HEALTHY LIFESTYLE




Alteplase
Alteplase.JPG

Alteplase

CLINICAL USE

Fibrinolytic drug:
  • Acute myocardial infarction
  • Pulmonary embolism
  • Acute ischaemic stroke
  • To unblock dialysis lines (unlicensed indication)

    DOSE IN NORMAL RENAL FUNCTION

  • Myocardial infarction: accelerated regimen (initiated within 6 hours) 15 mg IV bolus, 50 mg over 30 minutes, then 35 mg over 1 hour (total dose 100 mg); or (if initiated within 6–12 hours) 10 mg over 1–2 minutes followed by IV infusion of 50 mg over 1 hour, then 4 infusions each of 10 mg over 30 minutes (total dose – 100 mg over 3 hours)
  • Pulmonary embolism: 10 mg by IV injection over 1–2 minutes, followed by an infusion of 90 mg over 2 hours. Total dose should not exceed 1.5 mg/kg in patients who weigh <65 kg
  • Acute ischaemic stroke: 0.9 mg/kg over 60 minutes, 10% of dose as initial bolus; maximum 90 mg. Start within 3 hours of symptoms

    PHARMACOKINETICS

  • Molecular weight                           : 65 000 (non- glycosylated protein)
  • %Protein binding                           : No data
  • %Excreted unchanged in urine     : Minimal
  • Volume of distribution (L/kg)       : 0.1
  • half-life – normal/ESRD (hrs)      : α: 4–5 minutes; β: 40 minutes

    DOSE IN RENAL IMPAIRMENT

    GFR (mL/MIN)

  • 20 to 50     : Dose as in normal renal function
  • 10 to 20     : Dose as in normal renal function
  • <10           : Dose as in normal renal function

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                : Not dialysed. Dose as in normal renal function
  • HD                     : Not dialysed. Dose as in normal renal function
  • HDF/high flux   : Unknown dialysability. Dose as in normal renal function
  • CAV/VVHD      : Not dialysed. Dose as in normal renal function

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs
  • Risk of haemorrhage can be increased by the use of coumarin derivatives, platelet aggregation inhibitors, heparin, and other agents influencing coagulation

    ADMINISTRATION

    Reconstition

  • 50 mg vial: dissolve in 50 mL water for injection 20 mg vial: dissolve in
  • 20 mL water for injection. The reconstituted solutions can be further diluted (minimum concentration 0.2 mg/ mL) with sterile sodium chloride 0.9%

    Route

    IV

    Rate of Administration

    See under dose

    Comments

  • Water or glucose solution must NOT be used for dilution
  • 50 mg vial = 29 mega units/vial
  • 20 mg vial = 11.6 mega units/vial

    OTHER INFORMATION

  • Patients weighing less than 65 kg should receive a total dose of 1.5 mg/kg according to dose schedule
  • Allergic reactions are less likely with alteplase than streptokinase and repeated administration is possible
  • 1.7 g arginine in the 50 mg vial, 0.7 g arginine in 20 mg vial – may lead to hyperkalaemia in renal failure
  • Pay attention to potential bleeding sites during treatment
  • To unblock dialysis lines, use 2 mg in 2 mL down each lumen and leave in situ for at least 60 minutes or until the next dialysis session
  • Alternative regimens for unblocking dialysis lines: an infusion of 20 mg over 20 hours, or 50 mg over 12 hours
  • other drugs