目的评估替利定治疗腰椎间盘突出症合并神经根性疼痛的疗效和安全性。方法连续将94例接受髓核摘除术的腰椎间盘突出症合并神经根性疼痛患者,以1∶1随机分为替利定(T)组和氨酚羟考酮(O)组。T组患者于术前2 h及术后4、10、16 h予盐酸替利...目的评估替利定治疗腰椎间盘突出症合并神经根性疼痛的疗效和安全性。方法连续将94例接受髓核摘除术的腰椎间盘突出症合并神经根性疼痛患者,以1∶1随机分为替利定(T)组和氨酚羟考酮(O)组。T组患者于术前2 h及术后4、10、16 h予盐酸替利定口服溶液100 mg,po;O组患者于同一时间予氨酚羟考酮片(每片包含羟考酮5 mg+对乙酰氨基酚325 mg)1片,po。于术前和术后24 h以内评估患者疼痛视觉模拟评分(VAS),患者整体状态(PGA)评分,使用哌替啶的人数、用量以及不良反应。结果 T组患者在术后12和24 h VAS评分(2.7±1.8 vs 3.6±1.5;2.4±1.4 vs 3.1±1.5)和PGA评分(3.3±1.9 vs 4.1±1.8;2.7±1.5 vs 3.5±1.7)均显著低于O组患者(P<0.05)。同时,T组患者因出现难以忍受的疼痛而使用哌替啶进行解救的患者比例显著低于O组患者(8.5%vs 23.4%,P=0.049)。此外,2组患者出现不良反应如恶心、便秘、呕吐、嗜睡和头晕的比例之间差异均无统计学意义(P>0.05)。结论替利定治疗腰椎间盘突出症合并神经根性疼痛疗效优于氨酚羟考酮,而安全性与氨酚羟考酮相当。展开更多
This study was conducted to assess the pharmacokinetic characteristics of tilidine and its active metabolites nortilidine in healthy Chinese male and female volunteers. Nine healthy volunteers （4 male and 5 female） ...This study was conducted to assess the pharmacokinetic characteristics of tilidine and its active metabolites nortilidine in healthy Chinese male and female volunteers. Nine healthy volunteers （4 male and 5 female） were included in the study. Subjects were administered a single oral dose 50 mg tilidine hydrochloride oral solution. The plasma tilidine and nortilidine concentrations were determined by gas chromatography nitrogen phosphorous detection （GC-NPD）. The pharmacokinetic parameters were estimated from plasma concentration-time profiles using model independent method. The main pharmacokinetic data （mean4-SD） for tilidine and nortilidine were Cmax （63.39±28.99） and （122.53±23.23） ng/mL; Tmax （0.37±0.07） and （0.64±0.30） h; t1/2 （2.83±1.35） and （5.72±1.37） h; A UC0-∞ （101.59±41.85） and （577.13±189.77） ng.h/mL, respectively. The mean pharmacokinetic parameters for male and female were as follows： for tilidine： Cmax （73.88±40.88） and （55.014-15.16） ng/mL, Tmax （0.37±0.08） and （0.36±0.08） h, tl/2 （4.05±1.07） and （1.86±0.41） h, AUC0-∞ （119.004-55.11） and （87.66∞26.08） ng.h/mL; for nortilidine： Cmax （108.824-27.88） and （133.49-4-12.56） ng/mL, Tmax （0.94±0.13） and （0.40±0.09） h, t1/2 （4.66±1.18） and （6.57±0.84） h, AUC0-∞ （601.59±281.07） and （557.57±108.16） ng.h/mL. The t1/2 for tilidine in male was significantly higher than that in female, while Tmax for nortilidine in male was significantly higher than that in female. There was no serious adverse effects, but significant difference in the incidence of adverse effects was found between male and female. There was no sufficient pharmacokinetic reason to adjust the dose of tilidine when it was administered in Chinese patients.展开更多
文摘目的评估替利定治疗腰椎间盘突出症合并神经根性疼痛的疗效和安全性。方法连续将94例接受髓核摘除术的腰椎间盘突出症合并神经根性疼痛患者,以1∶1随机分为替利定(T)组和氨酚羟考酮(O)组。T组患者于术前2 h及术后4、10、16 h予盐酸替利定口服溶液100 mg,po;O组患者于同一时间予氨酚羟考酮片(每片包含羟考酮5 mg+对乙酰氨基酚325 mg)1片,po。于术前和术后24 h以内评估患者疼痛视觉模拟评分(VAS),患者整体状态(PGA)评分,使用哌替啶的人数、用量以及不良反应。结果 T组患者在术后12和24 h VAS评分(2.7±1.8 vs 3.6±1.5;2.4±1.4 vs 3.1±1.5)和PGA评分(3.3±1.9 vs 4.1±1.8;2.7±1.5 vs 3.5±1.7)均显著低于O组患者(P<0.05)。同时,T组患者因出现难以忍受的疼痛而使用哌替啶进行解救的患者比例显著低于O组患者(8.5%vs 23.4%,P=0.049)。此外,2组患者出现不良反应如恶心、便秘、呕吐、嗜睡和头晕的比例之间差异均无统计学意义(P>0.05)。结论替利定治疗腰椎间盘突出症合并神经根性疼痛疗效优于氨酚羟考酮,而安全性与氨酚羟考酮相当。
基金Major Project of National Science&Technology (Grant No.2009ZX09301-010)
文摘This study was conducted to assess the pharmacokinetic characteristics of tilidine and its active metabolites nortilidine in healthy Chinese male and female volunteers. Nine healthy volunteers （4 male and 5 female） were included in the study. Subjects were administered a single oral dose 50 mg tilidine hydrochloride oral solution. The plasma tilidine and nortilidine concentrations were determined by gas chromatography nitrogen phosphorous detection （GC-NPD）. The pharmacokinetic parameters were estimated from plasma concentration-time profiles using model independent method. The main pharmacokinetic data （mean4-SD） for tilidine and nortilidine were Cmax （63.39±28.99） and （122.53±23.23） ng/mL; Tmax （0.37±0.07） and （0.64±0.30） h; t1/2 （2.83±1.35） and （5.72±1.37） h; A UC0-∞ （101.59±41.85） and （577.13±189.77） ng.h/mL, respectively. The mean pharmacokinetic parameters for male and female were as follows： for tilidine： Cmax （73.88±40.88） and （55.014-15.16） ng/mL, Tmax （0.37±0.08） and （0.36±0.08） h, tl/2 （4.05±1.07） and （1.86±0.41） h, AUC0-∞ （119.004-55.11） and （87.66∞26.08） ng.h/mL; for nortilidine： Cmax （108.824-27.88） and （133.49-4-12.56） ng/mL, Tmax （0.94±0.13） and （0.40±0.09） h, t1/2 （4.66±1.18） and （6.57±0.84） h, AUC0-∞ （601.59±281.07） and （557.57±108.16） ng.h/mL. The t1/2 for tilidine in male was significantly higher than that in female, while Tmax for nortilidine in male was significantly higher than that in female. There was no serious adverse effects, but significant difference in the incidence of adverse effects was found between male and female. There was no sufficient pharmacokinetic reason to adjust the dose of tilidine when it was administered in Chinese patients.
