Tìm theo
Isosorbide Mononitrate
Các tên gọi khác (36 ) :
  • Corangin
  • Duride
  • Elantan
  • Imdur
  • Imtrate
  • Ismexin
  • Ismo
  • Ismox
  • Isosorbide mononitrate
  • Isosorbidi Mononitras
  • Medocor
  • Monicor
  • Mono corax
  • Monocedocard
  • Monocord
  • Monodur durules
  • Monoket
  • Monolong
  • Monomax
  • Mononit
  • Mononitrate d'Isosorbide
  • Mononitrato de Isosorbida
  • Monopront
  • Monosorb xl 60
  • Monosorbitrate
  • Monosordil
  • Nitramin
  • Olicard
  • Orasorbil
  • Pertil
  • Promocard
  • Sigacora
  • Sorbimon
  • Turimonit
  • Uniket
  • Vasdilat
Thuốc tim mạch
Thuốc Gốc
Small Molecule
CAS: 16051-77-7
ATC: C01DA14
ĐG : Actavis Group , http://www.actavis.com
CTHH: C6H9NO6
PTK: 191.1388
Isosorbide mononitrate is a drug used principally in the treatment of angina pectoris[1] and acts by dilating the blood vessels so as to reduce the blood pressure. It is sold by AstraZeneca under the trade name Imdur. Isosorbide mononitrate is used to for the the prophylactic treatment of angina pectoris; that is, it is taken in order to prevent or at least reduce the occurrence of angina. Research on Isosorbide mononitrate as a cervical ripener to reduce time at hospital to birth is supportive. Isosorbide mononitrate is an active metabolite of isosorbide dinitrate and exerts qualitatively similar effects. Isosorbide mononitrate reduces the workload of the heart by producing venous and arterial dilation. By reducing the end diastolic pressure and volume, isosorbide mononitrate lowers intramural pressure, hence leading to an improvement in the subendocardial blood flow. The net effect when administering isosorbide mononitrate is therefore a reduced workload for the heart and an improvement in the oxygen supply/demand balance of the myocardium. The adverse reactions which follow have been reported in studies with isosorbide mononitrate: Very common. Headache predominates (up to 30%) necessitating withdrawal of 2 to 3 % of patients, but the incidence reduces rapidly as treatment continues . Common. Tiredness, sleep disturbances (6%) and gastrointestinal disturbances (6%) have been reported during clinical trials with isosorbide mononitrate modified release tablets, but at a frequency no greater than for placebo. Hypotension (4 to 5%), poor appetite (2.5%), nausea (1%). Adverse effects associated with the clinical use of the drug are as expected with all nitrate preparations. They occur mainly in the early stages of treatment. Hypotension (4%) with symptoms such as dizziness and nausea (1%) have been reported. These symptoms generally disappear during long-term treatment. Other reactions that have been reported with isosorbide mononitrate modified release tablets include tachycardia, vomiting, diarrhoea, vertigo and heartburn
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C6H9NO6
Phân tử khối
191.1388
Monoisotopic mass
191.042987025
InChI
InChI=1S/C6H9NO6/c8-3-1-11-6-4(13-7(9)10)2-12-5(3)6/h3-6,8H,1-2H2/t3-,4+,5+,6+/m0/s1
InChI Key
InChIKey=YWXYYJSYQOXTPL-SLPGGIOYSA-N
IUPAC Name
(3R,3aS,6S,6aR)-6-hydroxy-hexahydrofuro[3,2-b]furan-3-yl nitrate
Traditional IUPAC Name
isosorbide mononitrate
SMILES
[H][C@]12OC[C@@H](O[N+]([O-])=O)[C@@]1([H])OC[C@@H]2O
Độ tan chảy
88-91 °C
Độ hòa tan
1.07E+005 mg/L
logP
-0.15
logS
-0.53
pKa (strongest acidic)
13.34
pKa (Strongest Basic)
-3.5
PSA
93.74 Å2
Refractivity
38.08 m3·mol-1
Polarizability
15.85 Å3
Rotatable Bond Count
2
H Bond Acceptor Count
6
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Dược Lực Học : Isosorbide-5-mononitrate, the long-acting metabolite of isosorbide dinitrate, is used as a vasodilatory agent in the management of angina pectoris. By dilating the vessels, it lowers the blood pressure and reduces the left ventricular preload and afterload, therefore, leads to a reduction of myocardial oxygen requirement.
Cơ Chế Tác Dụng : Isosorbide mononitrate is a drug used principally in the treatment of angina pectoris[1] and acts by dilating the blood vessels so as to reduce the blood pressure. It is sold by AstraZeneca under the trade name Imdur. Isosorbide mononitrate is used to for the the prophylactic treatment of angina pectoris; that is, it is taken in order to prevent or at least reduce the occurrence of angina. Research on Isosorbide mononitrate as a cervical ripener to reduce time at hospital to birth is supportive. Isosorbide mononitrate is an active metabolite of isosorbide dinitrate and exerts qualitatively similar effects. Isosorbide mononitrate reduces the workload of the heart by producing venous and arterial dilation. By reducing the end diastolic pressure and volume, isosorbide mononitrate lowers intramural pressure, hence leading to an improvement in the subendocardial blood flow. The net effect when administering isosorbide mononitrate is therefore a reduced workload for the heart and an improvement in the oxygen supply/demand balance of the myocardium. The adverse reactions which follow have been reported in studies with isosorbide mononitrate: Very common. Headache predominates (up to 30%) necessitating withdrawal of 2 to 3 % of patients, but the incidence reduces rapidly as treatment continues . Common. Tiredness, sleep disturbances (6%) and gastrointestinal disturbances (6%) have been reported during clinical trials with isosorbide mononitrate modified release tablets, but at a frequency no greater than for placebo. Hypotension (4 to 5%), poor appetite (2.5%), nausea (1%). Adverse effects associated with the clinical use of the drug are as expected with all nitrate preparations. They occur mainly in the early stages of treatment. Hypotension (4%) with symptoms such as dizziness and nausea (1%) have been reported. These symptoms generally disappear during long-term treatment. Other reactions that have been reported with isosorbide mononitrate modified release tablets include tachycardia, vomiting, diarrhoea, vertigo and heartburn Similar to other nitrites and organic nitrates, Isosorbide Mononitrate is converted to nitric oxide (NO), an active intermediate compound which activates the enzyme guanylate cyclase (Atrial natriuretic peptide receptor A). This stimulates the synthesis of cyclic guanosine 3',5'-monophosphate (cGMP) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells, eventually resulting in the dephosphorylation of the myosin light chain of the smooth muscle fiber. The subsequent release of calcium ions results in the relaxation of the smooth muscle cells and vasodilation.
Dược Động Học :
▧ Absorption :
100%
▧ Volume of Distribution :
* 0.6 to 0.7 L/kg
▧ Protein binding :
5%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Isosorbide mononitrate is primarily metabolized by the liver, but unlike oral isosorbide dinitrate, it is not subject to first-pass metabolism. Isosorbide mononitrate is cleared by denitration to isosorbide and glucuronidation as the mononitrate, with 96% of the administered dose excreted in the urine within 5 days and only about 1% eliminated in the feces. At least six different compounds have been detected in urine, with about 2% of the dose excreted as the unchanged drug and at least five metabolites.
▧ Half Life :
5 hours
▧ Clearance :
* 120–122 mL/min [Single dose of 60 mg PO] * 151–187 mL/min [Single dose of extended-release tablet 60 mg PO] * 132-151 mL/min [Multiple doses of extended release tablet 60 mg PO] * 119-140 mL/min [Multiple doses of extended release tablet 120 mg PO]
Độc Tính : Symptoms of overdose include vasodilatation, venous pooling, reduced cardiac output, and hypotension. There are no data suggesting what dose of isosorbide mononitrate is likely to be life-threatening in humans. In rats and mice, there is significant lethality at doses of 2000 mg/kg and 3000 mg/kg, respectively.
Chỉ Định : For the prevention of angina pectoris due to coronary artery disease and the treatment of acute and chronic angina pectoris, hypertension, and myocardial infarction.
Tương Tác Thuốc :
  • Avanafil Additive vasodilation. Concomitant therapy is contraindicated.
  • Dihydroergotamine Possible antagonism of action
  • Ergonovine Possible antagonism of action
  • Ergotamine Possible antagonism of action
  • Methylergometrine Possible antagonism of action
  • Methysergide Possible antagonism of action
  • Sildenafil Possible significant hypotension with this combination
  • Tadalafil The vasodilatory effects of Isosobide mononitrate may be increased by Tadalafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
  • Telithromycin Telithromycin may reduce clearance of Isosorbide Mononitrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Isosorbide Mononitrate if Telithromycin is initiated, discontinued or dose changed.
  • Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
  • Udenafil The vasodilatory effects of Isosobide mononitrate may be increased by Udenafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
  • Vardenafil The vasodilatory effects of Isosorbide mononitrate may be increased by Vardenafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of isosorbide mononitrate by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of isosorbide mononitrate if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Tablet - Oral
Tablet, extended release - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Chemydur
  • Công ty :
    Sản phẩm biệt dược : Corangin
  • Công ty :
    Sản phẩm biệt dược : Dilatrate
  • Công ty :
    Sản phẩm biệt dược : Duride
  • Công ty :
    Sản phẩm biệt dược : Elantan
  • Công ty :
    Sản phẩm biệt dược : Etimonis
  • Công ty :
    Sản phẩm biệt dược : Imdur
  • Công ty :
    Sản phẩm biệt dược : Imodur
  • Công ty :
    Sản phẩm biệt dược : Imtrate
  • Công ty :
    Sản phẩm biệt dược : Ismexin
  • Công ty :
    Sản phẩm biệt dược : Ismo
  • Công ty :
    Sản phẩm biệt dược : Ismox
  • Công ty :
    Sản phẩm biệt dược : Isomon
  • Công ty :
    Sản phẩm biệt dược : Isomonit
  • Công ty :
    Sản phẩm biệt dược : Isonorm
  • Công ty :
    Sản phẩm biệt dược : Medocor
  • Công ty :
    Sản phẩm biệt dược : Monicor
  • Công ty :
    Sản phẩm biệt dược : Monit
  • Công ty :
    Sản phẩm biệt dược : Mono Corax
  • Công ty :
    Sản phẩm biệt dược : Mono Mack
  • Công ty :
    Sản phẩm biệt dược : Monocedocard
  • Công ty :
    Sản phẩm biệt dược : Monoclair
  • Công ty :
    Sản phẩm biệt dược : Monocord
  • Công ty :
    Sản phẩm biệt dược : Monodur Durules
  • Công ty :
    Sản phẩm biệt dược : Monoket
  • Công ty :
    Sản phẩm biệt dược : Monolong
  • Công ty :
    Sản phẩm biệt dược : Monomax
  • Công ty :
    Sản phẩm biệt dược : Mononit
  • Công ty :
    Sản phẩm biệt dược : Monopront
  • Công ty :
    Sản phẩm biệt dược : Monosorb
  • Công ty :
    Sản phẩm biệt dược : Monosordil
  • Công ty :
    Sản phẩm biệt dược : Monotrate
  • Công ty :
    Sản phẩm biệt dược : Nitramin
  • Công ty :
    Sản phẩm biệt dược : Olicard
  • Công ty :
    Sản phẩm biệt dược : Olicardin
  • Công ty :
    Sản phẩm biệt dược : Orasorbil
  • Công ty :
    Sản phẩm biệt dược : Pertil
  • Công ty :
    Sản phẩm biệt dược : Plodin
  • Công ty :
    Sản phẩm biệt dược : Promocard
  • Công ty :
    Sản phẩm biệt dược : Sigacora
  • Công ty :
    Sản phẩm biệt dược : Solotrate
  • Công ty :
    Sản phẩm biệt dược : Sorbimon
  • Công ty :
    Sản phẩm biệt dược : Turimonit
  • Công ty :
    Sản phẩm biệt dược : Uniket
  • Công ty :
    Sản phẩm biệt dược : Vasdilat
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01020
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=27661
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506594
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07714
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00630
ChemSpider
http://www.chemspider.com/Chemical-Structure.25736.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0085-3306-03
PharmGKB
http://www.pharmgkb.org/drug/PA450126
Wikipedia
http://en.wikipedia.org/wiki/Isosorbide_mononitrate
RxList
http://www.rxlist.com/cgi/generic/isomono2.htm
Drugs.com
http://www.drugs.com/isosorbide_mononitrate.html
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