Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C24H31FO6.H2O |
Molecular Weight | 452.513 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O.[H][C@@]12C[C@@H](C)[C@](O)(C(=O)COC(C)=O)[C@@]1(C)C[C@H](O)[C@@]3(F)[C@@]2([H])CCC4=CC(=O)C=C[C@]34C
InChI
InChIKey=DPHFJXVKASDMBW-RQRKFSSASA-N
InChI=1S/C24H31FO6.H2O/c1-13-9-18-17-6-5-15-10-16(27)7-8-21(15,3)23(17,25)19(28)11-22(18,4)24(13,30)20(29)12-31-14(2)26;/h7-8,10,13,17-19,28,30H,5-6,9,11-12H2,1-4H3;1H2/t13-,17+,18+,19+,21+,22+,23+,24+;/m1./s1
Molecular Formula | C24H31FO6 |
Molecular Weight | 434.4977 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | H2O |
Molecular Weight | 18.0153 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdfhttp://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004071/WC500204050.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/67018038
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2003/13422slr035_maxidex_lbl.pdfhttp://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004071/WC500204050.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/67018038
Dexamethasone acetate (NEOFORDEX®) is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune response. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide or its analogues and with proteasome inhibitor (e.g. bortezomib).
CNS Activity
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9528963http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/004071/WC500204050.pdf
Curator's Comment: Known to be CNS penetrant in mouse. Human data not available.
Originator
Sources: DOI: 10.1021/ja01545a061https://www.ncbi.nlm.nih.gov/pubmed/13536856
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
4.6 nM [Kd] | |||
Target ID: CHEMBL2034 |
3.7 nM [Kd] | ||
Target ID: CHEMBL1994 |
0.73 nM [Kd] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | MAXIDEX Approved UseFor steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date1962 |
|||
Primary | MAXIDEX Approved UseSteroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe such as allergic conjunctivitis, acne rosacea, superficial punctate keratitis, herpes zoster keratitis, iritis, cyclitis, selected infective conjunctivitides when the inherent hazard of steroid use is accepted to obtain an advisable diminution in edema and inflammation; corneal injury from chemical, radiation, or thermal burns, or penetration of foreign bodies. Launch Date1962 |
|||
Primary | MAXIDEX Approved UseFor steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date1962 |
|||
Primary | MAXIDEX Approved UseFor steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date1962 |
|||
Primary | MAXIDEX Approved UseFor steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date1962 |
|||
Primary | MAXIDEX Approved UseFor steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date1962 |
|||
Primary | MAXIDEX Approved UseFor steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date1962 |
|||
Primary | MAXIDEX Approved UseFor steroid-responsive inflammatory ocular conditions for which a corticosteroid is indicated and where bacterial infection or a risk of bacterial ocular infection exists. Ocular steroids are indicated in inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe where the inherent risk of steroid use in certain infective conjunctivitis is accepted to obtain a diminution in edema and inflammation. They are also indicated in chronic anterior uveitis and corneal injury from chemical, radiation or thermal burns, or penetration of foreign bodies. The use of a combination drug with an anti-infective component is indicated where the risk of infection is high or where there is an expectation that potentially dangerous numbers of bacteria will be present in the eye. The particular anti-infective drug in this product is active against the following common bacterial eye pathogens: Staphylococcus aureus, Escherichia coli, Haemophilus influenzae, Klebsiella/Enterobacter species, Neisseria species, Pseudomonas aeruginosa. This product does not provide adequate coverage against Serratia marcescens, and Streptococci, including Streptococcus pneumoniae. Launch Date1962 |
|||
Primary | Neofordex Approved UseNeofordex is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Launch Date2016 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
9.87 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22047811 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
DEXAMETHASONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
51.2 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22047811 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
DEXAMETHASONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.93 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/22047811 |
2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered: |
DEXAMETHASONE plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
30% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/3806166 |
DEXAMETHASONE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
96 mg multiple, oral (total) |
unhealthy, 63 years (range: 30–78 years) n = 21 Health Status: unhealthy Age Group: 63 years (range: 30–78 years) Sex: M+F Population Size: 21 Sources: |
|
0.1 % 3 times / day multiple, ophthalmic Dose: 0.1 %, 3 times / day Route: ophthalmic Route: multiple Dose: 0.1 %, 3 times / day Sources: |
unhealthy, 68.3 years (range: 51.0 - 83.0 years) n = 77 Health Status: unhealthy Age Group: 68.3 years (range: 51.0 - 83.0 years) Sex: M+F Population Size: 77 Sources: |
Other AEs: Corneal erosion... |
0.6 mg/kg single, oral Dose: 0.6 mg/kg Route: oral Route: single Dose: 0.6 mg/kg Sources: |
unhealthy, children n = 6 Health Status: unhealthy Condition: Migraine Age Group: children Population Size: 6 Sources: |
Other AEs: Constipation... Other AEs: Constipation (below serious, 1 patient) Sources: |
10 mg single, intravenous Dose: 10 mg Route: intravenous Route: single Dose: 10 mg Sources: |
unhealthy n = 106 Health Status: unhealthy Condition: Migraine Population Size: 106 Sources: |
Other AEs: Drowsiness, Dizziness... Other AEs: Drowsiness (below serious, 19 patients) Sources: Dizziness (below serious, 3 patients) Adverse drug reaction NOS (below serious, 10 patients) |
12 mg 1 times / day multiple, intravenous Dose: 12 mg, 1 times / day Route: intravenous Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy n = 10 Health Status: unhealthy Condition: Knee Arthroplasty Population Size: 10 Sources: |
Other AEs: Wound dehiscence... Other AEs: Wound dehiscence (below serious, 1 patient) Sources: |
20 mg single, intravenous Dose: 20 mg Route: intravenous Route: single Dose: 20 mg Sources: |
unhealthy |
|
24 mg 1 times / day multiple, intravenous Dose: 24 mg, 1 times / day Route: intravenous Route: multiple Dose: 24 mg, 1 times / day Sources: |
unhealthy n = 10 Health Status: unhealthy Condition: Knee Arthroplasty Population Size: 10 Sources: |
Other AEs: Dizziness... Other AEs: Dizziness (below serious, 1 patient) Sources: |
8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Other AEs: Constipation, Dyspepsia... Other AEs: Constipation (below serious, 47 patients) Sources: Dyspepsia (below serious, 12 patients) Vomiting (below serious, 9 patients) Fatigue (below serious, 58 patients) Cholesterol high (below serious, 8 patients) Anorexia (below serious, 15 patients) Anxiety (below serious, 11 patient) Insomnia (below serious, 26 patients) Cough (below serious, 9 patients) Dyspnea (below serious, 20 patients) |
8 mg single, intravenous Dose: 8 mg Route: intravenous Route: single Dose: 8 mg Sources: |
pregnant n = 55 Health Status: pregnant Sex: F Population Size: 55 Sources: |
Other AEs: Incision site bleeding, Body temperature decrease... Other AEs: Incision site bleeding (below serious, 1 patient) Sources: Body temperature decrease (below serious, 2 patients) Shivering (below serious, 1 patient) Tachycardia (below serious, 1 patient) Transfusion (below serious, 1 patient) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Corneal erosion | 10% | 0.1 % 3 times / day multiple, ophthalmic Dose: 0.1 %, 3 times / day Route: ophthalmic Route: multiple Dose: 0.1 %, 3 times / day Sources: |
unhealthy, 68.3 years (range: 51.0 - 83.0 years) n = 77 Health Status: unhealthy Age Group: 68.3 years (range: 51.0 - 83.0 years) Sex: M+F Population Size: 77 Sources: |
Constipation | below serious, 1 patient | 0.6 mg/kg single, oral Dose: 0.6 mg/kg Route: oral Route: single Dose: 0.6 mg/kg Sources: |
unhealthy, children n = 6 Health Status: unhealthy Condition: Migraine Age Group: children Population Size: 6 Sources: |
Adverse drug reaction NOS | below serious, 10 patients | 10 mg single, intravenous Dose: 10 mg Route: intravenous Route: single Dose: 10 mg Sources: |
unhealthy n = 106 Health Status: unhealthy Condition: Migraine Population Size: 106 Sources: |
Drowsiness | below serious, 19 patients | 10 mg single, intravenous Dose: 10 mg Route: intravenous Route: single Dose: 10 mg Sources: |
unhealthy n = 106 Health Status: unhealthy Condition: Migraine Population Size: 106 Sources: |
Dizziness | below serious, 3 patients | 10 mg single, intravenous Dose: 10 mg Route: intravenous Route: single Dose: 10 mg Sources: |
unhealthy n = 106 Health Status: unhealthy Condition: Migraine Population Size: 106 Sources: |
Wound dehiscence | below serious, 1 patient | 12 mg 1 times / day multiple, intravenous Dose: 12 mg, 1 times / day Route: intravenous Route: multiple Dose: 12 mg, 1 times / day Sources: |
unhealthy n = 10 Health Status: unhealthy Condition: Knee Arthroplasty Population Size: 10 Sources: |
Dizziness | below serious, 1 patient | 24 mg 1 times / day multiple, intravenous Dose: 24 mg, 1 times / day Route: intravenous Route: multiple Dose: 24 mg, 1 times / day Sources: |
unhealthy n = 10 Health Status: unhealthy Condition: Knee Arthroplasty Population Size: 10 Sources: |
Anxiety | below serious, 11 patient | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Dyspepsia | below serious, 12 patients | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Anorexia | below serious, 15 patients | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Dyspnea | below serious, 20 patients | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Insomnia | below serious, 26 patients | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Constipation | below serious, 47 patients | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Fatigue | below serious, 58 patients | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Cholesterol high | below serious, 8 patients | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Cough | below serious, 9 patients | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Vomiting | below serious, 9 patients | 8 mg 1 times / day multiple, oral Dose: 8 mg, 1 times / day Route: oral Route: multiple Dose: 8 mg, 1 times / day Sources: |
unhealthy n = 147 Health Status: unhealthy Condition: Radiation-Induced Pain Flare Population Size: 147 Sources: |
Incision site bleeding | below serious, 1 patient | 8 mg single, intravenous Dose: 8 mg Route: intravenous Route: single Dose: 8 mg Sources: |
pregnant n = 55 Health Status: pregnant Sex: F Population Size: 55 Sources: |
Shivering | below serious, 1 patient | 8 mg single, intravenous Dose: 8 mg Route: intravenous Route: single Dose: 8 mg Sources: |
pregnant n = 55 Health Status: pregnant Sex: F Population Size: 55 Sources: |
Tachycardia | below serious, 1 patient | 8 mg single, intravenous Dose: 8 mg Route: intravenous Route: single Dose: 8 mg Sources: |
pregnant n = 55 Health Status: pregnant Sex: F Population Size: 55 Sources: |
Transfusion | below serious, 1 patient | 8 mg single, intravenous Dose: 8 mg Route: intravenous Route: single Dose: 8 mg Sources: |
pregnant n = 55 Health Status: pregnant Sex: F Population Size: 55 Sources: |
Body temperature decrease | below serious, 2 patients | 8 mg single, intravenous Dose: 8 mg Route: intravenous Route: single Dose: 8 mg Sources: |
pregnant n = 55 Health Status: pregnant Sex: F Population Size: 55 Sources: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
no | |||
Page: - |
yes | |||
Page: - |
yes | |||
Page: - |
yes | |||
Page: - |
yes | |||
Page: - |
yes | |||
Page: - |
yes | |||
Page: - |
yes | yes (co-administration study) Comment: These data demonstrate that dexamethasone at doses used clinically increased CYP3A4 activity with extensive intersubject variability and that the extent of CYP3A4 induction was, in part, predicted by the baseline activity of CYP3A4 in both healthy volunteers and human hepatocyte cultures. Page: - |
Drug as victim
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sources: https://pubmed.ncbi.nlm.nih.gov/17124593/ Page: - |
yes |
PubMed
Title | Date | PubMed |
---|---|---|
Blockade of cocaine-induced increases in adrenocorticotrophic hormone and cortisol does not attenuate the subjective effects of smoked cocaine in humans. | 1999 Sep |
|
Antenatal dexamethasone improves atrial natriuretic peptide receptors in hypoplastic lung in nitrofen-induced diaphragmatic hernia in rats. | 2000 |
|
Immune abnormalities in aneurysmal subarachnoid haemorrhage patients: relation to delayed cerebral vasospasm. | 2000 Apr |
|
Leptin production in adipocytes from morbidly obese subjects: stimulation by dexamethasone, inhibition with troglitazone, and influence of gender. | 2000 Aug |
|
Dexamethasone enhances ras-recision gene expression in cultured murine fetal lungs: role in development. | 2000 Aug |
|
Dexamethasone suppresses tumor necrosis factor-alpha-induced apoptosis in osteoblasts: possible role for ceramide. | 2000 Aug |
|
Effects of several glucocorticosteroids and PDE4 inhibitors on increases in total lung eosinophil peroxidase (EPO) levels following either systemic or intratracheal administration in sephadex- or ovalbumin-induced inflammatory models. | 2000 Aug |
|
TEL/AML1 gene fusion is related to in vitro drug sensitivity for L-asparaginase in childhood acute lymphoblastic leukemia. | 2000 Aug 1 |
|
Effects of dexamethasone on mitogen-activated protein kinases in mouse macrophages: implications for the regulation of 85 kDa cytosolic phospholipase A(2). | 2000 Aug 15 |
|
Dexamethasone-suppressible hypertension. | 2000 Aug 26 |
|
Suppressive effect of active hexose correlated compound (AHCC) on thymic apoptosis induced by dexamethasone in the rat. | 2000 Dec |
|
Effect of endogenous and exogenous prostaglandin E(2) on interleukin-1 beta-induced cyclooxygenase-2 expression in human airway smooth-muscle cells. | 2000 Dec |
|
Low doses of oral dexamethasone for hormone-refractory prostate carcinoma. | 2000 Dec 15 |
|
Prenatal exposure to high levels of glucocorticoids increases the susceptibility of cerebellar granule cells to oxidative stress-induced cell death. | 2000 Dec 19 |
|
Effect of polyunsaturated fatty acids on dexamethasone-induced gastric mucosal damage. | 2000 Feb |
|
Efficacy and harm of pharmacological prevention of acute mountain sickness: quantitative systematic review. | 2000 Jul 29 |
|
Dexamethasone induced cardiac hypertrophy in newborn rats is accompanied by changes in myosin heavy chain phenotype and gene transcription. | 2000 Jun |
|
Expression and induction of CYP1A1/1A2, CYP2A6 and CYP3A4 in primary cultures of human hepatocytes: a 10-year follow-up. | 2000 Jun |
|
Combined administration of G-CSF and dexamethasone for the mobilization of granulocytes in normal donors: optimization of dosing. | 2000 Jun |
|
Down-regulation of thyroid transcription factor-1 gene expression in fetal lung hypoplasia is restored by glucocorticoids. | 2000 Jun |
|
Functional probing of the human glucocorticoid receptor steroid-interacting surface by site-directed mutagenesis. Gln-642 plays an important role in steroid recognition and binding. | 2000 Jun 23 |
|
beta(3)-adrenoceptor regulation and relaxation responses in mouse ileum. | 2000 Mar |
|
Induction and regulation of xenobiotic-metabolizing cytochrome P450s in the human A549 lung adenocarcinoma cell line. | 2000 Mar |
|
Regulation of vitamin D-1alpha-hydroxylase and -24-hydroxylase expression by dexamethasone in mouse kidney. | 2000 Mar |
|
Glucocorticoids act within minutes to inhibit recruitment of signalling factors to activated EGF receptors through a receptor-dependent, transcription-independent mechanism. | 2000 May |
|
Effects of selected herbicides on cytokine production in vitro. | 2000 May 19 |
|
Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands. | 2000 May 19 |
|
Cognitive sequelae in children treated for acute lymphoblastic leukemia with dexamethasone or prednisone. | 2000 May-Jun |
|
Corticosteroids and cognitive function in humans: methodological considerations. | 2000 May-Jun |
|
Regulation of leptin release by troglitazone in human adipose tissue. | 2000 Nov |
|
Ocular hypertensive response to topical dexamethasone in children: a dose-dependent phenomenon. | 2000 Nov |
|
Efficacy of galectins in the amelioration of nephrotoxic serum nephritis in Wistar Kyoto rats. | 2000 Nov |
|
Ritonavir increases the level of active ADD-1/SREBP-1 protein during adipogenesis. | 2000 Nov 10 |
|
Dexamethasone-induced cardiogenic shock rescued by percutaneous cardiopulmonary support (PCPS) in a patient with pheochromocytoma. | 2000 Oct |
|
Antenatal dexamethasone enhances surfactant protein synthesis in the hypoplastic lung of nitrofen-induced diaphragmatic hernia in rats. | 2000 Oct |
|
Role of caspases in dexamethasone-induced apoptosis and activation of c-Jun NH2-terminal kinase and p38 mitogen-activated protein kinase in human eosinophils. | 2000 Oct |
|
Endotoxin augments cerebral hyperemic response to halothane by inducing nitric oxide synthase and cyclooxygenase. | 2000 Oct |
|
Endocrinologic and psychological effects of short-term dexamethasone in anorexia nervosa. | 2000 Sep |
|
ECT administration in a patient after craniotomy and gamma knife surgery: a case report and review. | 2000 Sep |
|
Modification of biophysical properties of lung epithelial Na(+) channels by dexamethasone. | 2000 Sep |
|
Involvement of tyrosine hydroxylase up regulation in dexamethasone-induced hypertension of rats. | 2000 Sep 8 |
|
Intractable nausea attributable to isolated deficiency of adrenocorticotropic hormone: prompt resolution after administration of glucocorticoid. | 2000 Sep-Oct |
|
A multicenter, randomized open study of early corticosteroid treatment (OSECT) in preterm infants with respiratory illness: comparison of early and late treatment and of dexamethasone and inhaled budesonide. | 2001 Feb |
|
Molecular and pharmacological evidence for modulation of kinin B(1) receptor expression by endogenous glucocorticoids hormones in rats. | 2001 Jan |
|
Evaluation of the myocilin (MYOC) glaucoma gene in monkey and human steroid-induced ocular hypertension. | 2001 Jan |
|
The clinical impact of metabolic bone disease in coeliac disease. | 2001 Jan |
|
Short term effects of corticosteroid pulse treatment on disease activity and the wellbeing of patients with active rheumatoid arthritis. | 2001 Jan |
|
Inhibition of NF-kappaB and AP-1 activation by R- and S-flurbiprofen. | 2001 Jan |
|
Adverse effects of early dexamethasone treatment in extremely-low-birth-weight infants. National Institute of Child Health and Human Development Neonatal Research Network. | 2001 Jan 11 |
|
Topical 0.1% indomethacin solution versus topical 0.1% dexamethasone solution in the prevention of inflammation after cataract surgery. The Study Group. | 2001 Jan-Feb |
Patents
Sample Use Guides
One or two drops topically in the conjunctival sac(s). In severe disease, drops may be used hourly. In
mild disease, drops may be used up to four to six times daily.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16971495
Caco-2 cells were treated with 1 μM dexamethasone and SGK1 mRNA levels were determined by Northern blot analysis. Figure 1A shows that dexamethasone rapidly induced SGK1 mRNA expression as early as 30 min and maintained the elevated expression for at least 24 h.
Substance Class |
Chemical
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Fri Dec 15 15:05:31 GMT 2023
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Fri Dec 15 15:05:31 GMT 2023
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DWN2WN457X
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NCI_THESAURUS |
C521
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DTXSID20204402
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DB14649
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DEXAMETHASONE ACETATE MONOHYDRATE
Created by
admin on Fri Dec 15 15:05:31 GMT 2023 , Edited by admin on Fri Dec 15 15:05:31 GMT 2023
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PRIMARY | Description: A white or almost white powder, odourless. Solubility: Practically insoluble in water; soluble in 40 parts of ethanol (~750 g/l) TS; slightly soluble in ether R.Category: Adrenoglucocorticoid. Storage: Dexamethasone acetate should be kept in a tightly closed container, protected from light. Labelling: The designation on the container of Dexamethasone acetate should state whether the substance is the monohydrateor is in the anhydrous form. | ||
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DWN2WN457X
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656823
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826
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55812-90-3
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C77414
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PARENT -> SALT/SOLVATE | |||
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ANHYDROUS->SOLVATE |
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ACTIVE MOIETY |