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药品详细

Nitroglycerin(硝酸甘油)

化学结构式图
中文名
硝酸甘油
英文名
Nitroglycerin
分子式
C3H5N3O9
化学名
2,3-bis(nitrooxy)propyl nitrate
分子量
Average: 227.0865
Monoisotopic: 227.002578773
CAS号
55-63-0
ATC分类
C01D Vasodilators Used in Cardiac Diseases
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A volatile vasodilator which relieves angina pectoris by stimulating guanylate cyclase and lowering cytosolic calcium. [PubChem]

生产厂家
  • Abraxis pharmaceutical products
  • Baxter healthcare corp
  • E fougera div altana inc
  • G pohl boskamp gmbh and co
  • Graceway pharmaceuticals llc
  • Hercon laboratories corp
  • Hospira inc
  • International medication systems ltd
  • Key pharmaceuticals inc sub schering plough corp
  • Kremers urban co
  • Luitpold pharmaceuticals inc
  • Mylan technologies inc
  • Novadel pharma inc
  • Novartis pharmaceuticals corp
  • Parke davis div warner lambert co
  • Pfizer pharmaceuticals ltd
  • Pohl boskamp
  • Rorer pharmaceutical corp sub rorer group
  • Sanofi aventis us llc
  • Smith and nephew solopak div smith and nephew
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Glycerol and Derivatives
Substructures
  • Glycerol and Derivatives
  • Oxoazaniums
  • Esters
  • Nitrates
适应症
药理
Indication For the prevention of angina
Pharmacodynamics Nitroglycerin, an organic nitrate, is available in many forms as a vasodilator. Nitroglycerin is used in the treatement of angina pectoris and perioperative hypertension, to produce controlled hypotension during surgical procedures, to treat hypertensive emergencies, and to treat congestive heart failure associated with myocardial infarction.
Mechanism of action Similar to other nitrites and organic nitrates, nitroglycerin is converted to nitric oxide (NO), an active intermediate compound which activates the enzyme guanylate cyclase. 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.
Absorption Not Available
Volume of distribution
  • 3 L/kg
Protein binding Not Available
Metabolism
Hepatic, cytochrome P450 (P450) is a key enzyme of organic nitrate biotransformation
Route of elimination Not Available
Half life 3 minutes
Clearance
  • 1 L/kg/min
Toxicity Increased intracranial pressure, with any or all of persistent throbbing headache, confusion, and moderate fever; Vertigo; Palpitations; Visual disturbances; Nausea and vomiting (possibly with colic and even bloody diarrhea); Syncope (especially in the upright posture); Air hunger and dyspnea, later followed by reduced ventilatory effort; Diaphoresis, with the skin either flushed or cold and clammy; Heart block and bradycardia; Paralysis; Coma; Seizures; Death.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State liquid
Experimental Properties
Property Value Source
melting point 13.5 °C PhysProp
boiling point 250 °C PhysProp
water solubility 1380 mg/L (at 20 °C) SEIDELL,A (1941)
logP 1.62 HANSCH,C ET AL. (1995)
logS -2.22 ADME Research, USCD
Predicted Properties
Property Value Source
water solubility 2.04e-01 g/l ALOGPS
logP 1.25 ALOGPS
logP 0.94 ChemAxon
logS -3 ALOGPS
pKa (strongest basic) -5.6 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 9 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 165.15 ChemAxon
rotatable bond count 8 ChemAxon
refractivity 40.6 ChemAxon
polarizability 15.56 ChemAxon
药物相互作用
Drug Interaction
Alteplase IV nitroglycerin may decrease the effect of alteplase.
Avanafil Additive vasodilation. Concomitant therapy is contraindicated.
Azilsartan medoxomil Pharmacodynamic synergist- increases effects.
Dihydroergotamine Possible antagonism of action
Dihydroergotoxine Possible antagonism of action
Ergonovine Possible antagonism of action
Ergotamine Possible antagonism of action
Methylergonovine Possible antagonism of action
Methysergide Possible antagonism of action
Sildenafil Possible significant hypotension with this combination
Tadalafil The vasodilatory effects of Nitroglycerin may be increased by Tadalafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Udenafil The vasodilatory effects of Nitroglycerin may be increased by Udenafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
Vardenafil The vasodilatory effects of Nitroglycerin may be increased by Vardenafil. Severe hypotension may occur. Concomitant therapy is contraindicated.
食物相互作用
  • Avoid alcohol.
  • Dissolve under the tongue.
  • Take on empty stomach: 1 hour before or 2 hours after meals.

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