地高辛与其它药物合用的相互作用

地高辛(Digoxinum)是目前临床较常用的强心甙。由于与其它药物合用后,有的可产生协同作用,有的可出现不良反应。临床上往往将这种不良反应误认为是强心甙本身的毒性反应,实际上是合用药相互作用所致。本文对地高辛与其它药物的相互作用作如下综述。     

卡托普利对兔体内地高辛药动学的影响

<正>近几年来,血管紧张素转换酶抑制剂(ACEI)卡托普利(Captopril简CPT),常与地高辛合用,治疗充血性心力衰竭,获得了良好效果.有文献报道,CPT与地高辛合用后可显著提高地高辛的血药浓度;另有报道,加服CPT前后,地高辛血药浓度,两者间无显著性差异.为了合理用药,减少药物的毒副作用,本实验在无其他药物干扰的情况下,就CPT对地高辛的药代动力学的影响,用家兔进行研究,为临床更合理地用药,提供依据.     

卡托普利对充血性心衰患者地高辛血药浓度的影响

冠心病心衰患者１５例，每天服用地高辛０．１２５ｍｇ或０．２５ｍｇ，当血清地高辛浓度（ＳＤＣ）达稳态后，加服卡托普利８天。结果表明：卡托普利可增加ＳＤＣ血浓度２７％。地高辛总体，计内外清除率分别减少３０．１％、３５．５％和３５．４％。内生肌酐清除率减少３０．１％。由于ＳＤＣ升高的幅高较小，临床未见洋地黄毒副反应。     

地高辛与其他心血管药物的相互作用

地高辛与其他心血管药物的相互作用李世海王淑芳（山东省荣军医院济南２５００１３）在心血管病治疗中，地高辛常与其他药物合用，人们对地高辛与其他心血管药物的相互作用进行了广泛的研究和探讨，本文就所收集的资料作一简述。１奎尼丁［１］奎尼丁可改变地高辛的药动学...     

卡托普利地高辛联合治疗肺心病心衰135例分析

我院2000～2004年使用地高辛加卡托普利联合治疗肺心病心衰135例，效果较好。现报道如下：     

浅议地高辛与中药配伍的不良相互作用

通过对地高辛与一些中药配伍应用发生相互作用的归纳总结,避免多药并用后导致药源性疾病的发生。     

Changes in Steady State Digoxin Pharmacokinetics during Quinidine Therapy in Cardiac Patients: Influence of Plasma Quinidine Concentration

Abstract: In seven cardiac patients on long-term digoxin therapy, digoxin kinetics were investigated — in the absence and presence of quinidine — after simultaneous administration of an oral digoxin dose and an intravenous ³H-digoxin bolus injection. From ³H-digoxin data quinidine was found to decrease both renal (from 1.19 ±0.35 to 0.86 ±0.21 ml/min./kg) (P<0.02) and extrarenal clearances of digoxin (from 0.85 ±0.24 to 0.49±0.23 ml/min./kg) (P<0.02), and to diminish the steady state distribution volume of the drug (from 6.78 ± 1.23 to 5.63 ± 1.64 l/kg) (P<0.02). Plasma half-life increased from 51.5 ±5.4 to 64.4±14.8 hrs (P<0.05), while urinary excretion half-life increased from 54.4±3.9 to 78.5± 14.1 hrs (P<0.01). Pharmacokinetic parameters derived from plasma and urinary digoxin data showed similar changes during quinidine therapy. Reduction in renal ³H-digoxin clearance occurred at subtherapeutic plasma quinidine levels and was independent of plasma quinidine, whereas reductions in extrarenal ³H-digoxin clearance and ³H-digoxin distribution volume were positively correlated to plasma quinidine concentrations (P<0.05).     

中医辩证方联合卡托普利治疗老年性高血压病186例疗效观察

目的观察中医辩证方联合卡托普利治疗老年性高血压病的临床效果。方法将我院186例老年性高血压病患者分为观察组93例(中医辩证方联合卡托普利)和对照组93例(单用卡托普利),对两组患者治疗后的降压效果进行对比。结果患者治疗后收缩压、舒张压较治疗之前均得到改善,而观察组明显优于对照组(P<0.05);观察组患者治疗后的总有效率为(96%),高于对照组的(86%)(P<0.05)。结论采用中医辩证方联合卡托普利治疗高血压病效果更为明显。     

厄贝沙坦联合卡托普利治疗心力衰竭的疗效观察

目的：观察厄贝沙坦联合卡托普利治疗心力衰竭的临床效果。方法：将2007年10月--2010年10月我院心内科心力衰竭患者150-N,随机分为厄贝沙坦组、卡托普利组和联合用药组,并分别应用厄贝沙坦、卡托普利、厄贝沙坦＋卡托普利治疗。观察治疗后3组疗效及不良反应。结果：3组总有效率及不良反应比较,厄贝沙坦组与卡托普利组间无显著性差异（X^2=0．21,P〉0．05）,卡托普利组、厄贝沙坦组与联合用药组比较差异均有统计学意义（P〈O．05）。结论：厄贝沙坦联合卡托普利治疗心力衰竭,稳定性好,耐受性佳,可有效提高患者生活质量、改善其预后。     

Lack of a pharmacokinetic interaction between a new smoking cessation therapy,varenicline, and digoxin in adult smokers

Objective

This study investigated the effect of varenicline on the multiple-dose pharmacokinetics of digoxin.

Methods

Eighteen smokers were randomized to receive digoxin (Lanoxicaps® 0.2 mg QD) with varenicline 1 mg BID or placebo for 14 days.

Results

Varenicline had no clinically relevant effect on the digoxin steady-state exposure, as evidenced by the 90% confidence intervals for the ratios of AUC_0–24 (87.5–108%) and C_min (83.8–116%) wholly contained within 80–125%. Digoxin C_max and T_max remained unchanged in the presence of varenicline, consistent with no apparent alteration in digoxin bioavailability. A minimal 11.3% increase in digoxin renal clearance was noted during varenicline treatment while having no impact on its systemic exposure. Results are supported by mechanistic evidence in Caco-2 cell monolayers that varenicline is neither a P-gp substrate nor an inhibitor of P-gp-mediated efflux of digoxin. Co-administration of varenicline and digoxin was well tolerated.

Conclusion

The results suggest that digoxin can be safely administered with varenicline without the need for dose adjustment.

     

硝苯地平联合卡托普利治疗原发性高血压的临床观察

目的:观察硝苯地平联合卡托普利治疗原发性高血压的临床疗效。方法:将116例原发性高血压患者随机均分为治疗组和对照组,停用其他降压药2周以上,均调节降压饮食、合理化运动。对照组口服卡托普利治疗,治疗组在对照组的基础上口服硝苯地平控释片治疗,8周后进行疗效评价。结果:治疗组总有效率为89.7%;对照组总有效率为70.7%,治疗组明显高于对照组(P<0.05)。治疗组收缩压和舒张压均较对照组降低,2组比较差异有统计学意义(P<0.05)。结论:硝苯地平联合卡托普利治疗原发性高血压效果优于单用卡托普利。     

卡托普利与美托洛尔治疗慢性心力衰竭的疗效观察

目的：探讨卡托普利与美托洛尔治疗慢性心力衰竭（CHF）的临床效果。方法：将2009年1月～2010年1月在本院治疗的CHF患者68例随机分为观察组和对照组,对照组给予一般治疗措施,观察组在对照组的基础上给予卡托普利与美托洛尔治疗。结果：治疗后两组患者收缩压（SBP）、舒张压（DBP）、心率（HR）及射血分数（EF）均明显低于治疗前,两者比较,差异有统计学意义（P〈0.05）。治疗后观察组患者SBP、DBP、HR及EF明显低于对照组,两组比较,差异有统计学意义（P〈0.05）。观察组总有效率为85.29%,对照组为61.76%,两组比较,差异有统计学意义（P〈0.05）。两组患者均未见明显的药物不良反应。结论：卡托普利和美托洛尔治疗CHF疗效显著,可改善患者预后,值得应用。     

A possible interaction between linezolid and digoxin: A case report of therapeutic drug monitoring

Drug-drug interactions lead to altered clinical effects, including adverse reactions. Therapeutic drug monitoring of digoxin is necessary due to its narrow therapeutic range. Linezolid can cause variable exposures in patients hospitalized in the intensive care unit owing to its possibility of drug-drug interactions. We present a patient with pneumonia and heart failure who experienced a possible drug interaction between linezolid and digoxin, resulting in high serum concentrations of both drugs. Also, the patient developed thrombocytopenia likely related to linezolid. The linezolid dose required to maintain sufficient levels had to reduce to 50% of the usual linezolid dose. A quarter dose of the standard digoxin dose was needed. Although the underlying mechanism of the drug interaction is unclear, we recommend conducting therapeutic drug monitoring when linezolid and digoxin are administered concurrently.     

两种不同方案治疗糖尿病肾病疗效观察

目的:探讨两种不同方案治疗糖尿病肾病(DN)的临床效果.方法:将我院住院治疗的DN患者60例随机分为观察组和对照组,观察组给予缬沙坦联合卡托普利,对照组给予辛伐他汀联合卡托普利.结果:治疗后两组患者收缩压、舒张压及MAP明显优于治疗前,两组比较差异有统计学意义(P＜0.05).治疗后观察组患者收缩压、舒张压及MAP与对照组比较差异无统计学意义(P＞0.05).治疗后两组患者Scr、UAER明显优于治疗前,两组比较差异有统计学意义(P＜0.05).治疗后观察组患者Scr、UAER与对照组比较差异无统计学意义(P＞0.05).两组治疗过程中均未出现明显不良反应.结论:两种方案治疗DN效果基本相同,临床应合理选择应用.     

Effect of diprafenone on the pharmacokinetics of digoxin

This study was conducted to investigate the effect of diprafenone on the steady-state pharmacokinetics of digoxin. Twelve healthy men, all rapid hydroxylators of debrisoquine, received digoxin (0.5 mg per day over 7 days with a loading dose of 2 × 1 mg) or digoxin and diprafenone (3 × 100 mg per day) in three different phases, without a wash-out period (phase 1, digoxin alone; phase 2, digoxin + diprafenone; phase 3, digoxin alone). Blood and urine samples were collected for pharmacokinetic analyses. Diprafenone caused a statistically significant increase in digoxin trough concentrations [1.4 (SD 0.2) vs 1.6 (0.3) ng ⋅ml⁻¹], AUC_0–24 values [41 (7) vs 48 (9) ng⋅h⋅ml⁻¹ and C_ss-max [3.9 (0.6) vs 5.5 (0.9) ng⋅ml⁻¹]. In all volunteers the parameters tended to return to the original values after administration of diprafenone was discontinued [1.4 (0.3) ng⋅ml⁻¹, 39 (11) ng⋅h⋅ml⁻¹, and 3.9 (1.1) ng⋅ml⁻¹ for trough concentration, AUC_0–24 and C_max respectively]. The mean relative magnitude of the increase in AUC_0–24 and trough concentration values corresponded to the mean relative decrease in the renal clearance of digoxin (in both cases approximately 20%). This suggests that the increase in AUC and C_ss was caused by reduced renal clearance of digoxin. Received: 10 July 1995 /Accepted in revised form: 5 October 1995     

关于混杂效应、交互效应的探讨

目的:探讨在实际处理数据时对混杂效应、交互效应的处理方法。方法:通过具体实例说明混杂效应、交互效应的概念及正确应用。结果:判断变量间是否存在交互效应,需要在模型中纳入变量间的乘积项并通过统计学检验来评价;判断某变量是否为混杂因素,需比较模型中没有纳入该变量时得到的粗估计值与该变量纳入模型时得到的校正估计值的差别是否具有实际意义的不同,而不是通过统计学检验来评价;结论:在对数据进行统计分析时,当某变量可能与其它变量存在交互作用,同时又考虑其可能为混杂因素时,应先考虑其是否存在可能的交互作用,因为研究因素的效应随其他变量的取值不同而变化,如交互作用无统计学意义,进一步评价其是否为混杂因素。