Tìm theo
Fludrocortisone
Các tên gọi khác (6 ) :
  • 9alpha-FLUOROCORTISOL
  • Fludrocortison
  • Fludrocortisona
  • Fludrocortisone
  • Fludrocortisonum
  • Fluohydrocortisone
Hormon, Nội tiết tố
Thuốc Gốc
Small Molecule
CAS: 127-31-1
ATC: H02AA02
ĐG : Amerisource Health Services Corp. , http://www.amerisourcebergen.com
CTHH: C21H29FO5
PTK: 380.4504
A synthetic mineralocorticoid with anti-inflammatory activity. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H29FO5
Phân tử khối
380.4504
Monoisotopic mass
380.199902243
InChI
InChI=1S/C21H29FO5/c1-18-7-5-13(24)9-12(18)3-4-15-14-6-8-20(27,17(26)11-23)19(14,2)10-16(25)21(15,18)22/h9,14-16,23,25,27H,3-8,10-11H2,1-2H3/t14-,15-,16-,18-,19-,20-,21-/m0/s1
InChI Key
InChIKey=AAXVEMMRQDVLJB-BULBTXNYSA-N
IUPAC Name
(1R,2S,10S,11S,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one
Traditional IUPAC Name
fludrocortisone
SMILES
[H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])CCC2=CC(=O)CC[C@]12C
Độ hòa tan
140 mg/L (at 25 °C)
logP
1.67
logS
-3.43
pKa (strongest acidic)
12.55
pKa (Strongest Basic)
-3.3
PSA
94.83 Å2
Refractivity
96.93 m3·mol-1
Polarizability
39.6 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
Dược Lực Học : Fludrocortisone is a synthetic adrenocortical steroid possessing very potent mineralocorticoid properties and high glucocorticoid activity. It is indicated as partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison’s disease and for the treatment of salt-losing adrenogenital syndrome. The physiologic action of fludrocortisone acetate is similar to that of hydrocortisone. However, the effects of fludrocortisone acetate, particularly on electrolyte balance, but also on carbohydrate metabolism, are considerably heightened and prolonged. Mineralocorticoids act on the distal tubules of the kidney to enhance the reabsorption of sodium ions from the tubular fluid into the plasma; they increase the urinary excretion of both potassium and hydrogen ions.
Cơ Chế Tác Dụng : A synthetic mineralocorticoid with anti-inflammatory activity. [PubChem] Fludrocortisone binds the mineralocorticoid receptor (aldosterone receptor). This binding (or activation of the mineralocorticoid receptor by fludrocortisone) in turn causes an increase in ion and water transport and thus raises extracellular fluid volume and blood pressure and lowers potassium levels.
Dược Động Học :

▧ Protein binding :
High
▧ Metabolism :
Hepatic, some renal.
▧ Half Life :
3.5 hours
Độc Tính : Effects of overexposure include irritation, cardiac edema, increased blood volume, hypertension, cardiac arrhythmias, enlargement of the heart, headaches, and weakness of the extremities.
Chỉ Định : For partial replacement therapy for primary and secondary adrenocortical insufficiency in Addison's disease and for the treatment of salt-losing adrenogenital syndrome.
Tương Tác Thuốc :
  • Acenocoumarol The corticosteroid, fludrocortisone, alters the anticoagulant effect, acenocoumarol.
  • Acetylsalicylic acid The corticosteroid, fludrocortisone, may decrease the effect of the salicylate, acetylsalicylic acid.
  • Ambenonium The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, ambenonium.
  • Amobarbital The barbiturate, amobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Anisindione The corticosteroid, fludrocortisone, alters the anticoagulant effect of anisindione.
  • Aprobarbital The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Bismuth Subsalicylate The corticosteroid, fludrocortisone, may decrease the effect of the salicylate, bismuth subsalicylate.
  • Butabarbital The barbiturate, butabarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Butalbital The barbiturate, butalbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Butethal The barbiturate, butethal, may decrease the effect of the corticosteroid, fludrocortisone.
  • Dicoumarol The corticosteroid, fludrocortisone, alters the anticoagulant effect of dicumarol.
  • Dihydroquinidine barbiturate The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, fludrocortisone.
  • Edrophonium The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, edrophonium.
  • Ethotoin The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, fludrocortisone.
  • Fosphenytoin The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, fludrocortisone.
  • Heptabarbital The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Hexobarbital The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Magnesium salicylate The corticosteroid, fludrocortisone, may decrease the effect of magnesium salicylate.
  • Mephenytoin The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, fludrocortisone.
  • Methohexital The barbiturate, methohexital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Methylphenobarbital The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Midodrine Increased arterial pressure
  • Neostigmine The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, neostigmine.
  • Pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Phenobarbital The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Phenytoin The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, fludrocortisone.
  • Primidone The barbiturate, primidone, may decrease the effect of the corticosteroid, fludrocortisone.
  • Pyridostigmine The corticosteroid, fludrocortisone, may decrease the effect of the anticholinesterase, pyridostigmine.
  • Quinidine barbiturate The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, fludrocortisone.
  • Rifampicin The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, fludrocortisone.
  • Salicylate-sodium The corticosteroid, fludrocortisone, may decrease the effect of the salicylate, salicylate-sodium.
  • Salsalate The corticosteroid, fludrocortisone, may decrease the effect of the salicylate, salsalate.
  • Secobarbital The barbiturate, secobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
  • Tacrine Tacrine and Fludrocortisone 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, fludrocortisone.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
  • Trisalicylate-choline The corticosteroid, fludrocortisone, may decrease the effect of the salicylate, trisalicylate-choline.
  • Vecuronium Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Fludrocortisone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
  • Warfarin The corticosteroid, fludrocortisone, alters the anticoagulant effect of warfarin.
Liều Lượng & Cách Dùng : Tablet - Oral
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Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00687
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=31378
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508616
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07004
ChemSpider
http://www.chemspider.com/Chemical-Structure.29111.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/42291-529-01
PharmGKB
http://www.pharmgkb.org/drug/PA164743961
Wikipedia
http://en.wikipedia.org/wiki/Fludrocortisone
RxList
http://www.rxlist.com/cgi/generic/fludro.htm
Drugs.com
http://www.drugs.com/cdi/fludrocortisone.html
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