GR122311X（枸橼酸铋雷尼替丁），一种治疗十二指肠溃疡的新药。

GR122311X (ranitidine bismuth citrate), a new drug for the treatment of duodenal ulcer.

作者信息

Bardhan K D, Dekkers C P, Lam S K, Nowak A, Schaffalitzky de Muckadell O B, Schutze K, Tildesley G, Kler L, Forster J K, Lacey L F

机构信息

Rotherham General Hospitals NHS Trust, UK.

出版信息

Aliment Pharmacol Ther. 1995 Oct;9(5):497-506. doi: 10.1111/j.1365-2036.1995.tb00412.x.

DOI:10.1111/j.1365-2036.1995.tb00412.x

PMID:8580269

Abstract

BACKGROUND

Ranitidine bismuth citrate (GR122311X) is a new drug which offers potential benefits in healing duodenal ulcers and prevention of relapse.

METHODS

This randomized, multi-centre double-blind study of 1620 patients compared the effect of 4 weeks of treatment with GR122311X 200 mg b.d. (n = 401), 400 mg b.d. (n = 404) or 800 mg b.d. (n = 404) or ranitidine hydrochloride 150 mg b.d. (n = 411) on the rates of duodenal ulcer healing and of overall success (ulcers healed and remaining ulcer free in the 24-week follow-up phase).

RESULTS

All four treatments were equally effective at ulcer healing (79%, 85%, 84% and 81% of patients, respectively). GR122311X 400 mg b.d. (38%) and 800 mg b.d. (37%) were significantly more effective than ranitidine hydrochloride 150 mg b.d. (32%) with respect to overall success (P = 0.050 and P = 0.030, respectively) but there was no difference with GR122311X 200 mg b.d. (31%). GR122311X caused effective, dose-related suppression of H. pylori (47%, 61% and 74%); H. pylori eradication rates were 18%, 21% and 22%. GR122311X was safe and well tolerated, with an adverse event profile similar to that of ranitidine hydrochloride 150 mg b.d. Median week 4 trough plasma bismuth levels were 1.3 ng/mL, 2.3 ng/mL and 3.3 ng/mL with GR122311X 200 mg b.d., 400 mg b.d. and 800 mg b.d. respectively. No individual plasma bismuth concentrations were of clinical concern.

CONCLUSIONS

GR122311X is a safe and effective ulcer healing drug, and provides a platform on which anti-H. pylori therapy can be based.

摘要

背景

枸橼酸铋雷尼替丁（GR122311X）是一种新药，在十二指肠溃疡愈合及预防复发方面具有潜在益处。

方法

这项针对1620例患者的随机、多中心双盲研究，比较了GR122311X 200mg每日两次（n = 401）、400mg每日两次（n = 404）或800mg每日两次（n = 404），以及盐酸雷尼替丁150mg每日两次（n = 411）治疗4周对十二指肠溃疡愈合率及总体成功率（溃疡愈合且在24周随访期内无溃疡复发）的影响。

结果

所有四种治疗在溃疡愈合方面同样有效（患者愈合率分别为79%、85%、84%和81%）。就总体成功率而言，GR122311X 400mg每日两次（38%）和800mg每日两次（37%）显著优于盐酸雷尼替丁150mg每日两次（32%）（P值分别为0.050和0.030），但与GR122311X 200mg每日两次（31%）无差异。GR122311X对幽门螺杆菌有有效且与剂量相关的抑制作用（47%、61%和74%）；幽门螺杆菌根除率分别为18%、21%和22%。GR122311X安全且耐受性良好，不良事件谱与盐酸雷尼替丁150mg每日两次相似。GR122311X 200mg每日两次、400mg每日两次和800mg每日两次在第4周时铋的血浆谷浓度中位数分别为1.3ng/mL、2.3ng/mL和3.3ng/mL。个体血浆铋浓度均无临床意义。