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OverviewMechanism of ActionHow To UseUsesBenfitsIndicationsDosage StrengthsDosage FormsDietary RestrictionsContraindicationsWarnings and Precautions for usingAdverse ReactionsOverdosage Clinical Pharmacology Clinical StudiesAuthored by Reviewed by References
Urokinase

Urokinase

Indications, Uses, Dosage, Drugs Interactions, Side effects
Urokinase
Medicine Type :
Allopathy
Prescription Type:
Prescription Required
Approval :
DCGI (Drugs Controller General of India)
Schedule
Schedule H
Pharmacological Class:
Thrombolytic class,
Therapy Class:
Anticoagulant,

Urokinase is an Anticoagulant agent belonging to the Thrombolytic class.

Urokinase is used in the treatment of pulmonary embolism and myocardial infarction, as well as to clear IV lines.

Urokinase is delivered intravenously, so the bioavailability is high and is rapidly cleared from the circulation by the liver and gets excreted mainly via urine; feces (small amounts). With an elimination half-life of 10-20 minutes.

The onset of Action of Urokinase is IV: Rapid (fibrinolysis).

The Duration of action of Urokinase is 12-24 hours

The Tmax of Urokinase was about 1-2 h after dosing.

The common side effects are dizziness, drowsiness, headache, weakness, Nausea, strong irregular heartbeat, swelling, and dizziness upon standing.

Urokinase is available in a dosage form, such as injection.

Urokinase is available in the USA, UK, Canada, Japan, and India.

Urokinase is a thrombolytic enzyme produced by the kidney and is extracted from human urine. It converts plasminogen to plasmin, thereby degrading fibrin, fibrinogen, and other procoagulant plasma proteins.

Urokinase is available in the form of a dosage form, such as an injection.

Urokinase is injected into a vein through an IV. A healthcare provider will give you this injection. Urokinase is given slowly, usually over a period of 12 hours, using a continuous infusion pump.

Urokinase is used in the treatment of pulmonary embolism and myocardial infarction, as well as to clear IV lines.

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

Urokinase is approved for its use in the following clinical indications:

  • Restoration of patency of intravascular catheters (central venous catheters and dialysis Catheters), blocked by a forming or recently formed Thrombus (extension of indication).
  • Treatment of arterial and venous occlusions caused by a forming or recently formed Thrombus, of pulmonary emboli, in particular when a recent thrombolytic treatment by Urokinase contraindicates its use.

Urokinase is available in various dosage strengths: 250000 intl units; 5000 intl units; 9000 intl units.

Urokinase is available in the form of a dosage form, such as an injection.

Urokinase is approved for the treatment of Myocardial Infarction:

Consume a diet high in vegetables, fruits, whole grains, low-fat dairy products, poultry, fish, legumes, non-tropical oils, and nuts, and reduce your intake of sweets, sugar-added beverages, and red meats. Limit saturated fat to 5-6% of calories. Reduce trans-fats. Consume no more than 2,400 mg/day of sodium.

Urokinase may be contraindicated in the following.

Active internal or clinically relevant bleeding, aneurysm, arteriovenous malformation, intracranial neoplasm or other neoplasms with risk of hemorrhage, known coagulation disorder (e.g., hemorrhagic diathesis), severe thrombocytopenia, recent severe gastrointestinal bleeding, severe uncontrolled hypertension (systolic >200 mmHg, diastolic >100 mmHg; grade III or IV hypertensive retinopathy), sepsis, acute pancreatitis, pericarditis, acute bacterial endocarditis. Recent CVA, trauma (including CPR), thoracic surgery, or neurosurgery (within two months); recent major surgery until primary wound healing; recent organ biopsy, lumbar puncture, or translumbar aortography (within ten days); recent obstetric delivery. Severe hepatic and renal impairment (unless the patient is receiving renal replacement treatment).

Pregnancy Warning

Pregnancy

Pregnancy Category B: Reproduction studies have been performed in mice and rats at doses up to 1,000 times the human dose and have revealed no evidence of impaired fertility or harm to the fetus due to urokinase injection. There are, however, no adequate and well-controlled studies on pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Food Warning

Salt Substitutes: Those who are taking Urokinase should avoid sodium, calcium, and magnesium-rich foods. The salts may reduce the blood-pressure-lowering effect of Urokinase.

The adverse reactions related to molecule Urokinase can be categorized as:

  • Common Adverse Effects: Haemorrhage, potential risk of transmission of infection, embolism including pulmonary or cholesterol embolism, infusion reactions (e.g., fever, chills, rigors). Rarely allergic reactions (e.g., bronchospasm, rash). Gastrointestinal disorders: Gingival bleeding, gastrointestinal or retroperitoneal hemorrhage, nausea, vomiting.
  • Less Common adverse effects: Gingival bleeding, gastrointestinal or retroperitoneal hemorrhage, nausea, vomiting.
  • Rare Adverse effects: Haematuria (microscopic), urogenital hemorrhage.

The clinically relevant drug interactions of Urokinase are briefly summarized here.

Thrombolytic agents, anticoagulants, or agents that affect platelet function (e.g., aspirin and other NSAIDs, dipyridamole, and dextrans) may further increase the risk of significant hemorrhage. Fibrinolysis may be delayed by contrast agents. It may enhance the risk of angioedema with ACE inhibitors.

Symptom: Hemorrhage.

Management:

Hemorrhage during therapy may be controlled with local pressure. Administer inhibitors (e.g., aprotinin, epsilon-aminocaproic acid, p-aminoethylbenzoic acid, tranexamic acid) in severe bleeding. Give human fibrinogen; factor XII packed RBC, or whole blood as necessary during serious cases.

Pharmacodynamics:

Urokinase is a serine protease that activates plasminogen into an active fibrinolytic protease. The Duration of action is short due to the short half-life. Patients should be counseled regarding the risk of bleeding, anaphylaxis, infusion reactions, and cholesterol embolization.

Pharmacokinetics:

  • Metabolism: IV: Rapidly cleared from the circulation by the liver.
  • Excretion: Mainly via urine; feces (small amounts). Elimination half-life: 10-20 minutes.
There are some clinical studies of the drug Urokinase mentioned below:
  1. https://clinicaltrials.gov/ct2/show/NCT00532493
  2. https://pubmed.ncbi.nlm.nih.gov/29414272/
  3. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3538493/
           4. https://ajp.psychiatryonline.org/doi/10.1176/appi.ajp.2018.17080913
  1. https://www.mims.com/india/drug/info/Urokinase ?type=full&mtype=generic
  2. https://go.drugbank.com/drugs/DB00590
  3. https://www.rxlist.com/consumer_Urokinase _cardura/drugs-condition.htm
  4. https://reference.medscape.com/drug/cardura-xl-Urokinase -342343
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Parthika Patel
Parthika Patel has completed her Graduated B.Pharm from SSR COLLEGE OF PHARMACY and done M.Pharm in Pharmaceutics. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751
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Dr JUHI SINGLA
Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow Medical college and done MD pharmacology from SGT UNIVERSITY Gurgaon. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751
Published on: 29 Oct 2022 7:53 PM GMT
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