Acebutolol Chemische Eigenschaften,Einsatz,Produktion Methoden
Chemische Eigenschaften
Crystalline Solid
Verwenden
Cardioselective ?adrenergic blocker. Antihypertensive; antianginal; antiarrhythmic (class II)
Definition
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.
Allgemeine Beschreibung
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.
Clinical Use
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.
Nebenwirkungen
Adverse effects include bradycardia, gastrointestinal
upset, dizziness, and headache.
Sicherheitsprofil
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
Stoffwechsel
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.
Vorsichtsmaßnahmen
Acebutolol should not be administered in cardiogenic
shock, uncontrolled heart failure, or severe bradycardia
or to patients with known hypersensitivity to the
drug.
Acebutolol Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
