70．鱼精蛋白

出处：按学科分类—医药、卫生 军事医学科学出版社《临床常用进口药物手册》第399页（5368字）

【中文释文】：

(罗氏)肝素拮抗药

〔成分〕

盐酸鱼精蛋白：有两种浓度的药液可供使用，均为每安瓿5ml：

鱼精蛋白1000(罗氏)，1ml中和1000U的肝素。

鱼精蛋白5000(罗氏)，1ml中和5000U的肝素。

〔性能〕

鱼精蛋白是单纯蛋白质，由少量几种氨基酸(其中主要是精氨酸)组成，鱼精蛋白是从各种鲑鱼睾丸中提取的。

鱼精蛋白与肝素结合形成无抗凝血活性的不溶解的盐类。

鱼精蛋白本身是抗促凝血酶原激酶，因而单独使用时能产生抗凝血作用。

〔适应证〕

对静脉或皮内给予肝素治疗后所致严重出血情况下的肝素灭活。体外循环或血液透析后，对肝素起灭活作用。

〔用法与用量〕

应用鱼精蛋白(罗氏)开始时实际上是在体外以1ml鱼精蛋白(罗氏)中和1000U肝素或肝素钠(商品名)的作用。

鱼精蛋白5000(罗氏)中和肝素5000U。然而鱼精蛋白的实际需要量取决于在血中循环的肝素量，即取决于所用的(Liqueniu)量多少以及注射后到血液中消失的时间。如不了解血中肝素的水平，建议最初所用鱼精蛋白用量不要超过1ml1000(罗氏)。最安全的措施只能是保持凝血酶时间正常才能使用鱼精蛋白，这种方法可避免本品过量。

通常对极少数病例治疗因肝素而引起的出血时，所需鱼精蛋白的剂量(罗氏)是最近所给与肝素剂量的50%(国际单位计算)。如肝素是静脉给药，那么鱼精蛋白的总量给予1000(罗氏)如肝素是皮下注射应静脉注射少部分拮抗剂，而大部分是以鱼精蛋白5000(罗氏)经肌肉途径给予。体外循环应用之后，为灭活肝素作用，根据所需要的剂量，鱼精蛋白1000(罗氏)，或鱼精蛋白5000(罗氏)两者均可使用。应根据反复的凝血试验(凝血酶时间、复钙时间)确定剂量。

鱼精蛋白(罗氏)不能中和双香豆素型抗凝剂的作用。

〔副作用〕

鱼精蛋白(罗氏)耐受良好。在极少数情况下，对鱼精蛋白敏感的病人可产生不耐性，可能引起休克。

实际临床经验表明，所需鱼精蛋白(罗氏)药量最好是用100～200ml生理盐水缓慢的静脉输注给药。

因为鱼精蛋白(罗氏)是一种抗凝血酶原激活酶。单独应用时能起抗凝血作用，并可引起出血。因此，用于中和肝素时，应小心，以避免鱼精蛋白过量。

〔包装〕

鱼精蛋白1000(罗氏)供静脉注射用：1安瓿含5ml

鱼精蛋白5000(罗氏)供静脉注射用：1安瓿含5ml

药物：存放在防止儿童拿到的地方。

〔生产厂家〕

瑞士巴塞尔豪夫迈罗氏公司

【外文释文】：

ROCHE

Heparin antagonist

Composition

Protamine hydrochloride：two strengths of solution are available，both in ampoules of 5 ml：

Protamine 1000(Roche)，1 ml of which neutralizes 1000 U of heparin．

Protamine 5000(Roche)，1 ml of which neutralizes 5000 U of heparin．

Properties

Protamines are simple proteins consisting of a relatively small number of aminoacids，the main one of which is arginine．Protamines are obtained from the testes of various species of salmon．

Protamines combine with heparin to form insoluble salts having no anticoagulant activity，Protamine is itself an antithromboplastin and so can exert an anticoagulant action when administered alone．

Indications

Inactivation of heparin in cases of severe haemorrhage following intravenous or subcutaneous administration of heparin．Inactivation of heparin following the use of extracorporeal circulation and haemodialysis．

Dosage and administration

The starting point for the administration of Protamine(Roche)is the fact that，in vitro，1 ml protamine 1000(Roche)neutralizes the action of 1 000 U heparin or(Liquemin)(Trade Mark)．

Protamine 5000(Roche)neutralizes the action of five times this quantity of heparin．

The amount of Protamine(Roche)actually required，however，depends on the amount of heparin circulating in the blood，i．e．，on the size of the dose of(Liquemin)administered and on the time that has elapsed since the injection，If the heparin level is unknown，it is recommended that not more than 1 ml Protamine l000(Roche)be administered iv，initially．The safest procedure is to administer Protamine only as long as it still normalizes the thrombin time，in this way，an excess of protamine can be avoided．

As a general guide，in the rare cases where it is necessary to treat haemorrhage caused by heparin，the dose of Protamine(Roche)to be administered is 50% of the last dose(in U)of heparin given．If the heparin was given intravenously，the whole dose should be administered intravenously in the form of Protamine 1000(Roche)；if the heparin was given subcutaneously，a small part of the antagonist should be administered intravenously and the larger part in the form of Protamine 5000(Roche)by the intramuscular route．

For inactivating heparin following the use of extracorporeal circulation，either Protamine 1000(Roche)or Protamine 5000(Roche)can be used，depending on the dose required．This dose should be determined on the basis of repeated blood coagulation tests(thrombin time，recalcification time)．

Protamine(Roche)dose not neutralize the action of anticoagulants of the coumarin type．

Side effects

Protamine(Roche)is well tolerated．In very rare cases，Protamine may in susceptible patients produce signs of intolerance，possibly resulting in shock．

Practical experience has shown that amount of Protamine(Roche)required is best administered slowly by iv infusion after diluting with 100-200 ml physiological saline．

Being an antithromboplastin，Protamine(Roche)can exert an anticoagulant action when administered alone and may produce haemorrhage．When used to neutralize heparin therefore，care should be taken to avoid an excess of Protamine．

Packs

Protamine 1000(Roche)for intravenous injection 1 ampoule 5ml

Protamine 5000(Roche)for intramuscular injection 1 ampoule 5ml

Medicine：keep out of reach of children．

Manufacturer

F．Hoffmann-La Roche Co．Ltd．，Basle，Switzerland