Effect of tamsulosin, a novel alpha 1-adrenoceptor antagonist, on urethral pressure profile in anaesthetized dogs.

Journal of autonomic pharmacology Pub Date : 1996-06-01
K Sudoh, H Tanaka, O Inagaki, M Asano, T Takenaka
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Abstract

1. The effect of tamsulosin (YM617, (R) (-)-S-[2-[[2-(o-ethoxyphenoxy)ethyl]amino] propyl]-2-methoxybenzenesulfonamide HCl), a potent and selective alpha 1-adrenoceptor antagonist, was examined on urethral pressure profile (UPP) and mean arterial blood pressure (MBP) in pentobarbital anaesthetized male dogs. 2. Selective alpha 1-adrenoceptor antagonists tamsulosin (1-100 micrograms kg-1 i.v.), prazosin (1-100 micrograms kg-1 i.v.) and bunazosin (1-100 micrograms kg-1 i.v.) produced a dose dependent reduction in prostatic pressure in the UPP. Doses required to reduce prostatic pressure in UPP by 30% were 3.6 +/- 0.8 (n = 8), 6.9 +/- 1.5 (n = 8) and 4.6 +/- 0.9 (n = 8) micrograms kg-1 i.v., respectively. At the highest dose, tamsulosin exerted less hypotensive effect than prazosin and bunazosin. 3. The calcium antagonist nicardipine (0.1-10 micrograms kg-1 i.v.) and angiotensin converting enzyme inhibitor captopril (10-1,000 micrograms kg-1 i.v.) reduced MBP in a dose dependent manner, but exerted no effect on prostatic pressure in the UPP. The diuretic trichloromethiazide (1-100 micrograms kg-1 i.v.) exerted no effect on UPP or MBP. Treatment with nicardipine (3 micrograms kg-1 i.v.), captopril (100 micrograms kg-1 i.v.) or trichlormethiazide (100 micrograms kg-1 i.v.) did not affect relaxant effect of tamsulosin on prostatic pressure in UPP, or potentiate its hypotensive effect. 4. These results suggest that the alpha 1-adrenoceptor regulates urethral pressure as well as blood pressure in anaesthetized dogs, and that alpha 1-adrenoceptor antagonists may be useful in the treatment of micturition disorders associated with benign prostatic hyperplasia. In addition, as tamsulosin decreased urethral pressure with less hypotension, and as its effect was not influenced by treatment with hypotensive drugs, it may be a useful drug for the treatment of micturition disorders with few cardiovascular side effects.

新型α - 1肾上腺素受体拮抗剂坦索罗辛对麻醉犬尿道压力谱的影响。
1. 研究了强效选择性α - 1肾上腺素受体拮抗剂坦索罗辛(YM617, (R) (-)- s -[2-[[2-(o-乙氧基苯氧基)乙基]氨基]丙基]-2-甲氧基苯磺酰胺HCl)对戊巴比妥麻醉雄性犬尿道压力谱(UPP)和平均动脉血压(MBP)的影响。2. 选择性α -1 -肾上腺素受体拮抗剂坦索罗辛(1-100微克kg-1静脉注射)、普拉唑辛(1-100微克kg-1静脉注射)和布纳唑辛(1-100微克kg-1静脉注射)在UPP中产生剂量依赖性的前列腺压降低。UPP患者前列腺压降低30%所需剂量分别为3.6 +/- 0.8 (n = 8)、6.9 +/- 1.5 (n = 8)和4.6 +/- 0.9 (n = 8)微克kg-1 i.v.。在最高剂量时,坦索罗辛的降压作用不如普唑嗪和布纳唑嗪。3.钙拮抗剂尼卡地平(0.1-10微克kg-1静脉注射)和血管紧张素转换酶抑制剂卡托普利(10- 1000微克kg-1静脉注射)以剂量依赖的方式降低MBP,但对UPP中的前列腺压没有影响。利尿剂三氯噻嗪(1 ~ 100微克kg-1静脉注射)对UPP和MBP无影响。尼卡地平(3微克kg-1静脉滴注)、卡托普利(100微克kg-1静脉滴注)或三氯甲基嗪(100微克kg-1静脉滴注)治疗不影响坦索罗辛对UPP患者前列腺压的松弛作用,也不增强其降压作用。4. 这些结果表明,α 1-肾上腺素能调节麻醉犬的尿道压力和血压,α 1-肾上腺素能拮抗剂可能有助于治疗与良性前列腺增生相关的排尿障碍。此外,由于坦索罗辛降低尿道压力,低血压较少,并且其效果不受降压药治疗的影响,因此它可能是一种治疗排尿障碍的有用药物,而且心血管副作用少。
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