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直肠内给予奥昔布宁的治疗效果

[Therapeutic effects of intrarectal administration of oxybutynin].

作者信息

Radziszewski Piotr, Borkowski Andrzej

机构信息

Katedry i Kliniki Urologii Akademii Medycznej w Warszawie.

出版信息

Wiad Lek. 2002;55(11-12):691-8.

Abstract

OBJECTIVES

Oxybutynin is a drug of choice in the treatment of the detrusor instability. However the therapeutic doses given orally produce very often side effects due to oxybutynin anticholinergic properties (atropine-like action). The responsible compound is mainly the active oxybutynin metabolite-N-desethyl-oxybutynin, which is the result of the oxybutynin metabolism in liver (so-called first pass metabolism). Therefore it seems, that an attempt of the drug administration via the intrarectal route is an interesting alternative, which maintains the high oxybutynin concentration with the simultaneous reduction of the N-desethyl-oxybutynin.

PATIENTS AND METHODS

We qualified 20 patients for our study (12 men and 8 women, mean age 45.6) with the urodynamically proven detrusor instability. Patients with a neurogenic origin of detrusor instability were excluded from the study. Patients treated with oral oxybutynin in a dose of 5 mg b.i.d. and with strongly pronounced atropine-like side effects, making impossible the continuation of the therapy were offered an intrarectal form of oxybutynin in a dose of 5 mg b.i.d. Treatment efficiency was evaluated on the base of the patients symptoms (side effects, urgency, incontinence, frequency).

RESULTS

15 patients (75%) had pronounced side effects, leading to the oral treatment discontinuation. The average time of the oral oxybutynin treatment was 1.5 weeks (3 days to 4 weeks). During the oral therapy these patients complained of the side effects of different magnitude: dry mouth (15 patients--100%), gastro-intestinal disorders (3 patients--20%), drowsiness (1 patient--6.7%). These side effects forced them to stop the oxybutynin oral therapy. After the change of the drug form from oral to the intrarectal one, none of the patients resigned from the treatment. 13.3% of the patients complained of the mild intensity dry mouth. After the one-month therapy period a complete disappearing of the unstable detrusor symptoms was reported by 5 patients (25%), while all others reported their significant reduction.

CONCLUSIONS

The intrarectal oxybutynin administration shows the therapeutic efficacy comparable with the intravesical administration with reference to unstable detrusor symptoms reduction. Intrarectal administration reduces the oxybutynin side effects in comparison with the oral one.

摘要

目的

奥昔布宁是治疗逼尿肌不稳定的首选药物。然而,口服给药的治疗剂量常常因奥昔布宁的抗胆碱能特性(类似阿托品的作用)而产生副作用。主要的活性化合物是奥昔布宁的代谢产物N - 去乙基奥昔布宁,它是奥昔布宁在肝脏代谢(所谓的首过代谢)的结果。因此,经直肠给药似乎是一种有趣的替代方法,它能维持较高的奥昔布宁浓度,同时降低N - 去乙基奥昔布宁的浓度。

患者与方法

我们选取了20例经尿动力学证实为逼尿肌不稳定的患者进行研究(12名男性和8名女性,平均年龄45.6岁)。排除逼尿肌不稳定源于神经源性的患者。曾口服5毫克每日两次剂量奥昔布宁且出现明显类似阿托品副作用而无法继续治疗的患者,改为经直肠给予5毫克每日两次剂量的奥昔布宁。根据患者症状(副作用、尿急、尿失禁、尿频)评估治疗效果。

结果

15例患者(75%)出现明显副作用,导致口服治疗中断。口服奥昔布宁的平均治疗时间为1.5周(3天至4周)。在口服治疗期间,这些患者抱怨了不同程度的副作用:口干(15例患者 - 100%)、胃肠道紊乱(3例患者 - 20%)、嗜睡(1例患者 - 6.7%)。这些副作用迫使他们停止口服奥昔布宁治疗。在将药物剂型从口服改为经直肠给药后,没有患者放弃治疗。13.3%的患者抱怨有轻度口干。经过一个月的治疗期后,5例患者(25%)报告不稳定逼尿肌症状完全消失,而其他所有患者报告症状明显减轻。

结论

经直肠给予奥昔布宁在减轻不稳定逼尿肌症状方面显示出与膀胱内给药相当的治疗效果。与口服给药相比,经直肠给药可减少奥昔布宁的副作用。

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