アミオダロン 化学特性,用途語,生産方法
効能
抗不整脈薬, カリウムチャネル遮断薬
説明
From the chemical point of view, amiodarone is completely different from other antiarrhythmics.
It has two iodide atoms and a diethylaminoethanol group as substituents in the
benzoyl part, and overall it is very similar to the structure of thyroxin-like molecules.
使用
antibacterial
定義
ChEBI: A member of the class of 1-benzofurans that is 1-benzofuran substituted by a butyl group at position 2 and a 4-[2-(diethylamino)ethoxy]-3,5-diiodobenzoyl group at position 3. It is a cardiovascular drug used for the treatment of cardiac dysrhythmias.
適応症
Clinical use of amiodarone is limited because of its high toxicity, which consists of cardiac
block, bradycardia, cardiac insufficiency, damaged thyroid gland function, neuropathology,
and increased sensitivity to light, all of which significantly limit use of
amiodarona, and it is only used in therapy for extremely serious tachyarrhythmias such as
reoccurring ventricular fibrillation and hemodynamic unstable ventricular tachycardia, and
only under supervision of a physician in a clinical situation.
生物学の機能
Amiodarone (Cordarone) is an iodine-containing benzofuran
derivative identified as a class III agent because it
predominantly prolongs action potentials. Amiodarone
also blocks sodium and calcium channels and is a noncompetitive
β-receptor blocker.Amiodarone is effective
for the treatment of most arrhythmias. Toxicity associated
with amiodarone has led the U. S. Food and Drug
Administration (FDA) to recommend that it be reserved
for use in patients with life-threatening arrhythmias.
一般的な説明
Amiodarone, 2-butyl-3-benzofuranyl-4-[2-(diethylamino)ethoxy]-3,5-diiodophenyl ketone (Cordarone),was introduced as an antianginal agent. It has very pronouncedclass III action and is especially effective in maintainingsinus rhythm in patients who have been treated bydirect current shock for atrial fibrillation. Like class IIIantiarrhythmic drugs, amiodarone lengthens the effective refractoryperiod by prolonging the action potential duration inall myocardial tissues. Amiodarone is eliminated very slowlyfrom the body, with a half-life of about 25 to 30 days after oraldoses. Although the drug has a broad spectrum of antiarrhythmicactivity, its main limitation is a slow onset of action.Drug action may not be initiated for several days, and thepeak effect may not be obtained for several weeks.
作用機序
Amiodarone’s antiarrhythmic action is connected to its ability to block K, Na, and
Ca2 channels while noncompetitively blocking α- and β-adrenergic receptors of the heart,
thus prolonging the action potential and effective refractive period of atrial cells, atrioventricular
junctions, and ventricles of the heart, which is accompanied by decreased automatism
of sinus node and slowing of atrioventricular conductivity.
臨床応用
Amiodarone has adverse effects involving many differentorgan systems. It also inhibits metabolism of drugscleared by oxidative microsomal enzymes. It contains iodinein its molecular structure and, as a result, has an effecton thyroid hormones. Hypothyroidism occurs in up to 11%of patients receiving amiodarone. The principal effect isthe inhibition of peripheral conversion of T4 to T3. Serumreverse T3 (rT3) is increased as a function of the dose as wellas the length of amiodarone therapy. As a result, rT3 levelshave been used as a guide for judging adequacy of amiodaronetherapy and predicting toxicity.
安全性プロファイル
Poison by intravenous and intraperitoneal routes. Human systemic effects by ingestion: photosensitivity of the skin. A flammable liquid. When heated to decomposition it emits very toxic fumes of Iand NO,. A coronary vasoddator
薬物相互作用
Amiodarone increases the hypoprothrombinemic response
to warfarin (an oral anticoagulant) by reducing
its metabolism. Patients receiving digoxin may undergo
an increase in serum digoxin concentrations when
amiodarone is added to the treatment regimen.
Amiodarone interferes with hepatic and renal elimination
of flecainide, phenytoin, and quinidine.
予防処置
Amiodarone is contraindicated in patients with sick sinus
syndrome and may cause severe bradycardia and secondand
third-degree atrioventricular block. Amiodarone
crosses the placenta and will affect the fetus, as evidenced
by bradycardia and thyroid abnormalities. The
drug is secreted in breast milk.
アミオダロン 上流と下流の製品情報
原材料
準備製品