Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C22H28FO8P.2Na |
Molecular Weight | 516.4046 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].[Na+].[H][C@@]12C[C@@H](C)[C@](O)(C(=O)COP([O-])([O-])=O)[C@@]1(C)C[C@H](O)[C@@]3(F)[C@@]2([H])CCC4=CC(=O)C=C[C@]34C
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 | Na |
Molecular Weight | 22.9898 |
Charge | 1 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | C22H28FO8P |
Molecular Weight | 470.4251 |
Charge | -2 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
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 |
---|---|---|
Effects of dexamethasone on tumor-induced brain edema and its distribution in the brain of monkeys. | 1979 Mar |
|
The role of pulmonary inflammation in the development of pulmonary hypertension in newborn with meconium aspiration syndrome (MAS). | 1999 |
|
ECC-1 human endometrial cells as a model system to study dioxin disruption of steroid hormone function. | 1999 Apr |
|
Functional assay of NF-kappaB translocation into nuclei by laser scanning cytometry: inhibitory effect by dexamethasone or theophylline. | 1999 Apr |
|
Overexpression of urokinase-type plasminogen activator in pancreatic adenocarcinoma is regulated by constitutively activated RelA. | 1999 Aug 12 |
|
Inhibition of transforming growth factor beta1-induced hepatoma cell apoptosis by liver tumor promoters: characterization of primary signaling events and effects on CPP32-like caspase activity. | 1999 Feb |
|
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 |
|
The anti-emetic efficacy of tropisetron plus dexamethasone in patients treated with high-dose chemotherapy and stem cell transplantation. | 1999 Mar |
|
Pharmacological validation of a feline model of steroid-induced ocular hypertension. | 1999 Mar |
|
Effect of dexamethasone on cyclophosphamide-induced cystitis in rats: lack of relation with bradykinin B1 receptor-mediated motor responses. | 1999 Mar 12 |
|
Effect of arsenite on induction of CYP1A, CYP2B, and CYP3A in primary cultures of rat hepatocytes. | 1999 May 15 |
|
Dexamethasone therapy increases infection in very low birth weight infants. | 1999 Nov |
|
Antenatal dexamethasone suppresses tumor necrosis factor-alpha expression in hypoplastic lung in nitrofen-induced diaphragmatic hernia in rats. | 1999 Nov |
|
Early (4-7 days of age) dexamethasone therapy for prevention of chronic lung disease in preterm infants. | 1999 Nov |
|
Dual action of nitric oxide in pathogenesis of indomethacin-induced small intestinal ulceration in rats. | 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 |
|
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 |
|
Dexamethasone-suppressible hypertension. | 2000 Aug 26 |
|
Acrylamide-regulated neurofilament expression in rat pheochromocytoma cells. | 2000 Jan 10 |
|
Expression and induction of CYP1A1/1A2, CYP2A6 and CYP3A4 in primary cultures of human hepatocytes: a 10-year follow-up. | 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 |
|
Induction and regulation of xenobiotic-metabolizing cytochrome P450s in the human A549 lung adenocarcinoma cell line. | 2000 Mar |
|
Patients with myelodysplastic syndromes benefit from palliative therapy with amifostine, pentoxifylline, and ciprofloxacin with or without dexamethasone. | 2000 Mar 1 |
|
Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands. | 2000 May 19 |
|
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 |
|
Ritonavir increases the level of active ADD-1/SREBP-1 protein during adipogenesis. | 2000 Nov 10 |
|
Antenatal dexamethasone enhances surfactant protein synthesis in the hypoplastic lung of nitrofen-induced diaphragmatic hernia in rats. | 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 |
|
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 |
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Molecular and pharmacological evidence for modulation of kinin B(1) receptor expression by endogenous glucocorticoids hormones in rats. | 2001 Jan |
|
Inhibition of NF-kappaB and AP-1 activation by R- and S-flurbiprofen. | 2001 Jan |
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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 |
|
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 Dec 15 15:35:21 GMT 2023
by
admin
on
Fri Dec 15 15:35:21 GMT 2023
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Record UNII |
AI9376Y64P
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Record Status |
Validated (UNII)
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Record Version |
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Common Name | English | ||
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
373212
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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||
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NCI_THESAURUS |
C521
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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||
|
EU-Orphan Drug |
EU/3/13/1158
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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Code System | Code | Type | Description | ||
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|
16961
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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41879
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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48933
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | RxNorm | ||
|
4462
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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1177032
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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756722
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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219-243-0
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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100000090542
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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CHEMBL1201302
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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C1362
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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AI9376Y64P
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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DBSALT000843
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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2392-39-4
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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m4215
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | Merck Index | ||
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SUB01615MIG
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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AI9376Y64P
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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SUB122698
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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ALTERNATIVE | |||
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DEXAMETHASONE SODIUM PHOSPHATE
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
|
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. | ||
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DTXSID3047429
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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PRIMARY | |||
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C004180
Created by
admin on Fri Dec 15 15:35:22 GMT 2023 , Edited by admin on Fri Dec 15 15:35:22 GMT 2023
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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
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||
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IMPURITY -> PARENT |
EP
|
||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (GC)
USP
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||
|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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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 |