イソプレナリン

イソプレナリン 化学特性,用途語,生産方法

• 解説

  イソプロテレノール，交感神経興奮薬で，β‐アドレナリン作動性受容体を興奮させる作用が強い。循環系に対しては，心臓の拍動数と収縮力を増大させ，末梢血管を拡張させる。平滑筋に対しては弛緩作用をもつが，気管支平滑筋でその作用はとくに顕著である。そのほか腸管，子宮などの運動も抑制する。血糖上昇作用はアドレナリンより弱いが，血中遊離脂肪酸上昇作用は同程度である。肝臓その他で主としてカテコール‐o‐メチルトランスフェラーゼによって代謝される。
  

• 用途

  β 受容体刺激薬気管支平滑筋を弛緩させる喘息治療薬

• 効能

  気管支拡張薬, βアドレナリン受容体作動薬

• 説明

  Isoproterenol is a representative of the sympathomimetic drugs with high selectivity to β- adrenoreceptors. As was already noted, the addition to compounds of a bulky iso-propyl or tert-butyl group at the nitrogen atom of the β-phenylethylamino skeleton is associated with higher affinity to β-adrenergic receptive regions than to α-adrenergic. Isoproterenol is devoid of significant α-adrenergic agonistic action. Activation of β1-adrenergic receptors in the heart increases positive chronotropic and ionotropic action. Peripheral vascular resistance is increased by the widening of blood vessels, primarily in skeletal muscle, but also in renal and mesenteric blood circulation, which is caused by the β2-adrenergic system.

• 使用

  Isoproterenol is used in bronchospasms, asthma, cardiac block, and shock.

• 定義

  ChEBI: A secondary amino compound that is noradrenaline in which one of the hydrogens attached to the nitrogen is replaced by an isopropyl group. A sympathomimetic acting almost exclusively on beta-adrenergic receptors, it is used (mainly as the hy rochloride salt) as a bronghodilator and heart stimulant for the management of a variety of cardiac disorders.

• 適応症

  Isoproterenol is administered almost exclusively by inhalation from metered-dose inhalers or from nebulizers. The response to inhaled isoproterenol and other inhaled adrenomimetics is instantaneous. The action of isoproterenol is short-lived, although an objective measurement of pulmonary function has shown an effective duration of up to 3 hours. When it is administered by inhalation, the cardiac effects of isoproterenol are relatively mild, although in some cases a substantial increase in heart rate occurs.

• 世界保健機関（WHO）

  Isoprenaline, a beta-adrenoreceptor agonist, was introduced in 1949 as treatment for a number of cardiac disorders and as a bronchial dilator for the symptomatic treatment of asthma. There is evidence that regular inhalation of bronchodilator drugs is associated, in some cases with exacerbation of the disease and with increased fatality rates. The underlying causes are disputed, but an increasing body of opinion now advocates regular maintenance therapy with inhaled, corticosteroids coupled with supplementary use as required of bronchial drugs to suppress exacerbations.

• 一般的な説明

  Isoproterenol is a nonselective and prototypical -agonist ( β2/ β1=1). After oral administration,the absorption of ISO is rather erratic and undependable.The principal reason for its poor absorption characteristicsand relatively short DOA is its facile metabolism by sulfateand glucuronide conjugation of the phenolic OH groupsand O-methylation by COMT. Because it is a catechol, it issensitive to light and air. Aqueous solutions become pinkon standing. Unlike E and NE, ISO does not appear to undergo oxidative deamination by MAO. The drug hasDOA of 1 to 3 hours after inhalation.

• 臨床応用

  Isoproterenol is used principally by inhalation for the management of bronchospasm. It is also used intravenously for asthma and as a stimulant in cardiac arrest.

• 安全性プロファイル

  Poison by ingestion, subcutaneous, intravenous, and intraperitoneal routes. An experimental teratogen. Other experimental reproductive effects. Human systemic effects by intramuscular route: increased pulse and cardac rate. A bronchodilator. Mutation data reported. When heated to decomposition it emits toxic fumes of NOx

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