Rosiglitazone and Metformin

Hypoglycaemic excluding Insulin · Biguanide/Thiazolidinedione

Indications

Type II diabetes, particularly in overweight patients, inadequately controlled by maximal tolerated doses of metformin or in triple therapy with a sulphonylurea inadequately controlled by maximal tolerated doses of metformin and a sulphonylurea.

Dosage

Adults: Dual therapy: Initially 1 tab of 2 mg/1000 mg tab, twice daily with or just after food. Increase to 2 tab of 2 mg/500 mg tab or 1 tab of 4 mg/1000 mg tab twice daily after 8 wk if greater glycaemic control is required. Triple therapy with a sulphonylureas: Initially 1 tab of 2 mg/1000 mg tab, twice daily with or just after food. When appropriate, this medicine may be used to substitute concomitant rosiglitazone and metformin in existing dual or triple therapy. Children: Not recommended.

Adverse Effects

Anaemia, hypoglycaemia, hypercholesterolaemia, weight gain, GI upset, dizziness, cardiac ischaemia, oedema, bone fractures.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Cardiac failure or history of cardiac failure, respiratory failure, recent MI, shock, hepatic impairment, acute alcohol intoxication, alcoholism, diabetic ketoacidosis, diabetic precoma, renal impairment, dehydration, severe infection, acute coronary syndrome. Precautions: Monitor renal function at least once per year in patients with normal renal function and at least 2-4 times per year in patients with raised creatinine levels and the elderly. Monitor for signs of fluid retention, including weight gain, or signs of cardiac failure (discontinue if deteriorates). Monitor for anaemia and risk factors for lactic acidosis. Monitor for signs of hepatic dysfunction; measure liver enzymes before treatment and periodically thereafter. Withdraw 48 hours before elective surgery. Exclude…

Interactions

Insulin, paclitaxel, intravascular iodinated contrast media. antihypertensives, diuretics or NSAIDs, glucocorticoids, beta2-agonists, ACE inhibitors, cimetidine, inhibitors and inducers of CYP2C8 including gemfibrozil, rifampicin.

Advice to Patient

Take with meals. Contact prescriber if there is persistent headache, nausea, diarrhoea, chest pain, rapid heartbeat, palpitations, unusual fatigue, muscle pain, weakness, vomiting, rapid weight gain, swelling of extremities or respiratory difficulties. Carry source of sugar at all times. Avoid alcohol. Monitor glucose level as advised by prescriber. Follow dietary and lifestyle changes as recommended by the prescriber.

Pharmacokinetics

ROSIGLITAZONE: Absorption: Oral: Well absorbed. Metabolism: Hepatic. Bioavailability: 99%. Half-life elimination: 3-4 hrs (single oral dose, independent of dose). Time to peak, plasma: 1 hr. Excretion: Urine (64%). Faeces (23%). METFORMIN: Onset of action: Within days, max effects up to 2 wks. Metabolism: Not metabolized by the liver. Bioavailability: Absolute: Fasting: 50%-60%. Half-life elimination: Plasma: 4-9 hrs. Blood: Approx. 17.6 hrs. Time to peak, serum: Immediate release: 2-3 hrs. Extended release: 7 hrs. (Range: 4-8 hrs). Excretion: Urine.

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.