Tìm theo
Betamethasone
Các tên gọi khác (13 ) :
  • 16beta-Methyl-1,4-pregnadiene-9alpha-fluoro-11beta,17alpha,21-triol-3,20-dione
  • 16β-Methyl-1,4-pregnadiene-9α-fluoro-11β,17α,21-triol-3,20-dione
  • 9-Fluoro-16beta-methylprednisolone
  • 9-Fluoro-16β-methylprednisolone
  • 9alpha-Fluoro-16beta-methylprednisolone
  • 9α-Fluoro-16β-methylprednisolone
  • beta-Methasone alcohol
  • Betadexamethasone
  • Betametasona
  • Betamethasone
  • Betamethasonum
  • Betamethasonvalerat Mikron
  • Rinderon
Hormon, Nội tiết tố
Thuốc Gốc
Small Molecule
CAS: 378-44-9
ATC: A07EA04, C05AA05, D07AC01, D07XC01, H02AB01, R01AD06, R03BA04, S01BA06, S01CB04, S02BA07, S03BA03
ĐG : Accra Pac Inc.
CTHH: C22H29FO5
PTK: 392.4611
A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724)
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-/m0/s1
InChI Key
InChIKey=UREBDLICKHMUKA-DVTGEIKXSA-N
IUPAC Name
(1R,2S,10S,11S,13S,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
betamethasone
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
232 °C
Độ hòa tan
66.5 mg/L (at 25 °C)
logP
1.94
logS
-3.77
pKa (strongest acidic)
12.42
pKa (Strongest Basic)
-3.3
PSA
94.83 Å2
Refractivity
102.49 m3·mol-1
Polarizability
40.88 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 : Betamethasone and its derivatives, betamethasone sodium phosphate and betamethasone acetate, are synthetic glucocorticoids. Used for its antiinflammatory or immunosuppressive properties, betamethasone is combined with a mineralocorticoid to manage adrenal insufficiency and is used in the form of betamethasone benzoate, betamethasone dipropionate, or betamethasone valerate for the treatment of inflammation due to corticosteroid-responsive dermatoses. Betamethasone and clotrimazole are used together to treat cutaneous tinea infections.
Cơ Chế Tác Dụng : A glucocorticoid given orally, parenterally, by local injection, by inhalation, or applied topically in the management of various disorders in which corticosteroids are indicated. Its lack of mineralocorticoid properties makes betamethasone particularly suitable for treating cerebral edema and congenital adrenal hyperplasia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p724) Betamethasone is a glucocorticoid receptor agonist. This leads to changes in genetic expression once this complex binds to the GRE. The antiinflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. 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. Betamethasone binds to plasma transcortin, and it becomes active when it is not bound to transcortin.
Dược Động Học :
▧ Absorption :
Minimal if applied topically.
▧ Protein binding :
64%
▧ Metabolism :
Hepatic
▧ Half Life :
5.6 hours
Độc Tính : Symptoms of overdose include burning, itching, irritation, dryness, folliculitis, hypertrichosis, acneiform eruptions, hypopigmentation, perioral dermatitis, allergic contact dermatitis, maceration of the skin, secondary infection, skin atrophy, striae, and miliaria.
Chỉ Định : Topical use (cream, lotion and ointment): for relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses
Topical use (foam): relief of the inflammatory and pruritic manifestations of corticosteroid-responsive dermatoses of the scalp
Systemic use: for the treatment of edocrine disorders, rheumatic disorders, collagen diseases, dermatological diseases, allergic states, ophthalmic diseases, respiratory diseases, hematologic disorders, neoplastic diseases, edematous states, gastrointestinal diseases, tuberculous meningitis and trichinosis.
Tương Tác Thuốc :
  • Acenocoumarol The corticosteroid, betamethasone, alters the anticoagulant effect, acenocoumarol.
  • Acetylsalicylic acid The corticosteroid, betamethasone, may decrease the effect of the salicylate, acetylsalicylic acid.
  • Ambenonium The corticosteroid, betamethasone, may decrease the effect of the anticholinesterase, ambenonium.
  • Amobarbital The barbiturate, amobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Anisindione The corticosteroid, betamethasone, alters the anticoagulant effect of anisindione.
  • Aprobarbital The barbiturate, aprobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Bismuth Subsalicylate The corticosteroid, betamethasone, may decrease the effect of the salicylate, bismuth subsalicylate.
  • Butabarbital The barbiturate, butabarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Butalbital The barbiturate, butalbital, may decrease the effect of the corticosteroid, betamethasone.
  • Butethal The barbiturate, butethal, may decrease the effect of the corticosteroid, betamethasone.
  • Dicoumarol The corticosteroid, betamethasone, alters the anticoagulant effect of dicumarol.
  • Dihydroquinidine barbiturate The barbiturate, dihydroquinidine barbiturate, may decrease the effect of the corticosteroid, betamethasone.
  • Edrophonium The corticosteroid, betamethasone, may decrease the effect of the anticholinesterase, edrophonium.
  • Ethotoin The enzyme inducer, ethotoin, may decrease the effect of the corticosteroid, betamethasone.
  • Fosphenytoin The enzyme inducer, fosphenytoin, may decrease the effect of the corticosteroid, betamethasone.
  • Heptabarbital The barbiturate, heptabarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Hexobarbital The barbiturate, hexobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Indacaterol Concomitant therapy may increase the risk of hypokalemia via intracellular shunting. Monitor for adverse effects and especially for cardiovascular effects associated with hypokalemia.
  • Magnesium salicylate The corticosteroid, betamethasone, may decrease the effect of magnesium salicylate.
  • Mephenytoin The enzyme inducer, mephenytoin, may decrease the effect of the corticosteroid, betamethasone.
  • Methohexital The barbiturate, methohexital, may decrease the effect of the corticosteroid, betamethasone.
  • Methylphenobarbital The barbiturate, methylphenobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Midodrine Increased arterial pressure
  • Pentobarbital The barbiturate, pentobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Phenobarbital The barbiturate, phenobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Phenytoin The enzyme inducer, phenytoin, may decrease the effect of the corticosteroid, betamethasone.
  • Primidone The barbiturate, primidone, may decrease the effect of the corticosteroid, betamethasone.
  • Pyridostigmine The corticosteroid, betamethasone, may decrease the effect of the anticholinesterase, pyridostigmine.
  • Quinidine barbiturate The barbiturate, quinidine barbiturate, may decrease the effect of the corticosteroid, betamethasone.
  • Rifampicin The enzyme inducer, rifampin, may decrease the effect of the corticosteroid, betamethasone.
  • Salicylate-sodium The corticosteroid, betamethasone, may decrease the effect of the salicylate, salicylate-sodium.
  • Salsalate The corticosteroid, betamethasone, may decrease the effect of the salicylate, salsalate.
  • Secobarbital The barbiturate, secobarbital, may decrease the effect of the corticosteroid, betamethasone.
  • Tacrine Tacrine and Betamethasone 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, betamethasone.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
  • Trisalicylate-choline The corticosteroid, betamethasone, may decrease the effect of the salicylate, trisalicylate-choline.
  • Vecuronium Vecuronium may increase the adverse neuromuscular effects of systemic corticosteroids, such as Betamethasone. Monitor for increased muscle weakness and signs of polyneuropathies and myopathy.
  • Warfarin The corticosteroid, betamethasone, alters the anticoagulant effect of warfarin.
Liều Lượng & Cách Dùng : Cream - Topical
Enema - Topical
Lotion - Topical
Ointment - Topical
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Defiante
    Sản phẩm biệt dược : Bentelan
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Betnovate
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Celestamine
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Celestone
  • Công ty :
    Sản phẩm biệt dược : DIPROLENE
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Diprosone
  • Công ty : LEO
    Sản phẩm biệt dược : Fucibet
  • Công ty :
    Sản phẩm biệt dược : LUXIQ
  • Công ty :
    Sản phẩm biệt dược : Procort
  • Công ty : Shionogi Seiyaku
    Sản phẩm biệt dược : Rinderon
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00443
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=9782
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505155
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00244
ChemSpider
http://www.chemspider.com/Chemical-Structure.9399.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0085-0942-05
PharmGKB
http://www.pharmgkb.org/drug/PA164754818
Wikipedia
http://en.wikipedia.org/wiki/Betamethasone
RxList
http://www.rxlist.com/cgi/generic2/betamet.htm
Drugs.com
http://www.drugs.com/cdi/betamethasone.html
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