Tìm theo
Mometasone
Các tên gọi khác (11 ) :
  • (+)-Mometasone
  • Mometason
  • Mometason furoat-1-Wasser
  • Mometasona
  • Mométasone
  • Mométasone (furoate de)
  • Mometasone Furoate
  • Mometasone Furoate Hydrate
  • Mometasonfuroat
  • Mometasoni furoas
  • Mometasonum
Thuốc điều trị bệnh da liễu
Thuốc Gốc
Small Molecule
CAS: 105102-22-5
ATC: D07AC13, D07XC03, R01AD09, R03BA07
ĐG : A-S Medication Solutions LLC , http://orders.a-smeds.com
CTHH: C22H28Cl2O4
PTK: 427.361
Mometasone is a medium-potency synthetic corticosteroid with antiinflammatory, antipruritic, and vasoconstrictive properties. Studies in asthmatic patients have demonstrated that mometasone provides a favorable ratio of topical to systemic activity due to its primary local effect along with the extensive hepatic metabolism and the lack of active metabolites. Though effective for the treatment of asthma, glucocorticoids do not affect asthma symptoms immediately. Maximum improvement in symptoms following inhaled administration of mometasone furoate may not be achieved for 1 to 2 weeks or longer after starting treatment. he 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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H28Cl2O4
Phân tử khối
427.361
Monoisotopic mass
426.136464798
InChI
InChI=1S/C22H28Cl2O4/c1-12-8-16-15-5-4-13-9-14(25)6-7-19(13,2)21(15,24)17(26)10-20(16,3)22(12,28)18(27)11-23/h6-7,9,12,15-17,26,28H,4-5,8,10-11H2,1-3H3/t12-,15+,16+,17+,19+,20+,21+,22+/m1/s1
InChI Key
InChIKey=QLIIKPVHVRXHRI-CXSFZGCWSA-N
IUPAC Name
(1R,2S,10S,11S,13R,14R,15S,17S)-1-chloro-14-(2-chloroacetyl)-14,17-dihydroxy-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one
Traditional IUPAC Name
mometasone
SMILES
[H][C@@]12C[C@@H](C)[C@](O)(C(=O)CCl)[C@@]1(C)C[C@H](O)[C@@]1(Cl)[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
Độ tan chảy
218-220 °C
Độ hòa tan
Practically insoluble.
logP
2.1
logS
-4.9
pKa (strongest acidic)
12.48
pKa (Strongest Basic)
-3.3
PSA
74.6 Å2
Refractivity
110.29 m3·mol-1
Polarizability
43.82 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
4
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Mometasone is a medium-potency synthetic corticosteroid with antiinflammatory, antipruritic, and vasoconstrictive properties. Studies in asthmatic patients have demonstrated that mometasone provides a favorable ratio of topical to systemic activity due to its primary local effect along with the extensive hepatic metabolism and the lack of active metabolites. Though effective for the treatment of asthma, glucocorticoids do not affect asthma symptoms immediately. Maximum improvement in symptoms following inhaled administration of mometasone furoate may not be achieved for 1 to 2 weeks or longer after starting treatment. When glucocorticoids are discontinued, asthma stability may persist for several days or longer. Mometasone has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 12 times that of dexamethasone, 7 times that of triamcinolone acetonide, 5 times that of budesonide, and 1.5 times that of fluticasone. The clinical significance of these findings is unknown.
Cơ Chế Tác Dụng : Mometasone is a medium-potency synthetic corticosteroid with antiinflammatory, antipruritic, and vasoconstrictive properties. Studies in asthmatic patients have demonstrated that mometasone provides a favorable ratio of topical to systemic activity due to its primary local effect along with the extensive hepatic metabolism and the lack of active metabolites. Though effective for the treatment of asthma, glucocorticoids do not affect asthma symptoms immediately. Maximum improvement in symptoms following inhaled administration of mometasone furoate may not be achieved for 1 to 2 weeks or longer after starting treatment. he 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. Unbound corticosteroids cross cell membranes and bind with high affinity to specific cytoplasmic receptors. Inflammation is decreased by diminishing the release of leukocytic acid hydrolases, prevention of macrophage accumulation at inflamed sites, interference with leukocyte adhesion to the capillary wall, reduction of capillary membrane permeability, reduction of complement components, inhibition of histamine and kinin release, and interference with the formation of 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. Mometasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 12 times that of dexamethasone, 7 times that of triamcinolone acetonide, 5 times that of budesonide, and 1.5 times that of fluticasone.
Dược Động Học :
▧ Absorption :
Nasal spray is virtually undetectable in plasma
▧ Protein binding :
98% to 99% (in a concentration range of 5 to 500 ng/mL).
▧ Metabolism :
Hepatic. Extensive metabolism to multiple metabolites. There are no major metabolites detectable in plasma. Upon in vitro incubation, one of the minor metabolites formed is 6ß-hydroxy-mometasone furoate. In human liver microsomes, the formation of the metabolite is regulated by cytochrome P-450 3A4.
▧ Half Life :
5.8 hours
Độc Tính : The potential for acute toxic effects following overdose with the mometasone inhaler is low. However, habitual overuse of the product can cause symptoms of steroid overload, including menstrual irregularities, acne, obesity, and muscle weakness. Single oral doses up to 8000 µg have been studied on human volunteers with no adverse events reported.
Chỉ Định : The inhaler is indicated for the maintenance treatment of asthma as prophylactic therapy. The nasal spray is indicated for the treatment of the nasal symptoms of seasonal allergic and perennial allergic rhinitis.
Liều Lượng & Cách Dùng : Cream - Topical
Lotion - Topical
Ointment - Topical
Spray - Intrasinal
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Merck
    Sản phẩm biệt dược : Asmanex
  • Công ty : Merck
    Sản phẩm biệt dược : Asmanex Twisthaler
  • Công ty : Essex pharma
    Sản phẩm biệt dược : Ecural
  • Công ty : Merck
    Sản phẩm biệt dược : Elocom
  • Công ty : Merck
    Sản phẩm biệt dược : Elocon
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Elomet
  • Công ty : Intas
    Sản phẩm biệt dược : Eziwin
  • Sản phẩm biệt dược : mometAid
  • Công ty : Merck
    Sản phẩm biệt dược : Nasonex
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Novasone
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00764
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07816
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0085-0370-01
PharmGKB
http://www.pharmgkb.org/drug/PA450541
Wikipedia
http://en.wikipedia.org/wiki/Mometasone
RxList
http://www.rxlist.com/cgi/generic2/momet1.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/nas1518.shtml
Drugs.com
http://www.drugs.com/cdi/mometasone-spray.html
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