rosiglitazone

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.

See how to identify renal failure stages according to GFR calculation

See how to diagnose irreversible renal disease

Home