Langsteger W, Lind P, Eber O
Wien Med Wochenschr. 1985 Sep 30;135(18):451-7.
In series of 20 patients suffering from atrial arrhythmias, hypertension or hyperkinetic heart syndrome in euthyroid subjects the effect of the new cardioselective beta-blocker celiprolol was examined when orally administered in doses of 300 mg per day against propranolol in a dosage of 160 mg per day. Celiprolol caused a significant reduction (p less than 0.01) of both systolic and diastolic blood pressure while propranolol showed simply a marked decrease in systolic blood pressure. A significant decrease in heart rate was observed with both drugs (p less than 0.01). TT3 and TT4 decreased only slightly when administering either celiprolol or propranolol. A further not significant drop in FT4 due to celiprolol is contrasted to a similarly not significant increase in FT4 when administering propranolol. A striking decrease in FT3 was induced by both drugs, although in the case of celiprolol this reduction became apparent only within a period of 3 weeks. Since only in cases of hyperthyroidism the number of beta-receptors has increased, the reduction of 5'deiodinase is possibly not so pronounced in euthyroidism. In this way an explanation may be found for a mild inhibition of conversion and a consequently missing increase in RT3. Neither celiprolol nor propranolol caused significant changes of laboratory findings, especially when considering triglycerides and creatinine values. Side effects could be lessened in nearly all cases and deterioration was not observed so that therapy never had to be discontinued. Celiprolol has to be considered as a further favourable cardioselective beta-blocker with intrinsic sympathicomimetic activity, causing a reasonable reduction in blood pressure and heart rate and moreover a propranolol-like effect in the peripheral metabolism of thyroid hormones in euthyroid patients.
在一组20例患有房性心律失常、高血压或甲状腺功能正常的高动力性心脏综合征患者中,研究了新型心脏选择性β受体阻滞剂塞利洛尔(每天口服300毫克)相对于普萘洛尔(每天160毫克)的效果。塞利洛尔使收缩压和舒张压均显著降低(p<0.01),而普萘洛尔仅使收缩压明显下降。两种药物均使心率显著降低(p<0.01)。服用塞利洛尔或普萘洛尔时,TT3和TT4仅略有下降。塞利洛尔导致FT4进一步非显著下降,与之形成对比的是,服用普萘洛尔时FT4有类似的非显著升高。两种药物均引起FT3显著下降,不过塞利洛尔的这种下降仅在3周内才明显。由于仅在甲状腺功能亢进的情况下β受体数量增加,在甲状腺功能正常时5'-脱碘酶的降低可能不那么明显。这样或许可以解释为何转化受到轻度抑制且RT3没有相应升高。塞利洛尔和普萘洛尔均未引起实验室检查结果的显著变化,尤其是在考虑甘油三酯和肌酐值时。几乎在所有情况下副作用都可减轻,未观察到病情恶化,因此治疗从未被迫中断。塞利洛尔必须被视为一种更有利的具有内在拟交感活性的心脏选择性β受体阻滞剂,它能合理降低血压和心率,而且在甲状腺功能正常的患者中对甲状腺激素的外周代谢有类似普萘洛尔的作用。