Tìm theo
Alcaftadine
Các tên gọi khác (5 ) :
  • 6,11-Dihydro-11-(1-Methyl-4-piperidinylidene)-5H-iMidazo[2,1-b][3]benzazepine-3-carboxaldehyde
  • Alcaftadina
  • Alcaftadinum
  • Lastacaft
  • Vilasta
anti inflammatory agents, histamine h1 antagonists
Thuốc Gốc
Small Molecule
CAS: 147084-10-4
CTHH: C19H21N3O
PTK: 307.3895
Alcaftadine is a H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. This drug was approved in July 2010.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C19H21N3O
Phân tử khối
307.3895
Monoisotopic mass
307.168462309
InChI
InChI=1S/C19H21N3O/c1-21-9-6-15(7-10-21)18-17-5-3-2-4-14(17)8-11-22-16(13-23)12-20-19(18)22/h2-5,12-13H,6-11H2,1H3
InChI Key
InChIKey=MWTBKTRZPHJQLH-UHFFFAOYSA-N
IUPAC Name
2-(1-methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),3,5,10,12-pentaene-6-carbaldehyde
Traditional IUPAC Name
alcaftadine
SMILES
CN1CCC(CC1)=C1C2=NC=C(C=O)N2CCC2=CC=CC=C12
Độ sôi
556.247 °C at 760 mmHg.
Độ hòa tan
slightly solubility
logP
3.202
logS
-3
pKa (Strongest Basic)
7.16
PSA
38.13 Å2
Refractivity
102.88 m3·mol-1
Polarizability
34.68 Å3
Rotatable Bond Count
1
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 : Following bilateral topical ocular administration of alcaftadine ophthalmic solution, 0.25%, the mean plasma Cmax of alcaftadine was approximately 60 pg/mL and the median Tmax occurred at 15 minutes. Plasma concentrations of alcaftadine were below the lower limit of quantification (10 pg/mL) by 3 hours after dosing. The mean Cmax of the active carboxylic acid metabolite was approximately 3 ng/mL and occurred at 1 hour after dosing. Plasma concentrations of the carboxylic acid metabolite were below the lower limit of quantification (100 pg/mL) by 12 hours after dosing.
Cơ Chế Tác Dụng : Alcaftadine is a H1 histamine receptor antagonist indicated for the prevention of itching associated with allergic conjunctivitis. This drug was approved in July 2010. Alcaftadine is a H1 histamine receptor antagonist and inhibitor of the release of histamine from mast cells. Decreased chemotaxis and inhibition of eosinophil activation has also been demonstrated.
Dược Động Học :

▧ Protein binding :
The protein binding of alcaftadine and the active metabolite are 39.2% and 62.7% respectively.
▧ Metabolism :
The metabolism of alcaftadine is mediated by non-CYP450 cytosolic enzymes to the active carboxylic acid metabolite.
▧ Route of Elimination :
Based on data following oral administration of alcaftadine, the carboxylic acid metabolite is primarily eliminated unchanged in the urine.
▧ Half Life :
The elimination half-life of the carboxylic acid metabolite is approximately 2 hours following topical ocular administration.
Chỉ Định : For the prevention of itching associated with allergic conjunctivitis.
Liều Lượng & Cách Dùng : Solution / drops - Ophthalmic - 0.25% (2.5 mg/mL)
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06766
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=19371515
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=99443288
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D06552
ChemSpider
http://www.chemspider.com/Chemical-Structure.14201635.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/68669-412-03
PharmGKB
http://www.pharmgkb.org/drug/PA165958399
RxList
http://www.rxlist.com/lastacaft-drug.htm
Drugs.com
http://www.drugs.com/pro/lastacaft.html
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