tenecteplase

Action and Spectrum

Actions and Spectrum: 

tenecteplase is a plasminogen activator that specifically activates plasminogen at the location of the clot in order to work. The primary building block of blood clots, fibrin, is broken down by plasmin once it is triggered, which dissolves the clot. 

tenecteplase is used to treat blood clots in several medical diseases, such as deep vein thrombosis, pulmonary embolism, and acute myocardial infarction. Treatment of clots that have already developed and been there for a considerable amount of time is ineffective. 

Drug Interaction

Adverse Reaction

Frequency not defined  

Fever 

Cholesterol embolization 

Nausea 

Reperfusion arrhythmias 

Allergic reaction 

Myocardial Infarction 

Vomiting 

>10% 

Minor bleeding (22%) 

Black Box Warning

Black Box Warning 

The warning states that tenecteplase should be used with caution in patients with a high risk of bleeding, such as those who have recently undergone surgery or undergone trauma, those who have a history of bleeding disorders, or those who have additional medical conditions that raise the risk of bleeding, according to the warning.  

tenecteplase should not be administered to individuals who have internal bleeding that is currently active, such as gastrointestinal bleeding or cerebral haemorrhage. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• In individuals with ongoing internal bleeding, such as gastrointestinal bleeding or brain haemorrhage, it is contraindicated in patients with a history of hypersensitivity or an allergic reaction to tenecteplase. 
• it should not be used in individuals who have experienced a stroke, transient ischemic attack (TIA), cerebral tumour, arteriovenous malformation, or aneurysm within the past six months. 

Caution: 

• If patient undergone surgery or have experienced trauma, have a history of bleeding problems, have uncontrolled hypertension, severe liver or renal illness, or have recently experienced gastrointestinal bleeding or genitourinary haemorrhage, one should exercise caution. 
• Those over the age of 65 and those with low body weight should also utilise the medication with caution. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: NA 

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 

tenecteplase is a genetically modified version of tissue plasminogen activator (tPA), a protein that breaks down blood clots by converting plasminogen to plasmin. 

tenecteplase has been altered to be more fibrin-specific than tPA, meaning that it has a stronger affinity for the fibrin component of blood clots and may, thus, dissolve clots more successfully. 

Pharmacodynamics 

tenecteplase’s pharmacodynamics include its capacity to stimulate the plasminogen system, which results in the breakdown of blood clots. 

The kind of plasminogen seen in blood clots, fibrin-bound plasminogen, is what tenecteplase specially targets. As it attaches to fibrin, it changes plasminogen into plasmin, a proteolytic enzyme that dissolves the clot and breaks down fibrin. 

Pharmacokinetics 

Absorption   

As tenecteplase is delivered intravenously, full and quick systemic absorption is guaranteed. 

Distribution 

tenecteplase is quickly absorbed by the body after intravenous injection and largely binds to fibrin in the blood clot. Its wide volume of distribution suggests that it is widely dispersed throughout the extravascular region. 

Metabolism 

The liver is the main site of tenecteplase metabolism, where proteolytic cleavage and degradation take place. The urine is where the metabolites are eliminated. 

Elimination and excretion 

tenecteplase and its metabolites are mostly excreted through the renal pathway. tenecteplase has a half-life of around 20 minutes, which indicates that it leaves the body quickly. 

Adminstartion

Administration:  

tenecteplase is given intravenously in a hospital environment under the direction of a medical expert skilled in the administration of thrombolytic drugs. 

tenecteplase is injected in a single bolus over the course of 5 seconds to treat acute myocardial infarction. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tenecteplase 

Why do we use tenecteplase? 

Acute massive pulmonary embolism and acute myocardial infarction are both treated with tenecteplase, a thrombolytic drug. 

The medication is used to dissolve blood clots that have developed in the arteries or veins in both disorders. These clots can impede blood flow, cause tissue damage, or even result in death.