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Plasminogen activator inhibitor-1: physiologic role, regulation, and the influence of common pharmacologic agents

James P Tsikouris1, Jose A Suarez, Gary E Meyerrose

  • 1Texas Tech University, Health Sciences Center, School of Pharmacy, Lubbock 79430, USA.

Journal of Clinical Pharmacology
|November 5, 2002
PubMed

Insights

Plasminogen activator inhibitor-1 (PAI-1) promotes thrombosis and heart attack recurrence. Certain medications like ACE inhibitors, estrogen, metformin, and pravastatin may favorably reduce PAI-1 levels.

Area of Science:

  • Cardiovascular Medicine
  • Hematology
  • Endocrinology

Background:

  • Plasminogen activator inhibitor-1 (PAI-1) is a key regulator of fibrinolysis.
  • Elevated PAI-1 levels are linked to thrombosis and acute myocardial infarction (heart attack).
  • Factors like the renin-angiotensin system, metabolic derangements, and hormone therapy influence PAI-1.

Purpose of the Study:

  • To review the influence of various pharmacological agents on PAI-1 production.
  • To identify treatments that may beneficially modulate PAI-1 levels.
  • To assess the impact of specific drugs on the fibrinolytic system.

Main Methods:

  • Literature review of clinical data.
  • Analysis of studies investigating PAI-1 levels in response to different medications.
  • Evaluation of the effects of ACE inhibitors, hormone replacement therapy, metformin, and statins on PAI-1.

Main Results:

  • Angiotensin-converting enzyme (ACE) inhibitors and estrogen therapy show promise in reducing PAI-1.
  • Metformin may decrease PAI-1 in diabetic patients but not in non-diabetics.
  • Pravastatin demonstrates the most compelling evidence among statins for favorably affecting PAI-1.

Conclusions:

  • Several common medications can modulate PAI-1 levels, potentially impacting thrombotic risk.
  • Targeting PAI-1 through these agents may offer therapeutic benefits in cardiovascular disease.
  • Further research is needed to fully elucidate the effects of statins on the fibrinolytic system.

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