Tìm theo
Pantoprazole
Các tên gọi khác (2) :
  • Pantoprazol
  • Pantoprazolum
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 102625-70-7
ATC: A02BC02
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C16H15F2N3O4S
PTK: 383.37
Pantoprazole is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H15F2N3O4S
Phân tử khối
383.37
Monoisotopic mass
383.075133083
InChI
InChI=1S/C16H15F2N3O4S/c1-23-13-5-6-19-12(14(13)24-2)8-26(22)16-20-10-4-3-9(25-15(17)18)7-11(10)21-16/h3-7,15H,8H2,1-2H3,(H,20,21)
InChI Key
InChIKey=IQPSEEYGBUAQFF-UHFFFAOYSA-N
IUPAC Name
6-(difluoromethoxy)-2-{[(3,4-dimethoxypyridin-2-yl)methane]sulfinyl}-1H-1,3-benzodiazole
Traditional IUPAC Name
5-(difluoromethoxy)-2-[(3,4-dimethoxypyridin-2-yl)methanesulfinyl]-3H-1,3-benzodiazole
SMILES
COC1=C(OC)C(CS(=O)C2=NC3=C(N2)C=C(OC(F)F)C=C3)=NC=C1
Độ tan chảy
Because of gradual degradation of pantoprazole sodium during heating, the melting point cannot be determined.
Độ hòa tan
Freely soluble in water.
logP
0.5
logS
-2.9
pKa (strongest acidic)
9.15
pKa (Strongest Basic)
3.55
PSA
86.33 Å2
Refractivity
90.05 m3·mol-1
Polarizability
35.17 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
6
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 : Pantoprazole is a substituted benzimidazole indicated for the short-term treatment (up to 16 weeks) in the healing and symptomatic relief of erosive esophagitis. Pantoprazole is a proton pump inhibitor (PPI) that suppresses the final step in gastric acid production.
Cơ Chế Tác Dụng : Pantoprazole is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease. Pantoprazole is a proton pump inhibitor (PPI) that suppresses the final step in gastric acid production by forming a covalent bond to two sites of the (H+,K+ )- ATPase enzyme system at the secretory surface of the gastric parietal cell. This effect is dose- related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus.
Dược Động Học :
▧ Absorption :
Pantoprazole is well absorbed. It undergoes little first-pass metabolism resulting in an absolute bioavailability of approximately 77%.
▧ Volume of Distribution :
* 11.0 to 23.6 L
▧ Protein binding :
98%
▧ Metabolism :
Pantoprazole is extensively metabolized in the liver through the cytochrome P450 (CYP) system. The main metabolic pathway is demethylation, by CYP2C19, with subsequent sulfation; other metabolic pathways include oxidation by CYP3A4. There is no evidence that any of the pantoprazole metabolites have significant pharmacologic activity.
▧ Route of Elimination :
After administration of a single intravenous dose of 14C-labeled pantoprazole to healthy, normal metabolizer subjects, approximately 71% of the dose was excreted in the urine with 18% excreted in the feces through biliary excretion.
▧ Half Life :
1 hour
▧ Clearance :
* 7.6-14.0 L/h
Độc Tính : Single intravenous doses of pantoprazole at 378, 230, and 266 mg/kg (38, 46, and 177 times the recommended human dose based on body surface area) were lethal to mice, rats and dogs, respectively. The symptoms of toxicity included hypoactivity, ataxia, hunched sitting, limb-splay, lateral position, segregation, absence of ear reflex, and tremor. There is limited experience regarding cases of human overdosage, and treatment should be symptomatic and supportive.
Chỉ Định : Short-term (up to 16 weeks) treatment of erosive esophagitis.
Tương Tác Thuốc :
  • Atazanavir This gastric pH modifier decreases the levels/effects of atazanavir
  • Cefditoren Proton pump inhibitors such as pantoprazole may decrease the serum concentration of cefditoren. If possible, avoid use of cefditoren with proton pump inhibitors (PPIs). Consider alternative methods to minimize/control acid reflux (eg, diet modification) or alternative antimicrobial therapy if use of PPIs can not be avoided.
  • Clopidogrel Pantoprazole may decrease serum concentrations of the active metabolite(s) of clopidogrel. Due to the possible risk for impaired clopidogrel effectiveness with this combination, clinicians should carefully consider the need for concurrent pantoprazole therapy in patients receiving clopidogrel. Monitor response to clopidogrel closely when using clopidogrel with pantoprazole. Whether there are differences among individual proton pump inhibitors is unclear. Other acid-lowering therapies (e.g., H2-receptor antagonists, antacids, etc.) do not appear to share this interaction with clopidogrel.
  • Dabigatran etexilate Proton pump inhibitors may decrease the bioavailability of dabigatran by 28% and increase inter-patient pharmacokinetic variability, especially in females. However, dose adjustment is not required.
  • Dabrafenib Proton pump inhibitors may alter the solubility of dabrafenib and reduce its bioavailability.
  • Dasatinib Pantoprazole may decrease the serum level of dasatinib.
  • Enoxacin Pantoprazole may decrease the absorption of enoxacin.
  • Indinavir Omeprazole decreases the absorption of indinavir
  • Itraconazole The proton pump inhibitor, pantoprazole, may decrease the absorption of itraconazole.
  • Ketoconazole The proton pump inhibitor, pantoprazole, may decrease the absorption of ketoconazole.
  • Rilpivirine Proton-pump inhibitors increase gastric pH which causes a decrease in the exposure of rilpivirine thus reducing efficacy.
  • Topotecan The BCRP/ABCG2 inhibitor, Pantaprazole, may increase the bioavailability and serum concentration of oral Topotecan. Monitor for change in the therapeutic and adverse effects of Topotecan if Pantaprazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Powder, for solution - Intravenous
Tablet, coated - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Pfizer
    Sản phẩm biệt dược : Pantoloc
  • Công ty :
    Sản phẩm biệt dược : Pantozol
  • Công ty :
    Sản phẩm biệt dược : Protonix
  • Công ty : Nycomed
    Sản phẩm biệt dược : Tecta
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00213
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4679
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504622
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C11806
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05353
ChemSpider
http://www.chemspider.com/Chemical-Structure.4517.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50241342
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0008-0923-51
PharmGKB
http://www.pharmgkb.org/drug/PA450774
Wikipedia
http://en.wikipedia.org/wiki/Pantoprazole
RxList
http://www.rxlist.com/cgi/generic3/protonix.htm
Drugs.com
http://www.drugs.com/cdi/pantoprazole.html
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