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QuickView for Rosiglitazone (compound)

Name: rosiglitazone
PubChem Compound ID: 10021239
Molecular formula: C18H19N3O3S
Molecular weight: 357.428 g/mol
Name: rosiglitazone
Name (isomeric): DB00412
Drug Type: small molecule
Rosiglitazone maleate; Rosigliazone maleate
Brand: Rosiglizole, Avandia
Brand name mixture: Avandaryl(Glimepiride + Rosiglitazone maleate), Avandamet(Metformin hydrochloride + Rosiglitazone maleate)
Category: Vasodilator Agents, Hypoglycemic Agents, Fibrinolytic Agents, Thazolidinediones
CAS number: 122320-73-4
Indication: For the treatment of Type II diabetes mellitus
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 ...
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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 ...
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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, rosiglitazone may be administered with or without food.
Protein binding: 99.8% bound to plasma proteins, primarily albumin.
Biotransformation: Hepatic. Rosiglitazone is extensively metabolized in the liver to inactive metabolites via N-demethylation, hydroxylation, and conjugation with sulfate and glucuronic acid. In vitro data have shown that Cytochrome (CYP) P450 isoenzyme 2C8 (CYP2C8) and to a minor extent CYP2C9 are involved in the hepatic metabolism of rosiglitazone.
Route of elimination: Following oral or intravenous administration of [14C]rosiglitazone maleate, approximately 64% and 23% of the dose was eliminated in the urine and in the feces, respectively.
Half Life: 3-4 hours
Clearance: Oral cl=3.03 +/- 0.87 L/hr [1 mg Fasting] Oral cl=2.89 +/- 0.71 L/hr [2 mg Fasting] Oral cl=2.85 +/- 0.69 L/hr [8 mg Fasting] Oral cl=2.97 +/- 0.81 L/hr [8 mg Fed] 3.15 L/hr [Population mean]
Toxicity: Side effects include fluid retention, congestive heart failure (CHF), liver disease
Affected organisms: Humans and other mammals
Drug interaction:
TretinoinThe moderate CYP2C8 inhibitor, Rosiglitazone, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Rosiglitazone is initiated, discontinued to dose changed.
RifampinRifampin reduces levels and efficacy of rosiglitazone
KetoconazoleKetoconazole increases the effect of rosiglitazone
ColesevelamBile Acid Sequestrants may decrease the absorption of Antidiabetic Agents (Thiazolidinedione). Separate the dosing of bile acid sequestrants and thiazolidinediones by at least 2 hours. Monitor for reduced effects of the antidiabetic agents.
GemfibrozilIncreases the effect and toxicity of rosiglitazone/pioglitazone
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