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硝普钠气雾剂与异丙肾上腺素气雾剂对组胺诱发豚鼠支气管哮喘作用的比较

Comparison of sodium nitroprusside and isoprenaline aerosols in histamine-induced bronchial asthma of the guinea pig.

作者信息

Kreye V A, Marquard E

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1979 Apr;306(3):203-7. doi: 10.1007/BF00507104.

Abstract
  1. Sodium nitroprusside (NP) is a potent relaxant of the guinea pig's tracheal smooth muscle contracted by carbachol or histamine. 2. At high doses, aerosols of NP delay the occurrence of symptoms of bronchial asthma in guinea pigs subjected to a histamine aerosol. However, the beta-adrenergic bronchodilator isoprenaline is at least 2,600 times more potent as an anti-asthmatic than NP on a molar basis. 3 NP and isoprenaline both reduce the blood pressure in rats when given either as infusion or as aerosol. The aerosol/infusion dosage ratio for comparable reductions of blood pressure were 1 for isoprenaline, and 10 for NP. After cessation of the application of the NP aerosol, the blood pressure rose more than twice as fast (t1/2 of blood pressure recovery) than after cessation of the application of the isoprenaline aerosol. 4. The poor antiasthmatic effect of NP aerosols may result from low permeability of the bronchial epithelium to the NP anion, from partial destruction in the airways or during tissue permeation, and from short half life of NP in the circulating blood. 5. Because of its inferiority to known bronchodilators, aerosols of NP cannot be recommended for the treatment of acute bronchial asthma.
摘要
  1. 硝普钠(NP)是一种强效的松弛剂,可使由卡巴胆碱或组胺收缩的豚鼠气管平滑肌松弛。2. 高剂量时,NP气雾剂可延迟接受组胺气雾剂的豚鼠支气管哮喘症状的出现。然而,β-肾上腺素能支气管扩张剂异丙肾上腺素在摩尔基础上作为抗哮喘药物的效力至少比NP高2600倍。3. NP和异丙肾上腺素静脉输注或制成气雾剂给药时均可降低大鼠血压。使血压产生相当程度降低的气雾剂/静脉输注剂量比,异丙肾上腺素为1,NP为10。停止使用NP气雾剂后,血压上升速度比停止使用异丙肾上腺素气雾剂后快两倍多(血压恢复的t1/2)。4. NP气雾剂抗哮喘效果不佳可能是由于支气管上皮对NP阴离子的通透性低、在气道或组织渗透过程中部分被破坏以及NP在循环血液中的半衰期短。5. 由于其相对于已知支气管扩张剂的劣势,不推荐使用NP气雾剂治疗急性支气管哮喘。

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