Tìm theo
Domperidone
Các tên gọi khác (6 ) :
  • 1-(3-(4-(5-chloro-2-oxo-2,3-Dihydrobenzo[D]imidazol-1-yl)piperidin-1-yl)propyl)-1H-benzo[D]imidazol-2(3H)-one
  • 5-chloro-1-(1-(3-(2-oxo-1-Benzimidazolinyl)propyl)-4-piperidyl)-2-benzimidazolinone
  • 5-chloro-1-(1-(3-(2-oxo-2,3-Dihydrobenzo[D]imidazol-1-yl)propyl)piperidin-4-yl)-1H-benzo[D]imidazol-2(3H)-one
  • 5-chloro-1-{1-[3-(2-oxo-2,3-dihydro-benzoimidazol-1-yl)-propyl]-piperidin-4-yl}-1,3-dihydro-benzoimidazol-2-one
  • Domperidona
  • Domperidonum
Thuốc đường tiêu hóa
Thuốc Gốc
Small Molecule
CAS: 57808-66-9
ATC: A03FA03
ĐG : Professional Co.
CTHH: C22H24ClN5O2
PTK: 425.911
A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C22H24ClN5O2
Phân tử khối
425.911
Monoisotopic mass
425.161852744
InChI
InChI=1S/C22H24ClN5O2/c23-15-6-7-20-18(14-15)25-22(30)28(20)16-8-12-26(13-9-16)10-3-11-27-19-5-2-1-4-17(19)24-21(27)29/h1-2,4-7,14,16H,3,8-13H2,(H,24,29)(H,25,30)
InChI Key
InChIKey=FGXWKSZFVQUSTL-UHFFFAOYSA-N
IUPAC Name
5-chloro-1-{1-[3-(2-oxo-2,3-dihydro-1H-1,3-benzodiazol-1-yl)propyl]piperidin-4-yl}-2,3-dihydro-1H-1,3-benzodiazol-2-one
Traditional IUPAC Name
domperidone
SMILES
ClC1=CC2=C(C=C1)N(C1CCN(CCCN3C(=O)NC4=CC=CC=C34)CC1)C(=O)N2
Độ tan chảy
242.5 °C
Độ hòa tan
0.986 mg/L
logP
3.90
logS
-3.7
pKa (strongest acidic)
12.52
pKa (Strongest Basic)
7.03
PSA
67.92 Å2
Refractivity
119.37 m3·mol-1
Polarizability
45.61 Å3
Rotatable Bond Count
5
H Bond Acceptor Count
3
H Bond Donor Count
2
Physiological Charge
1
Number of Rings
5
Bioavailability
1
Rule of Five
true
Ghose Filter
true
pKa
7.9
Dược Lực Học : Domperidone is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.
Cơ Chế Tác Dụng : A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms. [PubChem] Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which - among others - regulates nausea and vomiting
Dược Động Học :
▧ Absorption :
Fast
▧ Protein binding :
91%-93%
▧ Half Life :
7 hours
Độc Tính : Side effects include galactorrhea, gynecomastia, or menstrual irregularities.
Chỉ Định : For management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting.
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Roux-Ocefa
    Sản phẩm biệt dược : Euciton
  • Công ty : Sidus
    Sản phẩm biệt dược : Moperidona
  • Công ty : Janssen
    Sản phẩm biệt dược : Motilium
  • Sản phẩm biệt dược : Nauzelin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01184
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3151
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508314
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01745
ChemSpider
http://www.chemspider.com/Chemical-Structure.3039.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50241107
PharmGKB
http://www.pharmgkb.org/drug/PA134711056
Wikipedia
http://en.wikipedia.org/wiki/Domperidone
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