Pioglitazone detailed information

	WikiDoc Resources for Pioglitazone detailed information
Articles
Most recent articles on Pioglitazone detailed information Most cited articles on Pioglitazone detailed information Review articles on Pioglitazone detailed information Articles on Pioglitazone detailed information in N Eng J Med, Lancet, BMJ
Media
Powerpoint slides on Pioglitazone detailed information Images of Pioglitazone detailed information Photos of Pioglitazone detailed information Podcasts & MP3s on Pioglitazone detailed information Videos on Pioglitazone detailed information
Evidence Based Medicine
Cochrane Collaboration on Pioglitazone detailed information Bandolier on Pioglitazone detailed information TRIP on Pioglitazone detailed information
Clinical Trials
Ongoing Trials on Pioglitazone detailed information at Clinical Trials.gov Trial results on Pioglitazone detailed information Clinical Trials on Pioglitazone detailed information at Google
Guidelines / Policies / Govt
US National Guidelines Clearinghouse on Pioglitazone detailed information NICE Guidance on Pioglitazone detailed information NHS PRODIGY Guidance FDA on Pioglitazone detailed information CDC on Pioglitazone detailed information
Books
Books on Pioglitazone detailed information
News
Pioglitazone detailed information in the news Be alerted to news on Pioglitazone detailed information News trends on Pioglitazone detailed information
Commentary
Blogs on Pioglitazone detailed information
Definitions
Definitions of Pioglitazone detailed information
Patient Resources / Community
Patient resources on Pioglitazone detailed information Discussion groups on Pioglitazone detailed information Patient Handouts on Pioglitazone detailed information Directions to Hospitals Treating Pioglitazone detailed information Risk calculators and risk factors for Pioglitazone detailed information
Healthcare Provider Resources
Symptoms of Pioglitazone detailed information Causes & Risk Factors for Pioglitazone detailed information Diagnostic studies for Pioglitazone detailed information Treatment of Pioglitazone detailed information
Continuing Medical Education (CME)
CME Programs on Pioglitazone detailed information
International
Pioglitazone detailed information en Espanol Pioglitazone detailed information en Francais
Business
Pioglitazone detailed information in the Marketplace Patents on Pioglitazone detailed information
Experimental / Informatics
List of terms related to Pioglitazone detailed information

Pioglitazone detailed information
Clinical data
[[Regulation of therapeutic goods \|Template:Engvar data]]	EU EMA: by INN; US FDA: Actos;
Pregnancy; category	C;
Routes of; administration	oral
ATC code	A10BG03 (WHO) ;
Legal status
Legal status	PoM (UK), Rx (US);
Pharmacokinetic data
Protein binding	>99%
Metabolism	liver (CYP2C8)
Elimination half-life	3–7 hours
Excretion	in bile
Identifiers
	IUPAC name 5-((4-(2-(5-ethyl-2-pyridinyl); ethoxy)phenyl)methyl)-,(+-)-; 2,4-thiazolidinedione,;
CAS Number	111025-46-8;
PubChem CID	4829;
DrugBank	APRD00653;
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
Formula	C19H20N2O3S
Molar mass	356.44 g/mol
3D model (JSmol)	Interactive image;
	SMILES CCc1ccc(CCOc2ccc(cc2)CC2SC(=O)NC2=O)nc1;

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]

Please Take Over This Page and Apply to be Editor-In-Chief for this topic: There can be one or more than one Editor-In-Chief. You may also apply to be an Associate Editor-In-Chief of one of the subtopics below. Please mail us [2] to indicate your interest in serving either as an Editor-In-Chief of the entire topic or as an Associate Editor-In-Chief for a subtopic. Please be sure to attach your CV and or biographical sketch.

For patient information, click here

Pioglitazone is a prescription drug of the class thiazolidinedione with hypoglycemic (antihyperglycemic, antidiabetic) action. Pioglitazone is marketed as trademarks Actos in the USA and Glustin in Europe by the pharmaceutical company Takeda.

Pharmacology

Pioglitazone selectively stimulates nuclear receptor peroxisone proliferator-activated receptor gamma (PPARγ). 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.^[1]^[2]

Indications and usage

Pioglitazone is used for the treatment of diabetes mellitus type 2 (non-insulin-dependent diabetes mellitus, NIDDM) in monotherapy but usually 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.^[3]

Contraindications

Pioglitazone 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 effects

A 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.[3] The information was based on data from the ADOPT trial.[4] 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". The FDA Advisory Committee are currently (as of 2007) reviewing rosiglitazone data following an initial rejection of submitted data. Pioglitazone was not reviewed. A meta-analysis released subsequently showed that pioglitazone reduced the number of ischemic cardiac events rather than increase the risk.^[4]

Drug interactions

Sulfonamides, metformin, and insulin reciprocally exponentiate hypoglycemia. Therapy with pioglitazone increased risk for pregnancy in those taking oral contraception.

How supplied

Pioglitazone 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).

References

↑ Colca JR, McDonald WG, Waldon DJ, Leone JW, Lull JM, Bannow CA, Lund ET, Mathews WR (2004). "Identification of a novel mitochondrial protein ("mitoNEET") cross-linked specifically by a thiazolidinedione photoprobe". Am. J. Physiol. Endocrinol. Metab. 286 (2): E252–60. doi:10.1152/ajpendo.00424.2003. PMID 14570702.
↑ Paddock ML, Wiley SE, Axelrod HL, Cohen AE, Roy M, Abresch EC, Capraro D, Murphy AN, Nechushtai R, Dixon JE, Jennings PA (2007). "MitoNEET is a uniquely folded 2Fe 2S outer mitochondrial membrane protein stabilized by pioglitazone". Proc. Natl. Acad. Sci. U.S.A. 104 (36): 14342–7. doi:10.1073/pnas.0707189104. PMID 17766440.
↑ Belfort R, Harrison SA, Brown K, Darland C, Finch J, Hardies J, Balas B, Gastaldelli A, Tio F, Pulcini J, Berria R, Ma JZ, Dwivedi S, Havranek R, Fincke C, DeFronzo R, Bannayan GA, Schenker S, Cusi K (2006). "A placebo-controlled trial of pioglitazone in subjects with nonalcoholic steatohepatitis". N. Engl. J. Med. 355 (22): 2297–307. doi:10.1056/NEJMoa060326. PMID 17135584.
↑ Lincoff AM, Wolski K, Nicholls SJ, Nissen SE (2007). "Pioglitazone and risk of cardiovascular events in patients with type 2 diabetes mellitus: a meta-analysis of randomized trials". JAMA. 298 (10): 1180–8. doi:10.1001/jama.298.10.1180. PMID 17848652.

External links

Template:Oral hypoglycemics Template:SIB

de:Pioglitazon

Template:WikiDoc Sources

[pmid14570702-1] Colca JR, McDonald WG, Waldon DJ, Leone JW, Lull JM, Bannow CA, Lund ET, Mathews WR (2004). "Identification of a novel mitochondrial protein ("mitoNEET") cross-linked specifically by a thiazolidinedione photoprobe". Am. J. Physiol. Endocrinol. Metab. 286 (2): E252–60. doi:10.1152/ajpendo.00424.2003. PMID 14570702.

[pmid17766440-2] Paddock ML, Wiley SE, Axelrod HL, Cohen AE, Roy M, Abresch EC, Capraro D, Murphy AN, Nechushtai R, Dixon JE, Jennings PA (2007). "MitoNEET is a uniquely folded 2Fe 2S outer mitochondrial membrane protein stabilized by pioglitazone". Proc. Natl. Acad. Sci. U.S.A. 104 (36): 14342–7. doi:10.1073/pnas.0707189104. PMID 17766440.

[pmid17135584-3] Belfort R, Harrison SA, Brown K, Darland C, Finch J, Hardies J, Balas B, Gastaldelli A, Tio F, Pulcini J, Berria R, Ma JZ, Dwivedi S, Havranek R, Fincke C, DeFronzo R, Bannayan GA, Schenker S, Cusi K (2006). "A placebo-controlled trial of pioglitazone in subjects with nonalcoholic steatohepatitis". N. Engl. J. Med. 355 (22): 2297–307. doi:10.1056/NEJMoa060326. PMID 17135584.

[4] Lincoff AM, Wolski K, Nicholls SJ, Nissen SE (2007). "Pioglitazone and risk of cardiovascular events in patients with type 2 diabetes mellitus: a meta-analysis of randomized trials". JAMA. 298 (10): 1180–8. doi:10.1001/jama.298.10.1180. PMID 17848652.

[1]

[2]

[3]

[4]