Delayed argatroban treatment reduces edema in a rat model of intracerebral hemorrhage

Stroke. 2002 Dec;33(12):3012-8. doi: 10.1161/01.str.0000037673.17260.1b.

Abstract

Background and purpose: Studies indicate that thrombin plays an important role in intracerebral hemorrhage (ICH)-induced edema formation. Although thrombin is produced as the blood clots, it may be bound to fibrin and only gradually released from the clot. The time window for administration of a thrombin inhibitor to reduce ICH-induced edema is unknown. Whether this time window extends beyond the period when a thrombin inhibitor might exacerbate rebleeding is also unknown.

Methods: This study examines (1) whether argatroban, an inhibitor of both free and fibrin-bound thrombin, can reduce edema formation after intracerebral infusion of 100 micro L of blood in the rat; (2) the therapeutic time window for argatroban; and (3) whether argatroban promotes rebleeding in a model in which ICH was induced by intracerebral injection of collagenase.

Results: Intracerebral infusion of blood caused a marked increase in perihematomal water content. Intracerebral injection of argatroban 3 hours after ICH caused a significant reduction in edema measured at 48 hours (80.9+/-1.0% versus 82.6+/-0.8%; P<0.01). The systemic administration of high-dose argatroban (0.9 mg/h) starting 6 hours after ICH also significantly reduced edema (80.3+/-1.1% versus 82.0+/-1.3% in vehicle controls; P<0.05). There was no protection when the onset of argatroban administration was delayed to 24 hours after ICH or if a lower dose of argatroban (0.3 mg/h) was used. Argatroban did not increase collagenase-induced hematoma volume when given into the clot after 3 hours or given systemically at 6 hours.

Conclusions: Our data suggest that argatroban may be an effective therapy for ICH-induced edema.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antithrombins / administration & dosage*
  • Antithrombins / adverse effects
  • Antithrombins / pharmacokinetics
  • Arginine / analogs & derivatives
  • Brain / blood supply
  • Brain / drug effects
  • Brain / pathology
  • Brain Chemistry / drug effects
  • Brain Edema / pathology
  • Brain Edema / prevention & control*
  • Cerebral Hemorrhage / blood
  • Cerebral Hemorrhage / chemically induced
  • Cerebral Hemorrhage / pathology
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Hemoglobins / analysis
  • Infusions, Parenteral
  • Male
  • Microinjections
  • Pipecolic Acids / administration & dosage*
  • Pipecolic Acids / adverse effects
  • Pipecolic Acids / pharmacokinetics
  • Rats
  • Rats, Sprague-Dawley
  • Stereotaxic Techniques
  • Sulfonamides
  • Time Factors
  • Treatment Outcome
  • Water / analysis

Substances

  • Antithrombins
  • Hemoglobins
  • Pipecolic Acids
  • Sulfonamides
  • Water
  • Arginine
  • argatroban