Tìm theo
Lansoprazole
Các tên gọi khác (13 ) :
  • AG 1749
  • Bamalite
  • Lansoprazol
  • Lansoprazole
  • Lansoprazolum
  • Lanzol
  • Lanzopral
  • Lanzul
  • Limpidex
  • Monolitum
  • Ogastro
  • Opiren
  • Prevacid
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 103577-45-3
ATC: A02BC03
ĐG : Abbott Laboratories Ltd. , http://www.abbott.com
CTHH: C16H14F3N3O2S
PTK: 369.361
Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid. It is manufactured by TAP Pharmaceutical Products. Lansoprazole has been marketed for many years and is one of several PPI's available.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H14F3N3O2S
Phân tử khối
369.361
Monoisotopic mass
369.075882012
InChI
InChI=1S/C16H14F3N3O2S/c1-10-13(20-7-6-14(10)24-9-16(17,18)19)8-25(23)15-21-11-4-2-3-5-12(11)22-15/h2-7H,8-9H2,1H3,(H,21,22)
InChI Key
InChIKey=MJIHNNLFOKEZEW-UHFFFAOYSA-N
IUPAC Name
2-({[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methane}sulfinyl)-1H-1,3-benzodiazole
Traditional IUPAC Name
2-{[3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methanesulfinyl}-1H-1,3-benzodiazole
SMILES
CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=CC=C2N1
Độ tan chảy
178-182 °C
Độ hòa tan
0.97 mg/L
logP
1.9
logS
-3.2
pKa (strongest acidic)
9.35
pKa (Strongest Basic)
4.16
PSA
67.87 Å2
Refractivity
87.61 m3·mol-1
Polarizability
34.59 Å3
Rotatable Bond Count
6
H Bond Acceptor Count
4
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 : Lansoprazole, an acid proton-pump inhibitor similar to omeprazole, is used as an untiulcer drug in the treatment and maintenance of healing of duodenal or gastric ulcers, erosive and reflux esophagitis, NSAID-induced ulcer, Zollinger-Ellison syndrome, and Barrett's esophagus. Lansoprozole is active against Helicobacter pylori. The plasma elimination half-life of lansoprazole does not reflect its duration of suppression of gastric acid secretion. Thus, the plasma elimination half-life is less than two hours, while the acid inhibitory effect lasts more than 24 hours.
Cơ Chế Tác Dụng : Lansoprazole is a proton pump inhibitor which prevents the stomach from producing acid. It is manufactured by TAP Pharmaceutical Products. Lansoprazole has been marketed for many years and is one of several PPI's available. Lansoprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or histamine H2-receptor antagonist properties, but rather suppress gastric acid secretion by specific inhibition of the (H+,K+)-ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the parietal cell, Lansoprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. 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 :
The absorption of lansoprazole is rapid, with mean Cmax occurring approximately 1.7 hours after oral dosing, and relatively complete with absolute bioavailability over 80%.
▧ Protein binding :
97%
▧ Metabolism :
Hepatic. Two metabolites have been identified in measurable quantities in plasma (the hydroxylated sulfinyl and sulfone derivatives of lansoprazole). These metabolites have very little or no antisecretory activity. Lansoprazole is thought to be transformed into two active species which inhibit acid secretion by (H+,K+)-ATPase within the parietal cell canaliculus, but are not present in the systemic circulation.
▧ Route of Elimination :
Following single-dose oral administration of PREVACID, virtually no unchanged lansoprazole was excreted in the urine. In one study, after a single oral dose of 14C-lansoprazole, approximately one-third of the administered radiation was excreted in the urine and two-thirds was recovered in the feces. This implies a significant biliary excretion of the lansoprazole metabolites.
▧ Half Life :
1.5 (± 1.0) hours
Độc Tính : Symptoms of overdose include abdominal pain, nausea and diarrhea.
Chỉ Định : For the treatment of acid-reflux disorders (GERD), peptic ulcer disease, H. pylori eradication, and prevention of gastroinetestinal bleeds with NSAID use.
Tương Tác Thuốc :
  • Atazanavir This gastric pH modifier decreases the levels/effects of atazanavir
  • Bosutinib Concomitant lansoprazole (PPI) decreased bosutinib Cmax by 46% and AUC by 26% compared to bosutinib alone. Consider using short-acting antacids or H2 blockers instead of PPIs to avoid a reduction in bosutinib exposure. Separate antacid or H2 blocker dosing and BOSULIF dosing by more than 2 hours.
  • Cefditoren Proton pump inhibitors such as lansoprazole 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 Lansoprazole 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 lansoprazole therapy in patients receiving clopidogrel. Monitor response to clopidogrel closely when using clopidogrel with lansoprazole. 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.
  • Enoxacin Lansoprazole may decrease the absorption of enoxacin.
  • Indinavir Omeprazole decreases the absorption of indinavir
  • Itraconazole The proton pump inhibitor, lansoprazole, may decrease the absorption of itraconazole.
  • Ketoconazole The proton pump inhibitor, lansoprazole, may decrease the absorption of ketoconazole.
  • Prasugrel Lansoprazole is a CYP2C19 substrate which decreases AUC and Cmax of prasugrel. Despite these decreases, there was no significant reduction of inhibition of platelet aggregation.
  • Rilpivirine Proton-pump inhibitors increase gastric pH which causes a decrease in the exposure of rilpivirine thus reducing efficacy.
  • Sucralfate Sucralfate decreases the effect of lansoprazole
Liều Lượng & Cách Dùng : Capsule, delayed release - Oral
Tablet, delayed release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Takeda
    Sản phẩm biệt dược : Agopton
  • Công ty :
    Sản phẩm biệt dược : Bamalite
  • Công ty : Cipla Medpro
    Sản phẩm biệt dược : Lansoloc
  • Công ty : Cipla
    Sản phẩm biệt dược : Lanzol
  • Công ty : Pharma Investi
    Sản phẩm biệt dược : Lanzopral
  • Công ty : Ranbaxy
    Sản phẩm biệt dược : Lanzopran
  • Công ty : Sigma-Tau
    Sản phẩm biệt dược : Limpidex
  • Công ty : Salvat
    Sản phẩm biệt dược : Monolitum
  • Công ty : Takeda
    Sản phẩm biệt dược : Ogast
  • Công ty : Abbott
    Sản phẩm biệt dược : Ogastro
  • Công ty : Almirall
    Sản phẩm biệt dược : Opiren
  • Công ty : Novartis
    Sản phẩm biệt dược : Prevacid
  • Công ty : Novartis
    Sản phẩm biệt dược : Prevacid 24HR
  • Công ty : Novartis
    Sản phẩm biệt dược : Prevacid IV
  • Công ty : Novartis
    Sản phẩm biệt dược : Prevacid Solutab
  • Công ty : Takeda
    Sản phẩm biệt dược : Prosogan
  • Công ty : Takeda
    Sản phẩm biệt dược : Takepron
  • Công ty : Hormona
    Sản phẩm biệt dược : Ulpax
  • Công ty : Toprak
    Sản phẩm biệt dược : Zoprol
  • Công ty : Pfizer
    Sản phẩm biệt dược : Zoton
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00448
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3883
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508975
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00355
ChemSpider
http://www.chemspider.com/Chemical-Structure.3746.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0339-6489-11
PharmGKB
http://www.pharmgkb.org/drug/PA450180
Wikipedia
http://en.wikipedia.org/wiki/Lansoprazole
RxList
http://www.rxlist.com/cgi/generic/lansop.htm
Drugs.com
http://www.drugs.com/lansoprazole.html
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