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PioglitazoneSystematic (IUPAC) name5-(4-benzyl)thiazolidine-2,4-dioneIdentifiersCAS number111025-46-8ATC codeA10BG03PubChem4829DrugBankAPRD00653Chemical dataFormulaC19H20N2O3S Mol. mass356.44 g/molSMILESeMolecules & PubChemPharmacokinetic dataBioavailability ?Protein binding>99%Metabolismliver (CYP2C8)Half life3–7 hoursExcretionin bileTherapeutic considerationsLicence dataEU EMEA:link, US FDA:linkPregnancy cat.CLegal statusPOM(UK) ℞-only(US)RoutesoralPioglitazone is a prescription drug of the class thiazolidinedione (TZD) with hypoglycemic (antihyperglycemic, antidiabetic) action. Pioglitazone is marketed as trademarks Actos in the USA, Glustin in Europe and Zactos in Mexico by the pharmaceutical company Takeda.// PharmacologyPioglitazone selectively stimulates the nuclear receptor peroxisome proliferator-activated receptor gamma (PPAR-γ) and to a lesser extent PPAR-α. It modulates the transcription of the insulin-sensitive genes involved in the control of glucose and lipid metabolism in the lipidic, muscular tissues and in the liver. As a result, pioglitazone reduces insulin resistance in the liver and peripheral tissues; increases the expense of insulin-dependent glucose; decreases withdrawal of glucose from the liver; reduces quantity of glucose, insulin and glycated haemoglobin in the bloodstream. Although not clinically significant, pioglitazone decreases the level of triglycerides and increases that of high-density lipoproteins (HDL) without changing low-density lipoproteins (LDL) and total cholesterol in patients with disorders of the lipid metabolism, although statins are the drug of choice for this.More recently, pioglitazone and other active TZDs have been shown to bind to the outer mitochondrial membrane protein mitoNEET with affinity comparable to that of pioglitazone for PPARγ. Indications and usagePioglitazone is used for the treatment of diabetes mellitus type 2 (previously known as non-insulin-dependent diabetes mellitus, NIDDM) in monotherapy and in combination with sulfonylurea, metformin, or insulin. Pioglitazone has also been used to treat non-alcoholic steatohepatitis (fatty liver), but this use is presently considered experimental. ContraindicationsPioglitazone cannot be used in patients with a known hypersensitivity to pioglitazone, other thiazolidinediones or any of components of its pharmaceutical forms. It is ineffective and possibly harmful in diabetes mellitus type 1 and diabetic ketoacidosis. Its safety in pregnancy, lactation (breastfeeding) and people under 18 is not established.Given previous experiences with the related drug troglitazone, acute diseases of the liver are regarded as a contraindication for pioglitazone. Side effectsA press release by GlaxoSmithKline in February 2007 noted that there is a greater incidence of fractures of the upper arms, hands and feet in female diabetics given rosiglitazone compared with those given metformin or glyburide. The information was based on data from the ADOPT trial. Following release of this statement, Takeda also admitted that pioglitazone has similar implications for female patients.The risk of hypoglycemia is low in the absence of other drugs that lower blood glucose.Like other thiazolidinediones, pioglitazone can cause fluid retention and peripheral edema. As a result, it may precipitate congestive heart failure (which worsens with fluid overload in those at risk). It may cause anemia. Mild weight gain is common due to increase in subcutaneous adipose tissue. In studies, patients on pioglitazone had a slightly increased proportion of upper respiratory tract infection, sinusitis, headache, myalgia and tooth problems.On July 30, 2007 an Advisory Committee of the Food and Drug Administration concluded that the use of rosiglitazone for the treatment of type 2 diabetes was associated with a greater risk of "myocardial ischemic events" when compared to placebo, but when compared to other active comparators, there was no increased risk. Pioglitazone is currently being reviewed. A meta-analysis released subsequently showed that pioglitazone reduced the number of ischemic cardiac events rather than increase the risk, but increases CHF, a common class effect of the TZD's.. The PERISCOPE study compared pioglitazone with glimepiride in diabetics; atherosclerotic plaque volume was measured and followed over time. Glimepiride therapy had highly significant progression of plaque volume over time of 0.73 percent. In comparison, pioglitazone had a -0.16 percent regression in plaque volume. This is the first study to show that diabetic therapy slowed progression of atherosclerosis. Therapy with pioglitazone raised HDL, and lowered triglyceride and hsCRP; these are all beneficial effects on risk factors for coronary artery disease, however to date, no oral anti-diabetic drug has been shown to reduce the risk of cardiovascular complications. Drug interactionsSulfonamides, metformin, and insulin reciprocally exponentiate hypoglycemia. Therapy with pioglitazone increased risk for pregnancy in those taking oral contraception. How suppliedPioglitazone as Actos is supplied in oral tablets containing 15, 30 or 45 mg of pioglitazone base. It is also available in combination with metformin as ActoplusMet (tablets containing 15 mg pioglitazone and either 500 or 850 mg of metformin) or in combination with Amaryl as Duetact (tablets containing 30 mg pioglitazone and either 2 or 4 mg of Amaryl).
Relatos sobre la dominacion de la mente en el acto sexual. Actos online..Pioglitazone - Reduces insulin resistance in the liver and peripheral tissues; increases the expense of insulin-dependent glucose; decreases withdrawal of glucose from the liver; reduces quantity of glucose, insulin and glycated haemoglobin. Os trabalhadores atingidos por estes actos xenófobos são de nacionalidade portuguesa e italiana.Los actos terribles que cometieron los habitantes de Etapa 2, me recordaron la pelÃcula El señor de las moscas. Great Discounts.El acto de violencia que sufrió Rihanna por parte de su novio Chris Brown parece no encontrar sosiego, mucho menos cuando se ha dicho que la cantante de barbados retomó su relación amorosa.Con la presencia del gobernador Daniel Scioli, este jueves se llevó a cabo en la Casa de la Provincia de Buenos Aires el acto de presentación oficial del primer âFestival Internacional Folklore Buenos Airesâ que se realizará del 19 al 22 de este mes en el Anfiteatro del Lago ubicado en el Paseo del Bosque de la ciudad de La Plata. Actos medicine.Esta semana, milhares de trabalhadores ingleses do sector energético fizeram greves espontâneas devido à contratação de trabalhadores estrangeiros para trabalharem em Inglaterra (em Lindsey), na construção
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