Tìm theo
Azelastine
Các tên gọi khác (3) :
  • 4-(P-Chlorobenzyl)-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1-(2H)-phthalazinone
  • Azelastina
  • Azelastinum
Thuốc chống dị ứng & dùng trong các trường hợp quá mẫn
Thuốc Gốc
Small Molecule
CAS: 58581-89-8
ATC: R01AC03, R06AX19, S01GX07
ĐG : Apotex Inc. , http://www.apotex.com
CTHH: C22H24ClN3O
PTK: 381.898
Azelastine, a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is also available as a combination product of azelastine hydrochloride and fluticasone propionate called Dymista™. Dymista™ is indicated in patient over 12 years old for symptomatic relief of seasonal allergic rhinitis.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H24ClN3O
Phân tử khối
381.898
Monoisotopic mass
381.160790112
InChI
InChI=1S/C22H24ClN3O/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16/h2-3,6-11,18H,4-5,12-15H2,1H3
InChI Key
InChIKey=MBUVEWMHONZEQD-UHFFFAOYSA-N
IUPAC Name
4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-1,2-dihydrophthalazin-1-one
Traditional IUPAC Name
azelastine
SMILES
CN1CCCC(CC1)N1N=C(CC2=CC=C(Cl)C=C2)C2=CC=CC=C2C1=O
Độ tan chảy
225 °C (hydrochloride salt)
Độ hòa tan
Sparingly soluble (hydrochloride salt)
logP
4.9
logS
-4.6
pKa (Strongest Basic)
8.88
PSA
35.91 Å2
Refractivity
110.52 m3·mol-1
Polarizability
41.54 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Azelastine is a relatively selective histamine H1 antagonist, which inhibits the release of histamine and other mediators from cells (e.g. mast cells) involved in the allergic response. It has some affinity to H2 receptors. Based on in vitro studies using human cell lines, inhibition of other mediators involved in allergic reactions (e.g. leukotrienes and PAF) has been demonstrated with azelastine. Azelastine may also inhibit the accumulation and degranulation of eosinophils at the site of allergic inflammation.
Cơ Chế Tác Dụng : Azelastine, a phthalazine derivative, is an antihistamine and mast cell stabilizer available as a nasal spray for hay fever and as eye drops for allergic conjunctivitis. Azelastine is also available as a combination product of azelastine hydrochloride and fluticasone propionate called Dymista™. Dymista™ is indicated in patient over 12 years old for symptomatic relief of seasonal allergic rhinitis. Azelastine competes with histamine for the H1-receptor sites on effector cells and acts as an antagonist by inhibiting the release of histamine and other mediators involved in the allergic response.
Dược Động Học :
▧ Absorption :
Absorption of azelastine following ocular administration was relatively low. Systemic bioavailability is approximately 40% after nasal administration.
▧ Volume of Distribution :
* 14.5 L/kg
▧ Protein binding :
In-vitro studies in human plasma indicate that the plasma protein binding of azelastine and N-desmethylazelastine are approximately 88% and 97%, respectively.
▧ Metabolism :
Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system, however the exact cytochrome P450 isoenzyme involved has not been determined. The major metabolite, desmethylazelastine, also has H1-receptor antagonist activity.
▧ Route of Elimination :
Approximately 75% of an oral dose of radiolabeled azelastine hydrochloride was excreted in the feces with less than 10% as unchanged azelastine. Azelastine hydrochloride is oxidatively metabolized to the principal metabolite, N-desmethylazelastine, by the cytochrome P450 enzyme system.
▧ Half Life :
Elimination half-life (based on intravenous and oral administration) is 22 hours. Elimination half-life of the active metabolite, desmethylazelastine, is 54 hours (after oral administration of azelastine).
▧ Clearance :
* 0.5 L/h/kg [symptomatic patients]
Chỉ Định : For the symptomatic treatment of seasonal allergic rhinitis and non-allergic rhinitis, as well as symptomatic relief of ocular itching associated with allergic conjunctivitis.
Tương Tác Thuốc :
  • Dihydrocodeine Enhanced CNS depressant effects contraindicates concurrent use.
  • gabapentin enacarbil Avoid combination due to increased CNS depression.
  • Perampanel Avoid combination with azelastine or other CNS depressants due to the combined increase of CNS depression.
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Azelastine, 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.
  • Trimethobenzamide Trimethobenzamide and Azelastine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Concomitant therapy with triprolidine and azelastine, two anticholinergics and CNS depressants, may result in additive adverse/toxic effects. Monitor for enhanced anticholinergic and CNS depressant effects during concomitant therapy.
  • Trospium Trospium and Azelastine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Solution / drops - Ophthalmic
Spray, metered - Nasal - DYMISTA : 0.137MCG /SPRAY; 0.05MCG/SPRAY (AZELASTINE HYDROCHLORIDE; FLUTICASONE PROPIONATE)
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Astelin
  • Công ty :
    Sản phẩm biệt dược : Astepro
  • Công ty :
    Sản phẩm biệt dược : Optivar
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00972
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2267
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507582
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07768
ChemSpider
http://www.chemspider.com/Chemical-Structure.2180.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0037-7025-60
PharmGKB
http://www.pharmgkb.org/drug/PA448517
Wikipedia
http://en.wikipedia.org/wiki/Azelastine
RxList
http://www.rxlist.com/cgi/generic/optivar.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/opt1673.shtml
Drugs.com
http://www.drugs.com/cdi/azelastine-spray.html
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