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药品详细

Sevoflurane(七氟醚)

化学结构式图
中文名
七氟醚
英文名
Sevoflurane
分子式
C4H3F7O
化学名
1,1,1,3,3,3-hexafluoro-2-(fluoromethoxy)propane
分子量
Average: 200.0548
Monoisotopic: 200.007212153
CAS号
28523-86-6
ATC分类
N01A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Sevoflurane (2,2,2-trifluoro-1-[trifluoromethyl]ethyl fluoromethyl ether), also called fluoromethyl, is a sweet-smelling, non-flammable, highly fluorinated methyl isopropyl ether used for induction and maintenance of general anesthesia. Together with desflurane, it is replacing isoflurane and halothane in modern anesthesiology. [Wikipedia]

生产厂家
  • Abbott laboratories
  • Baxter healthcare corp
  • Halocarbon products corp
  • Piramal critical care 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
  • Ethers
Substructures
  • Alkyl Halides
  • Ethers
适应症
药理
Indication Used for induction and maintenance of general anesthesia in adult and pediatric patients for inpatient and outpatient surgery.
Pharmacodynamics Sevoflurane (also called fluoromethyl) is a halogenated ether used for induction and maintenance of general anesthesia. Together with desflurane, it is replacing isoflurane and halothane in modern anesthesiology. It is often administered in nitrous oxide and pure oxygen. After desflurane it is the volatile anesthetic with the fastest onset and offset. It induces muscle relaxation and reduces pains sensitivity by altering tissue excitability. It does so by decreasing the extent of gap junction mediated cell-cell coupling and altering the activity of the channels that underlie the action potential.
Mechanism of action Sevoflurane induces a reduction in junctional conductance by decreasing gap junction channel opening times and increasing gap junction channel closing times. Sevoflurane also activates calcium dependent ATPase in the sarcoplasmic reticulum by increasing the fluidity of the lipid membrane. It also appears to bind the D subunit of ATP synthase and NADH dehydogenase and also binds to the GABA receptor, the large conductance Ca2+ activated potassium channel, the glutamate receptor, and the glycine receptor.
Absorption Rapidly absorbed into circulation via the lungs, however solubility in the blood is low.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Relatively little biotransformation, only 5% is metabolized by cytochrome P450 CYP2E1 to hexafluoroisopropanol (HFIP) with release of inorganic fluoride and CO2. No other metabolic pathways have been identified for sevoflurane.

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

Substrate Enzymes Product
Sevoflurane
    Fluoride Details
    Sevoflurane
      CO2 Details
      Sevoflurane
        Hexafluoroisopropanol Details
        Route of elimination The low solubility of sevoflurane facilitates rapid elimination via the lungs. In vivo metabolism studies suggest that approximately 5% of the sevoflurane dose may be metabolized. Up to 3.5% of the sevoflurane dose appears in the urine as inorganic fluoride.
        Half life 15-23 hours
        Clearance Not Available
        Toxicity LC50=49881 ppm/hr (rat), LD50=10.8 g/kg (rat)
        Affected organisms
        • Humans and other mammals
        Pathways Not Available
        理化性质
        Properties
        State liquid
        Experimental Properties
        Property Value Source
        melting point < 25 °C PhysProp
        boiling point 58.5 °C PhysProp
        water solubility Very slightly soluble Not Available
        logP 2.4 Not Available
        Predicted Properties
        Property Value Source
        water solubility 1.48e+00 g/l ALOGPS
        logP 2.44 ALOGPS
        logP 2.27 ChemAxon
        logS -2.1 ALOGPS
        pKa (strongest acidic) 15.07 ChemAxon
        pKa (strongest basic) -4.5 ChemAxon
        physiological charge 0 ChemAxon
        hydrogen acceptor count 1 ChemAxon
        hydrogen donor count 0 ChemAxon
        polar surface area 9.23 ChemAxon
        rotatable bond count 4 ChemAxon
        refractivity 23.3 ChemAxon
        polarizability 9.83 ChemAxon
        药物相互作用
        食物相互作用
        Not Available

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