Follath F
Department of Internal Medicine, University Hospital Zürich, Switzerland.
J Cardiovasc Pharmacol. 1992;20 Suppl 2:S41-3.
Serum drug level monitoring facilitates dosage optimization of agents with a narrow therapeutic index. Concentration-dependent antiarrhythmic and toxic effects have been demonstrated for several class I drugs, whereas the concentration-effect relationships of class III antiarrhythmics are less well established. The efficacy and toxicity of amiodarone, in particular, may be determined more by extensive tissue deposition than by its serum concentration. Furthermore, accumulation of the active metabolite desethylamiodarone seems to play an additional role. The antiarrhythmic serum concentration range of sotalol is wide; monitoring is not required. The clinical utility of serum concentration measurements with the newly developed class III antiarrhythmic agents remains to be evaluated in properly planned therapeutic trials in patients with supraventricular and ventricular arrhythmias.
血清药物浓度监测有助于优化治疗指数狭窄药物的剂量。已证实几种I类药物具有浓度依赖性抗心律失常和毒性作用,而III类抗心律失常药物的浓度-效应关系尚不明确。特别是胺碘酮的疗效和毒性可能更多地取决于其在组织中的广泛沉积,而非血清浓度。此外,活性代谢产物去乙基胺碘酮的蓄积似乎也起了额外作用。索他洛尔的抗心律失常血清浓度范围较宽,无需进行监测。新型III类抗心律失常药物血清浓度测定的临床实用性仍有待在针对室上性和室性心律失常患者的适当规划治疗试验中进行评估。