Tìm theo
Hydrocortisone
Các tên gọi khác (12 ) :
  • (11beta)-11,17,21-Trihydroxypregn-4-ene-3,20-dione
  • 11beta-hydrocortisone
  • 11beta,17alpha,21-Trihydroxy-4-pregnene-3,20-dione
  • 11β-hydrocortisone
  • 17-Hydroxycorticosterone
  • 4-Pregnen-11beta,17alpha,21-triol-3,20-dione
  • Cortisol
  • Hidrocortisona
  • Hydrocortisone
  • Hydrocortisonum
  • Kendall's compound F
  • Reichstein's substance M
Hormon, Nội tiết tố
Thuốc Gốc
Small Molecule
CAS: 50-23-7
ATC: A01AC03, A07EA02, C05AA01, D07AA02, D07AB02, D07AB11, D07AC16, D07XA01, H02AB09, S01BA02, S01CB03, S02BA01
ĐG : Actavis Group , http://www.actavis.com
CTHH: C21H30O5
PTK: 362.4599
The main glucocorticoid secreted by the adrenal cortex. Its synthetic counterpart is used, either as an injection or topically, in the treatment of inflammation, allergy, collagen diseases, asthma, adrenocortical deficiency, shock, and some neoplastic conditions. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H30O5
Phân tử khối
362.4599
Monoisotopic mass
362.20932407
InChI
InChI=1S/C21H30O5/c1-19-7-5-13(23)9-12(19)3-4-14-15-6-8-21(26,17(25)11-22)20(15,2)10-16(24)18(14)19/h9,14-16,18,22,24,26H,3-8,10-11H2,1-2H3/t14-,15-,16-,18+,19-,20-,21-/m0/s1
InChI Key
InChIKey=JYGXADMDTFJGBT-VWUMJDOOSA-N
IUPAC Name
(1S,2R,10S,11S,14R,15S,17S)-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
hydrocortisone
SMILES
[H][C@@]12CC[C@](O)(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)CC[C@]12C
Độ tan chảy
220 °C
Độ hòa tan
320 mg/L (at 25 °C)
logP
1.61
logS
-2.97
pKa (strongest acidic)
12.58
pKa (Strongest Basic)
-2.8
PSA
94.83 Å2
Refractivity
97.4 m3·mol-1
Polarizability
39.55 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
-4.66
Dược Lực Học : Hydrocortisone is the most important human glucocorticoid. It is essential for life and regulates or supports a variety of important cardiovascular, metabolic, immunologic and homeostatic functions. Topical hydrocortisone is used for its anti-inflammatory or immunosuppressive properties to treat inflammation due to corticosteroid-responsive dermatoses. Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger a variety of important cardiovascular, metabolic, immunologic and homeostatic effects. Glucocorticoids are distinguished from mineralocorticoids and sex steroids by having different receptors, target cells, and effects. Technically, the term corticosteroid refers to both glucocorticoids and mineralocorticoids, but is often used as a synonym for glucocorticoid. Glucocorticoids suppress cell-mediated immunity. They act by inhibiting genes that code for the cytokines IL-1, IL-2, IL-3, IL-4, IL-5, IL-6, IL-8 and TNF-alpha, the most important of which is the IL-2. Reduced cytokine production limits T cell proliferation. Glucocorticoids also suppress humoral immunity, causing B cells to express lower amounts of IL-2 and IL-2 receptors. This diminishes both B cell clonal expansion and antibody synthesis. The diminished amounts of IL-2 also leads to fewer T lymphocyte cells being activated.
Cơ Chế Tác Dụng : The main glucocorticoid secreted by the adrenal cortex. Its synthetic counterpart is used, either as an injection or topically, in the treatment of inflammation, allergy, collagen diseases, asthma, adrenocortical deficiency, shock, and some neoplastic conditions. [PubChem] Hydrocortisone binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. The cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. In other words, the two main products in inflammation Prostaglandins and Leukotrienes are inhibited by the action of Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space, where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from neutrophils, macrophages and mastocytes. Additionally the immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.
Dược Động Học :
▧ Absorption :
Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption.
▧ Protein binding :
95%
▧ Metabolism :
Primarily hepatic via CYP3A4
▧ Route of Elimination :
Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.
▧ Half Life :
6-8 hours
Độc Tính : Side effects include inhibition of bone formation, suppression of calcium absorption and delayed wound healing
Chỉ Định : For the relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses. Also used to treat endocrine (hormonal) disorders (adrenal insufficiency, Addisons disease). It is also used to treat many immune and allergic disorders, such as arthritis, lupus, severe psoriasis, severe asthma, ulcerative colitis, and Crohn's disease.
Tương Tác Thuốc :
  • Acenocoumarol The corticosteroid, hydrocortisone, alters the anticoagulant effect, acenocoumarol.
  • Acetylsalicylic acid The corticosteroid, hydrocortisone, may decrease the effect of the salicylate, acetylsalicylic acid.
  • Ambenonium The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, ambenonium.
  • Amobarbital The barbiturate, amobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Anisindione The corticosteroid, hydrocortisone, alters the anticoagulant effect of anisindione.
  • Aprobarbital The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Bismuth Subsalicylate The corticosteroid, hydrocortisone, may decrease the effect of the salicylate, bismuth subsalicylate.
  • Butabarbital The barbiturate, butabarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Butalbital The barbiturate, butalbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Butethal The barbiturate, butethal, may decrease the effect of the corticosteroid, hydrocortisone.
  • Cholestyramine Cholestyramine may decrease the effect of hydrocortisone.
  • Colestipol Cholestyramine decreases the effect of hydrocortisone
  • Dicoumarol The corticosteroid, hydrocortisone, alters the anticoagulant effect of dicumarol.
  • Dihydroquinidine barbiturate The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, hydrocortisone.
  • Edrophonium The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, edrophonium.
  • Ethotoin The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, hydrocortisone.
  • Fosphenytoin The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, hydrocortisone.
  • Heptabarbital The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Hexobarbital The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Indacaterol Concomitant therapy may increase the risk of hypokalemia via intracellular shunting. Monitor for adverse effects and especially for cardiovascular effects associated with hypokalemia.
  • Linagliptin CYP3A4 inducers may decrease levels of linagliptin and diminish the hypoglycemic effect of antidiabetic agents. Monitor concomitant therapy closely.
  • Magnesium salicylate The corticosteroid, hydrocortisone, may decrease the effect of magnesium salicylate.
  • Mephenytoin The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, hydrocortisone.
  • Methohexital The barbiturate, methohexital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Methylphenobarbital The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Midodrine Increased arterial pressure
  • Neostigmine The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, neostigmine.
  • Pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Phenobarbital The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Phenytoin The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, hydrocortisone.
  • Primidone The barbiturate, primidone, may decrease the effect of the corticosteroid, hydrocortisone.
  • Pyridostigmine The corticosteroid, hydrocortisone, may decrease the effect of the anticholinesterase, pyridostigmine.
  • Quinidine barbiturate The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, hydrocortisone.
  • Rifampicin The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, hydrocortisone.
  • Salicylate-sodium The corticosteroid, hydrocortisone, may decrease the effect of the salicylate, salicylate-sodium.
  • Salsalate The corticosteroid, hydrocortisone, may decrease the effect of the salicylate, salsalate.
  • Secobarbital The barbiturate, secobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
  • Tacrine Tacrine and Hydrocortisone 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, hydrocortisone.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
  • Trisalicylate-choline The corticosteroid, hydrocortisone, may decrease the effect of the salicylate, trisalicylate-choline.
  • Vecuronium Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Hydrocortisone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
  • Warfarin The corticosteroid, hydrocortisone, alters the anticoagulant effect of warfarin.
Liều Lượng & Cách Dùng : Aerosol - Rectal
Cream - Topical
Enema - Rectal
Liquid - Topical
Lotion - Topical
Ointment - Ophthalmic
Ointment - Topical
Powder, for solution - Intramuscular
Powder, for solution - Intravenous
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : A-HYDROCORT
  • Công ty :
    Sản phẩm biệt dược : Acticort
  • Công ty :
    Sản phẩm biệt dược : Aeroseb HC
  • Công ty :
    Sản phẩm biệt dược : Ala-Scalp
  • Công ty :
    Sản phẩm biệt dược : Alacort
  • Công ty :
    Sản phẩm biệt dược : Algicirtis
  • Công ty :
    Sản phẩm biệt dược : Anusol HC
  • Công ty :
    Sản phẩm biệt dược : Aquanil HC
  • Công ty :
    Sản phẩm biệt dược : Beta-HC
  • Công ty :
    Sản phẩm biệt dược : CaldeCORT
  • Công ty :
    Sản phẩm biệt dược : Cetacort
  • Công ty :
    Sản phẩm biệt dược : Colocort
  • Công ty :
    Sản phẩm biệt dược : Cortaid
  • Công ty :
    Sản phẩm biệt dược : CORTEF
  • Công ty :
    Sản phẩm biệt dược : Cortenema
  • Công ty :
    Sản phẩm biệt dược : Cortifoam
  • Công ty :
    Sản phẩm biệt dược : Delacort
  • Công ty :
    Sản phẩm biệt dược : Ficortril
  • Công ty :
    Sản phẩm biệt dược : Genacort
  • Công ty :
    Sản phẩm biệt dược : Glycort
  • Công ty :
    Sản phẩm biệt dược : Komed HC
  • Công ty :
    Sản phẩm biệt dược : Lacticare HC
  • Công ty :
    Sản phẩm biệt dược : Locoid
  • Công ty :
    Sản phẩm biệt dược : Lubricort
  • Công ty :
    Sản phẩm biệt dược : Medicort
  • Công ty :
    Sản phẩm biệt dược : Meusicort
  • Công ty :
    Sản phẩm biệt dược : Micort-HC
  • Công ty :
    Sản phẩm biệt dược : Mildison
  • Công ty :
    Sản phẩm biệt dược : Nogenic HC
  • Công ty :
    Sản phẩm biệt dược : Nutracort
  • Công ty :
    Sản phẩm biệt dược : Nystaform-HC
  • Công ty :
    Sản phẩm biệt dược : Otocort
  • Công ty :
    Sản phẩm biệt dược : Pandel
  • Công ty :
    Sản phẩm biệt dược : Penecort
  • Công ty :
    Sản phẩm biệt dược : Permicort
  • Công ty :
    Sản phẩm biệt dược : Polcort H
  • Công ty :
    Sản phẩm biệt dược : Preparation H Hydrocortisone Cream
  • Công ty :
    Sản phẩm biệt dược : Prepcort
  • Công ty :
    Sản phẩm biệt dược : Prevex HC
  • Công ty :
    Sản phẩm biệt dược : Procto-Pak
  • Công ty :
    Sản phẩm biệt dược : Proctocort
  • Công ty :
    Sản phẩm biệt dược : Proctocream
  • Công ty :
    Sản phẩm biệt dược : Proctozone
  • Công ty :
    Sản phẩm biệt dược : Protocort
  • Công ty :
    Sản phẩm biệt dược : Remederm HC
  • Công ty :
    Sản phẩm biệt dược : Sanatison
  • Công ty :
    Sản phẩm biệt dược : Scalpicin Capilar
  • Công ty :
    Sản phẩm biệt dược : Schericur
  • Công ty :
    Sản phẩm biệt dược : Sigmacort
  • Công ty :
    Sản phẩm biệt dược : Solu-Cortef
  • Công ty :
    Sản phẩm biệt dược : Synacort
  • Công ty :
    Sản phẩm biệt dược : Systral Hydrocort
  • Công ty :
    Sản phẩm biệt dược : Texacort
  • Công ty :
    Sản phẩm biệt dược : Timocort
  • Công ty :
    Sản phẩm biệt dược : U-Cort
  • Công ty :
    Sản phẩm biệt dược : Westcort
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00741
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=5754
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505089
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C00735
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00088
ChemSpider
http://www.chemspider.com/Chemical-Structure.5551.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=22476
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0009-0142-01
PharmGKB
http://www.pharmgkb.org/drug/PA449905
Wikipedia
http://en.wikipedia.org/wiki/Hydrocortisone
RxList
http://www.rxlist.com/cgi/generic/hydrocortisone.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/hyd1199.shtml
Drugs.com
http://www.drugs.com/cdi/hydrocortisone.html
... loading
... loading