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QuickView for Pioglitazone (compound)

Name: pioglitazone
PubChem Compound ID: 4829
Molecular formula: C19H20N2O3S
Molecular weight: 356.44 g/mol
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
Name (isomeric): DB01132
Drug Type: small molecule
Pioglitazonum [INN-Latin]; pioglitazone HCl; Pioglitazone [Ban:Inn]; Pioglitazona [INN-Spanish]; Pioglitazone Hydrochloride
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
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:
Take without regard to meals. Food slightly delays absorption rate but extent of absorption is not affected.
Drug interaction:
TretinoinThe moderate CYP2C8 inhibitor, Pioglitazone, may decrease the metabolism and clearance of oral Tretinoin. Monitor for changes in Tretinoin effectiveness and adverse/toxic effects if Pioglitazone is initiated, discontinued to dose changed.
TramadolPioglitazone may decrease the effect of Tramadol by decreasing active metabolite production.
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.
Somatropin recombinantSomatropin may antagonize the hypoglycemic effect of pioglitazone. Monitor for changes in fasting and postprandial blood sugars.
MestranolPossible loss of contraceptive effect
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