Tìm theo
Dexamethasone
Các tên gọi khác (10 ) :
  • 1-Dehydro-16alpha-methyl-9alpha-fluorohydrocortisone
  • 1-Dehydro-16α-methyl-9α-fluorohydrocortisone
  • 16alpha-Methyl-9alpha-fluoro-1-dehydrocortisol
  • 16α-Methyl-9α-fluoro-1-dehydrocortisol
  • 9alpha-Fluoro-16alpha-methylprednisolone
  • 9α-Fluoro-16α-methylprednisolone
  • Decadron
  • Dexametasona
  • Dexamethasone
  • Dexamethasonum
Hormon, Nội tiết tố
Thuốc Gốc
Small Molecule
CAS: 50-02-2
ATC: A01AC02, C05AA09, D07AB19, D07XB05, D10AA03, H02AB02, R01AD03, S01BA01, S01CB01, S02BA06, S03BA01
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C22H29FO5
PTK: 392.4611
An anti-inflammatory 9-fluoro-glucocorticoid. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H29FO5
Phân tử khối
392.4611
Monoisotopic mass
392.199902243
InChI
InChI=1S/C22H29FO5/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,23)17(26)10-20(16,3)22(12,28)18(27)11-24/h6-7,9,12,15-17,24,26,28H,4-5,8,10-11H2,1-3H3/t12-,15+,16+,17+,19+,20+,21+,22+/m1/s1
InChI Key
InChIKey=UREBDLICKHMUKA-CXSFZGCWSA-N
IUPAC Name
(1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
Traditional IUPAC Name
dexamethasone
SMILES
[H][C@@]12C[C@@H](C)[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Độ tan chảy
170-229
Độ hòa tan
89 mg/L (at 25 °C)
logP
1.83
logS
-3.64
pKa (strongest acidic)
12.42
pKa (Strongest Basic)
-3.3
PSA
94.83 Å2
Refractivity
102.49 m3·mol-1
Polarizability
40.83 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
caco2 Permeability
-4.75
Dược Lực Học : Dexamethasone and its derivatives, dexamethasone sodium phosphate and dexamethasone acetate, are synthetic glucocorticoids. Used for its antiinflammatory or immunosuppressive properties and ability to penetrate the CNS, dexamethasone is used alone to manage cerebral edema and with tobramycin to treat corticosteroid-responsive inflammatory ocular conditions.
Cơ Chế Tác Dụng : An anti-inflammatory 9-fluoro-glucocorticoid. [PubChem] Dexamethasone is a glucocorticoid agonist. Unbound dexamethasone crosses cell membranes and binds with high affinity to specific cytoplasmic glucocorticoid receptors. This complex binds to DNA elements (glucocorticoid response elements) which results in a modification of transcription and, hence, protein synthesis in order to achieve inhibition of leukocyte infiltration at the site of inflammation, interference in the function of mediators of inflammatory response, suppression of humoral immune responses, and reduction in edema or scar tissue. The antiinflammatory actions of dexamethasone are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.
Dược Động Học :
▧ Absorption :
80-90%
▧ Protein binding :
70%
▧ Metabolism :
Hepatic.
▧ Half Life :
36-54 hours
Độc Tính : Oral, rat LD50: >3 gm/kg. Signs of overdose include retinal toxicity, glaucoma, subcapsular cataract, gastrointestinal bleeding, pancreatitis, aseptic bone necrosis, osteoporosis, myopathies, obesity, edemas, hypertension, proteinuria, diabetes, sleep disturbances, psychiatric syndromes, delayed wound healing, atrophy and fragility of the skin, ecchymosis, and pseudotumor cerebri.
Chỉ Định : Injection: for the treatment of endocrine disorders, rheumatic D=disorders, collagen diseases, dermatologic diseases, allergic statesc, ophthalmic diseases, gastrointestinal diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, cerebral edema.
Ophthalmic ointment and solution: for the treatment of steroid responsive inflammatory conditions of the palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe.
Ophthalmic solution only: for the treatment of steroid responsive inflammatory conditions of the external auditory meatus
Topic cream: for relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses
Oral aerosol: for the treatment of bronchial asthma and related corticosteroid responsive bronchospastic states intractable to adequate trial of conventional therapy
Intranasal aerosol: for the treatment of allergic ot inflammatory nasal conditions, and nasal polyps
Tương Tác Thuốc :
  • Acenocoumarol The corticosteroid, dexamethasone, alters the anticoagulant effect, acenocoumarol.
  • Acetylsalicylic acid The corticosteroid, dexamethasone, may decrease the effect of the salicylate, acetylsalicylic acid.
  • Ambenonium The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, ambenonium.
  • Aminoglutethimide Aminoglutethimide may decrease the effect of dexamethasone.
  • Amobarbital The barbiturate, amobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Anisindione The corticosteroid, dexamethasone, alters the anticoagulant effect of anisindione.
  • Aprepitant Aprepitant may increase the effect and toxicity of dexamethasone.
  • Aprobarbital The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Asparaginase Erwinia chrysanthemi Monitor therapy as asparaginase erwinia chrysanthemi may increase the serum concentration of dexamethasone due to a decrease of hepatic proteins necessary for dexamethasone metabolism.
  • Butabarbital The barbiturate, butabarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Butalbital The barbiturate, butalbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Butethal The barbiturate, butethal, may decrease the effect of the corticosteroid, dexamethasone.
  • Dabigatran etexilate P-Glycoprotein inducers such as dexamethasone may decrease the serum concentration of dabigatran etexilate. This combination should be avoided.
  • Dicoumarol The corticosteroid, dexamethasone, alters the anticoagulant effect of dicumarol.
  • Dihydroquinidine barbiturate The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, dexamethasone.
  • Edrophonium The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, edrophonium.
  • Estradiol valerate/Dienogest Affects CYP3A4 metabolism, decreases or effects levels of Estradiol valerate/Dienogest.
  • Ethotoin The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, dexamethasone.
  • Fosphenytoin The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, dexamethasone.
  • Heptabarbital The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Hexobarbital The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Imatinib Dexamethasone may decrease levels of imatinib.
  • Lurasidone Concomitant therapy with a CYP3A4 inducer will decrease levels of lurasidone. Coadministration with lurasidone is contraindicated. Will decrease Cmax of lurasidone by 85%.
  • Magnesium salicylate The corticosteroid, dexamethasone, may decrease the effect of magnesium salicylate.
  • Mephenytoin The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, dexamethasone.
  • Methohexital The barbiturate, methohexital, may decrease the effect of the corticosteroid, dexamethasone.
  • Methylphenobarbital The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Midodrine Increased arterial pressure
  • Neostigmine The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, neostigmine.
  • Pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Phenobarbital The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Phenytoin The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, dexamethasone.
  • Primidone The barbiturate, primidone, may decrease the effect of the corticosteroid, dexamethasone.
  • Pyridostigmine The corticosteroid, dexamethasone, may decrease the effect of the anticholinesterase, pyridostigmine.
  • Quinidine barbiturate The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, dexamethasone.
  • Rifampicin The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, dexamethasone.
  • Rilpivirine Strong inducers of CYP3A4 decrease the exposure of rilpivirine thus decreasing efficacy.
  • Roflumilast Affects CYP3A4 metabolism, decreases level or effect of roflumilast.
  • Salsalate The corticosteroid, dexamethasone, may decrease the effect of the salicylate, salsalate.
  • Secobarbital The barbiturate, secobarbital, may decrease the effect of the corticosteroid, dexamethasone.
  • Sunitinib Possible decrease in sunitinib levels
  • Tacrine Tacrine and Dexamethasone may independently exacerbate muscle weakness in myasthenia gravis patients. Monitor for additive muscle weakness effects.
  • Talbutal The barbiturate, talbutal, may decrease the effect of the corticosteroid, dexamethasone.
  • Telithromycin Co-administration may cause decreased Telithromycin and increased Dexamethasone plasma concentrations. Consider alternate therapy.
  • Temsirolimus Dexamethasone may increase the metabolism of Temsirolimus decreasing its efficacy. Concomitant therapy should be avoided.
  • Thalidomide Increased risk of dermatologic adverse effects and venous thromboembolic events (VTE). Consider VTE prophylaxis during concomitant therapy and monitor for adverse dematologic effects.
  • Tramadol Dexamethasone may decrease the effect of Tramadol by increasing Tramadol metabolism and clearance.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
  • Trazodone The CYP3A4 inducer, Dexamethasone, may decrease Trazodone efficacy by increasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Dexamethasone is initiated, discontinued or dose changed.
  • Vandetanib Decreases levels of vandetanib by affecting CYP3A4 metabolism. Contraindicated.
  • Vecuronium Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Dexamethasone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of dexamethasone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of dexamethasone if voriconazole is initiated, discontinued or dose changed.
  • Warfarin The corticosteroid, dexamethasone, alters the anticoagulant effect of warfarin.
Liều Lượng & Cách Dùng : Elixir - Oral
Liquid - Intramuscular
Liquid - Intravenous
Liquid - Oral
Ointment - Ophthalmic
Solution - Intravenous
Solution - Ophthalmic
Solution / drops - Ophthalmic
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Baycadron
  • Công ty : Sidus
    Sản phẩm biệt dược : Decadron
  • Công ty :
    Sản phẩm biệt dược : Maxidex
  • Công ty :
    Sản phẩm biệt dược : OZURDEX
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01234
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5743
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508930
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00292
ChemSpider
http://www.chemspider.com/Chemical-Structure.5541.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=18207
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0703-3524-03
PharmGKB
http://www.pharmgkb.org/drug/PA449247
Wikipedia
http://en.wikipedia.org/wiki/Dexamethasone
RxList
http://www.rxlist.com/cgi/generic/dexameth.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/dec1118.shtml
Drugs.com
http://www.drugs.com/cdi/dexamethasone-drops.html
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