ソタロール 化学特性,用途語,生産方法
効能
抗不整脈薬, β遮断薬, カリウムチャネル遮断薬
定義
ChEBI: A sulfonamide that is N-phenylmethanesulfonamide in which the phenyl group is sustituted at position 4 by a 1-hydroxy-2-(isopropylamino)ethyl group. It has both beta-adrenoreceptor blocking (Vaughan Williams Class II) and
ardiac action potential duration prolongation (Vaughan Williams Class III) antiarrhythmic properties. It is used (usually as the hydrochloride salt) for the management of ventricular and supraventricular arrhythmias.
世界保健機関（WHO）
Sotalol is a non-selective?-adrenoreceptor antagonist. It should
be noted that when stopping sotalol the dose should be reduced gradually.
一般的な説明
Sotalol, 4＇[1-hydroxy-2-(isopropylamino)ethyl]methylsulfonanilide (Betapace), is a relatively new antiarrhythmicdrug, characterized most often as a class IIIagent, and although it has effects that are related to the classII agents, it is not therapeutically considered a class II antiarrhythmic.It contains a chiral center and is marketed as theracemic mixture. Because of its enantiomers, its mechanismof action spans two of the antiarrhythmic drug classes. Thel(-) enantiomer has both β-blocking (class II) and potassiumchannel-blocking (class III) activities. The d(+) enantiomerhas class III properties similar to those of the (-) isomer,but its affinity for the -adrenergic receptor is 30 to 60 timeslower.
臨床応用
The sotalol enantiomers produce different effects onthe heart. Class III action of d-sotalol in the sinus node isassociated with slowing of sinus heart rate, whereas -adrenergicblockade contributes to the decrease in heart rate observedwith 1- or d,1-sotalol. Sotalol is not metabolized, noris it bound significantly to proteins. Elimination occurs byrenal excretion, with more than 80% of the drug eliminatedunchanged. Sotalol is characteristic of class III antiarrhythmicdrugs, in that it prolongs the duration of the action potentialand, thus, increases the effective refractory period of myocardialtissue. It is distinguished from the other class III drugs(amiodarone and bretylium) because of its -adrenergicreceptor–blocking action.
副作用
Side effects of sotalol include those attributed to both
β-adrenoceptor blockade and proarrhythmic effects.
This arrhythmia is a serious threat, as it may lead to ventricular
fibrillation. Adverse effects attributable to its β-
blocker activity include fatigue, dyspnea, chest pain,
headache, nausea, and vomiting.
薬物相互作用
Drugs with inherent QT interval–prolonging activity
(i.e., thiazide diuretics and terfenadine) may enhance
the class III effects of sotalol.
予防処置
The contraindications that apply to other β-adrenoceptor
blocking agents also apply to sotalol. In addition, hypokalemia
and drugs known to prolong the QT interval
may be contraindicated, as they enhance the possibility
of proarrhythmic events.
ソタロール 上流と下流の製品情報
原材料
準備製品