Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H28FO8P.2Na |
Molecular Weight | 516.4055 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@]1([H])C[C@@]2([H])[C@]3([H])CCC4=CC(=O)C=C[C@]4(C)[C@]3([C@]([H])(C[C@]2(C)[C@]1(C(=O)COP(=O)([O-])[O-])O)O)F.[Na+].[Na+]
InChI
InChIKey=PLCQGRYPOISRTQ-FCJDYXGNSA-L
InChI=1S/C22H30FO8P.2Na/c1-12-8-16-15-5-4-13-9-14(24)6-7-19(13,2)21(15,23)17(25)10-20(16,3)22(12,27)18(26)11-31-32(28,29)30;;/h6-7,9,12,15-17,25,27H,4-5,8,10-11H2,1-3H3,(H2,28,29,30);;/q;2*+1/p-2/t12-,15+,16+,17+,19+,20+,21+,22+;;/m1../s1
Molecular Formula | C22H28FO8P |
Molecular Weight | 470.4259 |
Charge | -2 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | Na |
Molecular Weight | 22.9898 |
Charge | 1 |
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 Date-2.377728E11 |
|||
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 Date-2.37859193E11 |
|||
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 Date-2.377728E11 |
|||
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 Date-2.377728E11 |
|||
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 Date-2.37859193E11 |
|||
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 Date-2.377728E11 |
|||
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 Date-2.377728E11 |
|||
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 Date-2.377728E11 |
|||
Primary | Neofordex Approved UseNeofordex is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Launch Date1.45799997E12 |
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 |
---|---|---|
Effects of dexamethasone on tumor-induced brain edema and its distribution in the brain of monkeys. | 1979 Mar |
|
ECC-1 human endometrial cells as a model system to study dioxin disruption of steroid hormone function. | 1999 Apr |
|
Glucocorticoids inhibit proliferation and adhesion of the IL-3-dependent mast cell line, MC/9, to NIH/3T3 fibroblasts, with an accompanying decrease in IL-3 receptor expression. | 1999 Apr |
|
Overexpression of urokinase-type plasminogen activator in pancreatic adenocarcinoma is regulated by constitutively activated RelA. | 1999 Aug 12 |
|
The glucocorticoid receptor is essential for maintaining basal and dexamethasone-induced repression of the murine corticosteroid-binding globulin gene. | 1999 Aug 20 |
|
Antiemetic efficacy of granisetron plus dexamethasone in bone marrow transplant patients receiving chemotherapy and total body irradiation. | 1999 Feb |
|
Dexamethasone induced alterations in the levels of proteases involved in blood pressure homeostasis and blood coagulation in rats. | 1999 Jul |
|
[Iatrogenic Cushing syndrome and mutatio tarda caused by dexamethasone containing nose drops]. | 1999 Jul |
|
Induction of stromelysin gene expression by tumor necrosis factor alpha is inhibited by dexamethasone, salicylate, and N-acetylcysteine in synovial fibroblasts. | 1999 Jun |
|
Nitric oxide, superoxide radicals and mast cells in pathogenesis of indomethacin-induced small intestinal lesions in rats. | 1999 Mar |
|
Pharmacological validation of a feline model of steroid-induced ocular hypertension. | 1999 Mar |
|
Intestinal damage induced by zinc deficiency is associated with enhanced CuZn superoxide dismutase activity in rats: effect of dexamethasone or thyroxine treatment. | 1999 May |
|
Effect of arsenite on induction of CYP1A, CYP2B, and CYP3A in primary cultures of rat hepatocytes. | 1999 May 15 |
|
Effects of theophylline, dexamethasone and salbutamol on cytokine gene expression in human peripheral blood CD4+ T-cells. | 1999 Nov |
|
Early (4-7 days of age) dexamethasone therapy for prevention of chronic lung disease in preterm infants. | 1999 Nov |
|
Pharmacological and histopathological study of cyclophosphamide-induced hemorrhagic cystitis - comparison of the effects of dexamethasone and Mesna. | 1999 Oct |
|
Dexamethasone increases eNOS gene expression and prevents renal vasoconstriction induced by cyclosporin. | 1999 Sep |
|
Melatonin regulates glucocorticoid receptor: an answer to its antiapoptotic action in thymus. | 1999 Sep |
|
Morphine induced allodynia in a child with brain tumour. | 1999 Sep 4 |
|
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 |
|
TEL/AML1 gene fusion is related to in vitro drug sensitivity for L-asparaginase in childhood acute lymphoblastic leukemia. | 2000 Aug 1 |
|
Dexamethasone-suppressible hypertension. | 2000 Aug 26 |
|
Low doses of oral dexamethasone for hormone-refractory prostate carcinoma. | 2000 Dec 15 |
|
Antenatal dexamethasone enhances endothelin receptorB expression in hypoplastic lung in nitrofen-induced diaphragmatic hernia in rats. | 2000 Feb |
|
Inhibition of carrageenan-induced edema by indomethacin or sodium salicylate does not prevent the increase of nerve growth factor in the rat hind paw. | 2000 Jan 14 |
|
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 |
|
Induction and regulation of xenobiotic-metabolizing cytochrome P450s in the human A549 lung adenocarcinoma cell line. | 2000 Mar |
|
Ticlopidine-induced aplastic anemia: development of chromosomal abnormalities and response to immunosuppressive therapy. | 2000 Mar |
|
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 |
|
Efficacy of galectins in the amelioration of nephrotoxic serum nephritis in Wistar Kyoto rats. | 2000 Nov |
|
Endocrinologic and psychological effects of short-term dexamethasone in anorexia nervosa. | 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 |
|
Genomic screening for genes silenced by DNA methylation revealed an association between RASD1 inactivation and dexamethasone resistance in multiple myeloma. | 2009 Jul 1 |
|
Triptolide enhances the sensitivity of multiple myeloma cells to dexamethasone via microRNAs. | 2012 Jun |
|
Novel phosphatidylinositol 3-kinase inhibitor NVP-BKM120 induces apoptosis in myeloma cells and shows synergistic anti-myeloma activity with dexamethasone. | 2012 Jun |
|
CEP-18770 (delanzomib) in combination with dexamethasone and lenalidomide inhibits the growth of multiple myeloma. | 2012 Nov |
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
Created
by
admin
on
Edited
Fri Jun 25 21:03:56 UTC 2021
by
admin
on
Fri Jun 25 21:03:56 UTC 2021
|
Record UNII |
AI9376Y64P
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Brand Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Brand Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
Classification Tree | Code System | Code | ||
---|---|---|---|---|
|
FDA ORPHAN DRUG |
373212
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
||
|
NCI_THESAURUS |
C521
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
||
|
EU-Orphan Drug |
EU/3/13/1158
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
16961
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | |||
|
48933
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | RxNorm | ||
|
219-243-0
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | |||
|
CHEMBL1201302
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | |||
|
C1362
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | |||
|
AI9376Y64P
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | |||
|
DBSALT000843
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | |||
|
2392-39-4
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | |||
|
M4215
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | Merck Index | ||
|
SUB01615MIG
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | |||
|
SUB122698
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
ALTERNATIVE | |||
|
DEXAMETHASONE SODIUM PHOSPHATE
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | Description: A white or almost white, crystalline powder.Solubility: Freely soluble in water; slightly soluble in ethanol (~750 g/L) TS; practically insoluble in dichloromethane R.Category: Adrenal hormone.Storage: Dexamethasone sodium phosphate should be kept in a tightly closed container, protected from light.Additional information: Dexamethasone sodium phosphate is very hygroscopic. Even in the absence of light it is graduallydegraded on exposure to a humid atmosphere, the decomposition being faster at higher temperatures. Dexamethasone sodiumphosphate may exhibit polymorphism. | ||
|
1177032
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | USP-RS | ||
|
2392-39-4
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY | |||
|
C004180
Created by
admin on Fri Jun 25 21:03:56 UTC 2021 , Edited by admin on Fri Jun 25 21:03:56 UTC 2021
|
PRIMARY |
Related Record | Type | Details | ||
---|---|---|---|---|
|
PARENT -> SALT/SOLVATE |
Related Record | Type | Details | ||
---|---|---|---|---|
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
||
|
IMPURITY -> PARENT |
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (GC)
USP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
correction factor: for the calculation of content, multiply the peak area of impurity A by 0.75
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
|
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |