
Congenital adrenal hyperplasia
Nonsuppurative thyroiditis
Hypercalcemia associated with cancer
2. Rheumatic Disorders
As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in:
Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy)
Ankylosing spondylitis
Acute and subacute bursitis
Synovitis of osteoarthritis
Acute nonspecific tenosynovitis
Post-traumatic osteoarthritis
Psoriatic arthritis
Epicondylitis
Acute gouty arthritis
3. Collagen Diseases
During an exacerbation or as maintenance therapy in selected cases of:
Systemic lupus erythematosus
Systemic dermatomyositis (polymyositis)
Acute rheumatic carditis
4. Dermatologic Diseases
Bullous dermatitis herpetiformis
Severe erythema multiforme (Stevens-Johnson syndrome)
Severe seborrheic dermatitis
Exfoliative dermatitis
Mycosis fungoides
Pemphigus
Severe psoriasis
5. Allergic States
Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment:
Seasonal or perennial allergic rhinitis
Drug hypersensitivity reactions
Serum sickness
Contact dermatitis
Bronchial asthma
Atopic dermatitis
6. Ophthalmic Diseases
Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as:
Allergic corneal marginal ulcers
Herpes zoster ophthalmicus
Anterior segment inflammation
Diffuse posterior uveitis and choroiditis
Sympathetic ophthalmia
Keratitis
Optic neuritis
Allergic conjunctivitis
Chorioretinitis
Iritis and iridocyclitis
7. Respiratory Diseases
Symptomatic sarcoidosis
Berylliosis
Loeffler's syndrome not manageable by other means
Fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy
Aspiration pneumonitis
8. Hematologic Disorders
Idiopathic thrombocytopenic purpura in adults
Secondary thrombocytopenia in adults
Acquired (autoimmune) hemolytic anemia
Erythroblastopenia (RBC anemia)
Congenital (erythroid) hypoplastic anemia
9. Neoplastic Diseases
For palliative management of:
Leukemias and lymphomas in adults
Acute leukemia of childhood
10. Edematous States
To induce a diuresis or remission of proteinuria in the nephrotic syndrome, without uremia, of the idiopathic type or that due to lupus erythematosus.
11. Gastrointestinal Diseases
To tide the patient over a critical period of the disease in:
Ulcerative colitis
Regional enteritis
12. Nervous System
Acute exacerbations of multiple sclerosis
13. Miscellaneous
Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculous chemotherapy.
Trichinosis with neurologic or myocardial involvement. Launch Date1957 |
|||
Primary | MEDROL Approved UseINDICATIONS AND USAGE
MEDROL Tablets are indicated in the following conditions:
1. Endocrine Disorders
Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the first choice; synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy mineralocorticoid supplementation is of particular importance).
Congenital adrenal hyperplasia
Nonsuppurative thyroiditis
Hypercalcemia associated with cancer
2. Rheumatic Disorders
As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in:
Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy)
Ankylosing spondylitis
Acute and subacute bursitis
Synovitis of osteoarthritis
Acute nonspecific tenosynovitis
Post-traumatic osteoarthritis
Psoriatic arthritis
Epicondylitis
Acute gouty arthritis
3. Collagen Diseases
During an exacerbation or as maintenance therapy in selected cases of:
Systemic lupus erythematosus
Systemic dermatomyositis (polymyositis)
Acute rheumatic carditis
4. Dermatologic Diseases
Bullous dermatitis herpetiformis
Severe erythema multiforme (Stevens-Johnson syndrome)
Severe seborrheic dermatitis
Exfoliative dermatitis
Mycosis fungoides
Pemphigus
Severe psoriasis
5. Allergic States
Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment:
Seasonal or perennial allergic rhinitis
Drug hypersensitivity reactions
Serum sickness
Contact dermatitis
Bronchial asthma
Atopic dermatitis
6. Ophthalmic Diseases
Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as:
Allergic corneal marginal ulcers
Herpes zoster ophthalmicus
Anterior segment inflammation
Diffuse posterior uveitis and choroiditis
Sympathetic ophthalmia
Keratitis
Optic neuritis
Allergic conjunctivitis
Chorioretinitis
Iritis and iridocyclitis
7. Respiratory Diseases
Symptomatic sarcoidosis
Berylliosis
Loeffler's syndrome not manageable by other means
Fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy
Aspiration pneumonitis
8. Hematologic Disorders
Idiopathic thrombocytopenic purpura in adults
Secondary thrombocytopenia in adults
Acquired (autoimmune) hemolytic anemia
Erythroblastopenia (RBC anemia)
Congenital (erythroid) hypoplastic anemia
9. Neoplastic Diseases
For palliative management of:
Leukemias and lymphomas in adults
Acute leukemia of childhood
10. Edematous States
To induce a diuresis or remission of proteinuria in the nephrotic syndrome, without uremia, of the idiopathic type or that due to lupus erythematosus.
11. Gastrointestinal Diseases
To tide the patient over a critical period of the disease in:
Ulcerative colitis
Regional enteritis
12. Nervous System
Acute exacerbations of multiple sclerosis
13. Miscellaneous
Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculous chemotherapy.
Trichinosis with neurologic or myocardial involvement. Launch Date1957 |
|||
Primary | MEDROL Approved UseINDICATIONS AND USAGE
MEDROL Tablets are indicated in the following conditions:
1. Endocrine Disorders
Primary or secondary adrenocortical insufficiency (hydrocortisone or cortisone is the first choice; synthetic analogs may be used in conjunction with mineralocorticoids where applicable; in infancy mineralocorticoid supplementation is of particular importance).
Congenital adrenal hyperplasia
Nonsuppurative thyroiditis
Hypercalcemia associated with cancer
2. Rheumatic Disorders
As adjunctive therapy for short-term administration (to tide the patient over an acute episode or exacerbation) in:
Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy)
Ankylosing spondylitis
Acute and subacute bursitis
Synovitis of osteoarthritis
Acute nonspecific tenosynovitis
Post-traumatic osteoarthritis
Psoriatic arthritis
Epicondylitis
Acute gouty arthritis
3. Collagen Diseases
During an exacerbation or as maintenance therapy in selected cases of:
Systemic lupus erythematosus
Systemic dermatomyositis (polymyositis)
Acute rheumatic carditis
4. Dermatologic Diseases
Bullous dermatitis herpetiformis
Severe erythema multiforme (Stevens-Johnson syndrome)
Severe seborrheic dermatitis
Exfoliative dermatitis
Mycosis fungoides
Pemphigus
Severe psoriasis
5. Allergic States
Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment:
Seasonal or perennial allergic rhinitis
Drug hypersensitivity reactions
Serum sickness
Contact dermatitis
Bronchial asthma
Atopic dermatitis
6. Ophthalmic Diseases
Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as:
Allergic corneal marginal ulcers
Herpes zoster ophthalmicus
Anterior segment inflammation
Diffuse posterior uveitis and choroiditis
Sympathetic ophthalmia
Keratitis
Optic neuritis
Allergic conjunctivitis
Chorioretinitis
Iritis and iridocyclitis
7. Respiratory Diseases
Symptomatic sarcoidosis
Berylliosis
Loeffler's syndrome not manageable by other means
Fulminating or disseminated pulmonary tuberculosis when used concurrently with appropriate antituberculous chemotherapy
Aspiration pneumonitis
8. Hematologic Disorders
Idiopathic thrombocytopenic purpura in adults
Secondary thrombocytopenia in adults
Acquired (autoimmune) hemolytic anemia
Erythroblastopenia (RBC anemia)
Congenital (erythroid) hypoplastic anemia
9. Neoplastic Diseases
For palliative management of:
Leukemias and lymphomas in adults
Acute leukemia of childhood
10. Edematous States
To induce a diuresis or remission of proteinuria in the nephrotic syndrome, without uremia, of the idiopathic type or that due to lupus erythematosus.
11. Gastrointestinal Diseases
To tide the patient over a critical period of the disease in:
Ulcerative colitis
Regional enteritis
12. Nervous System
Acute exacerbations of multiple sclerosis
13. Miscellaneous
Tuberculous meningitis with subarachnoid block or impending block when used concurrently with appropriate antituberculous chemotherapy.
Trichinosis with neurologic or myocardial involvement. Launch Date1957 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
213 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12174030 |
32 mg single, intravenous dose: 32 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
METHYLPREDNISOLONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
931 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12174030 |
32 mg single, intravenous dose: 32 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
METHYLPREDNISOLONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
2.3 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/12174030 |
32 mg single, intravenous dose: 32 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
METHYLPREDNISOLONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
23% |
METHYLPREDNISOLONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
1000 mg/kg single, intravenous Highest studied dose Dose: 1000 mg/kg Route: intravenous Route: single Dose: 1000 mg/kg Sources: |
unhealthy, 0-15 years Health Status: unhealthy Age Group: 0-15 years Sex: M+F Sources: |
|
1250 mg 1 times / day multiple, oral Highest studied dose Dose: 1250 mg, 1 times / day Route: oral Route: multiple Dose: 1250 mg, 1 times / day Sources: |
unhealthy, 18–59 years Health Status: unhealthy Age Group: 18–59 years Sex: M+F Sources: |
|
120 mg 1 times / week multiple, intramuscular Highest studied dose Dose: 120 mg, 1 times / week Route: intramuscular Route: multiple Dose: 120 mg, 1 times / week Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubs.acs.org/doi/abs/10.1021/mp900163d Page: - |
no | |||
Page: - |
yes | |||
Page: - |
yes |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: - |
yes | |||
Page: - |
yes | |||
Sources: http://epubs.surrey.ac.uk/855783/1/27606608.pdf Page: - |
yes | |||
Page: - |
yes |
PubMed
Title | Date | PubMed |
---|---|---|
Hypotension, bradycardia, and asystole after high-dose intravenous methylprednisolone in a monitored patient. | 1998 Jul |
|
Therapeutic dilemma: crescentic mesangiocapillary glomerulonephritis type 1 in a patient on antituberculous therapy with rifampicin. | 1999 Jan |
|
Pulse methylprednisolone therapy for arthritis causing muscle weakness. | 1999 Sep |
|
Use of epidural steroids after discectomy may predispose to infection. | 2000 Feb 15 |
|
[Lactic acidosis: a complication of spinal cord injury in multiple trauma]. | 2000 Jun |
|
A case of normotensive scleroderma renal crisis after high-dose methylprednisolone treatment. | 2000 Jun |
|
[A senile case of acute necrotizing myopathy presenting prolonged severe muscle paralysis due to high dose glucocorticoid and muscle relaxant]. | 2000 Mar |
|
Selective involvement of the choroid plexus on cerebral magnetic resonance images: a new radiological sign in patients with systemic lupus erythematosus with neurological symptoms. | 2001 Feb |
|
[Contact allergy caused by poison ivy (Toxicodendron spp]. | 2001 Feb |
|
Lupus nephritis in children: prognostic significance of clinicopathological findings. | 2001 Feb |
|
[Psychological and behavioral disorders with good outcome in neurosarcoidosis]. | 2001 Feb |
|
[Value of abdominal-pelvic computed tomography in adult rheumatoid purpura]. | 2001 Feb |
|
Multiple corticosteroid allergies. | 2001 Feb |
|
Contact allergy to miripirium chloride in Depo-Medrol. | 2001 Feb |
|
[Is it useful to perform a (67)gallium scintigraphy in the follow-up of patients with gastric lymphoma?]. | 2001 Feb |
|
Childhood bullous pemphigoid developed after the first vaccination. | 2001 Feb |
|
Idiopathic IgA nephropathy with segmental necrotizing lesions of the capillary wall. | 2001 Feb |
|
Graft failure in a patient with systemic lupus erythematosus (SLE) treated with high-dose immunosuppression and autologous stem cell rescue. | 2001 Jan |
|
A three or more drug combination as effective therapy for moderate or severe chronic graft-versus-host disease. | 2001 Jan |
|
Two cases of severe bronchopneumonia due to influenza A (H3N2) virus: detection of influenza virus gene using reverse transcription polymerase chain reaction. | 2001 Jan |
|
Preventive effects of lecithinized superoxide dismutase and methylprednisolone on spinal cord injury in rats: transcriptional regulation of inflammatory and neurotrophic genes. | 2001 Jan |
|
High-dose methylprednisolone therapy in multiple sclerosis induces apoptosis in peripheral blood leukocytes. | 2001 Jan |
|
Severe arthralgia and myalgia due to high-dose methylprednisolone pulse therapy cured by potassium infusion in a patient with diffuse proliferative lupus nephritis. | 2001 Jan |
|
Complete recovery from juvenile pemphigus vulgaris. | 2001 Jan-Feb |
|
Management of cutaneous hemangiomas: a retrospective analysis of 1109 cases and comparison of conventional dose prednisolone with high-dose methylprednisolone therapy. | 2001 Jan-Feb |
|
Recurrent orbital inflammation from metastatic orbital carcinoid tumor. | 2001 Mar |
|
[Intramural hematoma of the large intestine caused by cytomegalovirus vasculitis in a patient with SLE]. | 2001 Mar |
|
[Value of methylprednisolone perfusions in the corticodependent forms of Horton's disease]. | 2001 Mar |
|
Use of daclizumab as initial immunosuppression in liver transplant recipients with impaired renal function. | 2001 Mar |
|
Chronic eosinophilic pneumonia presenting with recurrent massive bilateral pleural effusion : case report. | 2001 Mar |
|
Systemic glucocorticoids in severe exacerbations of COPD. | 2001 Mar |
|
Steroids for acute exacerbations of COPD : how long is enough? | 2001 Mar |
|
Methylprednisolone does not benefit patients undergoing coronary artery bypass grafting and early tracheal extubation. | 2001 Mar |
|
Effects of preoperative steroid administration on surgical stress in hepatic resection: prospective randomized trial. | 2001 Mar |
|
Intrathecal methylprednisolone for postherpetic neuralgia. | 2001 Mar 29 |
|
Intrathecal methylprednisolone for postherpetic neuralgia. | 2001 Mar 29 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/pro/medrol.html
Each Medrol Tablet (methylprednisolone) for oral administration contains 2 mg, 4 mg, 8 mg, 16 mg or 32 mg of methylprednisolone. The initial dosage of Medrol Tablets may vary from 4 mg to 48 mg of methylprednisolone per day depending on the specific disease entity being treated.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26339357
Treatment with methylprednisolone concentrations above 50 uM could ignificantly reduce the proliferation activity of human CLL cell line MEC-1 by 23.34%, 30.73%, 30.57% after 24 h, and 28.48%, 42.35%, 44.56% after 48 h respectively
Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 17:47:17 GMT 2025
by
admin
on
Mon Mar 31 17:47:17 GMT 2025
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Record UNII |
43502P7F0P
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C521
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DTXSID7023302
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5877
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155323
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53-36-1
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200-171-3
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SUB03255MIG
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1770
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Methylprednisolone acetate
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48985
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DBSALT001157
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1436006
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6889
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C48003
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43502P7F0P
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C000873
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m7454
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100000091568
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43502P7F0P
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CHEMBL650
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