アセブトロール 化学特性,用途語,生産方法
効能
抗不整脈薬, 血圧降下薬, 血管拡張薬, β1遮断薬
化学的特性
Crystalline Solid
使用
Cardioselective ?adrenergic blocker. Antihypertensive; antianginal; antiarrhythmic (class II)
定義
ChEBI: An ether that is the 2-acetyl-4-(butanoylamino)phenyl ether of the primary hydroxy group of 3-(propan-2-ylamino)propane-1,2-diol.
一般的な説明
Acebutolol is one of the very few β-blockers whosemetabolite plays a significant role in its pharmacological actions.This drug is absorbed well from the gastrointestinaltract, but it undergoes extensive first-pass metabolic conversionto diacetolol by hydrolytic conversion of the amidegroup to the amine, followed by acetylation of the amine. After oral administration, plasma levels of diacetololare higher than those of acebutolol. Diacetolol is also aselective β1-blocker with partial agonistic activity; it has littlemembrane-stabilizing activity. It has a longer half-life (8–12hours) than the parent drug and is excreted by the kidneys.
臨床応用
Acebutolol (Sectral) is a cardioselective 1-adrenoceptor
blocking agent that also has some minor membrane
stabilizing effects on the action potential. Acebutolol is effective in the management of the patient
with essential hypertension, angina pectoris, and ventricular
arrhythmias. Antiarrhythmic effects are observed
with the patient both at rest and taking exercise.
副作用
Adverse effects include bradycardia, gastrointestinal
upset, dizziness, and headache.
安全性プロファイル
Moderately toxic by intravenousroute. Human systemic effects by ingestion: developmentalabnormalities of the cardiovascular and respiratory systems;effects on newborn in biochemical and metabolicabnormalities and reduced growth statistics. A humanter
代謝
About half of an orally administered dose of acebutolol
(Sectral) is absorbed. Approximately 25% of the
drug is bound to plasma proteins, and its plasma halflife
is about 4 hours.Metabolism of acebutolol produces
a metabolite with -blocking activity whose half-life is
10 hours.
予防処置
Acebutolol should not be administered in cardiogenic
shock, uncontrolled heart failure, or severe bradycardia
or to patients with known hypersensitivity to the
drug.
アセブトロール 上流と下流の製品情報
原材料
準備製品