Tìm theo
Clevidipine
Các tên gọi khác (2) :
  • Clevidipine butyrate
  • Cleviprex
Thuốc Gốc
Small Molecule
CAS: 166432-28-6
CTHH: C21H23Cl2NO6
PTK: 456.316
Clevidipine is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood pressure reduction when oral therapy is not an option.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C21H23Cl2NO6
Phân tử khối
456.316
Monoisotopic mass
455.090242887
InChI
InChI=1S/C21H23Cl2NO6/c1-5-7-15(25)29-10-30-21(27)17-12(3)24-11(2)16(20(26)28-4)18(17)13-8-6-9-14(22)19(13)23/h6,8-9,18,24H,5,7,10H2,1-4H3
InChI Key
InChIKey=KPBZROQVTHLCDU-UHFFFAOYSA-N
IUPAC Name
methyl 5-{[(butanoyloxy)methoxy]carbonyl}-4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3-carboxylate
Traditional IUPAC Name
methyl 5-{[(butanoyloxy)methoxy]carbonyl}-4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3-carboxylate
SMILES
CCCC(=O)OCOC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC(Cl)=C1Cl)C(=O)OC
Độ hòa tan
2.67e-03 g/l
logP
4.09
logS
-5.2
pKa (Strongest Basic)
5.31
PSA
90.93 Å2
Refractivity
113.93 m3·mol-1
Polarizability
45.12 Å3
Rotatable Bond Count
10
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Clevidipine belongs to a well-known class of drugs called dihydropyridine calcium channel antagonists. Clevidpine is the first third generation intravenous dihydropyridine calcium channel blocker. In vitro studies demonstrated that clevidipine acts by selectively relaxing the smooth muscle cells that line small arteries, resulting in arterial dilation, widening of the artery opening, and without reducing central venous pressure or reducing cardiac output.
Cơ Chế Tác Dụng : Clevidipine is a dihydropyridine L-type calcium channel blocker that is selective for vascular smooth muscle and is indicated for blood pressure reduction when oral therapy is not an option. Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, clevidipine inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue.
Dược Động Học :

▧ Protein binding :
>99.5%
▧ Metabolism :
Clevidipine is rapidly hydrolyzed to inactive metabolites by esterases in arterial blood.
▧ Route of Elimination :
urine 63-74%, feces 7-22%
▧ Half Life :
1 minute
Chỉ Định : For the treatment of hypertension.
Tương Tác Thuốc :
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Liều Lượng & Cách Dùng : Emulsion - Intravenous - 100mL single use vial with 0.5 mg/mL clevidipine.
Emulsion - Intravenous - 50mL single use vial with 0.5 mg/mL clevidipine.
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB04920
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D08892
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/65293-005-50
Wikipedia
http://en.wikipedia.org/wiki/Clevidipine
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