Tìm theo
Milrinone
Các tên gọi khác (4 ) :
  • 1,6-Dihydro-2-methyl-6-oxo(3,4'-bipyridine)-5-carbonitrile
  • Milrinona
  • Milrinone
  • Milrinonum
platelet aggregation inhibitors, cardiotonic agents, phosphodiesterase 3 inhibitors, vasodilator agents
Thuốc Gốc
Small Molecule
CAS: 78415-72-2
ATC: C01CE02
ĐG : Alchymars SPA
CTHH: C12H9N3O
PTK: 211.2194
A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase activity in myocardium and vascular smooth muscle. Milrinone is a derivative of amrinone and has 20-30 times the ionotropic potency of amrinone. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H9N3O
Phân tử khối
211.2194
Monoisotopic mass
211.074561925
InChI
InChI=1S/C12H9N3O/c1-8-11(9-2-4-14-5-3-9)6-10(7-13)12(16)15-8/h2-6H,1H3,(H,15,16)
InChI Key
InChIKey=PZRHRDRVRGEVNW-UHFFFAOYSA-N
IUPAC Name
6-methyl-2-oxo-5-(pyridin-4-yl)-1,2-dihydropyridine-3-carbonitrile
Traditional IUPAC Name
milrinone
SMILES
CC1=C(C=C(C#N)C(=O)N1)C1=CC=NC=C1
Độ tan chảy
>300 °C
Độ hòa tan
Slightly soluble
logP
0.4
logS
-3
pKa (strongest acidic)
7.54
pKa (Strongest Basic)
4.82
PSA
65.78 Å2
Refractivity
61.14 m3·mol-1
Polarizability
21.46 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Milrinone, a synthetic dimethylxanthine derivative structurally related to theophylline and caffeine, is used in the treatment of peripheral vascular diseases and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.
Cơ Chế Tác Dụng : A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase activity in myocardium and vascular smooth muscle. Milrinone is a derivative of amrinone and has 20-30 times the ionotropic potency of amrinone. [PubChem] Milrinone inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, Milrinone also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity.
Dược Động Học :
▧ Absorption :
Milrinone is rapidly and almost completely absorbed after oral administration. Bioavailability is 92% (in healthy volunteers).
▧ Volume of Distribution :
* 0.38 liters/kg [intravenous injections of 12.5 mcg/kg to 125 mcg/kg to congestive heart failure patients] * 0.45 liters/kg [intravenous infusions of 0.20 mcg/kg/min to 0.70 mcg/kg/min to congestive heart failure patients]
▧ Protein binding :
70 to 80%
▧ Metabolism :
There are five metabolites but the O-glucuronide represents the major pathway of biotransformation.
▧ Route of Elimination :
The primary route of excretion of milrinone in man is via the urine.
▧ Half Life :
2.3 hours
▧ Clearance :
* 0.13 L/kg/hr [congestive heart failure patients, following IV injections of 12.5 mcg/kg to 125 mcg/kg] * 0.14 L/kg/hr [congestive heart failure patients, following infusions of 0.2 mcg/kg/min to 0.7 mcg/kg/min]
Độc Tính : LD50 = 0.3 mg/L in rats
Chỉ Định : Indicated for the treatment of congestive heart failure.
Liều Lượng & Cách Dùng : Liquid - Intravenous
Solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Corotrop
  • Công ty :
    Sản phẩm biệt dược : Corotrope
  • Công ty :
    Sản phẩm biệt dược : Milrila
  • Công ty :
    Sản phẩm biệt dược : Primacor
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00235
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4197
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507838
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07224
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00417
ChemSpider
http://www.chemspider.com/Chemical-Structure.4052.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=15296
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/55390-078-01
PharmGKB
http://www.pharmgkb.org/drug/PA164749171
Wikipedia
http://en.wikipedia.org/wiki/Milrinone
RxList
http://www.rxlist.com/cgi/generic3/milrin.htm
Drugs.com
http://www.drugs.com/cdi/milrinone.html
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