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 详细处方信息以本药内容附件PDF文件（201071419162813.pdf）的“原文Priscribing Information”为准
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部分中文Coretec处方资料（仅供参考）

【中文品名】盐酸奥普力农

【药效类别】强心药>氨力农类，血管扩张药

【通用药名】OLPRINONE HYDROCHLORIDE

【别　　名】Coatec, Coretec, Loprinone, E-1020

【化学名】5-(Imidazo[1,2-a]pyridin-6-yl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carbonitrile hydrochloride monohydrate

【原研厂家】Eisai (Originator)卫材

【CA登记号】[119615-63-3]

【分 子 式】CHNOPS·

【用　　途】心脏兴奋剂，用于治疗对其它治疗无效的急性心功能不全。在由冠脉阻塞或心得安产生的急性心衰中，静注本品30微克/公斤可逆转心脏抑制。

【概述】心力衰竭(Cardiac Dysfunction)，又称充血性心力衰竭（CHF），是指在静脉回流正常的情况下，由于原发的心脏损害引起心排血量减少，不能满足组织代谢需要的一种综合征。临床上以肺循环和(或)体循环瘀血以及组织血液灌注不足为主要特征。随着心血管病诊疗技术的进步，许多在急性期死亡率极高的疾病如急性心肌梗塞，由于采用了溶栓等治疗手段，早期死亡率已大大降低，相反却使得心力衰竭发病率逐年增加。另外，随着人类寿命不断延长，心肌老化也成为心衰的重要原因。心衰已成为21世纪人类面临的最难以克服的疾病。心功能衰竭是冠心病、高血压等心脏病的终末阶段，其预后比恶性肿瘤还差，随时危及生命。心衰的死亡率极高，有统计表明，重度心衰患者死亡率高达50％，心衰患者得病2年后死亡率高达30—40％，6年后高达70％，而且患病3年内约有一半患者会因心衰加重反复住院。盐酸奥普力农是一种磷酸二酯酶（PDE）III抑制剂，具有正性肌力作用和血管扩张作用，主要通过抑制磷酸二酯酶，使心肌细胞内环磷酸腺苷（CAMP）浓度增高，细胞内钙增加，心肌收缩力加强，心排血量增加。

【国外上市情况】盐酸奥普力农是由日本卫材株式会社开发的一种磷酸二酯酶抑制剂，主要用于急性心力衰竭。1996年4月24日由日本厚生省批准上市，上市剂型为注射液，规格为5ml：5mg和150ml：9mg，商品名为コアテック注®，英文商品名为Coretec®。

【与同类产品比较】急性和慢性充血性心衰的基本治疗药物主要有儿茶酚胺类和磷酸二酯酶Ⅲ抑制剂。儿茶酚胺类因正性肌力和增加心率作用不能有效分离，有致心律失常的可能，因而在临床应用上受到限制。磷酸二酯酶Ⅲ抑制剂目前为治疗心衰的主要药物， 最先应用的PDE- Ⅲ抑制药是氨力农（amrinone），临床有效，但长期口服后约15%患者出现血小板减少，另有心律失常、肝功能减退。现仅供短期静脉滴注用。其代替品米力农（milrinone）抑酶作用较前者强20倍，临床应用有效，能缓解症状、提高运动耐力，不良反应较少，未见引起血小板减少。但近来报道久用后疗效并不优于地高辛，易引起心律失常，病死率较高，也仅供短期静脉给药用。依诺昔酮（enoximone）治疗中、重度CHF疗效与米力农相似，其病死率较对照组为高，不可长期口服用。其他有待临床观察的药还有匹罗昔酮（piroximone），匹莫苯（pimobendan）,维司力农（Vesnarinone）等。奥普力农在增加心肌收缩功能的同时能够改善舒张功能。而且还具有舒张阻力和容量血管的作用。强心扩管双重功效显著改善心功能不全症状，有利于预后、改善生活质量；临床实验证明本药在不增加心肌的耗氧量情况下，增大心输出量，同时减轻心脏的前后负荷，比儿茶酚胺类制剂的改善心功能有效率高。且较少引起心律不齐。奥普力农提高心脏指数（CI）及降低周围血管阻力与米力农程度相当，对大动脉舒张压和肺动脉压作用较米力农强。

Product name：Olprinone Hydrochloride

CAS NO.：106730-54-0

Use：Asthma Therapy, Bronchodilators, CARDIOVASCULAR DRUGS, Heart Failure Therapy, RESPIRATORY DRUGS, Phosphodiesterase III Inhibitors
 
Effects of olprinone, a new phosphodiesterase inhibitor, on gastric intramucosal acidosis and systemic inflammatory responses following hypothermic cardiopulmonary bypass.
 
Background: Phosphodiesterase (PDE) III inhibitors have both an inotropic and a peripheral vasodilatory effect, and also inhibit the activation of macrophages. Thus a newly developed PDE III inhibitor, olprinone, could modify gastric intramucosal pH (pHi), systemic oxygen consumption, and systemic inflammatory responses in patients undergoing cardiac surgery with cardiopulmonary bypass (CPB). Methods: We studied 23 patients. In 15 patients, olprinone (0.1 or 0.2 μg · kg 1 · min 1) was administered from the commencement of CPB until their admission to the ICU. The other 8 patients received placebo. The pHi and regional CO2 tension (PrCO2) were assessed by a capnometric air tonometry. Systemic inflammatory responses were evaluated by serum interleukin-6 (IL-6), IL-10, and leucocyte counts. Results: The pHi and PCO2-gap, the difference between PrCO2 and arterial CO2 tension (PaCO2), showed a transient decrease and an increase after CPB, respectively. Although olprinone did not affect pHi, olprinone at 0.2 μg · kg 1 · min 1 significantly lessened post-CPB increase in PCO2-gap. Olprinone at 0.2 μg · kg 1 · min 1 significantly increased IL-10 and reduced the extent of leucocytosis, while it did not affect IL-6 levels. At the same dosage, olprinone also lessened the surge in systemic oxygen uptake index (V˙O2) and augmented the increase in mixed oxygen saturation (SvˉO2) both of which occurred after CPB. At 0.1 μg · kg 1 · min 1, however, olprinone did not show any significant effect. Conclusion: Our results suggest that olprinone at 0.2 μg · kg 1 · min 1 suppresses gastric intramucosal acidosis and systemic inflammation following CPB.

Effect of Olprinone Administration for a Hepatic Venous Oxygen Saturation during Pringle's Maneuver

BackgroundPringle's maneuver (hepatic artery and portal vein clamp technique at the same time) is effective technique for bleeding control in major liver resection. However, it is possible that the hepatic ischemia induces ischemia-reperfusion injury. Therefore, appropriate maintenance of intraoperative hepatic blood flow is important for persistense liver function. It is that Olprinone hydrochloride (OLP) is a new phosphodiesterase III inhibitor with positive inotropic and vasodilator properties and increase hepatic artery and portal vein blood flow. However, it is possible that OLP causes hypotension and therefore the hepatic blood flow increase (1). In this study, we measured hepatic venous saturation (ShvO2) and examined the effects of OLP on hepatosplanchnic circulation during Pringle's maneuver.

Materials and Methods We performed a study of combined medications with continuous ShvO2 monitoring during pancreaticoduodenectomy in 20 patients of ASA 1 or 3 physical status. And we divided into two groups: control group (C group, n=10) and OLP (0.3μg/kg/min) group (OLP group, n=10). After induction, two kinds of Swan-Ganz catheters was inserted into the pulmonary artery and the hepatic vein (Edwards Lifesciences, 774HF75, D750HF75) from the right internal jugular vein in a fluoroscopy.

These catheters were connected to the Vigilance CEDV monitor (Edwards Lifesciences, Irvine, CA). Pringle's manuever was performed intermittently with 10 minutes clamp and 10 minutes declamp. We measured hemodynamics, arterial saturation (SaO2), mixed venous saturation (SvO2), ShvO2 analysis value and hepatic venous lactate value during clamp and declamp. Additionally, effective hepatic blood flow (EHBF) was measured during Pringle's maneuver by DDG analyser (DDG – 2001, NIHON KOHDEN Ltd, Japan) with indocyanine green (ICG). The data are presented as mean standerd deviation (SD). Data were analyzed with paired t-test or two-way ANOVA. A probability of less than 5% was considered to indicate significance.

Results Hemodynamics did not change at all measurement points. Additionally, OLP group was significantly high compared with control groups in ShvO2 and EHBF (figure 1, figure 2).

Discussion:The hepatic blood flow comes usually blood flow from hepatic artery, portal vein or collateral circulation.In OLP group, ShvO2 and EHBF increase, but venous blood lactate value decrease during Pringle's maneuver.

The reason of it is speculated that blood flow of collateral circulation was increased in OLP.
Conclusions These results suggest that OLP enhances hepatosplanchnic blood flow and thus may be beneficial in protecting the hepatosplanchnic organs during Pringle's maneuver.

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 详细处方信息以本药内容附件PDF文件（201071419162813.pdf）的“原文Priscribing Information”为准
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