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柳氮磺胺吡啶和磺胺吡啶对溃疡性结肠炎患者直肠给药和口服给药后的比较药代动力学

Comparative pharmacokinetics of sulphasalazine and sulphapyridine after rectal and oral administration to patients with ulcerative colitis.

作者信息

Allgayer H, Kruis W, Eisenburg J, Paumgartner G

出版信息

Eur J Clin Pharmacol. 1984;26(2):275-7. doi: 10.1007/BF00630300.

DOI:10.1007/BF00630300
PMID:6144549
Abstract

Rectal administration of sulphasalazine to patients with ulcerative colitis has recently been shown to have similar therapeutic activity but fewer side effects than oral treatment. The present study is a comparison of the pharmacokinetics of sulphasalazine (SASP) and its metabolite sulphapyridine (SP) after rectal and oral administration of SASP to 6 patients with ulcerative colitis. The areas under the concentration-time curves (AUC) and the maximum concentrations (Cmax) of SASP and SP were significantly lower after rectal than oral administration of SASP (p less than 0.05). These findings support the view that the lower frequency of side effects after rectal administration of SASP may result from the lower plasma levels of SASP and SP.

摘要

最近研究表明,对溃疡性结肠炎患者直肠给药柳氮磺胺吡啶,其治疗活性与口服治疗相似,但副作用更少。本研究比较了6例溃疡性结肠炎患者直肠和口服柳氮磺胺吡啶(SASP)后,柳氮磺胺吡啶(SASP)及其代谢产物磺胺吡啶(SP)的药代动力学。直肠给药SASP后,SASP和SP的浓度-时间曲线下面积(AUC)和最大浓度(Cmax)显著低于口服给药(p小于0.05)。这些发现支持以下观点:直肠给药SASP后副作用发生率较低,可能是由于SASP和SP的血浆水平较低所致。

相似文献

1
Comparative pharmacokinetics of sulphasalazine and sulphapyridine after rectal and oral administration to patients with ulcerative colitis.柳氮磺胺吡啶和磺胺吡啶对溃疡性结肠炎患者直肠给药和口服给药后的比较药代动力学
Eur J Clin Pharmacol. 1984;26(2):275-7. doi: 10.1007/BF00630300.
2
Placental transfer of sulphasalazine and sulphapyridine and some of its metabolites.
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3
Saliva: plasma concentration relationships for sulphapyridine following sulphasalazine administration to normal volunteers and patients with inflammatory bowel disease.唾液:对正常志愿者和炎症性肠病患者给予柳氮磺胺吡啶后磺胺吡啶的唾液与血浆浓度关系。
Br J Clin Pharmacol. 1980 Jan;9(1):91-4. doi: 10.1111/j.1365-2125.1980.tb04802.x.
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A comparison of serum concentrations of sulphasalazine and some of its metabolites after therapy by the oral or rectal route.口服或直肠给药治疗后柳氮磺胺吡啶及其某些代谢产物血清浓度的比较。
Pharmatherapeutica. 1984;3(8):551-5.
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[Individualized sulfasalazine treatment of ulcerative colitis and monitoring of patient compliance by determining sulfapyridine serum concentration].
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Steady-state kinetics of 5-aminosalicylic acid and sulfapyridine during sulfasalazine prophylaxis in ulcerative colitis.
Scand J Gastroenterol. 1986 Aug;21(6):693-700. doi: 10.3109/00365528609011102.
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本文引用的文献

1
Cortisone in ulcerative colitis; final report on a therapeutic trial.可的松治疗溃疡性结肠炎;一项治疗试验的最终报告
Br Med J. 1955 Oct 29;2(4947):1041-8. doi: 10.1136/bmj.2.4947.1041.
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Retrograde colonic spread of sulphasalazine enemas.柳氮磺胺吡啶灌肠剂的结肠逆行扩散。
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Sulfasalazine intolerance. A retrospective survey of the reasons for discontinuing treatment with sulfasalazine in patients with chronic inflammatory bowel disease.柳氮磺胺吡啶不耐受。对慢性炎症性肠病患者停用柳氮磺胺吡啶治疗原因的回顾性调查。
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Pharmacokinetics of rectal drug administration, Part II. Clinical applications of peripherally acting drugs, and conclusions.直肠给药的药代动力学,第二部分。外周作用药物的临床应用及结论。
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Rectal drug administration: clinical pharmacokinetic considerations.直肠给药:临床药代动力学考量
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6
Sulphasalazine retention enemas in ulcerative colitis: a double-blind trial.柳氮磺胺吡啶保留灌肠治疗溃疡性结肠炎:一项双盲试验。
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7
On the efficacy of ready-made-up commercially available salicylazosulphapyridine enemas in the treatment of proctitis, proctosigmoiditis and ulcerative colitis involving rectum, sigmoid and descending colon.关于市售柳氮磺胺吡啶灌肠剂治疗直肠炎、直肠乙状结肠炎以及累及直肠、乙状结肠和降结肠的溃疡性结肠炎的疗效
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8
A controlled therapeutic trial of long-term maintenance treatment of ulcerative colitis with sulphazalazine (Salazopyrin).柳氮磺胺吡啶(水杨酸偶氮磺胺吡啶)对溃疡性结肠炎进行长期维持治疗的对照治疗试验。
Gut. 1973 Dec;14(12):923-6. doi: 10.1136/gut.14.12.923.
9
The metabolism of salicylazosulphapyridine in ulcerative colitis. I. The relationship between metabolites and the response to treatment in inpatients.柳氮磺胺吡啶在溃疡性结肠炎中的代谢。I. 住院患者中代谢产物与治疗反应的关系
Gut. 1973 Aug;14(8):631-41. doi: 10.1136/gut.14.8.631.
10
Adverse reactions during salicylazosulfapyridine therapy and the relation with drug metabolism and acetylator phenotype.柳氮磺胺吡啶治疗期间的不良反应及其与药物代谢和乙酰化酶表型的关系。
N Engl J Med. 1973 Sep 6;289(10):491-5. doi: 10.1056/NEJM197309062891001.