Tìm theo
Zanamivir
Các tên gọi khác (12 ) :
  • (2R,3R,4S)-3-(acetylamino)-4-Carbamimidamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid
  • 4-Guanidino-2,4-dideoxy-2,3-dehydro-N-acetylneuraminic acid
  • 4-Guanidino-neu5ac2en
  • 5-(acetylamino)-2,6-Anhydro-4-carbamimidamido-3,4,5-trideoxy-D-glycero-D-galacto-non-2-enonic acid
  • 5-acetamido-2,6-Anhydro-3,4,5-trideoxy-4-guanidino-D-glycero-D-galacto-non-2-enonic acid
  • GANA
  • GNA
  • Modified sialic acid
  • Relenza
  • Zanamavir
  • ZANAMIVIR
  • ZMR
antiviral agents, enzyme inhibitors
Thuốc Gốc
Small Molecule
CAS: 139110-80-8
ATC: J05AH01
ĐG : Dispensing Solutions , http://www.drxdispensing.com
CTHH: C12H20N4O7
PTK: 332.3098
A guanido-neuraminic acid that is used to inhibit neuraminidase. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H20N4O7
Phân tử khối
332.3098
Monoisotopic mass
332.133199014
InChI
InChI=1S/C12H20N4O7/c1-4(18)15-8-5(16-12(13)14)2-7(11(21)22)23-10(8)9(20)6(19)3-17/h2,5-6,8-10,17,19-20H,3H2,1H3,(H,15,18)(H,21,22)(H4,13,14,16)/t5-,6+,8+,9+,10+/m0/s1
InChI Key
InChIKey=ARAIBEBZBOPLMB-UFGQHTETSA-N
IUPAC Name
(2R,3R,4S)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid
Traditional IUPAC Name
zanamivir
SMILES
[H][C@]1(OC(=C[C@H](N=C(N)N)[C@H]1NC(C)=O)C(O)=O)[C@H](O)[C@H](O)CO
Độ hòa tan
7.31e+00 g/l
logP
-3
logS
-1.7
pKa (strongest acidic)
3.25
pKa (Strongest Basic)
11.93
PSA
200.72 Å2
Refractivity
76.19 m3·mol-1
Polarizability
31.24 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
10
H Bond Donor Count
7
Physiological Charge
0
Number of Rings
1
Bioavailability
0
Dược Lực Học : Zanamivir, an antiviral agent, is a neuraminidase inhibitor indicated for treatment of uncomplicated acute illness due to influenza A and B virus in adults and pediatric patients 7 years and older who have been symptomatic for no more than 2 days. Zanamivir has also been shown to significantly inhibit the human sialidases NEU3 and NEU2 in the micromolar range (Ki 3.7 +/-0.48 and 12.9+/-0.07 microM, respectively), which could account for some of the rare side effects of zanamivir.
Cơ Chế Tác Dụng : A guanido-neuraminic acid that is used to inhibit neuraminidase. [PubChem] The proposed mechanism of action of zanamivir is via inhibition of influenza virus neuraminidase with the possibility of alteration of virus particle aggregation and release. By binding and inhibiting the neuraminidase protein, the drug renders the influenza virus unable to escape its host cell and infect others.
Dược Động Học :
▧ Absorption :
Absolute bioavailability is very low following oral administration (2%). Following oral inhalation, bioavailability is 4% to 17%.
▧ Protein binding :
Zanamivir has limited plasma protein binding (<10%).
▧ Metabolism :
Not metabolized
▧ Route of Elimination :
It is excreted unchanged in the urine with excretion of a single dose completed within 24 hours. Unabsorbed drug is excreted in the feces.Zanamivir is renally excreted as unchanged drug.
▧ Half Life :
2.5-5.1 hours
▧ Clearance :
* 2.5 - 10.9 L/h [Following oral inhalation 10 mg] * 5.3 L/h [Normal renal function receiving IV single dose of 4 mg or 2 mg] * 2.7 L/h [Patients with mild and moderate renal impairement receiving IV single dose of 4 mg or 2 mg] * 0.8 L/h [Patients with severe renal impairement receiving IV single dose of 4 mg or 2 mg]
Chỉ Định : For the prevention and treatment of influenza A and B.
Liều Lượng & Cách Dùng : Powder - Respiratory (inhalation)
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00558
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60855
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508581
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C08095
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00902
ChemSpider
http://www.chemspider.com/Chemical-Structure.54842.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=4934
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0173-0681-01
PharmGKB
http://www.pharmgkb.org/drug/PA164740891
Wikipedia
http://en.wikipedia.org/wiki/Zanamivir
RxList
http://www.rxlist.com/cgi/generic2/zanam.htm
Drugs.com
http://www.drugs.com/cdi/zanamivir.html
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