Tìm theo
Desloratadine
Các tên gọi khác (4 ) :
  • 8-Chloro-11-piperidin-4-ylidene-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine
  • 8-chloro-6,11-dihydro-11-(4-Piperidinylidene)-5H-benzo(5,6)cyclohepta(1,2-b)pyridine
  • Descarboethoxyloratadine
  • DESLORATADINE
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 100643-71-8
ĐG : Apotheca Inc.
CTHH: C19H19ClN2
PTK: 310.821
Desloratadine is a second generation, tricyclic antihistamine that which has a selective and peripheral H1-antagonist action. It is the active descarboethoxy metabolite of loratidine (a second generation histamine). Desloratidine has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H19ClN2
Phân tử khối
310.821
Monoisotopic mass
310.123676325
InChI
InChI=1S/C19H19ClN2/c20-16-5-6-17-15(12-16)4-3-14-2-1-9-22-19(14)18(17)13-7-10-21-11-8-13/h1-2,5-6,9,12,21H,3-4,7-8,10-11H2
InChI Key
InChIKey=JAUOIFJMECXRGI-UHFFFAOYSA-N
IUPAC Name
13-chloro-2-(piperidin-4-ylidene)-4-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaene
Traditional IUPAC Name
desloratadine
SMILES
ClC1=CC2=C(C=C1)C(=C1CCNCC1)C1=C(CC2)C=CC=N1
Độ hòa tan
3.95e-03 g/l
logP
3.2
logS
-4.9
pKa (Strongest Basic)
9.73
PSA
24.92 Å2
Refractivity
101.04 m3·mol-1
Polarizability
34.35 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Desloratadine is a long-acting second-generation H1-receptor antagonist which has a selective and peripheral H1-antagonist action. Histamine is a chemical that causes many of the signs that are part of allergic reactions, such as the swelling of tissues. Histamine is released from histamine-storing cells (mast cells) and attaches to other cells that have receptors for histamine. The attachment of the histamine to the receptors causes the cell to be "activated," releasing other chemicals which produce the effects that we associate with allergies. Desloratadine blocks one type of receptor for histamine (the H1 receptor) and thus prevents activation of cells by histamine. Unlike most other antihistamines, Desloratadine does not enter the brain from the blood and, therefore, does not cause drowsiness.
Cơ Chế Tác Dụng : Desloratadine is a second generation, tricyclic antihistamine that which has a selective and peripheral H1-antagonist action. It is the active descarboethoxy metabolite of loratidine (a second generation histamine). Desloratidine has a long-lasting effect and does not cause drowsiness because it does not readily enter the central nervous system. Like other H1-blockers, Desloratadine competes with free histamine for binding at H1-receptors in the GI tract, uterus, large blood vessels, and bronchial smooth muscle. This blocks the action of endogenous histamine, which subsequently leads to temporary relief of the negative symptoms (eg. nasal congestion, watery eyes) brought on by histamine.
Dược Động Học :

▧ Protein binding :
82-87%
▧ Route of Elimination :
Desloratadine (a major metabolite of loratadine) is extensively metabolized to 3-hydroxydesloratadine, an active metabolite, which is subsequently glucuronidated. Approximately 87% of a 14C-desloratadine dose was equally recovered in urine and feces.
▧ Half Life :
50 hours
Chỉ Định : For the relief of symptoms of seasonal allergic rhinitis, perennial (non-seasonal) allergic rhinitis. Desloratidine is also used for the sympomatic treatment of pruritus and urticaria (hives) associated with chronic idiopathic urticaria.
Tương Tác Thuốc :
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Desloratadine, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
  • Triprolidine Triprolidine and Desloratadine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Desloratadine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Syrup - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Aerius
  • Công ty :
    Sản phẩm biệt dược : Claramax
  • Công ty :
    Sản phẩm biệt dược : Clarinex
  • Công ty :
    Sản phẩm biệt dược : NeoClarityn
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00967
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=124087
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507996
ChemSpider
http://www.chemspider.com/Chemical-Structure.110575.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50073179
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0085-1264-01
PharmGKB
http://www.pharmgkb.org/drug/PA164776964
Wikipedia
http://en.wikipedia.org/wiki/Desloratadine
RxList
http://www.rxlist.com/cgi/generic3/clarinex.htm
Drugs.com
http://www.drugs.com/cdi/desloratadine.html
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