What Is Alteplase?

Alteplase is a thrombolytic drug. The main component is glycoprotein, which contains 526 amino acids. It is mainly used in clinical treatment 1. for acute myocardial infarction and pulmonary embolism; 2. for acute ischemic stroke, deep vein thrombosis and other vascular diseases.

Chinese name: Alteplase

Foreign name: Alteplase
Alias: Alteplase, alteplase

Alteplase classification

Primary classification: Circulatory drugs. Secondary classification: Antithrombotic drugs. Third classification: Thrombolytic agents.

Alteplase drug name

Chinese name: alteplase

English name: Alteplase

Drug aliases: ateplase, atprese, suppository, tissue plasminogen activator, tissue plasminogen activator, recombinant tissue plasminogen activator, recombinant tissue plasmin Enzyme activator, Altonic, Human Tissue Plasminogen Activator, Acetivase, Alteplase, G-11021, G-11021 (Z-ChainForm), tissue-type plasminogen activator, t-PA, Plasvata, rt-PA ^[1]

Alteplase drug dosage form

Injection (powder): 20mg, 50mg.

Alteplase pharmacological effects

This medicine is a thrombolytic medicine, the main component is glycoprotein, containing 526 amino acids. The drug can bind fibrin through its lysine residues, and activate fibrinogen-bound plasminogen to transform into plasmin, which is significantly stronger than plasminogen in the activation cycle of the drug. Because this drug selectively activates plasminogen, it does not produce the bleeding complications common when using streptokinase. For acute myocardial infarction, intravenous administration of this drug can reopen obstructed coronary arteries ^[2-3] .

Alteplase pharmacokinetics

This drug is quickly eliminated from the blood after intravenous injection. After 5 minutes of administration, 50% of the total dose is eliminated from the blood. After 10 minutes of administration, the remaining amount in the body accounts for only 20% of the total dose; after 20 minutes of administration, the The remaining 10%. This medicine is mainly metabolized in the liver ^[1] .

Alteplase indication

1. For acute myocardial infarction and pulmonary embolism ^[3] .

2. For acute ischemic stroke, deep vein thrombosis and other vascular diseases. For arteriovenous fistula thrombosis ^[2] .

Alteplase contraindications

1. Hemorrhagic diseases (such as severe internal hemorrhage, cerebral hemorrhage in the near future, or craniocerebral surgery within 2 months, severe trauma or major surgery within 10 days, severe uncontrolled primary high Blood pressure, pregnancy and 14 days postpartum, women, patients with bacterial endocarditis and acute pancreatitis).

2. Patients with intracranial tumors, arteriovenous malformations or aneurysms ^[3] .

3. Patients with known hemorrhagic constitution (including using warfarin, having used heparin within 48 hours before stroke, and having a platelet count of less than 100,000 / mm ³ ).

4. Acute ischemic stroke may be accompanied by subarachnoid hemorrhage or epileptic seizures ^[1-2] .

Alteplase considerations

1. Use with caution: (1) patients with cerebrovascular disease; (2) patients with hypertension; (3) patients with acute pericarditis; (4) patients with severe liver dysfunction; (5) patients with infectious thrombophlebitis; (6) ) Elderly patients (greater than 75 years old); (7) patients taking oral anticoagulants; (8) active menstrual bleeding. 2. Electrocardiogram should be monitored during medication. 3. This drug can not be compatible with other drugs for intravenous drip, nor can it be shared with other drugs for intravenous drip. 4. Foreign data reports that the solutions compatible with this drug are: (1) glucose solution or sodium chloride: 500 g / ml of this drug can be added to a 5% glucose solution or a 0.9% sodium chloride solution. Stable in glass or polyvinyl chloride container for 8 hours; (2) Sterile water for injection: Sterile water for injection has no bacteriostatic effect, and can be used to prepare alteplase at a concentration of 1 mg / ml, but it is not used as a further step. Of dilution. 5. Foreign data report that the solutions that are incompatible with this drug are: (1) bacteriostatic water for injection: benzyl alcohol bacteriostatic water for injection and parabens bacteriostatic water for injection are not used to formulate alteplase Solution; (2) Balanced salt solution: The balanced salt solution is mixed with the drug, and precipitation occurs within 24 hours at room temperature. If it is left at -20 ° C for 24 hours, the light scattering after melting increases, which indicates that the drug has changed. 6. When the patient's prothrombin time exceeds 15 seconds, the simultaneous use of this drug and oral anticoagulants is prohibited. 7. Bleeding at the injection site can be seen when using this medicine, but it does not affect continued medication, and should be discontinued if signs of bleeding are found. 8. The maximum daily dose of this drug should not exceed 150mg, otherwise it will increase the risk of intracranial hemorrhage ^[2] .

Alteplase adverse reactions

1. Blood system: Bleeding is the most common. The types of bleeding associated with thrombolytic therapy include gastrointestinal, urogenital, retroperitoneal, or intracranial bleeding. Superficial or superficial bleeding mainly occurs at the site of invasive procedures (such as vein incisions, arterial punctures, recently done The surgical site). In addition, epidural and subfascial hematomas have been reported. Systemic fibrinolysis is rarer than with streptokinase, but the incidence of bleeding is similar. 2. Cardiovascular system: (1) Arrhythmia: When using this medicine to treat acute myocardial infarction, reperfusion arrhythmia can occur during revascularization, such as accelerated ventricular autonomic rhythm, bradycardia or ventricular premature beats. These reactions are usually benign and can be controlled by standard antiarrhythmic treatments, but they may cause re-myocardial infarction and enlargement of the infarct size. The incidence of arrhythmias is similar to that of intravenous streptokinase. (2) Reocclusion of blood vessels: After the blood vessels are opened, continue to use anticoagulation with heparin, otherwise blood clots may form again, resulting in reocclusion of blood vessels. Cholesterol crystal embolism has been reported after thrombolytic therapy with this drug. 3. Central nervous system: intracranial hemorrhage and seizures may occur. 4. Urogenital system: There are reports of retroperitoneal hemorrhage caused by renal angiomyolipoma immediately after administration. 5. Skeletal / muscular system: Knee hemorrhagic synovitis can occur. 6. Others: allergic reactions ^[2] .

Alteplase dosage

1. Intravenous injection: Dissolve 50 mg of this drug to a concentration of 1 mg / ml and administer it by injection. 2. Intravenous infusion: Dissolve 100 mg of this drug in 500 ml of physiological saline for injection, and complete the drip in the following way within 3 hours, that is, inject 10 mg of this drug in the first 2 minutes, inject 50 mg in the next 60 minutes, and finish the remaining in the last 120 minutes 40mg. 1. Front loading method: The total dose is 100mg, 15mg is injected by bolus, then 50mg is intravenously infused within 30min, and the remaining 35mg is intravenously infused within 1h. 2. According to the weight method: firstly inject 15mg by intravenous bolus, then intravenously inject 0.75mg / kg in 30min, and then intravenously inject 0.5mg / kg in 1h. 3. Two bolus method: a total of 100mg, divided into two intravenous bolus injections, with an interval of 30min, this method can have a recanalization rate of 88% ^[2] .

Corresponding effects of alteplase drugs

1. When co-administered with other drugs that affect blood coagulation (including acenocoumarol, anisindione, biscoumarin, phenylindanedione, warfarin, heparin), it will significantly increase the risk of bleeding. 2. When combined with etibeptide, the risk of bleeding is increased due to the additional anticoagulant effect. 3. Nitroglycerin can increase the blood flow of the liver, thereby increasing the clearance rate of the drug, reducing the plasma concentration of the drug, reducing coronary reperfusion, prolonging reperfusion time, and increasing reocclusion ^[2] .

Alteplase expert review

This product has the function of promoting the fibrinolytic system activity in the body, but unlike streptokinase and urokinase, this product can specifically convert plasminogen in the thrombus to plasmin, thereby exerting the function of dissolving the thrombus. It is mostly used in clinical treatment of various freshly formed thrombi. This product exists in serine proteases in vascular endothelial cells and tissues, which can selectively bind to fibrin on the surface of thrombus and activate fibrinogen-bound plasminogen to transform into plasmin. This product has strong affinity for fibrin due to its two cyclic structures, so it can selectively activate plasminogen in the thrombus after administration, and then play a thrombolytic effect. Because this product selectively activates plasminogen that binds to fibrin, it does not produce the bleeding complications common when using streptokinase. It is mainly used to treat acute myocardial infarction and pulmonary embolism ^[1-2] .