Name: | rosiglitazone |
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PubChem Compound ID: | 10021239 |
Molecular formula: | C18H19N3O3S |
Molecular weight: | 357.428 g/mol |
Name: | rosiglitazone |
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Name (isomeric): | DB00412 |
Drug Type: | small molecule |
Synonyms: |
Rosiglitazone maleate; Rosigliazone maleate
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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 |
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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 ...
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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: |
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