Tìm theo
Bepotastine
Các tên gọi khác (1) :
  • TAU-284DS
mast cell stabilizers
Thuốc Gốc
Small Molecule
CAS: 125602-71-3
ĐG : ISTA Pharmaceuticals , http://www.istavision.com
CTHH: C21H25ClN2O3
PTK: 388.888
Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. Bepotastine was approved in Japan for use in the treatment of allergic rhinitis and uriticaria/puritus in July 2000 and January 2002, respectively, and is marketed by Tanabe Seiyaku Co., Ltd. under the brand name Talion. It is available in oral and opthalmic dosage forms in Japan. The opthalmic solution is FDA approved since Sept 8, 2009 and is under the brand name Bepreve.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H25ClN2O3
Phân tử khối
388.888
Monoisotopic mass
388.155370383
InChI
InChI=1S/C21H25ClN2O3/c22-17-8-6-16(7-9-17)21(19-4-1-2-12-23-19)27-18-10-14-24(15-11-18)13-3-5-20(25)26/h1-2,4,6-9,12,18,21H,3,5,10-11,13-15H2,(H,25,26)
InChI Key
InChIKey=YWGDOWXRIALTES-UHFFFAOYSA-N
IUPAC Name
4-{4-[(4-chlorophenyl)(pyridin-2-yl)methoxy]piperidin-1-yl}butanoic acid
Traditional IUPAC Name
bepotastine
SMILES
OC(=O)CCCN1CCC(CC1)OC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1
Độ hòa tan
5.03e-02 g/l
logP
0.55
logS
-3.9
pKa (strongest acidic)
4.1
pKa (Strongest Basic)
9.39
PSA
62.66 Å2
Refractivity
105.1 m3·mol-1
Polarizability
42.18 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. It belongs to the second-generation piperidine chemical class. It is a mast cell stabilizer and suppresses the migration of eosinophils into inflamed tissues. Furthermore, bepotastine does not interact with serotonin, muscarinic, benzodiazepine, and beta-adrenergic receptor that would otherwise result in adverse reactions such as dry mouth or sonmolence. Onset of action = 0.25 hours; Duration of action = 12-24 hours;
Cơ Chế Tác Dụng : Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor. Bepotastine was approved in Japan for use in the treatment of allergic rhinitis and uriticaria/puritus in July 2000 and January 2002, respectively, and is marketed by Tanabe Seiyaku Co., Ltd. under the brand name Talion. It is available in oral and opthalmic dosage forms in Japan. The opthalmic solution is FDA approved since Sept 8, 2009 and is under the brand name Bepreve. Because of a type 1 hypersensitivity reaction cascade that is triggered by antigen exposure, allergic conjunctivitis occurs. Allergen exposure is followed by conjunctival mast cell degranulation and histamine released as a result of the formation of complementary IgE cross-links on the conjunctiva. Due to the release of histamine, symptoms such as itching can be observed. Bepotastine works to relieve itchy eyes by three primary mechanisms of action. It is a non-sedating, selective antagonist of the histamine 1 (H1) receptor, a mast cell stabilizer, and it suppresses the migration of eosinophils into inflamed tissues to prevent tissue damage and worsening of allergic inflammation of the conjunctiva.
Dược Động Học :
▧ Absorption :
Tmax, after single dose, opthalmic = 1.2 hours; Cmax, 1.5%, opthalmic dose = 7.3 ±1.9 ng/mL; After 24 hours post-installation, levels of bepotastine are below quantifiable limit of 2 ng/mL. Minimal systemic absorption with opthalmic dosage form.
▧ Protein binding :
55.4% mean plasma protein binding with 10 mg oral dose. Extent of protein binding is independent of plasma drug concentration.
▧ Metabolism :
Minimal metabolism via CYP enzymes
▧ Route of Elimination :
When a oral dose of 2.5 - 40 mg bepotastine is given, 75%-90% of the dose was excreted unchanged in the urine by 24 hours.
▧ Half Life :
Elimination half life = 2.5 hours
Chỉ Định : For the symptomatic treatment of itchy eyes (caused by IgE-induced mast cell degranulation) due to allergic conjunctivitis.
Liều Lượng & Cách Dùng : Solution - Ophthalmic - 1.5%
Tablet - Oral - 10 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Ista Pharms
    Sản phẩm biệt dược : Bepreve
  • Công ty :
    Sản phẩm biệt dược : Talion
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04890
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=2350
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504940
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01654
ChemSpider
http://www.chemspider.com/Chemical-Structure.2260.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/54868-6299-0
PharmGKB
http://www.pharmgkb.org/drug/PA164781356
Wikipedia
http://en.wikipedia.org/wiki/Bepotastine
RxList
http://www.rxlist.com/bepreve-drug.htm
PDRhealth
http://www.pdrhealth.com/drugs/bepreve
Drugs.com
http://www.drugs.com/cdi/bepotastine-eye-drops.html
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