Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H31O8P |
Molecular Weight | 454.4505 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@](O)(C(=O)COP(O)(O)=O)[C@@]1(C)C[C@H](O)[C@@]3([H])[C@@]2([H])C[C@]([H])(C)C4=CC(=O)C=C[C@]34C
InChI
InChIKey=PWTIEVRZANUUHG-PJHHCJLFSA-N
InChI=1S/C22H31O8P/c1-12-8-14-15-5-7-22(26,18(25)11-30-31(27,28)29)21(15,3)10-17(24)19(14)20(2)6-4-13(23)9-16(12)20/h4,6,9,12,14-15,17,19,24,26H,5,7-8,10-11H2,1-3H3,(H2,27,28,29)/t12-,14-,15-,17-,19+,20-,21-,22-/m0/s1
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 n = 26 Health Status: unhealthy Condition: sickle cell disease Age Group: 0-15 years Sex: M+F Population Size: 26 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 n = 24 Health Status: unhealthy Condition: multiple sclerosis relapse Age Group: 18–59 years Sex: M+F Population Size: 24 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 |
---|---|---|
Use of epidural steroids after discectomy may predispose to infection. | 2000 Feb 15 |
|
[A senile case of acute necrotizing myopathy presenting prolonged severe muscle paralysis due to high dose glucocorticoid and muscle relaxant]. | 2000 Mar |
|
The development of clinical signs of rheumatoid synovial inflammation is associated with increased synthesis of the chemokine CXCL8 (interleukin-8). | 2001 |
|
Three cases of C-ANCA-positive vasculitis treated with immunoadsorption: possible benefit in early treatment. | 2001 Feb |
|
Steroid-resistant kidney transplant rejection: diagnosis and treatment. | 2001 Feb |
|
[Is it useful to perform a (67)gallium scintigraphy in the follow-up of patients with gastric lymphoma?]. | 2001 Feb |
|
Glucocorticoid inhibition of neuropathic hyperalgesia and spinal Fos expression. | 2001 Feb |
|
Postnatal glucocorticoids in very preterm infants: "the good, the bad, and the ugly"? | 2001 Feb |
|
Cytokine characteristics of jaundice in mouse liver. | 2001 Feb 7 |
|
Pharmacoeconomic study of tacrolimus-based versus cyclosporine-based immunosuppressive therapy following liver transplantation. | 2001 Feb-Mar |
|
Prospective randomized trial of tacrolimus and prednisone versus tacrolimus, prednisone, and mycophenolate mofetil: complete report on 350 primary adult liver transplantations. | 2001 Feb-Mar |
|
Graft failure in a patient with systemic lupus erythematosus (SLE) treated with high-dose immunosuppression and autologous stem cell rescue. | 2001 Jan |
|
[Anesthetic management for mitral valve replacement in a patient with idiopathic hypereosinophilic syndrome]. | 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 |
|
New treatment for postherpetic neuralgia. | 2001 Jan |
|
High-dose methylprednisolone therapy in multiple sclerosis induces apoptosis in peripheral blood leukocytes. | 2001 Jan |
|
Conservative management of Gradenigo syndrome in a child. | 2001 Jan |
|
High-dose methylprednisolone treatment in experimental focal cerebral ischemia. | 2001 Jan |
|
Osteonecrosis of the femoral head after allogeneic bone marrow transplantation. | 2001 Jan |
|
The contribution of indocyanine green angiography to the appraisal and management of Vogt-Koyanagi-Harada disease. | 2001 Jan |
|
Spinal cord injury. | 2001 Jan |
|
Enhancement of goblet cell hyperplasia and airway hyperresponsiveness by salbutamol in a rat model of atopic asthma. | 2001 Jan |
|
Glucocorticoid receptor-mediated suppression of activator protein-1 activation and matrix metalloproteinase expression after spinal cord injury. | 2001 Jan 1 |
|
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 |
|
The impact of attaining a minimal disease state after high-dose melphalan and autologous transplantation for multiple myeloma. | 2001 Mar |
|
Use of daclizumab as initial immunosuppression in liver transplant recipients with impaired renal function. | 2001 Mar |
|
Intrathecal methylprednisolone for postherpetic neuralgia. | 2001 Mar 29 |
|
[Comparison of two different treatments of lateral humeral epicondylitis--"tennis elbow". A randomized controlled trial]. | 2001 Mar 5 |
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
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244-869-6
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1D9M23IY4Y
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63018
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DTXSID30944908
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22252-38-6
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SALT/SOLVATE (PARENT)
SUBSTANCE RECORD