部份中文甲磺酸萘莫司他处方资料（仅供参考）
药品英文名
Nafamostat
药品别名
甲磺酸萘莫司他、FUT、Futhan、Nafamostat Mesilate
药物剂型
注射剂：10mg。
药理作用
本药为合成的丝氨酸蛋白水解酶抑制药，具有抗凝、抗纤维蛋白溶酶和抗血小板聚集的作用。具体作用特点如下：
1.酶抑制作用：本药对胰蛋白酶、激肽释放酶(血管舒缓素)、血纤维蛋白溶酶、纤维蛋白酶以及补体系统经典途径的CL-r、CL-s等胰蛋白酶样丝氨酸蛋白酶有很强的选择性抑制作用；对磷脂酶A2也有抑制作用。体外对与α2-巨球蛋白结合的胰蛋白酶也有抑制作用。
2.对实验性急性胰腺炎的作用：大鼠和兔静脉滴注本药，对胰蛋白酶、肠激酶以及内毒素经胰管逆行注入而引起的各种实验性胰腺炎，可抑制由胰腺炎引起的胰酶活性上升以及进入血中的酶的活性，并降低死亡率。
3.对激肽释放酶-激肽系统的作用：对胰腺炎患者给予本药，可改善由激肽释放酶激活引起的激肽原总量的减少。
4.对血液凝固与纤维蛋白溶解系统的作用：本药通过抑制纤维蛋白酶和凝血因子Ⅻa和Ⅹa而产生抗凝作用。体外实验还发现，本药可抑制血小板聚集。动物实验中，本药静脉给药可使兔被激活的部分凝血活酶(凝血激酶)时间以及尿激酶激活的纤维蛋白块溶解时间延长。由于肝素有增加出血的危险性，故本药可作为肝素的替代物。
5.对补体系统的作用：对于静脉注射溶血素引起的全身性福斯曼嗜异性休克的豚鼠，口服及静脉注射本药均能延长其生命。
药动学
健康男子在90min内静脉滴注本药10mg、20mg和40mg，60～90min内血药浓度达峰值，分别为16.4ng/ml、61.5ng/ml和93.2ng/ml。在各组织中分布的药物浓度由高至低依次为肾、肝脏、肺及胰，均大于血药浓度。本药从血液中清除迅速，停药后1h血药浓度下降至5ng/ml以下，给药后4h仅从肝脏中可检出。药物主要在血和肝脏中代谢，由肾脏排泄。
适应证
1.用于急性胰腺炎、慢性胰腺炎急性恶化。
2.也用于血液透析、冠状动脉搭桥术、肝脏切除术时的抗凝，以及肾小球肾炎伴系统性红斑狼疮或混合型冷球蛋白血症(Cryoglobulimemia)。
禁忌证
对本药过敏者。
注意事项
1.本药粉针剂溶解后应立即使用。出现皮疹、红斑、瘙痒等过敏症状时，应停药。出现休克症状时应立即停药。
2.慎用：
(1)过敏体质者。
(2)有过敏史者。
(3)活动性出血(可因持续输注本药而增加出血的危险性)者。
(4)严重高血压(增加脑出血的危险性)患者(国外资料)。
(5)严重血小板减少症(增加出血的危险性)患者(国外资料)。
(6)高钾血症(使用本药可能加重高钾血症)患者(国外资料)。
(7)小儿。
3.药物对妊娠的影响：孕妇慎用本药。
4.药物对哺乳的影响：哺乳妇女慎用本药。
5.用药前后及用药时应当检查或监测：
应定期监测：
(1)血常规、血小板计数及血清钾。
(2)激活的部分凝血活酶时间(APTT)、活化全血凝固时间(ACT)、凝血因子Ⅱ时间(PT)、凝血酶-抗凝血酶复合物(TAT)、α2纤溶酶抑制物-纤溶酶复合物(PIC)、凝血因子Ⅰ和纤维蛋白降解产物(FDP)。       
不良反应
未见严重的不良反应。主要不良反应有：
1.过敏反应：皮疹、红斑、瘙痒等(1.7%)。
2.消化系统：恶心、腹泻(0.3%)等胃肠道反应，也可出现丙氨酸氨基转移酶、天门冬氨酸氨基转移酶升高(0.5%)。
3.血液：白细胞减少和血小板增加。
4.局部：注射部位红肿、疼痛较少见。
5其他：胸部不适、头痛等。
国外不良反应参考：
1.血液：连续血液透析的患者使用本药抗凝时可引起出血(发生率为4%)，但发生率明显低于使用肝素(67%)和低分子肝素者(29%)。也有引起嗜酸性粒细胞增多的报道，停药后即恢复正常。
2.中枢神经系统：罕见头痛和倦怠，但与本药的因果关系尚不明确。
3.代谢/内分泌系统：有引起高钾血症的报道。
4.胃肠道：畏食、恶心、呕吐罕见，与本药的因果关系尚不明确。
5.其他：有引起过敏反应的个案报道。        
用法用量
1.成人常规剂量：静脉滴注：一次10mg，溶于5%葡萄糖注射液500ml中静脉滴注2h，一日1～2次。根据病情适当增减剂量。
2.儿童常规剂量：体外循环：接受体外膜式氧合(Extracorporeal membraneoxygenation)的新生儿，可用本药(加小剂量肝素)降低血液并发症。平均剂量为每小时0.48mg/kg(剂量范围为每小时0.29～1.1mg/kg)。
药物相应作用
尚不明确。
Name of drug classification
Proteolytic enzyme inhibitor
Sales name
Nafetat for Injection
composition
Nafetat for Injection
It contains 100 mg of nafamostat mesilate in one vial.
200 mg of D-mannitol as an additive, and a pH adjusting agent.
Contraindication
Patients with a history of hypersensitivity to the ingredients of this drug
Indication or effect
Painful intravascular coagulation (DIC)
Prevention of coagulation of perfused blood during extravascular circulation of hemorrhagic lesions or bleeding tendencies (hemodialysis and plasmapheresis)
When used for general intravascular coagulation (DIC)
Normally, the daily dose is dissolved in 1,000 mL of 5% glucose injection, and 0.06 - 0.20 mg / kg per hour as nafamostat mesilate is continuously infused intravenously over 24 hours.
When used for preventing coagulation of perfused blood during extravascular circulation of patients with hemorrhagic lesions or bleeding tendencies
Normally, prior to the start of extracorporeal circulation, 20 μl of nafamostat mesilate is dissolved in 500 ml of physiological saline to wash and fill the inside of the blood circuit. After starting the extracorporeal circulation, Nafamostat mesilate is added at 20 - Dissolve 50 mg in 5% glucose injection and continue injection from anticoagulant injection line.
Incidentally, increase or decrease appropriately according to symptoms.
Preparation of injection solution
When using this drug, prepare injection solution according to the following procedure.
When used for general intravascular coagulation (DIC)
Add 1 mL or more of 5% dextrose injection or water for injection to 1 vial of this drug and dissolve completely.
Melt the dissolved solution into 5% dextrose injection.
When used for preventing coagulation of perfused blood during extravascular circulation of patients with hemorrhagic lesions or bleeding tendencies
Cleaning and filling in the blood circuit
Add 10 mL of 5% dextrose injection or water for injection to 1 vial of this drug and dissolve completely.
Mix the lysis solution containing 20 mg Nafamostat mesilate salt in physiological saline.
Extracorporeally
Add 10 mL of 5% dextrose injection or water for injection to 1 vial of this drug and dissolve completely.
Dissolve the dissolved solution to the volume of anticoagulant sustained injector and dilute with 5% dextrose injection.
Caution on dissolving
Since white turbidity or crystals may be precipitated, a solution containing physiological saline or inorganic salts should not be added directly to the vial.
Serious side effects
Shock, anaphylactoid symptoms (Frequency unknown)
As shock and anaphylactoid symptoms may occur, observe thoroughly and observe the blood pressure decrease, consciousness disturbance, dyspnea, bronchial asthma attack, wheezing, chest discomfort, abdominal pain, vomiting, fever, cold sweat, itching, flushing , Redness, numbness etc. appears immediately, discontinue administration and take appropriate measures.
Hyperkalemia (Frequency unknown)
Hyperkalemia may occur, so observe thoroughly especially when using potassium-containing preparations (infusion etc.), potassium holding diuretics and the like, especially if abnormalities are found, immediately administer it Discontinue and take appropriate measures.
An example of inducing arrhythmias by the expression of hyperkalemia has been reported.
Hyponatremia (Frequency unknown)
Since hyponatremia may occur, if abnormalities are observed, administration should be discontinued and appropriate measures should be taken.
Thrombocytopenia (frequency unknown)
Since thrombocytopenia may occur, observation such as blood test should be performed sufficiently, and if abnormality is observed, administration should be discontinued and appropriate measures should be taken.
Leukopenia (Frequency unknown)
As leukopenia may occur, observe blood tests thoroughly, if abnormalities are observed discontinue administration and take appropriate measures.
Liver dysfunction, jaundice (frequency unknown)
Liver dysfunction accompanied by elevation of AST (GOT), ALT (GPT), γ-GTP etc., jaundice may appear, so observe thoroughly and if abnormality is found, discontinue administration To carry out Do treatment.
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