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Urokinase information from DrugsUpdate  

See Available Brands of Urokinase in India

P - Contraindicated in pregnancy

Urokinase (Abbokinase), also called urokinase-type Plasminogen Activator (uPA), is a serine protease (EC 3.4.21.73). Urokinase was originally isolated from human urine, but is present in several physiological locations, such as blood stream and the extracellular matrix. The primary physiological substrate is plasminogen, which is an inactive zymogen form of the serine protease plasmin. Activation of plasmin triggers a proteolysis cascade which, depending on the physiological environment participate in thrombolysis or extracellular matrix degradation. This links urokinase to vascular diseases and cancer.

Pharmacodynamics

Pharmacokinetics

Urokinase, an enzyme isolated from human urine, directly converts plasminogen into plasmin, which is a proteolytic enzyme with fibrinolytic effects. It is a fibrin non-specific thrombolytic as it affects both unbound and fibrin bound plasminogen.

Metabolism
Hepatic; rapidly cleared from the circulation after IV administration.

Excretion
20 min (elimination half-life).

Urokinase Indications / Urokinase Uses

Information Not Available

Urokinase Adverse Reactions / Urokinase Side Effects

Bleeding, pyrexia, haematuria, thromboembolic episodes, hypersensitivity reactions.

Potentially Fatal: Severe bleeding, anaphylaxis.

Precautions

Urokinase can cause bleeding that usually is not serious. However, serious bleeding may occur in some people.


Overdosage


Symptoms: Haemorrhage. Management: Inhibitors such as tranexamic acid can be given. In serious cases, human fibrinogen, Factor XII, packed red cells or whole blood may be given as needed. Avoid using dextran for volume deficiency correction.


 

Special Precautions

Any vascular punctures or invasive procedures should be avoided as far as possible during, and immediately before and after urokinase therapy and if unavoidable done with great care. External chest compression. Caution in conditions eg, possibility of left heart thrombus, subacute bacterial endocarditis, coagulation defects, cerebrovascular disease, diabetic retinopathy and any conditions in which bleeding could be dangerous. Monitor for reperfusion arrhythmias when used in MI.

Other Drug Interactions

Reduced thrombolytic effect when given again some time later due to development of high levels of antibodies.

Potentially Fatal: Platelet inhibitors eg, aspirin and indometacin can potentiate the action of urokinase and cause haemorrhage. Heparin and oral anticoagulants may increase risk of bleeding.

Other Interactions

Information Not Available

Dosage

Intravenous
Deep vein thrombosis
Adult: Initially, 4400 units/kg dissolved in 15 ml of sodium chloride 0.9%, infused IV over 10 minutes followed by 4400 units/kg/hr for 12-24 hr.

Intravenous
Peripheral arterial thromboembolism
Adult: As solution containing 2000 units/ml: Infuse into the clot via a catheter at a rate of 4000 units/minute for 2 hr. Monitor response using angiography. If clot is not removed, advance the catheter into the occluded vessel and continue infusion at the same rate for another 2 hr. May repeat procedure, if needed, up to 4 times. Once blood flow is re-established, partially withdraw the catheter and continue infusing at 1000 units/minute until the remaining clot has lysed.

Intravenous
Pulmonary embolism
Adult: Initially, 4400 units/kg dissolved in 15 ml sodium chloride 0.9%, infused over 10 min followed by 4400 units/kg/hr for 12 hr. Alternatively, 15000 units/kg as bolus Inj into the pulmonary artery; may repeat inj, adjust dose according to plasma fibrinogen concentrations up to 3 times in 24 hr.

Parenteral
Acute myocardial infarction
Adult: 6000 units/min infused into the coronary artery for 2 hr preceded by IV heparin. Alternatively, 2-3 million units IV is given over 45-90 min.

Irrigation
Break down of clots in hyphaema
Adult: To prepare the solution: Dissolve 5000 units in 2 ml of sterile distilled water. Irrigate the anterior chamber slowly with 0.3 ml of the solution; leave solution in situ for 3 minutes and then wash out with saline. Repeat procedure 5 times. If residual clot is still present at the end of the treatment, leave 0.3 ml of the solution in the anterior chamber for 24-48 hr.

Injection
Clearance of occluded catheters and shunts
Adult: 5000 - 25000 units in 2 ml sodium chloride 0.9% instilled into affected IV catheter or shunt and clamped for up to 4 hr. Aspirate the lysate and repeat the procedure if needed. Alternatively, infuse a solution containing 5000 units of urokinase in 200 mL of sodium chloride 0.9% into the device over 30 minutes.

Food(before/after)

Information Not Available

List of Contraindications

Urokinase and Pregnancy

Contraindicated in pregnancy.


Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Urokinase and Lactation

Information Not Available

Urokinase and Children

Information Not Available

Urokinase and Geriatic

Information Not Available

Urokinase and Other Contraindications

Active internal bleeding; history of cerebrovascular accident; recent (within 2 mth) trauma of any kind including surgery; aneurysm; known bleeding diathesis; severe uncontrolled hypertension. Recent history of peptic ulcer disease, oesophageal varices, ulcerative colitis or other bleeding GI lesions; pancreatitis; subacute bacterial endocarditis; coagulation defects including those due to liver or kidney disease, or after recent surgery, childbirth or trauma. Increased risk of cerebral bleeding e.g. recent stroke or cerebral neoplasm. Pregnancy.

Storage

Injection
Store below 25°C.

Intravenous

Store below 25°C.

Irrigation
Store below 25°C.

Parenteral

Store below 25°C.

Lab interference

Injection
Store below 25°C.

Intravenous

Store below 25°C.

Irrigation
Store below 25°C.

Parenteral

Store below 25°C.

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