Name: | troglitazone |
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PubChem Compound ID: | 5591 |
Molecular formula: | C24H27NO5S |
Molecular weight: | 441.541 g/mol |
Synonyms: |
CI-991; Rezulin; GR 92132X; (+/-)-5-[4-[(6-hydroxy-2,5,7,8-tetramethylchroman-2-yl)methoxy]benzyl]-2,4-thiazolidinedione; D00395; 5-(4-(6-Hydroxy-2,5,7,8-tetramethylchroman-2-ylmethoxy)benzyl)thiazolidine-2,4-dione; 5-[[4-[(3,4-Dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)methoxy]phenyl]methyl]-2,4-thiazolidinedione; (+-)-all-rac-5-(p-((6-Hydroxy-2,5,7,8-tetramethyl-2-chromanyl)methoxy)benzyl)-2,4-thiazolidinedione; Troglitazone (JAN/USAN); 2,4-thiazolidinedione, 5-[[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)methoxy]phenyl]methyl]-.
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Name: | troglitazone |
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Name (isomeric): | DB00197 |
Drug Type: | small molecule |
Brand: | Prelay, Romglizone, Noscal, Rezulin, Romozin, Resulin |
Category: | Vasodilator Agents, Hypoglycemic Agents, Antineoplastic Agents, Fibrinolytic Agents, Platelet Aggregation Inhibitors |
CAS number: | 97322-87-7 |
Indication: | For the treatment of Type II diabetes mellitus. It is used alone or in combination with a sulfonylurea, metformin, or insulin as an adjunct to diet and exercise. |
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Pharmacology: |
Troglitazone is an oral antihyperglycemic agent which acts primarily by decreasing insulin resistance. Troglitazone is used in the management of type II diabetes (noninsulin-dependent diabetes mellitus (NIDDM) also known as adult-onset diabetes). It improves sensitivity to insulin in muscle and adipose tissue and inhibits hepatic gluconeogenesis. T...
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Mechanism of Action: |
Troglitazone is a thiazolidinedione antidiabetic agent that lowers blood glucose by improving target cell response to insulin. It has a unique mechanism of action that is dependent on the presence of insulin for activity. Troglitazone decreases hepatic glucose output and increases insulin dependent glucose disposal in skeletal muscle. Its mechanism...
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Absorption: | Absorbed rapidly. Food increases the extent of absorption by 30% to 85%. |
Protein binding: | > 99% (primarily to serum albumin) |
Biotransformation: | A sulfate conjugate metabolite (Metabolite 1) and a quinone metabolite (Metabolite 3) have been detected in the plasma of healthy males. A glucuronide conjugate (Metabolite 2) has been detected in the urine and also in negligible amounts in the plasma. In healthy volunteers and in patients with type 2 diabetes, the steady-state concentration of Metabolite 1 is six to seven times that of troglitazone and Metabolite 3. In in vivo drug interaction studies, troglitazone has been shown to induce cytochrome P450 CYP3A4 at clinically relevant doses. |
Half Life: | 16-34 hours |
Affected organisms: | Humans and other mammals |
Drug interaction: |
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