Hirota M, Ohtani H, Hanada E, Kotaki H, Sawada Y, Iga T
Department of Pharmacy, The University of Tokyo Hospital, Faculty of Medicine, The University of Tokyo, Japan.
Life Sci. 1998;62(24):2159-69. doi: 10.1016/s0024-3205(98)00193-3.
Plasma potassium concentration plays an important role in the induction of arrhythmia and is closely related to the arrhythmogenicity of various drugs. We quantitatively analyzed the influence of plasma potassium concentration on QT intervals before drug administration and on drug-induced QT prolongation, to estimate the risk of drug-induced arrhythmia under hypokalaemic conditions. The hypokalaemic models were produced by intraperitoneal administration of furosemide and hydrochlorothiazide in male Sprague-Dawley rats. The relationship between the changes in QT intervals and time profiles of plasma quinidine (QND) concentration were analyzed during constant intravenous infusion of QND (10 or 30 mg/kg/h) and post infusion in normal and hypokalaemic rats. The plasma QND concentration reached the therapeutic range (3-7 microg/ml) at the high infusion rate (30 mg/kg/h). No pharmacokinetic differences between normal and hypokalaemic rats were observed. QND induced QT prolongation in parallel with the plasma concentration without hysteresis. Although the potency of QND for QT prolongation was not affected by hypokalaemia, the QT intervals before drug administration were significantly prolonged in hypokalaemic rats (65.90 +/- 1.40 vs 56.60 +/- 0.748 msec, mean +/- SEM, p < 0.0001). Thus, the prolongation of QT intervals before drug administration may act as a risk factor of arrhythmia under hypokalaemic conditions.
血浆钾浓度在心律失常的诱发中起重要作用,且与各种药物的致心律失常性密切相关。我们定量分析了给药前血浆钾浓度对QT间期以及对药物诱导的QT延长的影响,以评估低钾血症情况下药物诱发心律失常的风险。通过对雄性Sprague-Dawley大鼠腹腔注射呋塞米和氢氯噻嗪建立低钾血症模型。在正常大鼠和低钾血症大鼠持续静脉输注奎尼丁(QND,10或30mg/kg/h)期间及输注后,分析QT间期变化与血浆QND浓度的时间曲线之间的关系。在高输注速率(30mg/kg/h)时,血浆QND浓度达到治疗范围(3 - 7μg/ml)。未观察到正常大鼠和低钾血症大鼠之间的药代动力学差异。QND诱导的QT延长与血浆浓度呈平行关系,无滞后现象。虽然低钾血症不影响QND延长QT的效能,但低钾血症大鼠给药前的QT间期显著延长(65.90±1.40 vs 56.60±0.748毫秒,平均值±标准误,p<0.0001)。因此,给药前QT间期的延长可能是低钾血症情况下心律失常的一个危险因素。