Tìm theo
Esomeprazole
Các tên gọi khác (7 ) :
  • (−)-omeprazole
  • (S)-(−)-omeprazole
  • (S)-omeprazole
  • Esomeprazol
  • Ésoméprazole
  • Esomeprazolum
  • Perprazole
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 161796-78-7
ĐG : AQ Pharmaceuticals Inc. , http://www.aqpharmaceuticals.com
CTHH: C17H19N3O3S
PTK: 345.416
A highly effective inhibitor of gastric acid secretion used in the therapy of stomach ulcers and zollinger-ellison syndrome. The drug inhibits the H(+)-K(+)-ATPase (H(+)-K(+)-exchanging ATPase) in the proton pump of gastric parietal cells. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H19N3O3S
Phân tử khối
345.416
Monoisotopic mass
345.114712179
InChI
InChI=1/C17H19N3O3S/c1-10-8-18-15(11(2)16(10)23-4)9-24(21)17-19-13-6-5-12(22-3)7-14(13)20-17/h5-8H,9H2,1-4H3,(H,19,20)/t24-/s2
InChI Key
InChIKey=SUBDBMMJDZJVOS-FQKVKQEKNA-N
IUPAC Name
5-methoxy-2-[(S)-(4-methoxy-3,5-dimethylpyridin-2-yl)methanesulfinyl]-1H-1,3-benzodiazole
Traditional IUPAC Name
5-methoxy-2-[(S)-(4-methoxy-3,5-dimethylpyridin-2-yl)methanesulfinyl]-1H-1,3-benzodiazole
SMILES
COC1=CC2=C(NC(=N2)[S@@](=O)CC2=NC=C(C)C(OC)=C2C)C=C1
Độ tan chảy
155 °C
Độ hòa tan
Very slightly soluble in water
logP
0.6
logS
-3
pKa (strongest acidic)
9.68
pKa (Strongest Basic)
4.77
PSA
77.1 Å2
Refractivity
93.66 m3·mol-1
Polarizability
35.81 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
5
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Esomeprazole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and H. pylori eradication to reduce the risk of duodenal ulcer recurrence. Esomeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase at the secretory surface of the gastric parietal cell. By doing so, it inhibits acid secretion into the gsatric lumen. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.
Cơ Chế Tác Dụng : A highly effective inhibitor of gastric acid secretion used in the therapy of stomach ulcers and zollinger-ellison syndrome. The drug inhibits the H(+)-K(+)-ATPase (H(+)-K(+)-exchanging ATPase) in the proton pump of gastric parietal cells. [PubChem] Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. By acting specifically on the proton pump, Esomeprazole blocks the final step in acid production, thus reducing gastric acidity.
Dược Động Học :
▧ Absorption :
90%
▧ Volume of Distribution :
* 16 L [healthy volunteers]
▧ Protein binding :
97%
▧ Metabolism :
Mainly hepatic. Esomeprazole is completely metabolized by the cytochrome P450 system via CYP2C19 and CYP3A4. Metabolism produces inactive hydroxy and desmethyl metabolites, which have no effect on gastric acid secretion. Less than 1% of the parent drug is excreted in urine.
▧ Route of Elimination :
Approximately 80% of the administered dose of esomeprazole is excreted as metabolites in urine and the remaining 20% is excreted in feces.
▧ Half Life :
1-1.5 hours
Độc Tính : Blurred vision, confusion, drowsiness, dry mouth, flushing headache, nausea, rapid heartbeat, sweating
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
  • Cefditoren Proton pump inhibitors such as esomeprazole 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 Esomeprazole 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 esomeprazole therapy in patients receiving clopidogrel. Monitor response to clopidogrel closely when using clopidogrel with esomeprazole. 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 Esomeprazole may decrease the absorption of enoxacin.
  • Indinavir Omeprazole decreases the absorption of indinavir
  • Itraconazole The proton pump inhibitor, esomeprazole, may decrease the absorption of itraconazole.
  • Ketoconazole The proton pump inhibitor, esomeprazole, 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.
  • Tipranavir Tipranavir, co-administered with Ritonavir, may decrease the plasma concentration of Esomeprazole. Consider alternate therapy or increase the dose of Esomeprazole based on the therapeutic response.
Liều Lượng & Cách Dùng : Capsule, delayed release - Oral - 20 mg
Capsule, delayed release - Oral - 40 mg
Granule, for suspension - Oral - 10 mg per packet
Granule, for suspension - Oral - 20 mg per packet
Granule, for suspension - Oral - 40 mg per packet
Injection - Intravenous - 20 mg
Injection - Intravenous - 40 mg
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Delta
    Sản phẩm biệt dược : Alenia
  • Công ty : Usawa
    Sản phẩm biệt dược : Awa-Block
  • Công ty : Simesa
    Sản phẩm biệt dược : Axagon
  • Công ty : Prater
    Sản phẩm biệt dược : Cor
  • Công ty : Biotoscana
    Sản phẩm biệt dược : Cronopep
  • Công ty : Krka
    Sản phẩm biệt dược : Emanera
  • Công ty : Aristopharma
    Sản phẩm biệt dược : Emep
  • Công ty : HYGIA
    Sản phẩm biệt dược : Emozul
  • Sản phẩm biệt dược : ES-OD
  • Công ty : HYGIA
    Sản phẩm biệt dược : Esmep
  • Công ty : Asiatic Lab
    Sản phẩm biệt dược : Eso
  • Công ty : Micro Labs
    Sản phẩm biệt dược : Esofag
  • Công ty : Nova Argentia
    Sản phẩm biệt dược : Esogastrosedol
  • Công ty : Ibn Sina
    Sản phẩm biệt dược : Esolok
  • Công ty : Marfan
    Sản phẩm biệt dược : Esomarfan
  • Công ty : RAK
    Sản phẩm biệt dược : Esomenta
  • Công ty : ACI
    Sản phẩm biệt dược : Esomep
  • Công ty : Genfar S.A
    Sản phẩm biệt dược : Esomeprazol Genfar
  • Công ty : Maquifarma
    Sản phẩm biệt dược : Esopral
  • Công ty : Centaur
    Sản phẩm biệt dược : Esorest
  • Công ty : Malesci
    Sản phẩm biệt dược : Lucen
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Nexiam
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Nexium
  • Công ty : AstraZeneca
    Sản phẩm biệt dược : Nexium i.v.
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00736
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01984
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0186-6020-01
PharmGKB
http://www.pharmgkb.org/drug/PA10075
Wikipedia
http://en.wikipedia.org/wiki/Esomeprazole
RxList
http://www.rxlist.com/cgi/generic3/esomeprazole.htm
Drugs.com
http://www.drugs.com/cdi/esomeprazole.html
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