CLINICAL USE

Type 2 diabetes mellitus

DOSE IN NORMAL RENAL FUNCTION

4–8 mg daily in 1–2 divided doses

PHARMACOKINETICS

  • Molecular weight                           :357.4 (473.5 as maleate)
  • %Protein binding                           :99.8
  • %Excreted unchanged in urine     : 0 (66% as metabolites)
  • Volume of distribution (L/kg)       :14 litres
  • half-life – normal/ESRD (hrs)      :3–4/Unchanged

    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. Use with caution
  • <10           : Dose as in normal renal function. Use with caution

    DOSE IN PATIENTS UNDERGOING RENAL REPLACEMENT THERAPIES

  • CAPD                :Unlikely to be dialysed. Dose as in GFR <10 mL/min
  • HD                     :Not dialysed. Dose as in GFR <10 mL/min
  • HDF/high flux   :Unknown dialysability. Dose as in GFR <10 mL/min
  • CAV/VVHD      :Unlikely to be dialysed. Dose as in GFR=10-20 mL/min

    IMPORTANT DRUG INTERACTIONS

    Potentially hazardous interactions with other drugs

  • Antibacterials: concentration reduced by rifampicin – consider increasing rosiglitazone doseLipid-lowering agents: concentration increased by gemfibrozil – consider reducing rosiglitazone dose

    ADMINISTRATION

    Reconstition

    –

    Route

    Oral

    Rate of Administration

    –

    Comments

    –

    OTHER INFORMATION

    Measure liver function prior to initiating therapy, and then at regular intervalsShould not be used in patients with heart failure or history of heart failure; incidence of heart failure is increased when rosiglitazone is combined with insulinShould not be used in patients with acute coronary syndrome. Patients should be closely monitored for signs of heart failureMay be associated with a small increased risk of cardiac ischaemia particularly in combination with insulin. The combination of rosiglitazone and insulin should be used only in exceptional cases, and under close supervision
    Rosiglitazone is contraindicated for co- administration with insulin in the UK but not in the USANot recommended for use in patients with ischaemic heart disease or peripheral arterial disease; in patients with history of ischaemic heart disease rosiglitazone should only be used after careful evaluation of the patient’s individual risk
    Rosiglitazone is extensively metabolised in the liver. Some of the metabolites are active, and are largely excreted in the urine.

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