部分中文米屈肼处方资料（仅供参考）
中文名称 米屈肼
商品名称：Mildronāts®
商品名称：Mildronate® GX
英文名称：Mildronate
别名：THP，MET-88，Meldonium，Mildronāts or Quaterine
剂型和规格：。
水针规格0.5g/5ml。
胶囊剂： 250mg，500mg
适应症：
心血管疾病
稳定性心绞痛，慢性心力衰竭，心肌病，功能性心血管系统故障；急性和慢性局部缺血发作；高负荷生理和心理情绪下工作能力降低；脑血管疾病、脑部损伤和脑炎后的恢复期。酒精戒断症状。
用法用量：
水针：静注，成人500mg-1.0g/天，分1-2次给药，个半天使用会出现局部刺激作用。用于酒精截断症状，每次500mg，每天4次，服用7-10天。
药理作用创新点：
膜保护作用 心机缺血时引起心肌细胞的紧张反应，使线粒体内脂肪酸分解增加，细胞中脂肪酸代谢物堆积，细胞膜装置遭到破坏，细胞内Ca++增加。能量优化作用 米屈肼可减少长链酰基肉毒碱的堆积，从而可抑制肉毒碱依赖的脂肪酸氧化，使缺氧心肌的能量代谢从脂肪酸氧化转化为更有利的葡萄糖氧化，即促使糖酵解途径的厌氧性氧化，故本品具有抗缺氧效用和心脏保护活性。对能量代谢酶的影响 米屈肼还能阻止异丙肾上腺素诱导加强的血中乳酸脱氢酶（心肌特异同工酶）肝脏异生活性，防止肌酸磷酸激酶活性的增加。对肉毒碱排泄的影响 另有研究表明，米屈肼在体内除竞争性抑制丁酸甜菜碱羟化酶，阻断肉毒碱的生物合成外，还竞争性的影响肉毒碱在肾脏的重吸收。对缺血心脏的保护 在心肌缺血区域，阻塞的前降支不仅降低了组织水平的ATP、ADP和肌磷酸，还增加了组织水平的AMP和乳酸盐，降低能荷潜势的价值。实验结果表明米屈肼可抑制脂肪酸的β-氧化从而对缺血心肌的能量代谢是非常有利的。
保质期 - 4年。
上市情况：
目前，临床常用的传统治疗心肌缺血的药物有下述几类：硝酸酯类、β受体阻滞剂、钙通道阻滞剂及降血脂类等。它们的作用机制主要是松弛血管平滑肌，使血管平滑肌和冠状动脉扩张，降低心肌耗氧量及降低血脂。因冠心病病人的死亡率仍然居高不下。心肌缺血再灌注时的代谢紊乱一直受到医药工作者的高度关注，近年来，改善心肌代谢的药物在抗心肌缺血再灌注性损伤方面的作用受到诸多学者的重视。 米屈肼(又称THP，MET-88和mildronate)是一种新型心脏保护药。
Mildronate(Meldonium) all forms 60 x 500 mg, 40 x 250 mg, 10 vials x5 ml
Mildronate is a structural analogue of a precursor of carnitine - gamma-butyrobetaine (GBB). Mildronate inhibits the activity of gamma-butyrobetain-hydroxylase, causing a decrease of carnitine biosynthesis and long-chain fatty acids transport through cell membranes. It prevents the accumulation of Acyl-CoA and Acyl-carnitine, the metabolites of long-chain fatty acids in cells, thus diminishing their adverse effects.
Under the conditions of ischemia, Mildronate activates the anaerobic glycolysis and stimulates the ATP production, and transport, restores the balance between oxygen delivery and consumption.
Decrease of carnitine concentration results in activation of synthesis of gamma-butyrobetaine, which possess vasodilatating activity.Mildronate exerts cardio protective effect. In the case of chronic congestive heart failure it augments myocardial contractility, increases the tolerance of the organism to physical overload. In patients with II-III stage stable angina pectoris Mildronate increases the physical capacity and decreases the number of angina pectoris attacks.
In the cases of acute and chronic ischemic cerebrovascular disturbances Mildronate ameliorates cerebral blood flow in the ischemic region, promoting redistribution of blood flow in favour of ischemic zone.Mildronate is also characterised by a tonic effect. It prevents functional disturbances of somatic and vegetative nervous system
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Product Ingridients:
•Mildronate
Therapeutic actions:
Mildronate is a structural analogue of a precursor of carnitine - gamma-butyrobetaine (GBB). Mildronate inhibits the activity of gamma-butyrobetain-hydroxylase, causing a decrease of carnitine biosynthesis and long-chain fatty acids transport through cell membranes. It prevents the accumulation of Acyl-CoA and Acyl-carnitine, the metabolites of long-chain fatty acids in cells, thus diminishing their adverse effects.
Under the conditions of ischemia, Mildronate activates the anaerobic glycolysis and stimulates the ATP production, and transport, restores the balance between oxygen delivery and consumption.
Decrease of carnitine c |
