Trenk D, Lühr A, Radkow N, Jähnchen E
Arzneimittelforschung. 1985;35(8):1286-8.
The effect of propranolol treatment on the steady-state plasma levels of ketanserin was evaluated in 6 patients suffering from borderline hypertension and in 2 healthy volunteers. All subjects received ketanserin 40 mg b.i.d. for 21 days. From day 8 to 14 of the study propranolol was given additionally in a dose of 80 mg bid. This dose of propranolol had to be reduced in 3 subjects because of side effects. Steady-state plasma concentrations (measured 4-6 h after the dose) of ketanserin varied from 51.0 +/- 13.6 to 67.8 +/- 13.8 ng/ml (mean +/- SEM) during the entire study period. Treatment with propranolol (plasma concentrations ranged from 45.7 +/- 15.8 to 65.7 +/- 11.4 ng/ml) did not significantly alter the plasma concentrations of ketanserin. The same was true for the minimal plasma concentrations of ketanserin measured at the end of each treatment period. Blood pressure decreased during the 21 days treatment period with ketanserin (mean systolic blood pressure decreased from 144 +/- 5 to 123 +/- 7 and diastolic from 81 +/- 3 to 72 +/- 5 mmHg). Propranolol had a slight additional hypotensive effect. Heart rate decreased during treatment with propranolol. It is concluded that simultaneous oral treatment with propranolol in doses up to 160 mg/day does not alter the first-pass metabolism and the elimination kinetics of ketanserin.
在6例临界高血压患者和2名健康志愿者中评估了普萘洛尔治疗对酮色林稳态血浆水平的影响。所有受试者每日两次服用40mg酮色林，共21天。在研究的第8天至14天，额外给予80mg bid的普萘洛尔。由于副作用，3名受试者不得不减少普萘洛尔的剂量。在整个研究期间，酮色林的稳态血浆浓度（给药后4 - 6小时测量）在51.0 +/- 13.6至67.8 +/- 13.8 ng/ml（平均值 +/- 标准误）之间变化。普萘洛尔治疗（血浆浓度范围为45.7 +/- 15.8至65.7 +/- 11.4 ng/ml）并未显著改变酮色林的血浆浓度。每个治疗期结束时测量的酮色林最低血浆浓度情况也是如此。在使用酮色林治疗的21天期间血压下降（平均收缩压从144 +/- 5降至123 +/- 7，舒张压从81 +/- 3降至72 +/- 5 mmHg）。普萘洛尔有轻微的额外降压作用。使用普萘洛尔治疗期间心率下降。结论是，每日口服剂量高达160mg的普萘洛尔同时治疗不会改变酮色林的首过代谢和消除动力学。
