reteplase

Action and Spectrum

Actions and Spectrum: 

reteplase works by attaching to and activating the plasminogen enzyme, which is subsequently transformed into plasmin. An enzyme called plasmin cleaves the fibrin meshwork that keeps blood clots together, dissolving them. reteplase works by dissolving the clot and allowing blood flow to return to the injured region. 

reteplase’s therapeutic range is restricted to the management of pulmonary embolism and acute myocardial infarction. Deep vein thrombosis and stroke-related blood clots are not treated with it. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Cholesterol embolization, intracranial hemorrhage, anemia, gastrointestinal/ genitourinary bleeding  

Cardiogenic shock 

Muscle pain 

Reperfusion arrhythmias, hypotension 

Nausea, vomiting 

Cardiac reinfarction 

Injection site reaction, allergic reaction 

Fever, dizziness, severe headache 

Black Box Warning

Black Box Warning 

There is a black box warning on reteplase for the possibility of bleeding, which can be serious and occasionally deadly. reteplase should not be administered to patients who are actively bleeding or have a history of bleeding problems. 

The risk factors include recent surgery or trauma, uncontrolled hypertension, and stroke history. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Those who have previously had hypersensitivity to reteplase, other tissue plasminogen activators, or any of the formulation’s ingredients should not use reteplase. 

Caution: 

• reteplase should not be administered to patients who have a history of bleeding problems or who are presently suffering active bleeding. 
• If reteplase is taken, patients who recently underwent surgery or sustained trauma may have a higher risk of bleeding and should be properly monitored. 
• Those with severe hypertension should be closely watched while using reteplase since it can lower blood pressure. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: C 

Lactation: Excretion into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

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 available 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 

Tissue plasminogen activator (t-PA), an enzyme that encourages the dissolution of blood clots, is present in recombinant form as reteplase. It works as a thrombolytic agent by attaching to plasminogen and turning it into plasmin, which then breaks down fibrin, the major building block of blood clots. 

Pharmacodynamics 

reteplase’s pharmacodynamics are connected to how it functions as a thrombolytic drug. reteplase attaches to plasminogen, transforming it into plasmin, which subsequently breaks down fibrin, the primary building block of blood clots.

This encourages the clot to dissolve and aids in restoring blood flow to the injured region. As compared to other thrombolytic medications, reteplase has a very short duration of effect.  

Pharmacokinetics 

Absorption   

When reteplase is delivered intravenously, full bioavailability and a quick commencement of action are guaranteed. 

Distribution 

With a volume of distribution of around 0.07 L/kg, reteplase is dispersed throughout the body. To plasma proteins, it does not bind 

Metabolism 

The liver is where reteplase is mostly digested and divided into smaller pieces. reteplase’s precise metabolic routes are not fully understood. 

Elimination and excretion 

reteplase has a half-life of around 13 minutes and is mostly eliminated from the body through the kidneys. A dosage provided is eliminated unaltered in the urine in amounts of 20 to 30%. 

Adminstartion

Administration:  

In a hospital or clinical environment, reteplase is delivered as an intravenous (IV) injection. The dosage is usually administered as a single bolus injection and is determined by the patient’s weight. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: reteplase 

Why do we use reteplase? 

A thrombolytic drug called reteplase is used to treat pulmonary embolism (PE) and acute myocardial infarction (AMI). 

reteplase is used in AMI to dissolve blood clots in the coronary arteries, restoring blood flow to the heart muscle and minimising cardiac damage. 

reteplase is a medication used in PE to dissolve blood clots in the pulmonary arteries, which can aid with oxygenation and lower the risk of consequences.