Tìm theo
Levocabastine
Các tên gọi khác (3) :
  • Levocabastin
  • Levocabastina
  • Levocabastinum
histamine h1 antagonists non sedating
Thuốc Gốc
Small Molecule
CAS: 79516-68-0
ATC: R01AC02, S01GX02
ĐG : Novartis AG , http://www.novartis.com
CTHH: C26H29FN2O2
PTK: 420.5191
Levocabastine is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine was discovered at Janssen Pharmaceutica in 1979.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C26H29FN2O2
Phân tử khối
420.5191
Monoisotopic mass
420.221306387
InChI
InChI=1S/C26H29FN2O2/c1-19-17-29(16-15-26(19,24(30)31)21-5-3-2-4-6-21)23-11-13-25(18-28,14-12-23)20-7-9-22(27)10-8-20/h2-10,19,23H,11-17H2,1H3,(H,30,31)/t19-,23?,25?,26-/m1/s1
InChI Key
InChIKey=ZCGOMHNNNFPNMX-YHYDXASRSA-N
IUPAC Name
(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid
Traditional IUPAC Name
(3S,4R)-1-[4-cyano-4-(4-fluorophenyl)cyclohexyl]-3-methyl-4-phenylpiperidine-4-carboxylic acid
SMILES
C[C@@H]1CN(CC[C@]1(C(O)=O)C1=CC=CC=C1)C1CCC(CC1)(C#N)C1=CC=C(F)C=C1
Độ hòa tan
>0.5 mg/mL
logP
5
logS
-5.1
pKa (strongest acidic)
3.71
pKa (Strongest Basic)
10.32
PSA
64.33 Å2
Refractivity
118.48 m3·mol-1
Polarizability
45.72 Å3
Rotatable Bond Count
4
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Levocabastine is a selective histamine H1-receptor antagonist exerting inhibitory effects on the release of chemical mediators from mast cells and on the chemotaxis of polymorphonuclear leukocytes and eosinophils. Both histamine and antigens induced conjunctivitis can be inhibited by levocabastine. Levocabastine can also reduce symptoms of allergic rhinitis by preventing an increase in vascular permeability of nasal mucosa.
Cơ Chế Tác Dụng : Levocabastine is a selective second-generation H1-receptor antagonist used for allergic conjunctivitis. Levocabastine was discovered at Janssen Pharmaceutica in 1979. Levocabastine is a potent, selective histamine H1-receptor antagonist. It works by competing with histamine for H1-receptor sites on effector cells. It thereby prevents, but does not reverse, responses mediated by histamine alone. Levocabastine does not block histamine release but, rather, prevents histamine binding and activity. Levocabastine also binds neurotensin 2 receptors and serves as a neurotensin agonist. This can induce some degree of analgesia.
Dược Động Học :
▧ Absorption :
After instillation in the eye, levocabastine is systemically absorbed, albeit at low levels.
▧ Metabolism :
Mostly unchanged. 10 to 20% is metabolized to the acylglucuronide of levocabastine.
▧ Half Life :
36 hours (after oral administration)
Độc Tính : Adverse effects include visual disturbances, dry mouth, cough, nausea, eyelid edema and lacrimation.
Chỉ Định : As an ophthalmic for the temporary relief of the signs and symptoms of seasonal allergic conjunctivitis. Also used as a nasal spray for allergic rhinitis.
Liều Lượng & Cách Dùng : Solution / drops - Ophthalmic
Suspension - Nasal
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Livostin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01106
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=54385
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505909
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01717
ChemSpider
http://www.chemspider.com/Chemical-Structure.49123.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/58768-610-10
PharmGKB
http://www.pharmgkb.org/drug/PA164742988
Wikipedia
http://en.wikipedia.org/wiki/Levocabastine
RxList
http://www.rxlist.com/cgi/generic2/livostin.htm
Drugs.com
http://www.drugs.com/mtm/levocabastine-ophthalmic.html
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