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Indications and Dosage
Oral
Type 2 diabetes mellitus Adult: As monotherapy or in combination w/ metformin or sulphonylurea or w/ both: 4 mg/day, may increase after 8-12 wk to max 8 mg/day if response is inadequate. Doses can be given in single or 2 divided doses.
Elderly: No dosage adjustment needed. |
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Renal Impairment
No dosage adjustment needed.
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Hepatic Impairment
Baseline ALT>2.5x upper limit of normal (ULN): Avoid.
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Administration
May be taken with or without food.
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Contraindications
New York Heart Association (NYHA) class I to IV heart failure, history of heart failure, ischaemic heart disease, acute coronary syndrome, active hepatic disease or patients w/ ALT>2.5x upper limit of normal (ULN). Not to be used in treatment of type 1 DM or diabetic ketoacidosis. Concomitant use w/ insulin and nitrates.
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Special Precautions
Patients w/ oedema, at risk of heart failure, mild hepatic enzyme elevations (ALT≤2.5x ULNat baseline), anaemia. Hepatic and renal impairment. Pregnancy and lactation.
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Adverse Reactions
Increased risk of bone fracture in women; wt gain (dose-related), hyperglycaemia, GI disturbances, increased appetite, headache, palpitations, muscle cramps, peripheral oedema, fluid retention, upper resp tract infection, injury, sinusitis, fatigue, diarrhoea, dizziness, paraesthesia, back pain, arthralgia, alopecia, dyspnoea, leucopenia, thrombocytopenia, decreased haematocrit and haemoglobin (dose-related); increased total cholesterol, LDL- and HDL-cholesterol. Rarely, urticaria, rash, pruritus, diabetic macular oedema.
Potentially Fatal: CHF, MI; hepatotoxicity. |
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Patient Counseling Information
Contraception is recommended in premenopausal anovulatory women as rosiglitazone may cause resumption of ovulation.
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Monitoring Parameters
Monitor liver function, ALT concentrations, signs and symptoms of oedema or heart failure.
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Drug Interactions
May increase plasma levels w/ CYP2C8 inhibitors (e.g. ketoconazole, trimethoprim, gemfibrozil). May decrease plasma levels w/ rifampicin. May increase risk of heart failure and oedema w/ NSAIDs.
Potentially Fatal: Increased risk of CHF and MI w/ insulin and nitrates. |
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Food Interaction
Avoid use w/ alcohol as it may cause hypoglycaemia.
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Action
Description: Rosiglitazone is a thiazolidinedione antidiabetic agent which improves insulin sensitivity by lowering blood glucose level w/o increasing pancreatic insulin secretion. It is also a potent peroxisome proliferator-activated receptor-γ agonist, which increases the transcription of insulin-responsive genes involved in the control of glucose production, transport and utilisation.
Onset: Delayed. Duration: Up to 12 wk. Pharmacokinetics: Absorption: Well absorbed from the GI tract after oral admin. Bioavailability: 99%. Time to peak plasma concentration: Approx 1 hr. Distribution: It crosses the placenta. Volume of distribution: 17.6 L. Plasma protein binding: 99.8% (mainly albumin). Metabolism: Extensively metabolised via CYP2C8 isoenzyme and minimally via CYP2C9 isoenzyme. Excretion: Via urine (approx 64%); faeces (approx 23%). Elimination half-life: 3-4 hr. |
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Storage
Store between 15-30°C. Protect from light.
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MIMS Class
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References
Anon. Rosiglitazone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 29/10/2013. Avandia (GlaxoSmithKline LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 29/10/2013. Avandia: REMS - Risk of Cardiovascular Events. U.S. FDA. https://www.fda.gov/. Accessed 29/10/2013. Buckingham R (ed). Rosiglitazone. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 29/11/2013. McEvoy GK, Snow EK, Miller J et al (eds). Rosiglitazone Maleate. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 29/10/2013.
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