Tìm theo
Beclomethasone
Các tên gọi khác (35 ) :
  • (11beta,16beta)-9-chloro-11-Hydroxy-16-methyl-17,21-bis(1-oxopropoxy)pregna-1,4-diene-3,20-dione
  • 9-chloro-11beta-Hydroxy-16beta-methylpregna-1,4-diene-3,20-dione 17,21-dipropionate
  • 9-chloro-11β,17,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione
  • 9-chloro-16beta-Methyl-11beta,17,21-trihydroxypregna-1,4-diene-3,20-dione 17,21-dipropionate
  • 9α-chloro-16β-methylprednisolone
  • Aerobec
  • Aldecin
  • Anceron
  • Andion
  • Beclacin
  • Becloforte
  • Beclomet
  • Beclometasone
  • Beclometasone 17,21-dipropionate
  • Beclometasone dipropionate
  • Beclomethasone dipropionate
  • Beclorhinol
  • Becloval
  • Beclovent
  • Becodisks
  • Beconase
  • Beconasol
  • Becotide
  • Clenil-a
  • Entyderma
  • Inalone
  • Korbutone
  • Propaderm
  • Rino-clenil
  • Sanasthmax
  • Sanasthmyl
  • Vancenase
  • Vanceril
  • Viarex
  • Viarox
Thuốc tác dụng trên đường hô hấp
Thuốc Gốc
Small Molecule
CAS: 5534-09-8
ATC: A07EA07, D07AC15, R01AD01, R03BA01
ĐG : 3M Health Care , http://www.3m.com
CTHH: C28H37ClO7
PTK: 521.042
Beclomethasone dipropionate is a prodrug of the free form, Beclomethasone (beclomethasone-17-monopropionate). An anti-inflammatory, synthetic corticosteroid, it is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma and allergic rhinitis (seasonal and perennial). Beclometasone dipropionate is also being investigated for oral treatment in mild-to-moderate Crohn's disease of ileal or ileal-right colonic localisation and for "topical" use mild-to-moderate graft versus host disease. It is marketed under several brand names such as Qnasl (US) and Rivanase AQ (Canada).
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C28H37ClO7
Phân tử khối
521.042
Monoisotopic mass
520.222781245
InChI
InChI=1S/C28H37ClO7/c1-6-23(33)35-15-22(32)28(36-24(34)7-2)16(3)12-20-19-9-8-17-13-18(30)10-11-25(17,4)27(19,29)21(31)14-26(20,28)5/h10-11,13,16,19-21,31H,6-9,12,14-15H2,1-5H3/t16-,19-,20-,21-,25-,26-,27-,28-/m0/s1
InChI Key
InChIKey=KUVIULQEHSCUHY-XYWKZLDCSA-N
IUPAC Name
2-[(1R,2S,10S,11S,13S,14R,15S,17S)-1-chloro-17-hydroxy-2,13,15-trimethyl-5-oxo-14-(propanoyloxy)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-14-yl]-2-oxoethyl propanoate
Traditional IUPAC Name
2-[(1R,2S,10S,11S,13S,14R,15S,17S)-1-chloro-17-hydroxy-2,13,15-trimethyl-5-oxo-14-(propanoyloxy)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-14-yl]-2-oxoethyl propanoate
SMILES
[H][C@@]12C[C@H](C)[C@](OC(=O)CC)(C(=O)COC(=O)CC)[C@@]1(C)C[C@H](O)[C@@]1(Cl)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Độ tan chảy
117-120 °C
Độ hòa tan
49.39 mg/L
logP
1.3
logS
-5.4
pKa (strongest acidic)
13.85
pKa (Strongest Basic)
-3.3
PSA
106.97 Å2
Refractivity
134.79 m3·mol-1
Polarizability
54.41 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
MDDR-Like Rule
true
Dược Lực Học : Beclometasone, a synthetic halogenated glucocorticoid with antiinflammatory and vasoconstrictive effects, is used for treating steroid-dependent asthma, allergic or nonallergic rhinitis, or recurrent nasal polyps.
Cơ Chế Tác Dụng : Beclomethasone dipropionate is a prodrug of the free form, Beclomethasone (beclomethasone-17-monopropionate). An anti-inflammatory, synthetic corticosteroid, it is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma and allergic rhinitis (seasonal and perennial). Beclometasone dipropionate is also being investigated for oral treatment in mild-to-moderate Crohn's disease of ileal or ileal-right colonic localisation and for "topical" use mild-to-moderate graft versus host disease. It is marketed under several brand names such as Qnasl (US) and Rivanase AQ (Canada). Unbound corticosteroids cross cell membranes and bind with high affinity to specific cytoplasmic receptors. The result includes 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 corticosteroids are thought to involve phospholipase A2 inhibitory proteins, lipocortins, which control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes. For the investigated use in the treatment of GvHD or Crohn's, beclometasone acts by binding to interleukin-13 to inhibit cytokines, which in turn inhibits inflammatory chemicals downstream.
Dược Động Học :
▧ Absorption :
Mean peak plasma concentration was 88pg/ml at 0.5 hour
▧ Volume of Distribution :
The steady state volume of distribution for beclomethasone dipropionate is 20 L, and for it's active metabolite, beclomethasone-17-monopropionate, it is much larger at 424 L.
▧ Protein binding :
87% to albumin and transcortin
▧ Metabolism :
Metabolism mediated via esterase enzymes that are found in most tissues. Undergoes rapid and extensive conversion to beclomenthasone-17-monopropionate (17-BMP) during absorption
▧ Route of Elimination :
Irrespective of the route of administration (injection, oral or inhalation), BDP and its metabolites are mainly excreted in the feces. Less than 10% of the drug and its metabolites are excreted in the urine.
▧ Half Life :
2.8 hours
▧ Clearance :
High plasma clearance after intravenous administration (150 and 120 L/hour).
Độc Tính : The acute toxicity of beclometasone dipropionate is low. The only harmful effect that follows inhalation of large amounts of the drug over a short period of time is suppression of hypothalamic-pituitary-adrenal (HPA) function. Chronic: The excessive use of beclometasone dipropionate over a long period could lead to adrenal suppression.
Chỉ Định : Used in the maintenance treatment of asthma as prophylactic therapy in patients 5 years of age and older, and in treating symptoms for allergic rhinitis (seasonal or perennial) in patients 12 years of age and older. Also being investigated for oral treatment in mild-to-moderate Crohn's disease of ileal or ileal-right colonic localisation and for "topical" use mild-to-moderate graft versus host disease.
Liều Lượng & Cách Dùng : Aerosol, metered - Nasal
Aerosol, metered - Nasal - 0.08MG/ACTUATION
Aerosol, metered - Respiratory (inhalation)
Cream - Topical
Spray - Nasal
Suspension - Nasal
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Teva
    Sản phẩm biệt dược : Aerobec
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Aldecin
  • Công ty :
    Sản phẩm biệt dược : Anceron
  • Công ty :
    Sản phẩm biệt dược : Andion
  • Công ty : Mayado Seiyaku
    Sản phẩm biệt dược : Beclacin
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Becloforte
  • Công ty : Orion
    Sản phẩm biệt dược : Beclomet
  • Công ty : Chiesi
    Sản phẩm biệt dược : Beclorhinol
  • Công ty :
    Sản phẩm biệt dược : Becloval
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Beclovent
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Becodisks
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Beconase
  • Công ty :
    Sản phẩm biệt dược : Beconasol
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Becotide
  • Công ty :
    Sản phẩm biệt dược : Clenil-A
  • Công ty :
    Sản phẩm biệt dược : Entyderma
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Inalone
  • Công ty :
    Sản phẩm biệt dược : Korbutone
  • Sản phẩm biệt dược : orBec
  • Công ty : GlaxoSmithKline
    Sản phẩm biệt dược : Propaderm
  • Sản phẩm biệt dược : Qnasl
  • Công ty : Teva Respiratory
    Sản phẩm biệt dược : QVAR
  • Công ty : Chiesi
    Sản phẩm biệt dược : Rino-Clenil
  • Công ty :
    Sản phẩm biệt dược : Rivanase
  • Công ty : Chiesi
    Sản phẩm biệt dược : Sanasthmax
  • Công ty :
    Sản phẩm biệt dược : Sanasthmyl
  • Công ty :
    Sản phẩm biệt dược : Vancenase
  • Công ty :
    Sản phẩm biệt dược : Vanceril
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00394
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C06842
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D07495
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/59310-175-40
PharmGKB
http://www.pharmgkb.org/drug/PA448547
Wikipedia
http://en.wikipedia.org/wiki/Beclometasone_dipropionate
RxList
http://www.rxlist.com/qvar-drug.htm
Drugs.com
http://www.drugs.com/cdi/beclomethasone-spray.html
... loading
... loading