Chemical Property of Deflazacort
Chemical Property:
- Appearance/Colour:COA
- Vapor Pressure:4.13E-14mmHg at 25°C
- Melting Point:255-256.5 °C
- Refractive Index:1.675
- Boiling Point:595.4 °C at 760 mmHg
- PKA:14.30±0.70(Predicted)
- Flash Point:313.9 °C
- PSA：102.26000
- Density:1.41 g/cm3
- LogP:1.99880
- Storage Temp.:-20°C Freezer
- Solubility.:DMSO: ≥20mg/mL
- XLogP3:2
- Hydrogen Bond Donor Count:1
- Hydrogen Bond Acceptor Count:7
- Rotatable Bond Count:4
- Exact Mass:441.21513771
- Heavy Atom Count:32
- Complexity:996
- Purity/Quality:
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99.00% *data from raw suppliers
Deflazacort-d3 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- Safety Statements:
24/25
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC1=NC2(C(O1)CC3C2(CC(C4C3CCC5=CC(=O)C=CC45C)O)C)C(=O)COC(=O)C
- Isomeric SMILES:CC1=N[C@@]2([C@H](O1)C[C@@H]3[C@@]2(C[C@@H]([C@H]4[C@H]3CCC5=CC(=O)C=C[C@]45C)O)C)C(=O)COC(=O)C
- Recent ClinicalTrials:Deflazacort vs. Prednisolone in Acute-stage ABPA
- Recent EU Clinical Trials:Deflazacort TREATment in LMNA related congenital muscular dystrophy: study of clinical effectiveness and search for reliable biomarkers.
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Description
Deflazacort (trade name Emflaza among others) is a glucocorticoid used as an anti-inflammatory and immunosuppressant. It belongs to a group of medicines called corticosteroids. It is sometimes referred to simply as an oral steroid.
Deflazacort is an inactive prodrug which is metabolized rapidly to the active drug 21-desacetyldeflazacort.It is used to treat a wide variety of conditions. Some examples include autoimmune diseases (for example, systemic lupus erythematosus (SLE), autoimmune hepatitis, sarcoidosis), joint and muscle diseases (for example, rheumatoid arthritis), and allergies and asthma.
Cardiff can be specially designed for the third generation of corticosteroids, anti-inflammatory, anti-allergy, and it increased gluconeogenesis and so on. It acts as prednisolone 10~20 times of the dragon, 40 times as hydrocortisone. This product has no mutagenic effect. This product, labeled with C14 study, shows that the product of the gastrointestinal tract rapidly absorbed, reaching the peak blood concentration after 1~2h, forming the active substance by hydrolysis, and the latter further metabolic processes is similar with other corticosteroids, as well as the active metabolite T1/2 is 2 h and the rats are mainly distributed in the kidney and hematopoietic system and other organizations.
Figure 1 is a deflazacort formula. Deflazacort is an antiinflammatory
treatment of rheumatoid arthritis. Its antirheumatic potency i s similar to that of prednisone, while its hyperglycernic and calcium depleting effects are reportedly less.
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Drug interactions
Cardiff may have unique row potassium, and it should pay more attention when combined with diuretics.
When combined with the drug having enzymatic action (rifampicin, phenobarbital, etc.), the corticosteroids should be properly increment.
Erythromycin, estrogen can inhibit the activity of this product and the metabolism, when combined with appropriate reductions. Potentially hazardous interactions with other drugsAldesleukin: avoid concomitant useAntibacterials: metabolism accelerated by rifamycins;
metabolism possibly inhibited by erythromycin;
concentration of isoniazid possibly reduced.Anticoagulants: efficacy of coumarins and
phenindione may be altered.Antiepileptics: metabolism accelerated by
carbamazepine, fosphenytoin, phenobarbital,
phenytoin and primidoneAntifungals: increased risk of hypokalaemia with
amphotericin - avoid; metabolism possibly inhibited
by itraconazole and ketoconazoleAntivirals: concentration possibly increased by
ritonavir.Ciclosporin: rare reports of convulsions in patients
on ciclosporin and high-dose corticosteroids;
increased half-life of deflazacort.Cobicistat: concentration increased by cobicistat -
avoid.Diuretics: enhanced hypokalaemic effects of
acetazolamide, loop diuretics and thiazide diuretics.Vaccines: high dose corticosteroids can impair
immune response to vaccines; avoid with live
vaccines.
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Uses
Deflazacort-d3, is the labeled analogue of Deflazacort (D228975), a systemic corticosteroid, and a derivative of prednisolone. Used for rheumatoid arthritis and lupus. antiinflammatory A systemic corticosteroid. A derivative of prednisolone. Used for rheumatoid arthritis and lupus
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Clinical Use
Glucocorticoid:Suppression of inflammatory and allergic disorders
