Pop T, Treese N, Cremer G M, Haegele K D, Meyer J
Int J Cardiol. 1986 Aug;12(2):223-32. doi: 10.1016/0167-5273(86)90245-7.
MDL 17.043, a nonglycoside, noncatecholamine imidazolone derivative with phosphodiesterase inhibiting activity, has been shown to possess both positive inotropic and vasodilator properties. In the present study, the electrophysiological effects of intravenous MDL 17.043 were assessed in 10 patients undergoing programmed right atrial stimulation for diagnostic purposes. MDL 17.043 was administered as a single intravenous bolus injection of 1.5 mg/kg body weight over 4 min followed by an intravenous infusion of 0.75 mg/kg body weight over 20 min. With the dosage schedule used, the MDL 17.043 plasma levels achieved were similar to those previously reported to be associated with significant hemodynamic improvement of congestive heart failure. Electrophysiological measurements were performed before and during MDL 17.043 administration. MDL 17.043 consistently shortened basic sinus cycle length, sinus node recovery time and sinuatrial conduction time and decreased Wenckebach cycle length, atrioventricular and atrial refractoriness leading to positive chronotropic and dromotropic effects.
MDL 17.043是一种具有磷酸二酯酶抑制活性的非糖苷、非儿茶酚胺咪唑啉酮衍生物,已被证明具有正性肌力和血管舒张特性。在本研究中,对10名因诊断目的而接受程控右心房刺激的患者评估了静脉注射MDL 17.043的电生理效应。MDL 17.043以1.5 mg/kg体重的单次静脉推注在4分钟内给药,随后以0.75 mg/kg体重在20分钟内静脉输注。按照所使用的给药方案,所达到的MDL 17.043血浆水平与先前报道的与充血性心力衰竭显著血流动力学改善相关的水平相似。在MDL 17.043给药前和给药期间进行电生理测量。MDL 17.043持续缩短基础窦性周期长度、窦房结恢复时间和窦房传导时间,并缩短文氏周期长度、房室和心房不应期,导致正性变时和变传导效应。