イソプレナリン 化學(xué)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(dòng)性受容體を興奮させる作用が強(qiáng)い。循環(huán)系に対しては，心臓の拍動(dòng)數(shù)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(yùn)動(dòng)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 受容體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アドレナリン受容體作動(dòng)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.
適応癥
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(jī)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
イソプレナリン 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品