Core pharmacology

Class Group

Fibrinolytic

Legacy Cicm Level

Level 3

Introduction

Recombinant tissue plasminogen activator

Presentation

administered IV and dosing depends on the indication (AMI and PE use bolus followed by infusion. Stroke uses infusion). All thrombolytics except streptokinase are prepared with heparin.

Mechanism of action

It is a glycoprotein that only becomes activated when bound to thrombus bound-plasminogen. This activation then leads to the conversion of plasminogen to plasmin, which cleaves fibrin into fibrin degradation products, such d-dimers.
This mechanism of activation decreases the systemic effects

Adverse Effects Toxicity

Haemorrhage (cease drug, resuscitate +- tranexamic acid)
Cardiovascular- reperfusion arrhythmias and hypotension during treatment of MI
Reperfusion pain

Volume of distribution

Small Vd of 2-4L

Metabolism

Undergoes hepatic metabolism to smaller peptides.

Excretion

Undergoes biphasic elimination, with rapid plasma clearance.