部份中文奥普力农处方资料（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。 完整处方资料附件 1）：http://www.info.pmda.go.jp/go/pack/2119407A1020_1_09/ 2）：http://www.info.pmda.go.jp/go/pack/2119407G1022_1_06/ Coatec Injection(Olprinone Hydrochloride Hydrate) Therapeutic category name Acute heart failure treatment agent Brand Name CORETEC Note 5mg composition This drug is a colorless clear injection containing the following ingredients, have been filled in colorless ampoules of one-point cut. Active Ingredients: olprinone hydrochloride hydrate Amount in the first tube (5mL): 5mg Additives: citric acid hydrate Amount in the first tube (5mL): 2.1mg Additives: sodium hydroxide Amount in the first tube (5mL): appropriate amount Additives: D- sorbitol Amount in the first tube (5mL): 250mg Contraindication Patients with hypertrophic obstructive cardiomyopathy [There is a possibility that exacerbate the left ventricular outflow tract stenosis] Women suspected of being pregnant or pregnant [See section "pregnant women, maternal, administration to nursing women, etc."] Efficacy or effect It is administered other drugs if the effect is insufficient in the state of the following Acute heart failure Usually, to adults, this drug injection solution as it is, or physiological saline solution, diluted with glucose solution or the like, intravenously administered slowly over a period of body weight 1kg per 10μg 5 minutes as olprinone hydrochloride hydrate, continue for one minute the per 0.1~0.3μg / kg for intravenous drip infusion. It should be noted that the infusion dose is appropriately increased or decreased depending on the condition of the patient, in the case where there is a need can be increased up to 0.4μg/kg per minute. Careful administration Patients with serious tachyarrhythmia [This drug because of the baroreceptor reflection by the positive chronotropic action and vasodilating action, which may exacerbate the arrhythmia] Patients with severe coronary artery disease [This drug has a positive inotropic effect, there is a possibility that exacerbate coronary artery disease] Patients with impaired renal function [With the decrease in renal function, elimination half-life of this drug is likely to be longer. Further, there is a possibility to worsen renal function impairment] Low blood pressure significantly patient [This preparation has a vasodilating effect, more may reduce the blood pressure] The elderly [see section "administration to the elderly."] Clinically significant adverse reactions Ventricular fibrillation, ventricular tachycardia (including Torsades de pointes), decreased blood pressure Ventricular fibrillation (less than 0.1% to 5%), ventricular tachycardia (including Torsades de pointes) (less than 0.1% to 5%), because it may decrease in blood pressure (less than 0.1% to 5%) appears, abnormalities are observed case, to stop the weight loss or administration and take appropriate action. Renal dysfunction Because there is that renal dysfunction (less than 0.1% to 5%) may occur. Patients should be carefully monitored, and if any abnormalities are observed, discontinue administration and take appropriate action. Pharmacology Pharmacological action Heart contractile force enhancing action The force of contraction of the guinea pig and the dog isolated cardiac muscle enhanced in a concentration-dependent manner, to enhance cardiac contractility of anesthesia and awakening dogs(LVdP /dtmax) in a dose-dependent manner by intravenous administration. Vasodilating action Isolated rat aorta of noradrenaline and KCl contraction, as well as a concentration-dependent manner inhibits the phenylephrine contraction of the dog isolated femoral artery and saphenous vein. Also, in anesthetized dogs, reducing the total peripheral vascular resistance in a dose-dependent manner by intravenous administration, to increase the local blood flow by the administration within the artery. Improving action of the heart failure condition Propranolol heart failure using the anesthetized dog, in each disease model of heart failure due to heart failure and mitral regurgitation by the volume load and coronary artery ligation, heart contraction strength, showed a decrease in cardiac output increase, afterload and preload, heart failure to improve the condition markedly. In addition, a decrease in the expansion and fractional shortening of the left ventricular internal diameter in the propranolol heart failure markedly improved, capacity vasodilating action in heart failure model by mitral regurgitation has been suggested. Mechanism of action Heart contractile force enhancement The main mechanism of action is the selective inhibition of specific PDEIII to cAMP, is estimated to show a heart contractile force enhanced by the intracellular cAMP increase and peak Ca2 + level rise that occurs as a result. Vasodilatation The main mechanism of action is the selective inhibition of PDE III, is presumed to exhibit vasodilation by intracellular cAMP increase and Ca2 + levels decrease the resulting. Physicochemical knowledge of active ingredient General name Olprinone hydrochloride hydrate (Olprinone Hydrochloride Hydrate) Chemical name 1,2-dihydro-5- (imidazo [1,2-α] pyridin-6-yl) -6-methyl-2-oxo-3-pyridinecarbonitrile hydrochloride monohydrate Molecular formula C14H10N4O · HCl · H2O The molecular weight 304.73 Structural formula Physicochemical properties Olprinone hydrochloride hydrate is a white to pale yellowish white crystalline powder, no odor. It is freely soluble in formic acid, sparingly soluble in water, slightly soluble in methanol, ethanol (99.5), do not dissolve almost to acetic anhydride, acetic acid (100) or diethyl ether. ------------------------------------------------- 产地国家： 日本 原产地英文商品名: Coretec（コアテック注）5mg/5ml/Ampule 5Ampule (Minimum order qty: 4) 原产地英文药品名: Olprinone Hydrochloride Hydrate 中文参考商品译名: Coretec（コアテック注）5毫克/5毫升/安瓿 5安瓿 (最低订货量：4) 中文参考药品译名: 奥普力农盐酸盐水合物 生产厂家中文参考译名: 卫材有限公司 生产厂家英文名: Eisai Co ------------------------------------------------- 产地国家： 日本  原产地英文商品名: Coretec（コアテック注SB）9mg/150ml/bag 5bag(Minimum order qty: 4) 原产地英文药品名: Olprinone Hydrochloride Hydrate 中文参考商品译名: Coretec（コアテック注SB）9毫克/150毫升/袋 5袋 (最低订货量：4)  中文参考药品译名: 奥普力农盐酸盐水合物 生产厂家中文参考译名: 卫材有限公司 生产厂家英文名: Eisai Co