Uroquinasa

Uses

Uroquinasa injection is used for adults:

• For the lysis of acute massive pulmonary emboli, defined as obstruction of blood flow to a lobe or multiple segments.
• For the lysis of pulmonary emboli accompanied by unstable hemodynamics, i.e., failure to maintain blood pressure without supportive measures.

The diagnosis should be confirmed by objective means, such as pulmonary angiography or noninvasive procedures such as lung scanning.

Uroquinasa is also used to associated treatment for these conditions: Acute massive pulmonary embolism, Obstruction; Catheter, Infusion Catheter (Vascular), Pulmonary Embolism, Thromboembolism of the Coronary Artery, Thromboembolism of the Graft, Thromboembolism of the Peripheral Artery

How Uroquinasa works

Uroquinasa is a serine protease. It cleaves plasminogen to form the active fibrinolytic protease, plasmin.

Dosage

Uroquinasa dosage

Deep vein thrombosis: Initial loading dose of 4,400 IU/kg in 15 mL soln over 10 min, followed by 4,400 IU/kg/hr IV infusion for 12-24 hr.

Pulmonary embolism: Initial loading dose of 4,400 IU/kg in 15 mL soln over 10 min followed by 4,400 IU/kg/hr IV infusion for 12 hr.

Peripheral vascular occlusion: Infuse 2,500 IU/mL (500,000 IU in 200 mL) into clot at a rate of 4,000 IU/min for 2 hr.

Advance the catheter into the remaining occluded area & infuse at 4,000 IU/min for another 2 hr. This may be repeated up to 4 times.

Hyphaema: 5,000 IU in 2 mL saline soln is injected and withdrawn repeatedly over the iris. If residual clot remains, leave 0.3 mL in the anterior chamber for 24-48 hr to facilitate further dissolution.

Clotted arterio-venous shunts: Instill 5,000-25,000 IU into affected shunt limb & clamp for 2-4 hr, followed by aspiration of lysate. Repeat if necessary.

Side Effects

Overt bleeding, haemorrhagic complications, fever, haematuria, initial severe pain & dull ache in shunt limb.

Toxicity

Patients experiencing an overdose may present with bleeding. Treat patients with symptomatic and supportive measures which may include application of local pressure, administration of whole blood or plasma, and administration of aminocaproic acid.

Precaution

GI lesions & in multiple intracardiac or intravascular punctures as a consequence of cardiopulmonary resuscitation

Interaction

Concomitant use of oral anticoagulant or heparin & drugs that affect platelet function may increase risk of haemorrhage.

Food Interaction

• Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Uroquinasa Hypertension interaction

[Major] The use of thrombolytics is contraindicated in patients with an active bleed (internal), trauma

Risk versus benefit should be carefully considered in the following conditions and thrombolytic therapy administered with caution in patients with recent (10 days) serious GI bleed or recent (10 days) surgical procedure (coronary bypass graft, obstetrical delivery, organ biopsy, puncture of noncompressible vessel), left heart thrombus, subacute bacterial endocarditis, hemostatic defect, CV disease, diabetic hemorrhagic retinopathy, or pregnancy.

Clinical monitoring of hematopoietic, bleeding and coagulation functions is recommended prior to initiation of thrombolytic therapy.

Measures of fibrinolytic activity and

Uroquinasa Drug Interaction

Moderate: aspirinUnknown: spironolactone, sulfamethoxazole / trimethoprim, ubiquinone, copper gluconate, phenytoin, glycerin, sodium iodide, arginine, insulin isophane, acetaminophen, bioflavonoids, hydrocortisone, diazepam, valproic acid, thiamine, cyanocobalamin, pyridoxine, cholecalciferol, phytonadione

Uroquinasa Disease Interaction

Major: bleeding risksModerate: liver disease

Volume of Distribution

The volume of distribution of urokinase is 11.5L.

Elimination Route

Uroquinasa is delivered intravenously, so the bioavailability is high.

Half Life

Uroquinasa has a half life of 12.6±6.2 minutes.

Clearance

Data regarding the clearance of urokinase is not readily available.

Elimination Route

Uroquinasa is eliminated in the bile and urine.

Pregnancy & Breastfeeding use

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 1sttrimester (and there is no evidence of a risk in later trimesters).

Contraindication

Recent surgery or biopsy, severe HTN, severe hepatic or renal insufficiency. Pregnancy & immediate postpartum period.

Acute Overdose

If severe haemorrhage occurs, treatment with Uroquinasa-GCC must be stopped. Aprotinin and synthetic inhibitors eg, epsilon aminocaproic acid, tranexamic acid or p-aminomethylbenzoic acid can be used to inhibit the fibrinolytic action of Uroquinasa-GCC. In serious cases, human fibrinogen, Factor XIII, Cohn-Fraction I, packed red cells or whole blood can be given, as appropriate.

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