Pioglitazone
From Proteopedia
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Revision as of 11:40, 1 December 2010
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Better Known as: Actos
- Marketed By: Takeda Pharmaceuticals
- Major Indication: Hypoglycemia & Type 2 Diabetes
- Drug Class: PPAR-γ Agonist - Thiazolidinedione (Glitazones)
- Date of FDA Approval (Patent Expiration): 1999 (2011)
- 2009 Sales: $2.4 Billion [1]
- Why You Should Care: It is the best selling drug to treat Diabetes and is the 10th best selling drug in the United States.
- The following is a list of Pharmacokinetic Parameters. See: Pharmaceutical Drugs for more information
Pharmacokinetics
| Glitazone Pharmacokinetics Comparison at Equivalent Dosages [2][3][4][5] | |||||
|---|---|---|---|---|---|
| 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) | |||
References
- ↑ http://drugpatentwatch.com/ultimate/preview/tradename/index.php?query=ACTOS
- ↑ Kalliokoski A, Neuvonen M, Neuvonen PJ, Niemi M. No significant effect of SLCO1B1 polymorphism on the pharmacokinetics of rosiglitazone and pioglitazone. Br J Clin Pharmacol. 2008 Jan;65(1):78-86. Epub 2007 Jul 17. PMID:17635496 doi:10.1111/j.1365-2125.2007.02986.x
- ↑ Saad S, Agapiou DJ, Chen XM, Stevens V, Pollock CA. The role of Sgk-1 in the upregulation of transport proteins by PPAR-{gamma} agonists in human proximal tubule cells. Nephrol Dial Transplant. 2009 Apr;24(4):1130-41. Epub 2008 Nov 8. PMID:18997160 doi:10.1093/ndt/gfn614
- ↑ Young PW, Buckle DR, Cantello BC, Chapman H, Clapham JC, Coyle PJ, Haigh D, Hindley RM, Holder JC, Kallender H, Latter AJ, Lawrie KW, Mossakowska D, Murphy GJ, Roxbee Cox L, Smith SA. Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma. J Pharmacol Exp Ther. 1998 Feb;284(2):751-9. PMID:9454824
- ↑ Derosa G. Pioglitazone plus glimepiride: a promising alternative in metabolic control. Int J Clin Pract Suppl. 2007 Jun;(153):28-36. PMID:17594391 doi:10.1111/j.1742-1241.2007.01362.x
