Rosiglitazone

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Rosiglitazone, also known as Avandia

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Pharmacokinetics

Glitazone Pharmacokinetics Comparison at Equivalent Dosages
Parameter Pioglitazone (Actos) Rosiglitazone (Avandia)
Tmax (hr) 1.8 1
Cmax (ng/ml) 617 361
Bioavailability (%) 83 99
Protein Binding (%) 99 99
T1/2 (hr) 3-8 3-4
AUC (ng/ml/hr) 6244 2024
IC50 (nM) 360 10
Equivalent Dosage (mg) 30 4
Metabolism Hepatic
(CYP2C8) 		Hepatic
(CYP2C8)

For Pharmacokinetic Data References, See: References

Effectiveness

Effectiveness

A number of clinical trials were conducted and validated that Rosiglitazone dramatically reduces Fasting plasma glucose (FPG), a measure of the concentration of glucose in the blood, as well as Glycalated Hemoglobin (HbA1c), a measure of average glucose concentration over a long period of time. At two 4mg doses per day, Rosiglitazone reduced FPG by 40.8 mg/dl compared to 30mg/dl with Glyburide (the state of the art medication at the time). Further, the rate of hypoglycemia among glyburide treated patients was 12.1% while only 1.6% among Rosiglitazone treated patients. When combined with Metformin (another hypoglycemia medication), 45% of patients had a greater than 30mg/dl FPG decrease from baseline while 46% had a greater than .7% decrease in HbA1c, compared to 20% and 11%, respectively, for Metformin alone. Similar results were observed when Rosiglitazone was combined with Sulfonylurea (a third hypoglycemia medication). Efficacy comparisons between Rosiglitazone and Pioglitazone revealed minimal differences at equivalent dosage levels. [3] [4]

References

  1. ↑ http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=AVANDIA
  2. ↑ Nolte RT, Wisely GB, Westin S, Cobb JE, Lambert MH, Kurokawa R, Rosenfeld MG, Willson TM, Glass CK, Milburn MV. Ligand binding and co-activator assembly of the peroxisome proliferator-activated receptor-gamma. Nature. 1998 Sep 10;395(6698):137-43. PMID:9744270 doi:10.1038/25931
  3. ↑ Norris SL, Carson S, Roberts C. Comparative effectiveness of pioglitazone and rosiglitazone in type 2 diabetes, prediabetes, and the metabolic syndrome: a meta-analysis. Curr Diabetes Rev. 2007 May;3(2):127-40. PMID:18220664
  4. ↑ Park JY, Kim KA, Kang MH, Kim SL, Shin JG. Effect of rifampin on the pharmacokinetics of rosiglitazone in healthy subjects. Clin Pharmacol Ther. 2004 Mar;75(3):157-62. PMID:15001966 doi:10.1016/j.clpt.2003.10.003


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David Canner, Alexander Berchansky

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