urokinase

Action and Spectrum

Actions and spectrum: 

urokinase is a thrombolytic enzyme that is used to break down blood clots. Its action involves the conversion of plasminogen to plasmin, which helps dissolve fibrin clots in the blood vessels.

urokinase is used to treat conditions such as deep vein thrombosis, pulmonary embolism, and other clot-related disorders. Its spectrum of action is primarily related to clot dissolution and thrombolysis. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Haemorrhage 

allergic reactions 

Gingival bleeding 

nausea 

Decreased haematocrit 

increased transaminases 

Acidosis 

Muscle haemorrhage 

Stroke 

Haematuria 

intracranial haemorrhage 

Epistaxis 

Hypoxaemia 

Cyanosis 

haematoma 

cerebral haemorrhage 

Thromboembolism 

artery dissection 

Black Box Warning

Black Box Warning: 

There was no specific black box warning associated with urokinase. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Active Bleeding Disorders: urokinase should not be used in individuals with active bleeding disorders, such as hemophilia, or any condition that increases the risk of bleeding. 
• Recent Surgery or Trauma: It may be contraindicated in individuals who have had recent major surgery or trauma, as there is an increased risk of bleeding at surgical sites. 
• Severe Hypertension: urokinase may not be suitable for people with uncontrolled high blood pressure (hypertension). 
• Known Allergy or Sensitivity: Individuals who have a known allergy or hypersensitivity to urokinase or any of its components should not use the medication. 
• Recent Stroke: urokinase should be used with caution or avoided in individuals who have had a recent stroke, especially hemorrhagic stroke. 
• Intracranial Aneurysms: It should be used with caution or avoided in individuals with intracranial aneurysms, as there is a risk of bleeding.

Caution: 

• Hypotension: urokinase can cause a drop in blood pressure. Caution is required when administering urokinase to individuals with low blood pressure or those at risk of hypotension. Blood pressure should be monitored during treatment. 
• Coagulopathies: Patients with coagulopathies or conditions that affect blood clotting should receive urokinase with caution, as it may exacerbate bleeding disorders. 
• Renal Impairment: urokinase is primarily eliminated through the kidneys. Caution is advised when using urokinase in patients with renal impairment, as it may require dose adjustment to prevent excessive drug accumulation. 
• Liver Impairment: Although urokinase’s primary clearance route is renal, liver impairment may affect its metabolism and elimination. Close monitoring may be necessary in patients with liver dysfunction.

Comorbidities: 

• Cardiovascular Disease: the cardiovascular disease, such as heart attack or stroke, may have compromised blood vessels or underlying conditions that affect blood clotting. urokinase, as a thrombolytic agent, can increase the risk of bleeding, and caution is needed when treating such patients. 
• Hypertension: High blood pressure can increase the risk of bleeding during urokinase therapy. Patients with uncontrolled hypertension should be carefully monitored during treatment. 
• Diabetes: Patients with diabetes may have impaired wound healing and an increased risk of infection. Careful monitoring of wounds and infection control is essential when using urokinase in diabetic patients. 
• Gastrointestinal Disorders: Patients with gastrointestinal ulcers or bleeding disorders may be at increased risk of gastrointestinal bleeding during urokinase therapy.  

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into human milk: unknown  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

urokinase is a thrombolytic agent used in medical settings to dissolve blood clots. Its pharmacology revolves around its ability to activate plasminogen, an inactive precursor, into plasmin, an enzyme responsible for breaking down fibrin, the protein that forms blood clots. urokinase primarily acts on the fibrin present in blood clots, initiating their dissolution. It is administered intravenously and has a short half-life, making its effects rapid. This pharmacological action is valuable in treating conditions like acute ischemic stroke, pulmonary embolism, and deep vein thrombosis, where the rapid dissolution of clots is critical to restoring blood flow and preventing further complications. 

Pharmacodynamics: 

The pharmacodynamics of urokinase revolve around its ability to activate the enzyme plasminogen to plasmin. Plasmin is a proteolytic enzyme that plays a crucial role in breaking down fibrin, a protein involved in the formation of blood clots. When administered, urokinase binds to plasminogen on the surface of fibrin clots and converts it into plasmin. Plasmin then cleaves the fibrin meshwork within the clot, leading to its dissolution. This process is known as thrombolysis and is the primary mechanism by which urokinase exerts its pharmacological effect.  

Pharmacokinetics: 

Absorption 

urokinase is typically administered intravenously, allowing for rapid and complete absorption directly into the bloodstream. 

Distribution 

Once in the bloodstream, urokinase is distributed throughout the body. It primarily acts on the site of blood clots where plasminogen is available. urokinase does not have significant tissue distribution like many other drugs. 

Metabolism 

urokinase itself is not metabolized in the body. It acts as an enzyme to catalyze the conversion of plasminogen to plasmin, as described in its pharmacodynamics. 

Elimination and excretion 

urokinase is eliminated from the body primarily through renal clearance. The kidneys filter it from the blood, and it is excreted in the urine. 

Adminstartion

Administration: 

• Preparation: urokinase is supplied as a sterile lyophilized powder in vials. Healthcare professionals must reconstitute the powder with a sterile diluent according to the manufacturer’s instructions to prepare the solution for injection. 
• Intravenous (IV) Infusion: urokinase is usually administered as a continuous intravenous infusion. It may be administered through a dedicated IV line or incorporated into an existing IV line.  
• Continuous Monitoring: During urokinase infusion, the patient is closely monitored for signs of bleeding or other adverse reactions. Monitoring may include vital signs, laboratory tests (such as clotting parameters), and frequent assessment of the infusion site for signs of complications. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: urokinase 

Pronounced: (yoo-roh-kai-neys)  

Why do we use urokinase? 

• Pulmonary Embolism: urokinase can help dissolve blood clots that have travelled to the lungs, a condition known as pulmonary embolism. 
• Deep Vein Thrombosis (DVT): DVT is the formation of clots in the deep veins, often in the legs. urokinase can be used to manage this condition. 
• Arterial Thrombosis: urokinase may be used in certain cases of arterial thrombosis, were clots form in arteries. This can include conditions like acute limb ischemia. 
• Catheter Clearance: urokinase can be used to clear obstructed catheters, such as central venous catheters or dialysis catheters, when blood clots form within them. 
• Myocardial Infarction: In some cases, urokinase may be used in the treatment of myocardial infarction (heart attack) to restore blood flow to the coronary arteries.