アルブテロール 化学特性,用途語,生産方法
用途
サルブタモール(Salbutamol)は短時間作用性β2アドレナリン受容体刺激剤であり、喘息や慢性閉塞性肺疾患における気管支痙攣のリリーフに使われる。米国ではアルブテロール(米国一般名Albuterol)と呼ばれる。
サルブタモールは世界中でもっともよく処方されている気管支拡張剤であり、吸入(定量噴霧式吸入器、ネブライザー)、経口(錠剤、シロップ)の形で投薬される。
サルブタモールは気管支平滑筋のほかに、子宮平滑筋も弛緩させるため、早産防止のために静脈注射で投与されることもある(日本では用法外)。また、β刺激剤の副作用として脂肪燃焼、骨格筋増強の効果があり、海外ではダイエットやボディビルディングの目的でサルブタモールの錠剤が使用されることもある。
効能
気管支拡張薬, β2アドレナリン受容体作動薬
説明
Albuterol is a β2-adrenergic sympathomimetic amine with pharmacological similarities to
terbutaline. It has almost no effect on β1-adrenoreceptors of the heart. It has expressed
broncholytic effects—prevention or relief of bronchi spasms, lowering respiratory tract
resistance, and increasing the vital capacity of the lungs.
化学的特性
solid
使用
immune suppressant, antineoplastic, antiviral
定義
ChEBI: A member of the class of phenylethanolamines that is 4-(2-amino-1-hydroxyethyl)-2-(hydroxymethyl)phenol having a tert-butyl group attached to the nirogen atom. It acts as a beta-adrenergic agonist used in the treatment of asthma
and chronic obstructive pulmonary disease (COPD).
生物学の機能
Levalbuterol is the R-(–)-isomer of albuterol and is available only in solution to be administered via nebulizer. Because it is the active isomer, the dose is fourfold less than that of albuterol. Pirbuterol is the pyridine isostere of albuterol. It has pharmacokinetics similar to albuterol but is half as potent at the β2-receptor. Pirbuterol is only available as an inhaler, whereas albuterol comes in tablet, syrup, solution, and aerosol formulations.
一般的な説明
Standard for Supelco MIP SPE cartridges. For more information request Supelco Literature T407075, T706019, T706030, T706020. Salbutamol is classified under the β-agonist group of chemicals which are known to possess powerful pharmacological activities.
臨床応用
Albuterol has the N-t-butyl and a salicyl alcohol phenyl ring, which gives it optimal β2-selectivity. It is resistant to COMT and slowly metabolized by MAO, giving it good oral bioavailability. Its onset by inhalation is within 5 minutes, with a duration of action between 4 and 8 hours. It currently is the drug of choice for relief of the acute bronchospasm of an asthmatic attack.
副作用
Adverse effects of pirbuterol are nervousness, tremor, and headache, which is less than the profile for albuterol, which adds nausea, vomiting, dizziness, hypertension, insomnia, tachycardia, and palpitations.
環境運命予測
Tachycardia occurs as a reflex to the drop in mean arterial
pressure (MAP) or as a result of b-1 stimulus. b-Adrenergic
receptors in the locus coeruleus also regulate norepinephrineinduced
inhibitory effects, resulting in agitation, restlessness,
and hand tremor. Stimulation of nonpulmonary b2 receptors
may lead to an increase in heart rate, QTc interval prolongation,
nonspecific T-wave changes, skeletal muscle tremor, and slight
increases in blood glucose and nonesterified fatty acids. Hypokalemia
is more pronounced in patients receiving intravenous
albuterol. Hypotension is also known to occur mostly in overdose.
The buildup of cyclic AMP in the liver stimulates glycogenolysis
and an increase in serum glucose.
In skeletal muscle, this process results in increased lactate
production. Direct stimulus of sodium/potassium ATPase in
skeletal muscle produces a shift of potassium from the extracellular
space to the intracellular space. Relaxation of smooth
muscle produces a dilation of the vasculature supplying skeletal
muscle, which results in a drop in diastolic and MAP.Myocardial ischemia and infarction have been associated with
excessive tachycardia in elderly patients. The skin may be warm
and pink with evidence of diaphoresis.
アルブテロール 上流と下流の製品情報
原材料
準備製品