Milrinone米力农
别名:1,6-Dihydro-2-methyl-6-oxo-[3,4'-bipyridine]-5-carbonitrile; Corotrope; Milrila。2-甲基-6-氧-1,6-二氢-[3,4’双吡啶]-5甲腈。
所属类别:药物,心脑血管药物,强心药
用途: 强心药,具有增强心肌收缩力和直接扩张血管的作用 新型非苷类非儿茶酚胺类强心药,作用与氨吡酮相似,正性肌力作用强,约为氨力农的20~50倍,并有明显的扩张血管平滑肌作用,能降低心脏负荷,还能极好地改善肾脏和肌肉供血。口服和静脉均有效,无严重不良反应。用于慢性心力衰竭及充血性心力衰竭等严重的心力衰竭。
米力农注射液 米力农注射液磷酸二酯酶抑制剂,为氨力农的同类药物,作用机理与氨力农相同,兼有正性肌力作用和血管扩张作用。本品正性肌力作用主要是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。而与肾上腺素b1受体或心肌细胞Na+、K+ -ATP酶无关其血管扩张作用可能是直接作用于小动脉或所致,从而可降低心脏前、后负荷,降低左心室充盈压,改善左室功能,增加心脏指数,但对平均动脉压和心率无明显影响。本品对伴有传导阻滞的患者较安全。本品口服时不良反应较重,不宜长期应用。
药代动力学 静脉给药5~15分钟起生效,清除半衰期为2~3小时。蛋白结合率70%。
作用与用途 本品可使高血性心力衰竭患者体循环血管阻力、肺动脉平均压和肺毛细血管楔嵌压显著降低、心输出量、心脏指数和每搏指数增加,但不增加心肌耗氧量。 适用于充血性心力衰竭短期静脉用药。
用法 可用适量生理盐水或葡萄糖液稀释后,先按37.5μg/kg-50μg/kg缓慢静脉注射10分钟(注射过快,可能出现室性早搏),继续以0.375μg~0.75μg/kgmin静脉滴注,此后根据临床效应调整用量。
副作用 少数病人可有低血压、窦性心动过速、室性心律失常、血小板计数减少、肝、肾功能异常、及头痛、头晕、恶心、呕吐等。
药物相互作用 与常用强心药、利尿药、血管扩张药合用,临床未见不良相互作用,与多巴胺、多巴酚丁胺合用有协同作用。
禁忌症 严重室性心律失常。对本品过敏者。
注意事项 ①用药期间应监测心电图,心率及血压,必要时调整用量。 ②本品有较强的血管扩张作用,严重低血压或血容量不足者应慎用。 ③不宜用于重度辨膜狭窄症。 ④可能加重肥厚性心肌病的流出道梗阻。 ⑤合并用强利尿药时,应注意纠正血容量不足与电介质平衡。 ⑥对房颤或房扑患者,本品可增加房室传导、导致心室率增快,宜先用或联合应用控制心室率的药物。 ⑦肝肾功能损害严重者慎用。 ⑧尚无用于孕妇哺乳及儿童的经验,使用时权衡利弊。 ⑨用药期间应监测血小板计数。
Milrila - General Information: A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase activity in myocardium and vascular smooth muscle. Milrila is a derivative of amrinone and has 20-30 times the ionotropic potency of amrinone.
Pharmacology: Milrila, a synthetic dimethylxanthine derivative structurally related to theophylline and caffeine, is used in the treatment of peripheral vascular diseases and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.
Milrila Interactions: No untoward clinical manifestations have been observed in limited experience with patients in whom PRIMACOR was used concurrently with the following drugs: digitalis glycosides; lidocaine, quinidine; hydralazine, prazosin; isosorbide dinitrate, nitroglycerin; chlorthalidone, furosemide, hydrochlorothiazide, spironolactone; captopril; heparin, warfarin, diazepam, insulin; and potassium supplements.
Chemical Interactions
There is an immediate chemical interaction which is evidenced by the formation of a precipitate when furosemide is injected into an intravenous line of an infusion of PRIMACOR. Therefore, furosemide should not be administered in intravenous lines containing PRIMACOR.
Milrila Contraindications: PRIMACOR is contraindicated in patients who are hypersensitive to it.
Additional information about Milrila: Milrila Indication: Indicated for the treatment of congestive heart failure. Mechanism Of Action: Milrila inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, Milrila also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity. Drug Interactions: Not Available Food Interactions: Not Available Generic Name: Milrinone Synonyms: Milrinone Lactate Drug Category: Vasodilator Agents; Cardiotonic Agents Drug Type: Small Molecule; Approved Other Brand Names containing Milrinone: Corotrop; Corotrope; Milrila; Primacor; Absorption: Milrinone is rapidly and almost completely absorbed after oral administration. Bioavailability is 92% (in healthy volunteers). Toxicity (Overdose): LD50 = 0.3 mg/L in rats Protein Binding: 70 to 80% Biotransformation: There are five metabolites but the O-glucuronide represents the major pathway of biotransformation. Half Life: 2.3 hours Dosage Forms of Milrila: Solution Intravenous Liquid Intravenous Chemical IUPAC Name: 6-methyl-2-oxo-5-pyridin-4-yl-1H-pyridine-3-carbonitrile Chemical Formula: C12H9N3O Organisms Affected: Humans and other mammals |