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

H Bond Acceptor Count

H Bond Donor Count

Physiological Charge

Number of Rings

Bioavailability

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

Công ty : Allergan, Inc.

Sản phẩm biệt dược : Lastacaft

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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