Rosiglitazone
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Rosiglitazone
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| Systematic (IUPAC) name | |
| 5-((4-(2-(methyl-2-pyridinylamino) ethoxy)phenyl)methyl)- 2,4-thiazolidinedione | |
| Identifiers | |
| CAS number | 122320-73-4 |
| ATC code | A10BG02 |
| PubChem | 77999 |
| DrugBank | APRD00403 |
| Chemical data | |
| Formula | C18H19N3O3S |
| Mol. weight | 357.428 g/mol |
| Pharmacokinetic data | |
| Bioavailability | 99% |
| Protein binding | 99.8% |
| Metabolism | Hepatic (CYP2C8-mediated) |
| Half life | 3-4 hours |
| Excretion | Renal (64%) and fecal (23%) |
| Therapeutic considerations | |
| Licence data | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Oral |
Rosiglitazone is an anti-diabetic drug from the thiazolidinedione class. It is being marketed as Avandia® by the pharmaceutical company GlaxoSmithKline, both as a standalone preparation and in combination with metformin (Avandamet®). Another combination drug approved by the FDA is Avandaryl® (with glimepiride).
Like other thiazolidinediones, its mechanism of action is by activation of the intracellular receptor class of the peroxisome proliferator-activated receptors (PPARs), specifically PPARγ. Rosiglitazone is a pure ligand of PPARγ, and has no PPARα-binding action. Apart from its effect on insulin resistance, it appears to have an anti-inflammatory effect: nuclear factor kappa-B (NFκB) levels fall and inhibitor (IκB) levels increase in patients on rosiglitazone (Mohanty et al).
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[edit] References
- Mohanty P, Aljada A, Ghanim H, Hofmeyer D, Tripathy D, Syed T, al-Haddad W, Dhindsa S, Dandona P. Evidence for a potent antiinflammatory effect of rosiglitazone. J Clin Endocrinol Metab 2004; 89:2728-35. PMID 15181049.
[edit] Side-effects and contraindications
See main article: thiazolidinedione
