阿尼普酶（茵香酞化纤溶酶原一链激酶激活剂）为纤溶酶原和链激酶激活剂复合物的乙酞化物。在体内经脱酞化作用，自发恢复激活纤溶酶原的作用。本品半衰期可延长到90min ，可快速静脉注射并延长溶栓作用时间，是治疗急性心肌梗死安全而有效的药物，可降低再阻塞率，改善左室功能，提高近期和远期存活率。本品对血凝块无选择性，大剂量可致低凝状态或出血。也可引起过敏反应。

通用名称：阿尼普酶

英文名称：Anistreplase

中文别名：前尿激酶

【药理作用】

Classification: Thrombolytic enzyme

Action/Kinetics: Prepared by acylating human plasma derived from lys-plasminogen and purified streptokinase derived from group C beta-hemolytic streptococci. When prepared, anistreplase is an inactive derivative of a fibrinolytic enzyme although the compound can still bind to fibrin. Anistreplase is activated by deacylation and subsequent release of the anisoyl group in the blood stream. The production of plasmin from plasminogen occurs in both the blood stream and the thrombus leading to thrombolysis. Lyses thrombi obstructing coronary arteries and reduces the size of infarcts. t1/2: 70-120 min.

【适应症】

Management of AMI in adults, resulting in improvement of ventricular function and reduction of mortality. Treatment should be initiated as soon as possible after the onset of symptoms of AMI.

【用法用量】

IV only: 30 units over 2-5 min into an IV line or vein as soon as possible after onset of symptoms.

【注意事项】

Pregnancy Category: C

Contraindications: Use in active internal bleeding; within 2 months of intracranial or intraspinal surgery; recent trauma, including cardiopulmonary resuscitation; history of CVA; intracranial neoplasm; arteriovenous malformation or aneurysm; known bleeding diathesis; severe, uncontrolled hypertension; severe allergic reactions to streptokinase.

Special Concerns: Use with caution in nursing mothers. Safety and effectiveness have not been determined in children. NOTE: The risks of anistreplase therapy may be increased in the following conditions; thus, benefit versus risk must be assessed prior to use. Within 10 days of major surgery (e.g., CABG, obstetric delivery, organ biopsy, previous puncture of noncompressible vessels); cerebrovascular disease; within 10 days of GI or GU bleeding; within 10 days of trauma including cardiopulmonary resuscitation; SBP > 180 mm Hg or DBP > 110 mm Hg; likelihood of left heart thrombus (e.g., mitral stenosis with atrial fibrillation); SBE; acute pericarditis; hemostatic defects including those secondary to severe hepatic or renal disease; pregnancy; clients older than 75 years of age; diabetic hemorrhagic retinopathy or other hemorrhagic ophthalmic conditions; septic thrombophlebitis or occluded arteriovenous cannula at seriously infected site; clients on oral anticoagulant therapy; any condition in which bleeding constitutes a significant hazard or would be difficult to manage due to its location.

【不良反应】

Bleeding: Including at the puncture site (most common), nonpuncture site hematoma, hematuria, hemoptysis, GI hemorrhage, intracranial bleeding gum/mouth hemorrhage, epistaxis, anemia, eye hemorrhage. CV: Arrhythmias conduction disorders, hypotension; cardiac rupture chest pain, emboli (causal relationship to use of anistreplase unknown). Allergic: Anaphylaxis, bronchospasm angioedema, urticaria, itching, flushing, rashes, eosinophilia, delayed purpuric rash which may be associated with arthralgia, ankle edema, mild hematuria, GI symptoms, and proteinuria. GI: N&V. Hematologic: Thrombocytopenia. CNS: Agitation, dizziness, paresthesia, tremor, vertigo. Respiratory: Dyspnea, lung edema. Miscellaneous: Chills, fever, headache, shock.

【相互作用】

Increased risk of bleeding or hemorrhage if used with heparin, oral anticoagulants, vitamin K antagonists, aspirin, or dipyridamole.