Effects of lansoprazole on pharmacokinetics and metabolism of theophylline

The effect of the new substituted benzimidazole proton pump inhibitor, lansoprazole, on pharmacokinetics and metabolism of theophylline has been studied in healthy adults given oral lansoprazole 30 mg once daily for 11 days. On Days 4 and 11 of 300 mg aminophylline was simultaneously administered orally and blood samples for theophylline analysis were taken over 24 h. Urine samples were collected for up to 24 h and were assayed for theophylline and its major metabolites 1,3-dimethyluric acid (1,3-DMU), 1-methyluric acid (1-MU) and 3-methylxanthine (3-MX). The pharmacokinetic parameters of theophylline were determined, and the urinary recovery of unchanged theophylline and its major metabolites were calculated.After administration of lansoprazole for 4 days, no significant alteration in the terminal elimination half-life (t _1/2) or the mean residence time (MRT) was detected. However, there was a significant decrease of about 13% in the area under the plasma concentration-time curve (AUC) and a significant increase of about 19% in the apparent clearance (CL_app). Lansoprazole treatment for 11 days caused a significant decrease of approximately 12% in t _1/2 and about 10% in the MRT of theophylline, although neither AUC nor CL_app showed a significant alteration. The excretion of 3-MX in the urine was significantly increased by about 20% after lansoprazole treatment for 4 and 11 days, although there was no significant alteration in the excretion of unchanged theophylline, 1,3-DMU or 1-MU.The results indicate that repeated administration of lansoprazole to humans induces the hepatic microsomal P-450-dependent drug oxidation system that mediates N-1-demethylation of theophylline, consequently increasing its metabolism.     

Randomized Trial of Interferon-Alpha plus Ursodeoxycholic Acid versus Interferon plus Placebo in Patients with Chronic Hepatitis C Resistant to Interferon

Background: Ursodeoxycholic acid (UDCA) could potentiate the effect of interferon (IFN) in patients with chronic hepatitis C resistant to IFN. We compared the efficacy of IFN with that of a combination of IFN and UDCA. Methods: Patients were randomized to receive UDCA (13-15 mg/kg/day) (n = 47) or placebo (n = 44) plus interferon (3 MU three times weekly) for 6 months and were then followed up for 6 additional months. Results: At entry 30% of patients had cirrhosis, and 70% had HCV genotype 1. Five and four patients withdrew from the combination and the monotherapy groups, respectively. At 6 months alanine aminotransferase (ALAT) and gamma-glutamyl transferase (GGT) activities were significantly lower (P < 0.001) in the combination group than in the monotherapy group; the differences were no longer significant at 1 year. At 6 months ALAT activities normalized in 10 and 8 patients in the combination and the monotherapy groups, respectively (P = 0.67). In 10 of them (5 in each group) HCV RNA levels became undetectable. At 1 year four versus one patient had a sustained normalization of ALAT, and in one patient the HCV RNA became negative. There was no difference in the histologic progression. In this setting, in contrast to chronic cholestasis, UDCA administration induced an increase in total serum bile acids and did not change primary bile acids. Conclusions: An IFN plus UDCA combination is more effective than IFN alone in terms of ALAT but not in terms of the virologic response. These results favor the hypothesis that UDCA has an effect on the biochemical indices of cellular injury independent of a change in primary bile acids.     

兰索拉唑治疗慢性胃溃疡的效果及用药不良反应评价

目的评价兰索拉唑治疗慢性胃溃疡的效果及用药不良反应。方法100例慢性胃溃疡患者,通过随机数字编号分为对照组与研究组,每组50例。对照组给予奥美拉唑肠溶片治疗,研究组采用兰索拉唑肠溶胶囊治疗,比较两组生活质量评分、治疗效果、不良反应(腹泻、头痛)发生情况。结果治疗后,研究组生活质量评分(80.32±2.33)分高于对照组的(73.31±3.21)分,差异具有统计学意义(P<0.05)。研究组治疗总有效率96.00%高于对照组的84.00%,差异具有统计学意义(P<0.05)。研究组不良反应发生率4.00%低于对照组的16.00%,差异具有统计学意义(P<0.05)。结论兰索拉唑治疗慢性胃溃疡的临床效果显著,可以有效降低患者的用药后不良反应发生率,能够改善患者的生活质量水平。     

泮托拉唑与兰索拉唑治疗Hp感染活动性胃溃疡的成本-效果分析

目的:探讨泮托拉唑与兰索拉唑治疗幽门螺旋杆菌(Hp)感染活动性胃溃疡的成本-效果。方法:从本院2013年12月至2014年12月收治的Hp感染活动性胃溃疡患者中选择89例进行研究,按照治疗方法随机分为泮托拉唑组(45例)和兰索拉唑组(44例)。观察两组的药物经济学成本-效果,并进行比较。结果:泮托拉唑组和兰索拉唑组的临床总治愈率为82.22%和81.82%,(P>0.05)。泮托拉唑组和兰索拉唑组的药物经济学成本-效果比为4.74和5.62,(P<0.05)。结论:较之兰索拉唑,泮托拉唑治疗Hp感染活动性胃溃疡患者进行治疗可以获得更好的成本-效果,具有更高的药物经济学价值。     

胃得安胶囊联合兰索拉唑治疗胃溃疡的临床研究

目的探讨胃得安胶囊联合兰索拉唑治疗胃溃疡的临床效果。方法选取2016年7月—2018年7月天津市第五中心医院收治的胃溃疡患者96例,随机分成对照组(48例)和治疗组(48例)。对照组早餐前30 min口服兰索拉唑肠溶胶囊,30 mg/次,1次/d。治疗组在对照组基础上口服胃得安胶囊,2粒/次,3次/d。两组患者均连续治疗6周。观察两组患者临床疗效,同时比较治疗前后两组患者上腹痛评分、反酸评分、前列腺素(PG)E2、C反应蛋白(CRP)、白介素-17(IL-17)、超氧化物歧化酶(SOD)和脂质过氧化物(LPO)水平以及幽门螺杆菌根除率、溃疡愈合率及复发率。结果治疗后,对照组临床有效率为87.5%,显著低于治疗组的100.0%,两组比较差异有统计学意义(P0.05)。治疗后,两组患者中上腹痛评分和反酸评分均显著降低(P0.05),且治疗组患者中上腹痛评分和反酸评分明显低于对照组(P0.05)。治疗后,两组患者胃液中PGE2浓度及血清SOD水平均显著升高(P0.05),血清CRP、IL-17、LPO浓度则均显著降低(P0.05),且治疗组患者这些指标水平明显好于对照组(P0.05)。治疗后,治疗组幽门螺杆菌根除率、溃疡愈合率分别为93.8%、75.0%,均显著高于对照组(P0.05)。随访6个月,治疗组复发率为8.3%,比对照组的25%明显显著降低(P0.05)。结论胃得安胶囊联合兰索拉唑治疗胃溃疡的整体疗效切实,促进溃疡愈合,增强胃黏膜的防御功能及机体的抗氧化能力。     

不同剂量奥曲肽联合兰索拉唑治疗肝硬化合并上消化道出血疗效及安全性评价

目的评价不同剂量奥曲肽联合兰索拉唑治疗肝硬化合并上消化道出血疗效及安全性。方法 2013年5月-2016年5月收治的80例肝硬化合并上消化道出血患者均予奥曲肽联合兰索拉唑治疗,根据奥曲肽的剂量不同分为大剂量组（40例）与小剂量组（40例）,治疗前后分别彩超测定门静脉平均流速（PVV）与门静脉内径（PVD）,记录止血时间、输血例数、输血量及再出血例数,观察不良反应。结果治疗后2组PVV与PVD均明显改善（P<0.05）,组间比较无明显差异。大剂量组止血时间、输血率、输血量及再出血率均明显少于小剂量组（P<0.05）。大剂量组总有效率为90.0%,小剂量组为70.0%,两组比较差异显著（P<0.05）。大剂量组不良反应发生率与小剂量组无明显差异。结论大剂量奥曲肽联合兰索拉唑治疗肝硬化合并上消化道出血对止血作用有增益,且不会明显增加不良反应。     

荜铃胃痛颗粒联合兰索拉唑治疗慢性浅表性胃炎的临床研究

目的探讨荜铃胃痛颗粒联合兰索拉唑治疗慢性浅表性胃炎的安全性和有效性。方法选取2017年7月—2018年2月在杨陵示范区医院就诊的慢性浅表性胃炎患者120例,随机分成对照组(60例)和治疗组(60例)。对照组患者口服兰索拉唑肠溶片,1片/次,1次/d;治疗组患者在对照组的基础上口服荜铃胃痛颗粒,1袋/次,3次/d。两组患者均连续治疗6周。观察两组患者临床疗效,同时比较治疗前后两组患者视觉模拟评分(VAS)、日常生活能力量表(ADL)评分、前列腺素E2(PGE2)和表皮细胞生长因子(EGF)水平及不良反应情况。结果治疗后,对照组和治疗组临床总有效率分别为81.67%和95.00%,两组比较差异具有统计学意义(P0.05)。治疗后,两组患者VAS较治疗前显著降低(P0.05),ADL评分显著升高(P0.05),且治疗后治疗组VAS和ADL评分明显优于对照组(P0.05)。治疗后,两组患者PGE2较治疗前均显著升高(P0.05),EGF水平显著降低(P0.05),且治疗后治疗组PGE2和EGF水平明显优于对照组(P0.05)。治疗期间,治疗组不良反应发生率为3.33%,明显低于对照组的15.00%,两组比较差异具有统计学意义(P0.05)。结论荜铃胃痛颗粒联合兰索拉唑治疗慢性浅表性胃炎疗效显著,可显著改善患者生活质量,具有一定的临床推广应用价值。     

自拟安胃汤联合兰索拉唑对老年胃溃疡患者胃肠激素及IL-6水平的影响

目的探讨老年胃溃疡患者给予自拟安胃汤联合兰索拉唑治疗对胃肠激素及白细胞介素(IL-6)水平的影响。方法选取2018年1月至2020年12月在本院治疗的老年胃溃疡患者84例作为研究对象,按照随机数字表法分成观察组(42例)和对照组(42例),对照组给予兰索拉唑治疗,观察组给予自拟安胃汤联合兰索拉唑治疗,比较两组患者胃肠激素及IL-6水平。结果两组治疗后胃泌素(GAS)、胃动素(MOT)水平明显提高(P<0.05),观察组水平较对照组明显更高(P<0.05);两组治疗后IL-6水平明显降低(P<0.05),与对照组相比,观察组明显更低(P<0.05)。结论老年胃溃疡患者给予自拟安胃汤联合兰索拉唑治疗,能够改善胃肠激素及IL-6水平,应用价值较高。     

注射用兰索拉唑细菌内毒素检查法的建立

目的:建立注射用兰索拉唑的细菌内毒素检查法。方法:按照2010年版《中国药典》(二部)附录细菌内毒素检查法,采用2个厂家的鲎试剂对5个厂家的5批样品,通过预干扰和干扰试验确定样品最大无干扰质量浓度,并进行细菌内毒素检查。结果:将供试品溶液稀释到质量浓度为0.1 mg/ml时,不干扰细菌内毒素试验,其细菌内毒素限值为5 EU/mg。结论:采用细菌内毒素检查法检查注射用兰索拉唑中的细菌内毒素方法可行。     

某院门急诊注射用兰索拉唑合理用药调查分析

目的了解本院注射用兰索拉唑在门急诊应用的合理性。方法从HIS系统中调出本院2013年7月-2013年9月应用注射用兰索拉唑的电子处方,依据说明书,对注射用兰索拉唑的适应证、用法用量等进行合理性分析。结果共调出处方64张,存在不合理用药处方41张,不合格率64．1％。结论本院门急诊注射用兰索拉唑存在严重不合理应用情况,医院应加强管理,以提高注射用兰索拉唑使用的合理性。