Tìm theo
Nizatidine
Các tên gọi khác (5 ) :
  • Acinon
  • Axid
  • Nizatidina
  • Nizatidine
  • Nizatidinum
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 76963-41-2
ATC: A02BA04
ĐG : Affordable Pharmaceuticals LLC , http://www.affordablepharm.com
CTHH: C12H21N5O2S2
PTK: 331.457
A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H21N5O2S2
Phân tử khối
331.457
Monoisotopic mass
331.113666321
InChI
InChI=1S/C12H21N5O2S2/c1-13-11(6-17(18)19)14-4-5-20-8-10-9-21-12(15-10)7-16(2)3/h6,9,13-14H,4-5,7-8H2,1-3H3/b11-6+
InChI Key
InChIKey=SGXXNSQHWDMGGP-IZZDOVSWSA-N
IUPAC Name
dimethyl[(4-{[(2-{[(E)-1-(methylamino)-2-nitroethenyl]amino}ethyl)sulfanyl]methyl}-1,3-thiazol-2-yl)methyl]amine
Traditional IUPAC Name
nizatidine
SMILES
CN\C(NCCSCC1=CSC(CN(C)C)=N1)=C/[N+]([O-])=O
Độ tan chảy
130-132 °C
Độ hòa tan
10-33mg/mL
logP
1.1
logS
-3.9
pKa (Strongest Basic)
6.83
PSA
86.01 Å2
Refractivity
96.84 m3·mol-1
Polarizability
35.49 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
6
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Nizatidine is a competitive, reversible inhibitor of histamine at the histamine H2-receptors, particularly those in the gastric parietal cells. By inhibiting the action of histamine on stomach cells, nizatidine reduces stomach acid production. Nizatidine had no demonstrable antiandrogenic action. Full-dose therapy for the problems treated by nizatidine lasts no longer than 8 weeks. It has been demonstrated that treatment with a reduced dose of nizatidine is effective as maintenance therapy following healing of active duodenal ulcers.
Cơ Chế Tác Dụng : A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers. [PubChem] Nizatidine competes with histamine for binding at the H2-receptors on the gastric basolateral membrane of parietal cells. Competitive inhibition results in reduction of basal and nocturnal gastric acid secretions. The drug also decreases the gastric acid response to stimuli such as food, caffeine, insulin, betazole, or pentagastrin.
Dược Động Học :
▧ Absorption :
Rapid (bioavailability of nizatidine exceeds 70%)
▧ Volume of Distribution :
* 0.8 to 1.5 L/kg
▧ Protein binding :
35%
▧ Metabolism :
Hepatic. Less than 7% of an oral dose is metabolized as N2-monodes-methylnizatidine, an H2-receptor antagonist, which is the principal metabolite excreted in the urine. Other likely metabolites are the N2-oxide (less than 5% of the dose) and the S-oxide (less than 6% of the dose).
▧ Half Life :
1-2 hours
▧ Clearance :
* 40-60 L/h * 7 – 14 L/h [functionally anephric patients]
Độc Tính : Oral, rat LD50: 301 mg/kg. Symptoms of overdose include cholinergic-type effects including lacrimation, salivation, emesis, miosis, and diarrhea.
Chỉ Định : For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, active benign gastric ulcer, and active duodenal ulcer.
Tương Tác Thuốc :
  • Atazanavir This gastric pH modifier decreases the levels/effects of atazanavir
  • Cefditoren H2-Antagonists such as nizatidine may decrease the serum concentration of cefditoren. Cefditoren prescribing information recommends to avoid concomitant use with H2-antagonists (eg, famotidine, ranitidine) and antacids as well. Consider alternative methods to minimize/control acid reflux (eg, diet modification) or alternative antimicrobial therapy if use of H2-antagonists can not be avoided.
  • Enoxacin Nizatidine may decrease the absorption of enoxacin.
  • Itraconazole The H2-receptor antagonist, nizatidine, may decrease the absorption of itraconazole.
  • Ketoconazole The H2-receptor antagonist, nizatidine, may decrease the absorption of ketoconazole.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Acinon
  • Công ty : Eli Lilly
    Sản phẩm biệt dược : Axid
  • Công ty : Eli Lilly
    Sản phẩm biệt dược : Tazac
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00585
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3033637
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507554
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07270
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00440
ChemSpider
http://www.chemspider.com/Chemical-Structure.2298266.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-5150-91
PharmGKB
http://www.pharmgkb.org/drug/PA164752234
Wikipedia
http://en.wikipedia.org/wiki/Nizatidine
RxList
http://www.rxlist.com/cgi/generic/nizat.htm
Drugs.com
http://www.drugs.com/cdi/nizatidine.html
... loading
... loading