CLINICAL USE


Thrombolytic, used for acute myocardial infarction

DOSE IN NORMAL RENAL FUNCTION

10 units over 2 minutes; second dose of 10 units given 30 minutes later

PHARMACOKINETICS

  • Molecular weight &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :39571.1
  • %Protein binding &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :No data
  • %Excreted unchanged in urine &nbsp &nbsp : Negligible

  • Volume of distribution (L/kg) &nbsp &nbsp &nbsp :6–6.5 litres

  • half-life – normal/ESRD (hrs)&nbsp &nbsp &nbsp :Fibrinolytic half-life is 1.6 hours./IncreasedDominant (α) half-life is 14.6 +/– 6.7 minutesTerminal (β) half-life is 1.6 hrs +/– 39 minutes

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50 &nbsp &nbsp : Dose as in normal renal function
  • 10 to 20 &nbsp &nbsp : Dose as in normal renal function
  • <10 &nbsp &nbsp &nbsp &nbsp &nbsp : Dose as in normal renal function. Use with caution

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in GFR <10 mL/min

  • HD &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min
  • HDF/high flux &nbsp :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD &nbsp &nbsp &nbsp:Unknown dialysability. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugsAntiplatelets, heparin, vitamin K antagonists: increased risk of bleeding

    ADMINISTRATION

    Reconstition

    With diluent provided

    Route

    Slow IV

    Rate of Administration

    Over not more than 2 minutes

    Comments

    Use immediately once reconstituted Do not mix with heparin in the same line

    OTHER INFORMATION

    Heparin and aspirin should be given before and after reteplase therapy to reduce the risk of re-thrombosis but may increase the risk of bleedingHalf-life is increased in severe renal failure in animal modelsPossible increased risk of bleeding complications in severe renal impairment.
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