Composition: Rosiglitazone (as maleate) 4mg and 8mg.
Presentation: Film-coated tablets, 4mg orange, 8mg red-brown.
Action: Thiazolidinedione antihyperglycaemic.
Indications: Oral combination treatment of type 2 diabetes mellitus in patients with insufficient glycaemic control despite maximal tolerated dose of oral monotherapy with either metformin or a sulphonylurea. In combination with metformin only in obese patients. In combination with a sulphonylurea only in patients who show intolerance to metformin or for whom metformin is contraindicated.
Contraindications: Hypersensitivity to active substance or excipients; cardiac failure or history of cardiac failure; hepatic impairment; in combination with insulin.
Dosage and administration: Therapy is usually initiated at 4mg/day. Rosiglitazone may be given once or twice daily and may be taken with or without food. Should not be used as monotherapy.
Combination with metformin, dose can be increased to 8mg/day after eight weeks if greater glycaemic control is required.
Combination with sulphonylurea, there is currently no experience with doses above 4mg/day.
Elderly, no dose adjustment required.
Hepatic impairment, should not be used.
Mild to moderate renal impairment, no dose adjustment required. Should not be used in patients with severe renal impairment.
Children and adolescents (under 18 years), not recommended as no data are available.
Pregnancy, should not be used. Discontinue if a patient wishes to become pregnant or if pregnancy occurs.
Lactation, should not be used.
Overdosage: Limited data are available. In clinical studies, a single oral dose of up to 20mg was tolerated. With overdosing, supportive treatment should be initiated. Rosiglitazone is not cleared by haemodialysis.
Precautions: No clinical experience with rosiglitazone in triple combination therapy. Rosiglitazone can cause fluid retention and patients should be observed for signs and symptoms of heart failure, particularly those with reduced cardiac reserve. Discontinue if any deterioration in cardiac status occurs. Liver enzymes should be checked prior to initiating therapy in all patients and monitored periodically (see SPC). If jaundice is observed, therapy should be discontinued. Weight should be closely monitored. There is an increased risk of anaemia during treatment in patients with low haemoglobin levels.
Drug interactions: Concomitant administration with NSAIDs may increase the risk of oedema. Concomitant use with paclitaxel is likely to result in inhibition of the metabolism of rosiglitazone and caution should be taken.
Side effects: Rosiglitazone in combination with metformin: Common adverse reactions (greater than 1 per cent, less than 10 per cent) included anaemia, hypoglycaemia, hyperglycaemia, headache, diarrhoea, flatulence, nausea, abdominal pain, dyspepsia, fatigue; uncommon (greater than 0.1 per cent, less than 1 per cent) included hyperlipidaemia, lactic acidosis, diabetes mellitus aggravated, hypercholesterolaemia, dizziness, vomiting, anorexia, constipation. Rosiglitazone in combination with sulphonylurea: Common adverse effects included hypoglycaemia, hyperglycaemia, weight increase; uncommon effects included anaemia, thrombocytopenia, hypercholesterolaemia, hyperlipidaemia, hypertriglyceridaemia, somnolence, dizziness, headache, paresthesia, dyspnoea, abdominal pain, flatulence, nausea, appetite increased, alopecia, rash, fatigue, asthenia.
Net price: 4mg 28 £26.60, 56 £53.20; 8mg 28 £54.60.
Supplier: Smithkline Beecham Pharmaceuticals, Mundells, Welwyn Garden City, Hertfordshire AL7 1EY (tel 0808 100 2228, fax 0808 100 8802).
Legal class: POM.