Rosiglitazone
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| 5-((4-(2-(methyl-2-pyridinylamino) ethoxy)phenyl)methyl)- 2,4-thiazolidinedione | |
| CAS number 122320-73-4 | ATC code A10BG02 |
| Chemical formula | C18H19N3O3S |
| Molecular weight | 357.432 |
| Bioavailability | ? |
| Metabolism | ? |
| Elimination half-life | ? |
| Excretion | ? |
| Pregnancy category | ? |
| Legal status | ? |
| Routes of administration | ? |
In medicine and pharmacology, rosiglitazone is a member of the thiazolidinedione class of drugs.
It is being marketed as Avandia® by the pharmaceutical company GlaxoSmithKline, both as a standalone preparation and in combination with metformin (Avandamet®).
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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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.
Side-effects and contraindications
See main article: thiazolidinedione
See also
External links
- Diabetes monitor (http://www.diabetesmonitor.com/avandia.htm) article
- MedlinePlus (http://www.nlm.nih.gov/medlineplus/druginfo/medmaster/a699023.html) article
- Avandia / Rosiglitazone Fact Sheet (http://www.fact-sheets.com/health/drugs-medications/avandia/)