Name: | pioglitazone |
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PubChem Compound ID: | 4829 |
Molecular formula: | C19H20N2O3S |
Molecular weight: | 356.44 g/mol |
Synonyms: |
KBioGR_001619; Pioglitazonum [INN-Latin]; 2,4-Thiazolidinedione, 5-((4-(2-(5-ethyl-2-pyridinyl)ethoxy)phenyl)methyl)-; 2,4-Thiazolidinedione, 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]-, (+/-)-; Spectrum4_001130; (+/-)-5-[p-[2-(ethyl-2-pyridyl)ethoxy]benzyl]-2,4-thiazolidinedione; KBio3_001943; 2,4-Thiazolidinedione, 5-[[4-[2-(5-ethyl-2-pyridinyl)ethoxy]phenyl]methyl]- (9CI); Actos; Spectrum_001623.
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Name: | pioglitazone |
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Name (isomeric): | DB01132 |
Drug Type: | small molecule |
Synonyms: |
Pioglitazonum [INN-Latin]; pioglitazone HCl; Pioglitazone [Ban:Inn]; Pioglitazona [INN-Spanish]; Pioglitazone Hydrochloride
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Brand: | Actost, Actos, Glustin |
Brand name mixture: | ActoplusMet(Pioglitazone + Metformin) |
Category: | Hypoglycemic Agents, Thazolidinediones |
CAS number: | 111025-46-8 |
Indication: | Treatment of Type II diabetes mellitus |
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Pharmacology: |
Pioglitazone, 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. Pioglitazone targets insulin resistance and, hence, is used alone or in combination with insulin, metformin, or asulfonylurea as an an...
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Mechanism of Action: |
Pioglitazone 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 increases the transcription of insulin-responsive genes involved in the control of glucose production, transport, and utilization. In this w...
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Absorption: | Following oral administration, in the fasting state, pioglitazone is first measurable in serum within 30 minutes, with peak concentrations observed within 2 hours. Food slightly delays the time to peak serum concentration to 3 to 4 hours, but does not alter the extent of absorption. |
Protein binding: | > 99% |
Biotransformation: | Hepatic |
Route of elimination: | Following oral administration, approximately 15% to 30% of the pioglitazone dose is recovered in the urine. Renal elimination of pioglitazone is negligible, and the drug is excreted primarily as metabolites and their conjugates. It is presumed that most of the oral dose is excreted into the bile either unchanged or as metabolites and eliminated in the feces. |
Half Life: | 3-7 hours |
Clearance: | apparent cl=5 - 7 L/h [oral administration] |
Toxicity: | Hypogycemia; LD50=mg/kg (orally in rat) |
Affected organisms: | Humans and other mammals |
Food interaction: |
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Drug interaction: |
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