Rosiglitazone_maleate: profile and news

Committee for Medicinal Products for Human Use Summary of Positive ... Apr 28, 2006
...two antidiabetic agents with complimentary mechanisms of action to improve glycaemic control in patients with type 2 diabetes: rosiglitazone maleate, a member ... - PharmaLive.com (press release),

Latest Issue Of Alzheimer's & Dementia Explores New Ideas For ... Apr 23, 2006
...new hypothesis is supported by the results of 24-week randomized clinical trial of an unmarketed formulation of rosiglitazone maleate (Avandia, GlaxoSmithKline ... - Medical News Today (press release),

Other information

Indication
For the treatment of Type II diabetes mellitus

Pharmacology
Rosiglitazone, a member of the drug group known as the thiazolidinediones or "insulin sensitizers", is not chemically or functionally related to the alpha-glucosidase inhibitors, the biguanides, or the sulfonylureas. Rosiglitazone targets insulin resistance and, hence, is used alone or with metformine or sulfonylurea to improve glycemic control in patients with type 2 diabetes mellitus.

Mechanism Of Action
Rosiglitazone acts as an agonist at peroxisome proliferator activated receptors (PPAR) in target tissues for insulin action such as adipose tissue, skeletal muscle, and liver. Activation of PPAR-gamma receptors regulates the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this way, rosiglitazone enhances tissue sensitivity to insulin.

Drug Category
Vasodilator Agents; Hypoglycemic Agents; Fibrinolytic Agents; Thazolidinediones; ATC:A10BG02

Brand Names/Synonyms
Avandia; Rosigliazone Maleate; Rosiglitazone; Rosiglitazone Maleate; Rosiglitazone and Its Intermediates; Rosiglizole

Dosage Forms
Tablets

Absorption
The absolute bioavailability of rosiglitazone is 99%. Peak plasma concentrations are observed about 1 hour after dosing. Administration of rosiglitazone with food resulted in no change in overall exposure (AUC), but there was an approximately 28% decrease in Cmax and a delay in Tmax (1.75 hours). These changes are not likely to be clinically significant; therefore, AVANDIA may be administered with or without food.

Interactions
Interactions for Rosiglitazone:

An inhibitor of CYP2C8 (such as gemfibrozil) may increase the AUC of rosiglitazone and an inducer of CYP2C8 (such as rifampin) may decrease the AUC of rosiglitazone. Therefore, if an inhibitor or an inducer of CYP2C8 is started or stopped during treatment with rosiglitazone, changes in diabetes treatment may be needed based upon clinical response.

Chemical IUPAC Name
5-[[4-[2-(methyl-pyridin-2-yl-amino)ethoxy]phenyl]methyl]thiazolidine-2,4-dione

Chemical Formula
C18H19N3O3S

Half Life
3-4 hours

Drug Type
Approved Drug

# Accession No
APRD00403

CAS Registry Number
122320-73-4