HYDROCORTISONE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H30O5
Molecular Weight	362.4607
Optical Activity	UNSPECIFIED
Defined Stereocenters	7 / 7
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

C[C@@]12CCC(=O)C=C2CC[C@@]3([H])[C@]4([H])CC[C@](C(=O)CO)([C@@]4(C)C[C@@]([H])([C@@]31[H])O)O

InChI

InChIKey=JYGXADMDTFJGBT-VWUMJDOOSA-N

InChI=1S/C21H30O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h9,14-16,18,22,24,26H,3-8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C21H30O5
Molecular Weight	362.4607
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	7 / 7
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: http://www.drugbank.ca/drugs/DB00741
Curator's Comment:: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/008697s032_33lbl.pdf

Hydrocortisone is the main glucocorticoid secreted by the adrenal cortex. Its synthetic counterpart is used, either as an injection or topically, in the treatment of inflammation, allergy, collagen diseases, asthma, adrenocortical deficiency, shock, and some neoplastic conditions. Topical hydrocortisone is used for its anti-inflammatory or immunosuppressive properties to treat inflammation due to corticosteroid-responsive dermatoses. Hydrocortisone binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. The cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. In other words, the two main products in inflammation Prostaglandins and Leukotrienes are inhibited by the action of Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space, where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from neutrophils, macrophages and mastocytes. Additionally the immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding. For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Also used to treat endocrine (hormonal) disorders (adrenal insufficiency, Addisons disease). Hydrocortisone is also used to treat many immune and allergic disorders, such as arthritis, lupus, severe psoriasis, severe asthma, ulcerative colitis, and Crohn's disease.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Glucocorticoid receptor 167 Target ID: CHEMBL2034 Sources: http://www.drugbank.ca/drugs/DB00741	Agonist 2456	Congenital adrenal hyperplasia Rheumatoid arthritis Leukemia Bronchial asthma
Glucocorticoid receptor 167 Target ID: CHEMBL2034 Sources: https://www.genome.jp/dbget-bin/www_bget?dr:D01886\|http://drugcentral.org/drugcard/4569\|https://www.drugpatentwatch.com/p/generic-api/HYDROCORTISONE+PROBUTATE\|https://adisinsight.springer.com/drugs/800043715	Agonist 2456
Glucocorticoid receptor 167 Target ID: CHEMBL2034 Sources: https://www.drugbank.ca/drugs/DB14540 \| https://www.genome.jp/dbget-bin/www_bget?dr:D01619	Agonist 2456
apoptotic process 45 Target ID: GO:0006915 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10455320	Inhibitor 7701		50 nM [IC50]
Annexin A1 17 Target ID: P04083 Gene ID: 301 Gene Symbol: ANXA1 Target Organism: Homo sapiens (Human) Sources: http://www.drugbank.ca/drugs/DB00741	Agonist 2456
Intercellular adhesion molecule-1 17 Target ID: CHEMBL3070 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10669853	Inhibitor 7701	Bronchial asthma	0.100000000000000006 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Congenital adrenal hyperplasia 40 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/008697s032_33lbl.pdf	Primary	Glucocorticoid receptor	Approved 7997	Cortef Approved Use CORTEF 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 Non suppurative 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: Psoriatic arthritis Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy) Ankylosing spondylitis Acute and subacute bursitis Acute nonspecific tenosynovitis Acute gouty arthritis Post-traumatic osteoarthritis Synovitis of osteoarthritis Epicondylitis 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 Pemphigus Bullous dermatitis herpetiformis Severe erythema multiforme (Stevens-Johnson syndrome) Exfoliative dermatitis Mycosis fungoides Severe psoriasis Severe seborrheic dermatitis 5. Allergic States Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment: Seasonal or perennial allergic rhinitis Serum sickness Bronchial asthma Contact dermatitis Atopic dermatitis Drug hypersensitivity reactions 6. Ophthalmic Diseases Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as: Allergic conjunctivitis Keratitis Allergic corneal marginal ulcers Herpes zoster ophthalmicus Iritis and iridocyclitis Chorioretinitis Anterior segment inflammation Diffuse posterior uveitis and choroiditis Optic neuritis Sympathetic ophthalmia 7. Respiratory Diseases Symptomatic sarcoidosis Loeffler’s syndrome not manageable by other means Berylliosis 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 Date -538012800000
Rheumatoid arthritis 294 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/008697s032_33lbl.pdf	Primary	Glucocorticoid receptor	Approved 7997	Cortef Approved Use CORTEF 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 Non suppurative 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: Psoriatic arthritis Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy) Ankylosing spondylitis Acute and subacute bursitis Acute nonspecific tenosynovitis Acute gouty arthritis Post-traumatic osteoarthritis Synovitis of osteoarthritis Epicondylitis 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 Pemphigus Bullous dermatitis herpetiformis Severe erythema multiforme (Stevens-Johnson syndrome) Exfoliative dermatitis Mycosis fungoides Severe psoriasis Severe seborrheic dermatitis 5. Allergic States Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment: Seasonal or perennial allergic rhinitis Serum sickness Bronchial asthma Contact dermatitis Atopic dermatitis Drug hypersensitivity reactions 6. Ophthalmic Diseases Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as: Allergic conjunctivitis Keratitis Allergic corneal marginal ulcers Herpes zoster ophthalmicus Iritis and iridocyclitis Chorioretinitis Anterior segment inflammation Diffuse posterior uveitis and choroiditis Optic neuritis Sympathetic ophthalmia 7. Respiratory Diseases Symptomatic sarcoidosis Loeffler’s syndrome not manageable by other means Berylliosis 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 Date -538012800000
Leukemia 82 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/008697s032_33lbl.pdf	Palliative	Glucocorticoid receptor	Approved 7997	Cortef Approved Use CORTEF 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 Non suppurative 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: Psoriatic arthritis Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy) Ankylosing spondylitis Acute and subacute bursitis Acute nonspecific tenosynovitis Acute gouty arthritis Post-traumatic osteoarthritis Synovitis of osteoarthritis Epicondylitis 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 Pemphigus Bullous dermatitis herpetiformis Severe erythema multiforme (Stevens-Johnson syndrome) Exfoliative dermatitis Mycosis fungoides Severe psoriasis Severe seborrheic dermatitis 5. Allergic States Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment: Seasonal or perennial allergic rhinitis Serum sickness Bronchial asthma Contact dermatitis Atopic dermatitis Drug hypersensitivity reactions 6. Ophthalmic Diseases Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as: Allergic conjunctivitis Keratitis Allergic corneal marginal ulcers Herpes zoster ophthalmicus Iritis and iridocyclitis Chorioretinitis Anterior segment inflammation Diffuse posterior uveitis and choroiditis Optic neuritis Sympathetic ophthalmia 7. Respiratory Diseases Symptomatic sarcoidosis Loeffler’s syndrome not manageable by other means Berylliosis 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 Date -538012800000
Bronchial asthma 48 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/008697s032_33lbl.pdf	Primary	Intercellular adhesion molecule-1 Glucocorticoid receptor	Approved 7997	Cortef Approved Use CORTEF 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 Non suppurative 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: Psoriatic arthritis Rheumatoid arthritis, including juvenile rheumatoid arthritis (selected cases may require low-dose maintenance therapy) Ankylosing spondylitis Acute and subacute bursitis Acute nonspecific tenosynovitis Acute gouty arthritis Post-traumatic osteoarthritis Synovitis of osteoarthritis Epicondylitis 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 Pemphigus Bullous dermatitis herpetiformis Severe erythema multiforme (Stevens-Johnson syndrome) Exfoliative dermatitis Mycosis fungoides Severe psoriasis Severe seborrheic dermatitis 5. Allergic States Control of severe or incapacitating allergic conditions intractable to adequate trials of conventional treatment: Seasonal or perennial allergic rhinitis Serum sickness Bronchial asthma Contact dermatitis Atopic dermatitis Drug hypersensitivity reactions 6. Ophthalmic Diseases Severe acute and chronic allergic and inflammatory processes involving the eye and its adnexa such as: Allergic conjunctivitis Keratitis Allergic corneal marginal ulcers Herpes zoster ophthalmicus Iritis and iridocyclitis Chorioretinitis Anterior segment inflammation Diffuse posterior uveitis and choroiditis Optic neuritis Sympathetic ophthalmia 7. Respiratory Diseases Symptomatic sarcoidosis Loeffler’s syndrome not manageable by other means Berylliosis 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 Date -538012800000

C_max

Value	Dose	Co-administered	Analyte	Population
258 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/2050835	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		HYDROCORTISONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
1162 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/2050835	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		HYDROCORTISONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
1.82 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/2050835	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		HYDROCORTISONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
9.9% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/13700365			HYDROCORTISONE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
200 mg 4 times / day multiple, intramuscular Highest studied dose Dose: 200 mg, 4 times / day Route: intramuscular Route: multiple Dose: 200 mg, 4 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/32170323	unhealthy, 56 years (tange: 40-64 years) Health Status: unhealthy Age Group: 56 years (tange: 40-64 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/32170323	Sources: https://pubmed.ncbi.nlm.nih.gov/32170323
200 mg 4 times / day multiple, intravenous Highest studied dose Dose: 200 mg, 4 times / day Route: intravenous Route: multiple Dose: 200 mg, 4 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/32170323	unhealthy, 56 years (tange: 40-64 years) Health Status: unhealthy Age Group: 56 years (tange: 40-64 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/32170323	Sources: https://pubmed.ncbi.nlm.nih.gov/32170323
200 mg 4 times / day multiple, oral Highest studied dose Dose: 200 mg, 4 times / day Route: oral Route: multiple Dose: 200 mg, 4 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/32170323	unhealthy, 56 years (tange: 40-64 years) Health Status: unhealthy Age Group: 56 years (tange: 40-64 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/32170323	Sources: https://pubmed.ncbi.nlm.nih.gov/32170323
200 mg single, intravenous Highest studied dose Dose: 200 mg Route: intravenous Route: single Dose: 200 mg Sources: https://pubmed.ncbi.nlm.nih.gov/32170323	unhealthy, 56 years (tange: 40-64 years) Health Status: unhealthy Age Group: 56 years (tange: 40-64 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/32170323	Sources: https://pubmed.ncbi.nlm.nih.gov/32170323
2.5 % 4 times / day multiple, topical Dose: 2.5 %, 4 times / day Route: topical Route: multiple Dose: 2.5 %, 4 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/anda/2000/40310_Hydrocortisone_Prntlbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/anda/2000/40310_Hydrocortisone_Prntlbl.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/anda/2000/40310_Hydrocortisone_Prntlbl.pdf
1 mg/kg 4 times / day multiple, intravenous Dose: 1 mg/kg, 4 times / day Route: intravenous Route: multiple Dose: 1 mg/kg, 4 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT02044159	unhealthy, children Health Status: unhealthy Age Group: children Sources: https://clinicaltrials.gov/ct2/show/NCT02044159	Other AEs: Infection... Other AEs: Infection (below serious, 6 patients) Sources: https://clinicaltrials.gov/ct2/show/NCT02044159
0.5 mg/kg 4 times / day multiple, intravenous Dose: 0.5 mg/kg, 4 times / day Route: intravenous Route: multiple Dose: 0.5 mg/kg, 4 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01954056	unhealthy, neonate Health Status: unhealthy Age Group: neonate Sources: https://clinicaltrials.gov/ct2/show/NCT01954056	Other AEs: Hyperbilirubinemia, Hypertension... Other AEs: Hyperbilirubinemia (serious, 1 patient) Hypertension (serious, 1 patient) Adrenal insufficiency (serious, 1 patient) Sources: https://clinicaltrials.gov/ct2/show/NCT01954056

AEs

AE	Significance	Dose	Population
Infection	below serious, 6 patients	1 mg/kg 4 times / day multiple, intravenous Dose: 1 mg/kg, 4 times / day Route: intravenous Route: multiple Dose: 1 mg/kg, 4 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT02044159	unhealthy, children Health Status: unhealthy Age Group: children Sources: https://clinicaltrials.gov/ct2/show/NCT02044159
Adrenal insufficiency	serious, 1 patient	0.5 mg/kg 4 times / day multiple, intravenous Dose: 0.5 mg/kg, 4 times / day Route: intravenous Route: multiple Dose: 0.5 mg/kg, 4 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01954056	unhealthy, neonate Health Status: unhealthy Age Group: neonate Sources: https://clinicaltrials.gov/ct2/show/NCT01954056
Hyperbilirubinemia	serious, 1 patient	0.5 mg/kg 4 times / day multiple, intravenous Dose: 0.5 mg/kg, 4 times / day Route: intravenous Route: multiple Dose: 0.5 mg/kg, 4 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01954056	unhealthy, neonate Health Status: unhealthy Age Group: neonate Sources: https://clinicaltrials.gov/ct2/show/NCT01954056
Hypertension	serious, 1 patient	0.5 mg/kg 4 times / day multiple, intravenous Dose: 0.5 mg/kg, 4 times / day Route: intravenous Route: multiple Dose: 0.5 mg/kg, 4 times / day Sources: https://clinicaltrials.gov/ct2/show/NCT01954056	unhealthy, neonate Health Status: unhealthy Age Group: neonate Sources: https://clinicaltrials.gov/ct2/show/NCT01954056

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 657			inducer 22

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
	11-beta-HSD2 27	MRP2 100 MRP3 55

Drug as perpetrator

Target	Modality	Activity
MRP2 421	inducer 1333 Sources: https://pubmed.ncbi.nlm.nih.gov/15979871/ Page: -	no
CYP3A4 1462	inducer 1333 Sources: https://dmd.aspetjournals.org/content/30/9/1029.long Page: -	yes [EC50 0.6 uM]
Kv1.3 31	supressor 128 Sources: https://www.sciencedirect.com/science/article/pii/S0014299914007730 Page: -	yes [IC50 33.4 uM]
Kv1.5 40	supressor 128 Sources: https://www.sciencedirect.com/science/article/pii/S0014299914007730 Page: -	yes [IC50 33.4 uM]
GLUT4 17	supressor 128 Sources: https://pubmed.ncbi.nlm.nih.gov/26387653/ Page: -	yes
MRP3 200	inducer 1333 Sources: https://pubmed.ncbi.nlm.nih.gov/15979871/ Page: -	yes

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
11-beta-HSD2 27	substrate 2752 Sources: https://rep.bioscientifica.com/view/journals/rep/126/4/425.xml Page: -	major

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1392	inducer 25 Sources: https://www.sciencedirect.com/science/article/pii/S030372071930190X Page: -

Sourcing

Vendor/Aggregator	ID	URL
1PlusChem LLC	1P003ARM
A2B Chem	AB53122
AK Scientific	C481
AK Scientific	J10114
AK Scientific	J92891
APExBIO	B1951
AbovChem LLC	HY-N0583
Acros Organics	35245
Alfa Chemistry	A16292
Alinda	ALBB-025803
Alinda	IBS-E0731050
Angene	AGN-PC-0WH3U2
AstaTech	42245
BOC Sciences	50-23-7
Bide Pharmatech	BD134115
BioSynth	Q-201211
Bosche Scientific	H2132
Cayman Chemical	20739
Chem Scene	CS-2226
Chem4Pharma	C4PST426
ChemDiv	BB57-6734
ChemDiv	N046-0008
ChemShuttle	151488
Combi-Blocks	QA-0828
Compound Cloud	5754
Enamine	EN300-120630
Enamine	Z2786051549
Fluorochem	358100
Hangzhou APIChem Technology	AC-12902
Hangzhou Yuhao Chemical Technology	LT1240
IBScreen	BB_NC-00611
IBScreen	Bio-0648
KeyOrganics	AS-11651
Lab Network	LN00830918
Lab Seeker	SC-18577
MedChem Express	HY-N0583
MolPort	MolPort-001-794-637
Molnova	M14696
NCI Plated 2007	10483
NCI Plated 2007	23903
NCI Plated 2007	27390
Pharmeks	PHBB_NC-02501
Ryan Scientific	074-61028
Ryan Scientific	Minocycline_HCl
Selleck Chemicals	S1696
ShangHai Biochempartner	BCP09054
Sigma Aldrich	1316004
Sigma Aldrich	1316004\|USP
Sigma Aldrich	286095
Sigma Aldrich	286095\|ALDRICH
Sigma Aldrich	31719
Sigma Aldrich	31719\|SIAL
Sigma Aldrich	BP576
Sigma Aldrich	C-106
Sigma Aldrich	C-106\|CERILLIAN
Sigma Aldrich	H0135
Sigma Aldrich	H0135\|SIGMA
Sigma Aldrich	H0396
Sigma Aldrich	H0396\|SIGMA
Sigma Aldrich	H0888
Sigma Aldrich	H0888\|SIGMA
Sigma Aldrich	H1300000
Sigma Aldrich	H1300000\|SIAL
Sigma Aldrich	H3160
Sigma Aldrich	H3160\|SIGMA
Sigma Aldrich	H4001
Sigma Aldrich	H4001\|SIGMA
Sigma Aldrich	H6909
Sigma Aldrich	H6909\|SIGMA
Sigma Aldrich	PHR1014
Sigma Aldrich	PHR1014\|SIAL
Sigma Aldrich	Y0001092
Sigma Aldrich	Y0001092\|SIAL
StruChem	SC-18577
TargetMol	50-23-7
TargetMol	HMDB0000063
TargetMol	T1614
Tetrahedron	TS79645
TimTec	SBB012589
TimTec	ST069286
Tocris	4093
Toronto Research Chemicals	H714615
W&J PharmaChem	100374
ZINC	ZINC000013540519	http://zinc15.docking.org/substances/ZINC000013540519
mcule	MCULE-8463642691
mcule	MCULE-8953627920

PubMed

Title	Date	PubMed
Endocrine and metabolic effects of insulin sensitizers in the treatment of patients with polycystic ovary syndrome and hyperinsulinaemia.	2001	11150875
Individual differences in the diurnal cycle of salivary free cortisol: a replication of flattened cycles for some individuals.	2001 Apr	11166492
Circulatory support of the sick preterm infant.	2001 Feb	11162288
Interactions among paternal behavior, steroid hormones, and parental experience in male marmosets (Callithrix kuhlii).	2001 Feb	11161885
Menstrual cycle variation in spatial ability: relation to salivary cortisol levels.	2001 Feb	11161881
Modulation of P450 CYP3A4-dependent metabolism by P-glycoprotein: implications for P450 phenotyping.	2001 Feb	11160617
Glucocorticoids upregulate CD40 ligand expression and induce CD40L-dependent immunoglobulin isotype switching.	2001 Feb	11160161
Glucocorticoids protect against apoptosis induced by serum deprivation, cyclic adenosine 3',5'-monophosphate and p53 activation in immortalized human granulosa cells: involvement of Bcl-2.	2001 Feb	11159853
Regulation of phosphate uptake in primary cultured rabbit renal proximal tubule cells by glucocorticoids: evidence for nongenomic as well as genomic mechanisms.	2001 Feb	11159843
Plasma adrenocorticotropin and cortisol concentrations during acute hypoxemia after a reversible period of adverse intrauterine conditions in the ovine fetus during late gestation.	2001 Feb	11159829
The effects of epidural block on the distribution of lymphocyte subsets and natural-killer cell activity in patients with and without pain.	2001 Feb	11159252
Pulsatile growth hormone secretion decreases S-adenosylmethionine synthetase in rat liver.	2001 Feb	11158931
PTH and PTH-related peptide enhance steroid secretion from human adrenocortical cells.	2001 Feb	11158922
Urinary thromboxane, prostacyclin, cortisol, and 8-hydroxy-2'-deoxyguanosine in nonsmokers exposed and not exposed to environmental tobacco smoke.	2001 Feb	11158725
Postnatal glucocorticoids in very preterm infants: "the good, the bad, and the ugly"?	2001 Feb	11158479
Cooperative effects of STAT5 (signal transducer and activator of transcription 5) and C/EBPbeta (CCAAT/enhancer-binding protein-beta) on beta-casein gene transcription are mediated by the glucocorticoid receptor.	2001 Feb	11158330
Metabolic abnormalities in patients with adrenal incidentaloma.	2001 Feb	11158083
Is hydrocortisone clearance 50% slower in the evening than in the morning?	2001 Feb	11158078
Paraneoplastic hypercortisolism as a risk factor for severe infections in patients with malignant diseases.	2001 Feb	11158075
Cord blood leptin and insulin-like growth factor levels are independent predictors of fetal growth.	2001 Feb	11158070
Orexin A stimulates cortisol secretion from human adrenocortical cells through activation of the adenylate cyclase-dependent signaling cascade.	2001 Feb	11158046
Time course of 21-hydroxylase antibodies and long-term remission of subclinical autoimmune adrenalitis after corticosteroid therapy: case report.	2001 Feb	11158030
Aromatase p450 expression in a feminizing adrenal adenoma presenting as isosexual precocious puberty.	2001 Feb	11158024
Oral glucose augments the counterregulatory hormone response during insulin-induced hypoglycemia in humans.	2001 Feb	11158023
The patients with incidentally discovered adrenal adenoma (incidentaloma) are not at increased risk of osteoporosis.	2001 Feb	11158016
Food-dependent androgen and cortisol secretion by a gastric inhibitory polypeptide-receptor expressive adrenocortical adenoma leading to hirsutism and subclinical Cushing's syndrome: in vivo and in vitro studies.	2001 Feb	11158012
Human glucocorticoid feedback inhibition is reduced in older individuals: evening study.	2001 Feb	11158007
Troglitazone amplifies counterregulatory responses to hypoglycemia in nondiabetic subjects.	2001 Feb	11158003
Assessment of growth hormone dynamics in human immunodeficiency virus-related lipodystrophy.	2001 Feb	11158000
Fertility and body composition after laparoscopic bilateral adrenalectomy in a 30-year-old female with congenital adrenal hyperplasia.	2001 Feb	11157995
Electrophysiological effects of corticosteroids on the retinal pigment epithelium.	2001 Feb	11157885
Switch from systemic steroids to budesonide in steroid dependent patients with inactive Crohn's disease.	2001 Feb	11156638
Green fluorescent protein mutant as label in homogeneous assays for biomolecules.	2001 Feb 1	11161294
Carbachol induces homologous steroidogenic refractoriness of bovine fasciculata-reticularis cells.	2001 Feb 14	11165048
Post-dexamethasone cortisol level and memory performance in elderly depressed patients.	2001 Feb 2	11163298
Inhibition of cortisol secretion in dispersed head kidney cells of rainbow trout (Oncorhynchus mykiss) by endosulfan, an organochlorine pesticide.	2001 Jan	11161769
Human cervical tissue metabolizes the tobacco-specific nitrosamine, 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone, via alpha-hydroxylation and carbonyl reduction pathways.	2001 Jan	11159748
Tixocortol pivalate contact allergy in the GPMT: frequency and cross-reactivity.	2001 Jan	11156006
Serum allopregnanolone in women with postpartum "blues".	2001 Jan	11152912
Net amino acid flux across the fetal liver and placenta during spontaneous ovine parturition.	2001 Jan	11150831
Growth hormone deficiency caused by pituitary stalk interruption in Fanconi's anemia.	2001 Jan	11148528
Back to basics: early diagnosis and compliance improve final height outcome in congenital adrenal hyperplasia.	2001 Jan	11148504
Serum thyrotropin concentrations and bioactivity during sleep deprivation in depression.	2001 Jan	11146761
Intracellular regeneration of glucocorticoids by 11beta-hydroxysteroid dehydrogenase (11beta-HSD)-1 plays a key role in regulation of the hypothalamic-pituitary-adrenal axis: analysis of 11beta-HSD-1-deficient mice.	2001 Jan	11145573
Localization and developmental regulation of 11beta-hydroxysteroid dehydrogenase-1 and -2 in the baboon syncytiotrophoblast.	2001 Jan	11145568
Circadian variation in O6-alkylguanine-DNA alkyltransferase activity in circulating blood mononuclear cells of healthy human subjects.	2001 Jan 1	11149421
A population physiologically based pharmacokinetic/pharmacodynamic model for the inhibition of 11-beta-hydroxysteroid dehydrogenase activity by glycyrrhetic acid.	2001 Jan 1	11141355
Monohydroxylation and esterification as determinants of the effects of cis- and trans-9-octadecenoic acids on the permeation of hydrocortisone and 5-fluorouracil across hairless mouse skin in vitro.	2001 Jan 16	11165072
The use of chitosan gels as matrices for electrically-modulated drug delivery.	2001 Jan 29	11166412
Fetal hypothalamus-pituitary-adrenal axis on the road to parturition.	2001 Jan-Feb	11153525

Patents

Sample Use Guides

In Vivo Use Guide

The initial dosage of CORTEF (Hydrocortisone) Tablets may vary from 20 mg to 240 mg of hydrocortisone per day depending on the specific disease entity being treated.

Route of Administration: Oral

In Vitro Use Guide

Hydrocortisone concentration-dependently inhibited the current induced by 3 x 10(-5) M ACh with a half maximum inhibitory concentration (IC50) of 2.1 x 10(-4) M (in rats).

Substance Class	Chemical Created by `admin` on `Fri Jun 25 20:49:03 UTC 2021` Edited by `admin` on `Fri Jun 25 20:49:03 UTC 2021`
Record UNII	WI4X0X7BPJ
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

HYDROCORTISONE

Official Name

English

HYDROCORTISONE [ORANGE BOOK]

Common Name

English

HYDROCORTISONE [WHO-IP]

Common Name

English

HYDROCORTISONE ACETATE IMPURITY A [EP]

Common Name

English

HYDROCORTISONE COMPONENT OF CALMURID HC

Common Name

English

HYDROCORTISONE HYDROGEN SUCCINATE IMPURITY A [EP]

Common Name

English

PREDNISOLONE IMPURITY A [EP]

Common Name

English

HYDROCORTISONE [USP-RS]

Common Name

English

PROCTOCORT

Brand Name

English

ANUSOL HC

Brand Name

English

GLYCORT

Brand Name

English

HYDROCORTISONE COMPONENT OF PYOCIDIN

Common Name

English

CORTENEMA

Brand Name

English

HYDROCORTISONE [II]

Common Name

English

OTOCORT COMPONENT HYDROCORTISONE

Common Name

English

HYDROCORTISONE COMPONENT OF OTOBIOTIC

Common Name

English

HYDROCORTISONE SODIUM SUCCINATE IMPURITY A [EP]

Common Name

English

TEXACORT

Brand Name

English

PLENADREN

Brand Name

English

HYDROCORTISONE COMPONENT OF OTICAIR

Common Name

English

CORTEF

Brand Name

English

HYDROCORTISONE [VANDF]

Common Name

English

CORTISOL

Common Name

English

AEROSEB-HC

Brand Name

English

PREGN-4-ENE-3,20-DIONE, 11,17,21-TRIHYDROXY-, (11.BETA.)-

Systematic Name

English

NOGENIC HC

Brand Name

English

HYDROCORTISONE [MART.]

Common Name

English

STIE-CORT

Brand Name

English

EPICORT

Brand Name

English

OTOBIONE COMPONENT HYDROCORTISONE

Common Name

English

HYDROCORTISONE [USP MONOGRAPH]

Common Name

English

HYDROCORTISONE [MI]

Common Name

English

HYDROCORTONE

Brand Name

English

HYDROCORTISONE [GREEN BOOK]

Common Name

English

COLOCORT

Brand Name

English

HYDROCORTISONE COMPONENT OF OTOBIONE

Common Name

English

PEDIOTIC COMPONENT HYDROCORTISONE

Common Name

English

CALMURID HC COMPONENT HYDROCORTISONE

Common Name

English

SYNACORT

Brand Name

English

NSC-10483

Code

English

CORTRIL

Brand Name

English

FLEXICORT

Code

English

PYOCIDIN COMPONENT HYDROCORTISONE

Common Name

English

BETA-HC

Brand Name

English

ORLEX HC COMPONENT HYDROCORTISONE

Common Name

English

ACETASOL HC COMPONENT HYDROCORTISONE

Common Name

English

HYDROCORTISONE COMPONENT OF ACETASOL HC

Common Name

English

VOSOL HC COMPONENT HYDROCORTISONE

Common Name

English

CETACORT

Brand Name

English

CORT-DOME

Brand Name

English

DERMACORT

Brand Name

English

HYDROCORTISONUM [WHO-IP LATIN]

Common Name

English

BALNEOL-HC

Brand Name

English

OTICAIR COMPONENT HYDROCORTISONE

Common Name

English

HYDROCORTISONE COMPONENT OF ORLEX HC

Common Name

English

CIPRO HC COMPONENT HYDROCORTISONE

Common Name

English

HYDROCORTISONE COMPONENT OF OTOCORT

Common Name

English

HYDROCORTISONE [INN]

Common Name

English

HYDROCORTISONE COMPONENT OF VOSOL HC

Common Name

English

NUTRACORT

Brand Name

English

ACTICORT

Brand Name

English

PENECORT

Brand Name

English

HYDROCORTISONE [HSDB]

Common Name

English

HYDROCORTISONE COMPONENT OF PEDIOTIC

Common Name

English

HYDROCORTISONE [EP MONOGRAPH]

Common Name

English

ELDECORT

Brand Name

English

HYTONE

Brand Name

English

ALA-SCALP

Brand Name

English

HYDROCORTISONE COMPONENT OF ALPHADERM

Common Name

English

ALPHADERM COMPONENT HYDROCORTISONE

Common Name

English

11.BETA.,17,21-TRIHYDROXYPREGN-4-ENE-3,20-DIONE

Systematic Name

English

HYDROCORTISONE [WHO-DD]

Common Name

English

ALKINDI SPRINKLE

Brand Name

English

ALA-CORT

Brand Name

English

HYDROCORTISONE COMPONENT OF CIPRO HC

Common Name

English

OTOBIOTIC COMPONENT HYDROCORTISONE

Common Name

English

Classification Tree Code System Code

LIVERTOX

485