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心得安在临床上主要用于冠心病、高血压、心律失常等,目前国内仅有片剂和针剂两种剂型。口服心得安片生物利用度很低,服用小剂量时只有极少量能进入体循环。增大剂量,如3.2mg/kg口服,其生物利用度有所改善,但也仅为32%。由于个体生物可利用性的差异,口服后血药浓度的个体差异也相当大,据文献报道,5个自愿者口服80mg心得安后,他们的血药浓度最高和最低相差竟达7倍,而这5个人分别静脉注射10mg心得安后,其血药浓度最高的和最低仅相差2倍。这就造成了临床用药的麻烦,需要逐步增加剂量,以达到有效血药浓度。同时随着剂量的增大。其副作用也在增加,副作用的发生率可达9.9%。而静脉用药又比较麻烦,非急救一般不采用此法给药
Clinical experience mainly in coronary heart disease, hypertension, arrhythmia, the current domestic only tablets and injections two formulations. Oral propofol tablets bioavailability is very low, taking only a very small dose can enter the systemic circulation. Increased doses, such as oral 3.2mg / kg, improved its bioavailability, but only 32%. Due to differences in individual bioavailability, individual differences in plasma concentrations after oral administration are also quite large. According to the literature, after 5 doses of 80 mg of propofol were orally administered to 5 volunteers, the difference between their maximum and minimum plasma concentrations was as much as 7 times, These five individuals were intravenous injection of 10mg after the security, the highest and lowest plasma concentrations of only a difference of 2 times. This has caused the trouble of clinical medication, need to gradually increase the dose, in order to achieve effective plasma concentration. At the same time as the dose increases. The side effects are also increasing, the incidence of side effects up to 9.9%. The intravenous medication and more trouble, non-emergency treatment is generally not used this method