Rosiglitazone

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Rosiglitazone.png
Rosiglitazone chemical structure


Rosiglitazone

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).

Contents

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

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