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药品详细

Nitroprusside(硝普钠)

化学结构式图
中文名
硝普钠
英文名
Nitroprusside
分子式
C5FeN6O
化学名
pentacyano(nitroso)irondiuide
分子量
Average: 215.938
Monoisotopic: 215.948300785
CAS号
15078-28-1
ATC分类
C02D 未知
药物类型
small molecule
阶段
approved
商品名
Nipride;Nitropress;
同义名
Disodium nitroprusside dihydrate;Sodium nitroferricyanide dihydrate;Sodium Nitroprusside;Sodium nitroprusside dihydrate;
基本介绍

Nitroprusside serves as a source of nitric oxide, a potent peripheral vasodilator that affects both arterioles and venules (venules more than arterioles). Nitroprusside is often administered intravenously to patients who are experiencing a hypertensive emergency. [Wikipedia]

生产厂家
  • Abbott laboratories
  • Abbott laboratories pharmaceutical products div
  • Abraxis pharmaceutical products
  • Baxter healthcare corp anesthesia and critical care
  • Hoffmann la roche inc
  • Hospira inc
  • Teva parenteral medicines inc
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
  • Inorganic Ions and Gases
Substructures
  • Anions
  • Oxoazaniums
  • Nitriles and Derivatives
  • Cyanides
  • Cations
  • Inorganic Ions and Gases
适应症
ANTIHYPERTENSIVES 降血压;
药理
Indication For immediate reduction of blood pressure of patients in hypertensive crises, reduce bleeding during surgery, and for the treatment of acute congestive heart failure
Pharmacodynamics Nitroprusside a powerful vasodilator relaxes the vascular smooth muscle and produce consequent dilatation of peripheral arteries and veins. Other smooth muscle (e.g., uterus, duodenum) is not affected. Sodium nitroprusside is more active on veins than on arteries.
Mechanism of action One molecule of sodium nitroprusside is metabolized by combination with hemoglobin to produce one molecule of cyanmethemoglobin and four CN- ions; methemoglobin, obtained from hemoglobin, can sequester cyanide as cyanmethemoglobin; thiosulfate reacts with cyanide to produce thiocyanate; thiocyanate is eliminated in the urine; cyanide not otherwise removed binds to cytochromes. Cyanide ion is normally found in serum; it is derived from dietary substrates and from tobacco smoke. Cyanide binds avidly (but reversibly) to ferric ion (Fe+++), most body stores of which are found in erythrocyte methemoglobin (metHgb) and in mitochondrial cytochromes. When CN is infused or generated within the bloodstream, essentially all of it is bound to methemoglobin until intraerythrocytic methemoglobin has been saturated. Once activated to NO, it activates guanylate cyclase in vascular smooth muscle and increases intracellular production of cGMP. cGMP stimulates calcium movement from the cytoplasm to the endoplasmic reticulum and reduces calcium available to bind with calmodulin. This eventually leads to vascular smooth muscle relaxation and vessel dilatation.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Metabolized by reaction with hemoglobin to produce cyanmethemoglobin and cynide ions

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Nitroprusside
    cyanmethemoglobin Details
    Route of elimination One molecule of sodium nitroprusside is metabolized by combination with hemoglobin to produce one molecule of cyanmethemoglobin and four CN¯ ions, thiosulfate reacts with cyanide to produce thiocyanate, thiocyanate is eliminated in the urine.
    Half life Approximately 2 minutes
    Clearance Not Available
    Toxicity Overdosage of nitroprusside can be manifested as excessive hypotension or cyanide toxicity or as thiocyanate toxicity. The acute intravenous mean lethal doses (LD50) of nitroprusside in rabbits, dogs, mice, and rats are 2.8, 5.0, 8.4, and 11.2 mg/kg, respectively.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties Not Available
    Predicted Properties
    Property Value Source
    logP 0.071 ChemAxon
    pKa (strongest basic) -3.3 ChemAxon
    physiological charge -2 ChemAxon
    hydrogen acceptor count 6 ChemAxon
    hydrogen donor count 0 ChemAxon
    polar surface area 148.38 ChemAxon
    rotatable bond count 1 ChemAxon
    refractivity 39.44 ChemAxon
    polarizability 16.52 ChemAxon
    药物相互作用
    Drug Interaction
    Treprostinil Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
    食物相互作用
    Not Available

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