Context New bolus fibrinolytics derived from the human tissue-type plasmino
gen activator (tPA) have emerged as a means of dissolution of occlusive thr
ombosis associated with acute myocardial infarction.
Objective To review the new bolus fibrinolytic drugs derived from tPA, rete
plase, lanoteplase, and tenecteplase,
Data Sources The MEDLINE, EMBASE, and Current Contents databases were searc
hed for articles from 1983 to 2001, using the index terms pharmacokinetics,
pharmacodynamics, plasminogen activator, reteplase, lanoteplase, and tenec
teplase. Additional data sources included bibliographies of articles identi
fied on MEDLINE, EMBASE, and Current Content, inquiry of experts and pharma
ceutical companies, and preliminary data presented at recent national and i
nternational cardiology conferences.
Study Selection We selected for review studies that evaluated the pharmacok
inetics and pharmacodynamics of reteplase, lanoteplase, and tenecteplase, a
nd assessed the effects of these bolus fibrinolytic drugs on the angiograph
ic and immediate and long-term outcomes of patients, Of 138 articles identi
fied, 38 were analyzed.
Data Extraction Data quality was determined by publication in the peer-revi
ewed literature or presentation at an official cardiology society-sponsored
meeting.
Data Synthesis Tenecteplase and reteplase are comparable with accelerated i
nfusion recombinant tPA in terms of efficacy and safety but more convenient
because they are administered by bolus injection. Lanoteplase and heparin
bolus plus infusion is as effective as tPA with regard to mortality, but th
e rate of intracranial hemorrhage is significantly higher.
Conclusion Given the ease of administration and the similar outcomes compar
ed with accelerated infusion recombinant tPA, it is likely that a key compo
nent of contemporary reperfusion will include a bolus fibrinolytic.